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Find video protocols related to scientific articles indexed in Pubmed.
Efficient Synthesis and Characterization of Ergosterol Laurate in a Solvent-Free System.
J. Agric. Food Chem.
PUBLISHED: 11-19-2014
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Ergosterol and its derivatives have attracted much attention for a variety of health benefits, such as anti-inflammatory and antioxidant activities. However, ergosterol esters are advantageous because this compound has better solubility than the free ergosterol. In this work, ergosterol laurate was efficiently synthesized for the first time by direct esterification in a solvent-free system. The desired product was purified, characterized by Fourier transform infrared spectroscopy, mass spectrometry, and nuclear magnetic resonance, and finally confirmed to be ergosterol laurate. Meanwhile, the effect of various catalysts, catalyst dose, reaction temperature, substrate molar ratio, and reaction time were studied. Both the conversion of ergosterol and the selectivity of the desired product can reach above 89% under the selected conditions: sodium dodecyl sulfate + hydrochloric acid as the catalyst, 2:1 molar ratio of lauric acid/ergosterol, catalyst dose of 4% (w/w), 120 °C, and 2 h. The oil solubility of ergosterol and its laurate was also compared. The results showed that the solubility of ergosterol in oil was significantly improved by direct esterification with lauric acid, thus greatly facilitating the incorporation into a variety of oil-based systems.
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Birth weight is associated with placental fat mass- and obesity-associated gene expression and promoter methylation in a Chinese population.
J. Matern. Fetal. Neonatal. Med.
PUBLISHED: 11-15-2014
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Abstract Objective: To explore the relationship between birth weight and fat mass- and obesity-associated (FTO) gene expression and promoter methylation status in the Chinese population. Methods: Seventy-five neonates and their mothers were recruited from Yuying Children's Hospital of Wenzhou Medical University. Subjects were divided into three groups by birth weight: low (<3500 g, n=20), medium (3500-3999 g, n=30) and high (?4000 g, n=25). Placental FTO transcript levels and promoter methylation were determined by quantitative PCR and Sequenom MassARRAY®. Results: Placental FTO mRNA expression was significantly increased in the High- and Medium-weight groups compared to the Low-weight group (P=0.023). Methylation rates of CpG11 sites were significantly decreased in high-birth weight newborns (P=0.018). Multiple linear regressions showed placental FTO mRNA, maternal pre-pregnancy BMI, and CpG11 methylation rate were independently associated with increased fetal birth weight. Additionally, FTO mRNA expression was negatively associated with CpG6.7.8.9 methylation in mothers that underwent C-section. Conclusions: High placental FTO expression is associated with increased birth weight in Chinese neonates, and FTO promoter methylation level at a specific CpG site is negatively associated with birth weight. Further work is needed to determine the functionality of this CpG site in placentas.
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Leucogen Tablets at 60 mg Three Times per Day are Safe and Effective to Control Febrile Neutropenia.
Asian Pac. J. Cancer Prev.
PUBLISHED: 10-24-2014
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To investigate whether it is safe to use leucogen tablets 60 mg three times per day (180 mg for a day) and whether this regimen could reduce the incidence of febrile neutropenia caused by chemotherapy.
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The ERCC1 C118T Polymorphism Predicts Clinical Outcomes of Colorectal Cancer Patients Receiving Oxaliplatin-Based Chemotherapy: a Meta-analysis Based on 22 Studies.
Asian Pac. J. Cancer Prev.
PUBLISHED: 10-24-2014
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Although the predictive value of the excision repair cross-complementing group 1 (ERCC1) C118T polymorphism in clinical outcomes of patients with colorectal cancer (CRC) receiving oxaliplatin-based chemotherapy has been evaluated in numerous published studies, the conclusions are conflicting. Therefore, we performed the present meta-analysis to determine the precise role of the ERCC1 C118T polymorphism in this clinical situation and help optimize individual chemotherapy.
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[Endemic situation and control progress of taeniasis in western China].
Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi
PUBLISHED: 09-17-2014
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Taeniasis, caused by Taenia species, is one of the common zoonoses in China, particularly in the western region of China. Up to now, not enough attention has been given in the high prevalence and high burden of the diseases. In order to study the endemic patterns and control strategies of taeniasis, a series of epidemiological investigations, molecular researches and pilot control activities have been conducted in recent years. This paper reviews the relevant publications in taeniasis research over the last 10 years.
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Enantioselective aza-Morita-Baylis-Hillman reaction between acrylates and N-Boc isatin ketimines: asymmetric construction of chiral 3-substituted-3-aminooxindoles.
Org. Biomol. Chem.
PUBLISHED: 09-04-2014
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The first enantioselective aza-Morita–Baylis–Hillman reaction of acrylates with ketimines derived from isatins has been developed. With 2 mol% of chiral bifunctional phosphine-squaramide 4e, optically active 3-substituted-3-amino-2-oxindoles were obtained in excellent yields with up to 91% ee.
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Allicin prevents H?O?-induced apoptosis of HUVECs by inhibiting an oxidative stress pathway.
BMC Complement Altern Med
PUBLISHED: 08-30-2014
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Allicin, a primary ingredient of garlic, has been proposed to possess cardioprotective properties, which are commonly mediated by improved endothelial function.
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[Memory characteristic in boys with attention deficit/hyperactivity disorder comorbid learning disability].
Zhonghua Yi Xue Za Zhi
PUBLISHED: 08-26-2014
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To explore the memory characteristic in boys with attention-deficit/hyperactivity disorder (ADHD) plus learning disability (LD).
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Cloning and expression analysis of a peptidoglycan recognition protein in silkworm related to virus infection.
Gene
PUBLISHED: 08-21-2014
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In this study, the full-length cDNA of a peptidoglycan recognition protein named BmPGRP-S3 was identified from the silkworm, Bombyx mori by rapid amplification of cDNA ends. It is 807 bp and comprises the following: a 5'-untranslated region (UTR) with a length of 112 bp, a 3'-UTR with a length of 92 bp including a poly-adenylation signal sequence (AATAAA) and a poly(A) tail. The longest open reading frame (ORF) of BmPGRP-S3 is 603 bp and encodes a polypeptide of 200 amino acids with a predicted molecular weight of 22.3 kDa including a PGRP domain. Sequence similarity and phylogenic analysis results indicated that BmPGRP-S3 belongs to the group of insect PGRPs and is closer to BmPGRP-S4 with the highest identity of 68%. Fluorescent quantitative real-time PCR results revealed that the mRNA transcripts of BmPGRP-S3 were presented in all of the tissues, but were highest in the midgut. In the silkworm larvae infected with B. mori cytoplasmic polyhedrosis virus (BmCPV), the relative expression level of BmPGRP-S3 was upregulated. The DNA segment of a mature BmPGRP-S3 peptide was inserted into the expression plasmid pET-28a(+) to construct a recombinant expression plasmid. Western blot results revealed that mature BmPGRP-S3 could be detected in the hemolymph and midgut which were the most important immune tissues in silkworm. All the results suggested that BmPGRP-S3 may play an important role in the immune response of silkworm to BmCPV infection and provided helpful information for further studying the function of BmPGRP-S3 in silkworm.
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Bmovo-1 regulates ovary size in the silkworm, Bombyx mori.
PLoS ONE
PUBLISHED: 08-13-2014
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The regulation of antagonistic OVO isoforms is critical for germline formation and differentiation in Drosophila. However, little is known about genes related to ovary development. In this study, we cloned the Bombyx mori ovo gene and investigated its four alternatively spliced isoforms. BmOVO-1, BmOVO-2 and BmOVO-3 all had four C2H2 type zinc fingers, but differed at the N-terminal ends, while BmOVO-4 had a single zinc finger. Bmovo-1, Bmovo-2 and Bmovo-4 showed the highest levels of mRNA in ovaries, while Bmovo-3 was primarily expressed in testes. The mRNA expression pattern suggested that Bmovo expression was related to ovary development. RNAi and transgenic techniques were used to analyze the biological function of Bmovo. The results showed that when the Bmovo gene was downregulated, oviposition number decreased. Upregulation of Bmovo-1 in the gonads of transgenic silkworms increased oviposition number and elevated the trehalose contents of hemolymph and ovaries. We concluded that Bmovo-1 was involved in protein synthesis, contributing to the development of ovaries and oviposition number in silkworms.
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A predictive model for evaluating responsiveness to pemetrexed treatment in patients with advanced colorectal cancer.
Asian Pac. J. Cancer Prev.
PUBLISHED: 08-02-2014
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To highlight the potential factors that could predict the response rate of patients with metastatic colorectal cancer (mCRC) treated with pemetrexed combined chemotherapy after first- or second-line chemotherapy using the FOLFOX regimen.
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TNF-?-induced cardiomyocyte apoptosis contributes to cardiac dysfunction after coronary microembolization in mini-pigs.
J. Cell. Mol. Med.
PUBLISHED: 07-31-2014
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This experimental study was designed to clarify the relationship between cardiomyocyte apoptosis and tumour necrosis factor-alpha (TNF-?) expression, and confirm the effect of TNF-? on cardiac dysfunction after coronary microembolization (CME) in mini-pigs. Nineteen mini-pigs were divided into three groups: sham-operation group (n = 5), CME group (n = 7) and adalimumab pre-treatment group (n = 7; TNF-? antibody, 2 mg/kg intracoronary injection before CME). Magnetic resonance imaging (3.0-T) was performed at baseline, 6th hour and 1 week after procedure. Cardiomyocyte apoptosis was detected by cardiac-TUNEL staining, and caspase-3 and caspase-8 were detected by RT-PCR and immunohistochemistry. Furthermore, serum TNF-?, IL-6 and troponin T were analysed, while myocardial expressions of TNF-? and IL-6 were detected. Both TNF-? expression (serum level and myocardial expression) and average number of apoptotic cardiomyocyte nuclei were significantly increased in CME group compared with the sham-operation group. Six hours after CME, left ventricular end-systolic volume (LVESV) was increased and the left ventricular ejection fraction (LVEF) was decreased in CME group. Pre-treatment with adalimumab not only significantly improved LVEF after CME (6th hour: 54.9 ± 2.3% versus 50.4 ± 3.9%, P = 0.036; 1 week: 56.7 ± 4.2% versus 52.7 ± 2.9%, P = 0.041), but also suppressed cardiomyocyte apoptosis and the expression of caspase-3 and caspase-8. Meanwhile, the average number of apoptotic cardiomyocytes nuclei was inversely correlated with LVEF (r = -0.535, P = 0.022). TNF-?-induced cardiomyocyte apoptosis is likely involved in cardiac dysfunction after CME. TNF-? antibody therapy suppresses cardiomyocyte apoptosis and improves early cardiac function after CME.
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pH-responsive polymer-drug conjugates as multifunctional micelles for cancer-drug delivery.
Nanotechnology
PUBLISHED: 07-30-2014
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We developed a novel linear pH-sensitive conjugate methoxy poly(ethylene glycol)-4?-aminopodophyllotoxin (mPEG-NPOD-I) by a covalently linked 4?-aminopodophyllotoxin (NPOD) and PEG via imine bond, which was amphiphilic and self-assembled to micelles in an aqueous solution. The mPEG-NPOD-I micelles simultaneously served as an anticancer drug conjugate and as drug carriers. As a drug conjugate, mPEG-NPOD-I showed a significantly faster NPOD release at a mildly acidic pH of 5.0 and 4.0 than a physiological pH of 7.4. Notably, it was confirmed that this drug conjugate could efficiently deliver NPOD to the nuclei of the tumor cells and led to much more cytotoxic effects to A549, Hela, and HepG2 cancer cells than the parent NPOD. The half maximal inhibitory concentration (IC??) of mPEG-NPOD-I was about one order magnitude lower than that of the NPOD. In vivo, mPEG-NPOD-I reduced the size of the tumors significantly, and the biodistribution studies indicated that this drug conjugate could selectively accumulate in tumor tissues. As drug carriers, the mPEG-NPOD-I micelles encapsulated hydrophobic PTX with drug-loading efficiencies of 57% and drug-loading content of 16%. The loaded PTX also showed pH-triggered fast release behavior, and good additive cytotoxicity effect was observed for the PEG-NPOD-I/PTX. We are convinced that these multifunctional drug conjugate micelles have tremendous potential for targeted cancer therapy.
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[Application of space-time scan statistics in the analysis of spatial and temporal distribution of Oncomelania hupensis snails in Gaoyou County, Jiangsu Province].
Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi
PUBLISHED: 07-29-2014
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To investigate the distribution features of Oncomelania hupensis infested areas in Gaoyou County so as to formulate surveillance and intervention strategies.
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Serum matrix metalloproteinase-3 as a noninvasive biomarker of histological synovitis for diagnosis of rheumatoid arthritis.
Mediators Inflamm.
PUBLISHED: 07-23-2014
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To explore the correlation between matrix metalloproteinase- (MMP-) 3 and histological synovitis in rheumatoid arthritis (RA).
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Gordonia iterans sp. nov., isolated from a patient with pneumonia.
Int. J. Syst. Evol. Microbiol.
PUBLISHED: 07-22-2014
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A second novel clinical actinobacterial strain, designated IFM 10348(T), was isolated from the sputum of the same Japanese patient with bacterial pneumonia from whom the type strain of Gordonia araii had been isolated. The strains differed in phylogenetic position and drug-resistance profiles. The taxonomic position of strain IFM 10348(T) was clarified by phenotypic, chemotaxonomic and phylogenetic studies. Phylogenetic analyses based on 16S rRNA gene sequences clearly demonstrated that strain IFM 10348(T) occupied a distinct clade within the genus Gordonia and was related closely to Gordonia malaquae DSM 45064(T) and Gordonia hirsuta DSM 44140(T) (97.3 and 97.1% similarities, respectively). Strain IFM 10348(T) was also clearly differentiated from G. malaquae DSM 45064(T) and G. hirsuta DSM 44140(T) based on gyrB and secA1 gene sequence similarity values. Strain IFM 10348(T) had MK-9(H2) as the predominant menaquonine, contained meso-diaminopimelic acid, arabinose, galactose and glucosamine as cell-wall components, and contained C18:1?9c, summed feature 3 (C16:1?7c and/or C16:1?6c) and C16:0 as the major cellular fatty acids. Mycolic acids were present. The DNA G+C content of strain IFM 10348(T) was 68.0 mol%. DNA-DNA relatedness data coupled with the combination of genotypic and phenotypic data indicated that strain IFM 10348(T) represents a novel species of the genus Gordonia, for which the name Gordonia iterans sp. nov. is proposed. The type strain is IFM 10348(T) ( = CCTCC M2011245(T) = NCCB 100436(T)).
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Design, synthesis, mechanisms of action, and toxicity of novel 20(s)-sulfonylamidine derivatives of camptothecin as potent antitumor agents.
J. Med. Chem.
PUBLISHED: 07-08-2014
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Twelve novel 20-sulfonylamidine derivatives (9a-9l) of camptothecin (1) were synthesized via a Cu-catalyzed three-component reaction. They showed similar or superior cytotoxicity compared with that of irinotecan (3) against A-549, DU-145, KB, and multidrug-resistant (MDR) KBvin tumor cell lines. Compound 9a demonstrated better cytotoxicity against MDR cells compared with that of 1 and 3. Mechanistically, 9a induced significant DNA damage by selectively inhibiting Topoisomerase (Topo) I and activating the ATM/Chk related DNA damage-response pathway. In xenograft models, 9a demonstrated significant activity without overt adverse effects at 5 and 10 mg/kg, comparable to 3 at 100 mg/kg. Notably, 9a at 300 mg/kg (i.p.) showed no overt toxicity in contrast to 1 (LD50 56.2 mg/kg, i.p.) and 3 (LD50 177.5 mg/kg, i.p.). Intact 9a inhibited Topo I activity in a cell-free assay in a manner similar to that of 1, confirming that 9a is a new class of Topo I inhibitor. 20-Sulfonylamidine 1-derivative 9a merits development as an anticancer clinical trial candidate.
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[Diagnostic value of ultrasound imaging in chronic gouty arthritis].
Sichuan Da Xue Xue Bao Yi Xue Ban
PUBLISHED: 06-20-2014
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To determine the diagnostic value of ultrasound imaging in chronic gouty arthritis.
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Staging and risk factors of chronic kidney disease of outpatients in Shanghai.
Ren Fail
PUBLISHED: 06-18-2014
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We conducted a survey to determine the stages distribution of chronic kidney disease (CKD) using estimated glomerular filtration rate (eGFR) Study Equation and evaluate the risk factors for these patients.
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Catechins induced acute promyelocytic leukemia cell apoptosis and triggered PML-RAR¿ oncoprotein degradation.
J Hematol Oncol
PUBLISHED: 06-17-2014
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BackgroundIt has recently been reported that the extracts of green tea polyphenol have cancer preventive effects. In this study, we investigated the effect of the natural composition from green tea leaves Catechins on acute promyelocytic leukemia (APL).MethodsIn vitro, APL cell lines NB4, retinoic acid-resistant NB4-R1 and NB4-R2 were treated with different concentrations of Catechins. Cell viability and cell apoptosis were analyzed using MTT assay and flow cytometric assay, respectively. Expression of proteins related to apoptosis and PML-RAR¿ oncoprotein were assessed by Western blot. In vivo anti-tumor activity of Catechins was examined in nude mice xenografted with NB4 cells and in situ cell apoptosis was detected by terminal deoxytransferase-catalyzed DNA nick-end labeling assay.ResultsCatechins at micromolar concentration levels significantly inhibited APL cell proliferation and induced cell apoptosis, in association with mitochondria damage, ROS production and caspase activation. The anti-apoptotic Bcl-2 family member Bcl-xL was down regulated, with pro-apoptotic member Bax remaining unchanged. Moreover, Catechins induced the degradation of PML-RAR¿ oncoprotein. Catechins-mediated apoptotic effect was also observed in primary APL cells without affecting normal hematopoietic progenitor cells. In the murine xenograft model, Catechins remarkably inhibited tumor growth and induced in situ leukemic cell apoptosis.ConclusionsCatechins might be a potential candidate for APL treatment by activating intrinsic apoptotic pathway and targeting PML-RAR¿ oncoprotein.
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Design, synthesis, crystal structure, insecticidal activity, molecular docking, and QSAR studies of novel N3-substituted imidacloprid derivatives.
J. Agric. Food Chem.
PUBLISHED: 06-06-2014
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Three novel series of N3-substituted imidacloprid derivatives were designed and synthesized, and their structures were identified on the basis of satisfactory analytical and spectral ((1)H NMR, (13)C NMR, MS, elemental analysis, and X-ray) data. Preliminary bioassays indicated that all of the derivatives exhibited significant insecticidal activities against Aphis craccivora, with LC50 values ranging from 0.00895 to 0.49947 mmol/L, and the insecticidal activities of some of them were comparable to those of the control imidacloprid. Some key structural features related to their insecticidal activities were identified, and the binding modes between target compounds and nAChR model were also further explored by molecular docking. By comparing the interaction features of imidacloprid and compound 26 with highest insecticidal activity, the origin of the high insecticidal activity of compound 26 was identified. On the basis of the conformations generated by molecular docking, a satisfactory 2D-QSAR model with six selected descriptors was built using genetic algorithm-multiple linear regression (GA-MLR) method. The analysis of the built model showed the molecular size, shape, and the ability to form hydrogen bond were important for insecticidal potency. The information obtained in the study will be very helpful for the design of new derivatives with high insecticidal activities.
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Parameter comparison of white matter diffusion tensor imaging (DTI) in rhesus macaques (Macaca mulatta).
Zool. Res.
PUBLISHED: 05-29-2014
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In this study, we analyzed diffusion tensor imaging (DTI) results of brain white matter in rhesus macaques (Macaca mulatta) with four different parameter settings and found that the sequence A (b=1 000 s/mm(2), spatial resolution=1.25 mm×1.25 mm× 1.25 mm, numbers of direction=33, NSA=3) and B (b=800 s/mm(2), spatial resolution=1.25 mm×1.25 mm×1.25 mm, numbers of direction=33, NSA=3) could accurately track coarse fibers. The fractional anisotropy (FA) derived from sequence C (b=1 000s/mm(2), spatial resolution=0.55 mm×0.55 mm×2.5 mm, direction number=33, NSA=3) was too fuzzy to be used in tracking white matter fibers. By comparison, the high resolution and the FA with high contrast of gray matter and white matter derived from sequence D (b=800 s/mm(2), spatial resolution=1.0 mm×1.0 mm ×1.0 mm, numbers of direction=33, NSA=3) qualified in its application in tracking both thick and thin fibers, making it an optimal DTI setting for rhesus macaques.
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Down-regulating peroxisome proliferator-activated receptor-gamma coactivator-1beta alleviates the proinflammatory effect of rheumatoid arthritis fibroblast-like synoviocytes through inhibiting extracellular signal-regulated kinase, p38 and nuclear factor-kappaB activati
Arthritis Res. Ther.
PUBLISHED: 05-26-2014
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IntroductionRheumatoid arthritis (RA) is a chronic inflammatory disease leading to joint destruction and disability. Peroxisome proliferator-activated receptor-gamma coactivator-1beta (PGC-1ß) is a transcriptional coactivator that plays important roles in regulating multiple aspects of energy metabolism and cytokine signaling pathways. PGC-1ß overexpression leads to the attenuation of macrophage-mediated inflammation. In this study, we aimed to determine the expression of PGC-1ß in RA synovium and fibroblast-like synoviocytes (FLS), and explore the mechanisms of PGC-1ß on both the proinflammatory effects and apoptosis in RA-FLS.MethodsSynovium was obtained from 31 patients with active RA, as well as 13 osteoarthritis (OA) and 10 orthopedic arthropathies (Orth.A) as ¿less inflamed¿ disease controls. FLS were then isolated and cultured. Synovial PGC-1ß expression was determined by immunohistochemistry staining, while FLS PGC-1ß expression was detected by immunofluorescence staining, quantitative real-time PCR (qPCR) assay and western blot. PGC-1ß was depleted by lentivirus sh-RNA, and up-regulated by pcDNA3.1- PGC-1ß. The expression of proinflammatory cytokines, matrix metalloproteinases and receptor activator of nuclear factor-kappaB ligand was analyzed by qPCR, cytometric bead array and western blot. The expression of mitogen-activated protein kinases and nuclear factor-kappaB (NF-¿B) was determined by qPCR and western blot. Besides, cell apoptosis was examined using flow cytometry. The interaction between PGC-1ß and NF-¿B was performed by dual-luciferase reporter gene assays.Results(A) Synovial PGC-1ß was over-expressed in RA patients compared with OA or Orth.A patients. (B) PGC-1ß expression significantly increased in RA-FLS compared with OA-FLS. (C) PGC-1ß mediated the expression of proinflammatory cytokines and apoptosis through extracellular signal-regulated kinase (ERK), p38 and NF-¿B in RA-FLS. (D) PGC-1ß mediated NF-¿B transcription in RA-FLS, but did not affect ERK and p38.ConclusionThe results indicate that PGC-1ß may play important roles in the proinflammatory effects and apoptosis of RA-FLS.
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Antifungal activity of compounds extracted from Cortex Pseudolaricis against Colletotrichum gloeosporioides.
J. Agric. Food Chem.
PUBLISHED: 05-19-2014
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Cortex Pseudolaricis is the root bark of Pseudolarix amabilis Rehder, found only in China, and has been widely used in folk antifungal remedies in traditional Chinese medicine. In order to find the natural antifungal agents against mango anthracnose, eight compounds, namely pseudolaric acid A (1), ethyl pseudolaric acid B (2), pseudolaric acid B (3), pseudolaric acid B-O-?-d-glucoside (4), piperonylic acid (5), propionic acid (6), 3-hydroxy-4-methoxybenzoic acid (7), and 4-(3-formyl-5-methoxyphenyl) butanoic acid (8) were isolated from the ethanol extracts of Cortex Pseudolaricis by bioassay-guided fractionation and evaluated for in vitro antifungal activity against Colletotrichum gloeosporioides Penz. Results demonstrated that all of the eight compounds inhibited the mycelial growth of C. gloeosporioides at 5 ?g/mL. Among them, pseudolaric acid B and pseudolaric acid A showed the strongest inhibition with the EC50 values of 1.07 and 1.62 ?g/mL, respectively. Accordingly, both Pseudolaric acid B and Pseudolaric acid A highly inhibited spore germination and germ tube elongation of C. gloeosporioides. Dipping 100 ?g/mL pseudolaric acid B treatment exhibited more effective suppression on postharvest anthracnose in mango fruit when compared to the same concentration of carbendazim. Scanning electron microscopy observations revealed that pseudolaric acid B caused alterations in the hyphal morphology of C. gloeosporioides, including distortion, swelling, and collapse. Pseudolaric acid B caused the mycelial apexes to show an abnormal growth in dimensions with multiple ramifications in subapical expanded areas with irregular shape. These findings warrant further investigation into optimization of pseudolaric acid B to explore a potential antifungal agent for crop protection.
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Recent Progress on C-4-Modified Podophyllotoxin Analogs as Potent Antitumor Agents.
Med Res Rev
PUBLISHED: 05-16-2014
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Podophyllotoxin (PPT), as well as its congeners and derivatives, exhibits pronounced biological activities, especially antineoplastic effects. Its strong inhibitory effect on tumor cell growth led to the development of three of the most highly prescribed anticancer drugs in the world, etoposide, teniposide, and the water-soluble prodrug etoposide phosphate. Their clinical success as well as intriguing mechanism of action stimulated great interest in further modification of PPT for better antitumor activity. The C-4 position has been a major target for structural derivatization aimed at either producing more potent compounds or overcoming drug resistance. Accordingly, numerous PPT derivatives have been prepared via hemisynthesis and important structure-activity relationship (SAR) correlations have been identified. Several resulting compounds, including GL-331, TOP-53, and NK611, reached clinical trials. Some excellent reviews on the distribution, sources, applications, synthesis, and SAR of PPT have been published. This review focuses on a second generation of new etoposide-related drugs and provides detailed coverage of the current status and recent development of C-4-modified PPT analogs as anticancer clinical trial candidates.
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Design and synthesis of new 7-(N-substituted-methyl)-camptothecin derivatives as potent cytotoxic agents.
Bioorg. Med. Chem. Lett.
PUBLISHED: 05-09-2014
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A series of novel 7-(N-substituted-methyl)-camptothecin derivatives was designed, synthesized, and evaluated for in vitro cytotoxicity against four human tumor cell lines, A-549, MDA-MB-231, KB, and KBvin. All of the derivatives showed promising in vitro cytotoxic activity against the tested tumor cell lines, with IC50 values ranging from 0.0023 to 1.11 ?M, and were as or more potent than topotecan. Compounds 9d, 9e, and 9r exhibited the highest antiproliferative activity among all prepared derivatives. Furthermore, all of the compounds were more potent than paclitaxel against the multidrug-resistant (MDR) KBvin subline. With a concise efficient synthesis and potent cytotoxic profiles, especially significant activity towards KBvin, compounds 9d, 9e, and 9r merit further development as a new generation of camptothecin-derived anticancer clinical trial candidates.
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Reduction patterns of acute schistosomiasis in the People's Republic of China.
PLoS Negl Trop Dis
PUBLISHED: 05-01-2014
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Despite significant, steady progress in schistosomiasis control in the People's Republic of China over the past 50 years, available data suggest that the disease has re-emerged with several outbreaks of acute infections in the early new century. In response, a new integrated strategy was introduced.
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Rectification of impaired adipose tissue methylation status and lipolytic response contributes to hepatoprotective effect of betaine in a mouse model of alcoholic liver disease.
Br. J. Pharmacol.
PUBLISHED: 04-22-2014
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Overactive lipolysis in adipose tissue contributes to the pathogenesis of alcoholic liver disease (ALD); however, the mechanisms involved have not been elucidated. We previously reported that chronic alcohol consumption produces a hypomethylation state in adipose tissue. In this study we investigated the role of hypomethylation in adipose tissue in alcohol-induced lipolysis and whether its correction contributes to the well-established hepatoprotective effect of betaine in ALD.
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A folding study of Antarctic krill (Euphausia superba) alkaline phosphatase using denaturants.
Int. J. Biol. Macromol.
PUBLISHED: 04-11-2014
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To gain insight into the structural and folding mechanisms of Antarctic krill alkaline phosphatase (ALP), the enzyme was properly purified by (NH4)2SO4 fractionation and by both Sephadex G-75 and DEAE anion exchange chromatography. The purified enzyme (62.6 kDa; 2.62 unit/mg) was unstable at temperatures exceeding 30°C. Denaturants, such as sodium dodecyl sulfate (SDS), guanidine HCl, and urea, were applied to evaluate the folding mechanism, including kinetics and thermodynamics, of krill ALP. Sodium dodecyl sulfate elicited no significant effect on ALP activity even at excessively high concentrations (300 mM), whereas guanidine HCl and urea effectively inactivated the enzyme at concentrations of 2 and 3.5 M, respectively. Kinetic studies showed that the enzymatic inhibition by guanidine HCl and urea represented a first-order reaction that was a monophasic unfolding process. This process was found to be associated with conformational changes without significant transient free-energy changes. Additionally, the overall structural changes occurred proximally to the active site pocket. Our study provides new insight into ALP of the Antarctic krill, which lives in extreme environmental conditions.
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In vitro anti-inflammatory effects of diterpenoids and sesquiterpenoids from traditional Chinese medicine Siegesbeckia pubescens.
Bioorg. Med. Chem. Lett.
PUBLISHED: 03-31-2014
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Oxidative stress imposed by reactive oxygen species plays a crucial role in pathophysiology of inflammatory diseases. In the present study, sesquiterpenoids and diterpenoids isolated from Siegesbeckia pubescens, a Chinese traditional medicine used to treat arthritis, were evaluated for inhibition of NO production in activated RAW 264.7 macrophages and FMLP/CB induced O2(·-) generation and elastase release in human neutrophils. In the former assay, sesquiterpenoids were more potent than diterpenoids. The C-4 carbonyl group in the carabrane-type sesquiterpenoid 3 and the C-9 ether linkage in the germacrane sesquiterpene 7 were associated with the enhanced potency. Also, for the active ent-kaurane type diterpenoids, esterification of 17-OH with isobutyric acid and acetylation of 18-OH affected the inhibition of O2(·-) generation and elastase release. This report is the first to describe the inhibitory effects on oxidative stress of secondary metabolites from S. pubescens. Its findings suggest that active terpenoids from the herb could be used as lead anti-inflammatory agents.
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Purification, characterization, and unfolding studies of arginine kinase from Antarctic krill.
Int. J. Biol. Macromol.
PUBLISHED: 03-22-2014
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The regulation of enzymatic activity and unfolding studies of arginine kinase (AK) from various invertebrates have been the focus of investigation. To gain insight into the structural and folding mechanisms of AK from Euphausia superba (ESAK), we purified ESAK from muscle properly. The enzyme behaved as a monomeric protein with a molecular mass of about 40kDa and had pH and temperature optima of 8.0 and 30°C, respectively. The Km(Arg) and Km(ATP) for the synthesis of phosphoarginine were 0.30 and 0.47mM, respectively, and kcat/Km(Arg) was 282.7s(-1)/mM. A study of the inhibition kinetics of structural unfolding in the denaturant sodium dodecyl sulfate (SDS) was conducted. The results showed that ESAK was almost completely inactivated by 1.0mM SDS. The kinetics analyzed via time-interval measurements revealed that the inactivation was a first-order reaction, with the kinetic processes shifting from a monophase to biphase as SDS concentrations increased. Measurements of intrinsic and 1-anilinonaphthalene-8-sulfonate-binding fluorescence showed that SDS concentrations lower than 5mM did not induce conspicuous changes in tertiary structures, while higher concentrations of SDS exposed hydrophobic surfaces and induced conformational changes. These results confirmed that the active region of AK is more flexible than the overall enzyme molecule.
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Enhanced local Foxp3 expression in lung tissue attenuates airway inflammation in a mouse model of asthma.
J Asthma
PUBLISHED: 03-12-2014
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Bronchial asthma is a chronic inflammatory disease of the airway mediated by a Th2 immune response. A great deal of data has demonstrated that regulatory T cells (Tregs) have the ability to suppress Th2 immune responses and the transcription factor fork-head box protein 3 (Foxp3) is indispensable for the development of CD4?+?CD25?+?Tregs. In this study, we hypothesized that enhanced local Foxp3 expression in lung tissue could suppress Th2-mediated allergic asthma.
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Analysis of mutational characteristics of the drug-resistant gene katG in multi-drug resistant Mycobacterium tuberculosis L-form among patients with pneumoconiosis complicated with tuberculosis.
Mol Med Rep
PUBLISHED: 02-27-2014
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The aim of the present study was to investigate the mutational characteristics of drug?resistant genetic mutations in the katG gene to isoniazid (INH) in multi?drug resistant Mycobacterium tuberculosis (MTB) L?form among patients with pneumoconiosis complicated with tuberculosis (TB), in order to reduce the occurrence of drug resistance in patients, and gain further insight into the mechanisms underlying drug resistance in MDR?TB L?form. A total of 114 clinically isolated strains of MTB L?forms were collected. The MDR?TB L?forms were identified using a conventional antimicrobial susceptibility test (AST). The DNA genomes were extracted, the target genes were amplified by polymerase chain reaction technology and the hotspot mutational regions in the katG gene were analyzed by direct sequencing. The results of AST analysis demonstrated that there were 31 strains of MDR?TB L?forms in 114 clinical isolates. The mutation rate of katG was 61.29% (19/31) in INH?resistant isolates, mainly concentrated in codon 315 (Ser315Thr, 48.39% and Ser315Asn, 9.68%) and 431 (Ala431Val, 3.23%). Base substitutions were identified, however, no multisite mutations were found. No mutations in katG were identified in 10 INH?sensitive strains that were randomly selected. INH?resistance was more severe in MDR?TB L?form isolates among patients with pneumoconiosis complicated with TB. The substitution of highly conserved amino acids encoded by the katG gene resulted in the molecular mechanisms responsible for INH resistance in MDR?TB L?form isolates. It was also verified that the katG gene was in diversiform. The katG Ser315Thr mutation is one of the main causes of resistance to INH in MDR?TB L-form isolates.
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Piracetam ameliorated oxygen and glucose deprivation-induced injury in rat cortical neurons via inhibition of oxidative stress, excitatory amino acids release and P53/Bax.
Cell. Mol. Neurobiol.
PUBLISHED: 02-14-2014
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Our previous work has demonstrated that piracetam inhibited the decrease in amino acid content induced by chronic hypoperfusion, ameliorated the dysfunction of learning and memory in a hypoperfusion rat model, down-regulated P53, and BAX protein, facilitated the synaptic plasticity, and may be helpful in the treatment of vascular dementia. To explore the precise mechanism, the present study further evaluated effects of piracetam on Oxygen and glucose deprivation (OGD)-induced neuronal damage in rat primary cortical cells. The addition of piracetam to the cultured cells 12 h before OGD for 4 h significantly reduced neuronal damage as determined by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay and lactate dehydrogenase release experiments. Piracetam also lowered the levels of malondialdehyde, nitrogen monoxidum, and xanthine oxidase which was increased in the OGD cells, and enhanced the activities of superoxide dismutase and glutathione peroxidase, which were decreased in the OGD cells. We also demonstrated that piracetam could decrease glutamate and aspartate release when cortical cells were subjected to OGD. Furthermore, Western blot study demonstrated that piracetam attenuated the increased expression of P53 and BAX protein in OGD cells. These observations demonstrated that piracetam reduced OGD-induced neuronal damage by inhibiting the oxidative stress and decreasing excitatory amino acids release and lowering P53/Bax protein expression in OGD cells.
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Folding studies of arginine kinase from Euphausia superba using denaturants.
Appl. Biochem. Biotechnol.
PUBLISHED: 02-10-2014
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Arginine kinase (AK) is a key metabolic enzyme for maintaining energy balance in invertebrates and studies on AK from Euphausia superba might provide important insights into the metabolic enzymes in extreme climatic marine environments. A folding study of the AK from E. superba (ESAK) has not yet been reported. To gain insights into the structural and folding mechanisms of ESAK, the denaturants guanidine HCl and urea were applied in this study. We purified ESAK from the muscle of E. superba and evaluated the inhibition kinetics with structural unfolding studies under various conditions. The results revealed that ESAK was almost completely inactivated when using 1.0 M guanidine HCl and 8.25 M urea. The kinetics, characterized via time-interval measurements, showed that the inactivations by guanidine HCl and urea were first-order reactions, with the kinetic processes shifting from monophases to biphases as concentrations increased. Measurements of intrinsic and ANS (anilinonaphthalene-8-sulfonate)-binding fluorescences showed that guanidine HCl and urea induced conspicuous changes in tertiary structures and followed the regular unfolding mechanisms. Our study provides information regarding the folding of this muscle-derived metabolic enzyme and expands our knowledge and understanding of invertebrate metabolisms.
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Diagnostic performance of contrast-enhanced sonography and acoustic radiation force impulse imaging in solid liver lesions.
J Ultrasound Med
PUBLISHED: 01-23-2014
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The purpose of this study was to evaluate the diagnostic performance of contrast-enhanced sonography and acoustic radiation force impulse imaging (ARFI) in differential diagnosis of benign and malignant liver lesions.
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Toward synthesis of third-generation spin-labeled podophyllotoxin derivatives using isocyanide multicomponent reactions.
Eur J Med Chem
PUBLISHED: 01-15-2014
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Spin-labeled podophyllotoxins have elicited widespread interest due to their far superior antitumor activity compared to podophyllotoxin. To extend our prior studies in this research area, we synthesized a new generation of spin-labeled podophyllotoxin analogs via isocyanide multicomponent reactions and evaluated their cytotoxicity against four human cancer cell lines (A-549, DU-145, KB and KBvin). Most of the compounds exhibited potent cytotoxic activity against all four cell lines, notably against the drug resistant KBvin cancer cell line. Among the new analogs, compounds 12e (IC50: 0.60-0.75 ?M) and 12h (IC50: 1.12-2.03 ?M) showed superior potency to etoposide (IC50: 2.03 to >20 ?M), a clinically available anticancer drug. With a concise efficient synthesis and potent cytotoxic profiles, compounds 12e and 12h merit further development as a new generation of epipodophyllotoxin-derived antitumor clinical trial candidates.
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Cytoplasmic polyhedrosis virus-induced differential gene expression in two silkworm strains of different susceptibility.
Gene
PUBLISHED: 01-14-2014
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Digital gene expression (DGE) was performed to investigate the gene expression profiles of 4008 and p50 silkworm strains at 48 h after oral infection with BmCPV. 3,668,437 clean tags were identified in the BmCPV-infected p50 silkworms and 3,540,790 clean tags in the control p50. By contrast, 4,498,263 clean tags were identified in the BmCPV-infected 4008 silkworms and 4,164,250 clean tags in the control 4008. A total of 691 differentially expressed genes were detected in the infected 4008 DGE library and 185 were detected in the infected p50 DGE library, respectively. The expression profiles identified some important differentially expressed genes involved in signal transduction, enzyme activity and apoptotic changes, some of which were verified using quantitative real-time PCR (qRT-PCR). These results provide important clues on the molecular mechanism of BmCPV invasion and resistance mechanism of silkworms against BmCPV infection.
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Inhibition of Mus81 by siRNA enhances sensitivity to 5-FU in breast carcinoma cell lines.
Onco Targets Ther
PUBLISHED: 01-01-2014
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One of the most challenging aspects of breast carcinoma chemotherapy is the rapid acquirement of drug resistance. Improving the sensitivity to chemotherapeutic drugs is very important for successful treatment. Mus81 plays an important role in maintaining the stability of the genome and DNA repair. However, recent studies suggested that Mus81 expression levels correlate well with resistance to DNA-damaging drugs. The present study aimed to investigate the role of Mus81 on the chemosensitivity of breast carcinoma cells in response to 5-fluorouracil (5-FU), a chemotherapeutic drug that is widely used for treatment of breast malignancies.
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A high-throughput gene disruption methodology for the entomopathogenic fungus Metarhizium robertsii.
PLoS ONE
PUBLISHED: 01-01-2014
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Systematic gene disruption is a direct way to interrogate a fungal genome to functionally characterize the full suite of genes involved in various biological processes. Metarhizium robertsii is extraordinarily versatile, and it is a pathogen of arthropods, a saprophyte and a beneficial colonizer of rhizospheres. Thus, M. robertsii can be used as a representative to simultaneously study several major lifestyles that are not shared by the "model" fungi Saccharomyces cerevisiae and Neurospora crassa; a systematic genetic analysis of M. robertsii will benefit studies in other fungi. In order to systematically disrupt genes in M. robertsii, we developed a high-throughput gene disruption methodology, which includes two technologies. One is the modified OSCAR-based, high-throughput construction of gene disruption plasmids. This technology involves two donor plasmids (pA-Bar-OSCAR with the herbicide resistance genes Bar and pA-Sur-OSCAR with another herbicide resistance gene Sur) and a recipient binary plasmid pPK2-OSCAR-GFP that was produced by replacing the Bar cassette in pPK2-bar-GFP with a ccdB cassette and recombination recognition sites. Using this technology, a gene disruption plasmid can be constructed in one cloning step in two days. The other is a highly efficient gene disruption technology based on homologous recombination using a Ku70 deletion mutant (?MrKu70) as the recipient strain. The deletion of MrKu70, a gene encoding a key component involved in nonhomologous end-joining DNA repair in fungi, dramatically increases the gene disruption efficiency. The frequency of disrupting the conidiation-associated gene Cag8 in ?MrKu70 was 93% compared to 7% in the wild-type strain. Since ?MrKu70 is not different from the wild-type strain in development, pathogenicity and tolerance to various abiotic stresses, it can be used as a recipient strain for a systematic gene disruption project to characterize the whole suite of genes involved in the biological processes of M. robertsii.
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Validation of a novel clinical prediction score for severe coronary artery diseases before elective coronary angiography.
PLoS ONE
PUBLISHED: 01-01-2014
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Coronary artery disease (CAD) severity is associated with patient prognosis. However, few efficient scoring systems have been developed to screen severe CAD in patients with stable angina and suspected CAD before coronary angiography. Here, we present a novel scoring system for CAD severity before elective coronary angiography.
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Comparison of diagnostic efficacy of contrast-enhanced ultrasound, acoustic radiation force impulse imaging, and their combined use in differentiating focal solid thyroid nodules.
PLoS ONE
PUBLISHED: 01-01-2014
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A key limitation of conventional ultrasound (US) includes poor differentiation of benign from malignant thyroid nodules. Contrast-enhanced US (CEUS) and acoustic radiation force impulse (ARFI) could provide better characterization of focal thyroid nodules; however, no studies have compared their efficacies.
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[Distribution and activation of dendritic cells in immune thrombocytopenia patients].
Zhongguo Shi Yan Xue Ye Xue Za Zhi
PUBLISHED: 12-28-2013
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Defective dendritic cell (DC) functions have been implicated in ITP. The purpose of this study was to investigate the distribution and activation of dendritic cells in immune thrombocytopenia (ITP) patients. ITP patients were divided into 3 groups:the newly diagnosed, refractory and effective treatment group. The distributions of plasmacytoid dendritic cells(pDC) and myeloid dendritic cells(mDC) in peripheral blood, bone marrow and spleen were detected with flow cytometry. The expression level of CD80 and CD86 on surface of pDC and mDC was also detected with flow cytometry. The results indicated that the percentage of mDC was higher than that of pDC in all sites of all groups. The percentage of mDC and pDC in all site of refractory group was higher than that in newly diagnosed and effective groups, but the percentage of mDC in spleen of refractory group was obviously higher than that in other sites. The percentage of pDC was no significant different in all groups. The expression level of CD86 in all groups was higher than that of CD80, the expression level of CD80 was lower in mDC and pDC of all groups, but there was no obvious difference in all sites. The CD86 expression in all site of refractory group was higher than that in newly diagnosed and effective treatment groups, while the CD86 expression of mDC in spleen of newly diagnosed group obviouly higher than that in other sites. It is concluded that the distribntion abnormality of mDC and pDC exists in ITP patients, the mDC are more accumulated in spleen, and differentiation of mDC to maturity is more obvious in spleen, spleen-derived mDC significantly express CD86, spleen-derived mDC may play an important role in the pathogenesis of ITP.
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[Effects of Corbrin Shugan capsule on dimethylnitrosamine-induced hepatic fibrosis in rats].
Zhejiang Da Xue Xue Bao Yi Xue Ban
PUBLISHED: 10-30-2013
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To investigate the effects of Corbrin Shugan capsule on dimethylnitrosamine (DMN)-induced hepatic fibrosis in rats.
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Design, synthesis and cytotoxic activity of novel sulfonylurea derivatives of podophyllotoxin.
Bioorg. Med. Chem.
PUBLISHED: 10-01-2013
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Three series of novel sulfonylurea podophyllotoxin derivatives were designed, synthesized, and evaluated for in vitro cytotoxicity against four tumor cell lines (A-549, DU-145, KB and KBvin). Compounds 14c (IC50: 1.41-1.76?M) and 14e (IC50: 1.72-2.01?M) showed superior cytotoxic activity compared with etoposide (IC50: 2.03 to >20?M), a clinically available anticancer drug. Significantly, most of the compounds exhibited comparable cytotoxicity against the drug-resistant tumor cell line KBvin, while etoposide lost activity completely. Preliminary structure-activity relationship (SAR) correlations indicated that the 4-O-methyl functionality in podophyllotoxin analogues may be essential to maintain cytotoxic activity, while an arylsulfonylurea side chain at podophyllotoxins 4? position can significantly improve cytotoxic activity.
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Digital Gene Expression analysis in the midgut of 4008 silkworm strain infected with cytoplasmic polyhedrosis virus.
J. Invertebr. Pathol.
PUBLISHED: 09-16-2013
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Digital Gene Expression was performed to investigate the midgut transcriptome profile of 4008 silkworm strain orally infected with BmCPV. A total of 4,498,263 and 4,258,240 clean tags were obtained from the control and BmCPV-infected larvae. A total of 752 differentially expressed genes were detected, of which 649 were upregulated and 103 were downregulated. Analysis results of the Kyoto Encyclopedia of Genes and Genomes pathway showed that 334 genes were involved in the ribosome and RNA transport pathways. Moreover, 408 of the 752 differentially expressed genes have a GO category and can be categorized into 41 functional groups according to molecular function, cellular component and biological process. Differentially expressed genes involved in signaling, gene expression, metabolic process, cell death, binding, and catalytic activity changes were detected in the expression profiles. Quantitative real-time PCR was performed to verify the expression of these genes. The upregulated expression levels of Calreticulin, FK506-binding protein, and protein kinase c inhibitor gene probably led to a calcium-dependent apoptosis in the BmCPV-infected cells. The results of this study may serve as a basis for future research not only on the molecular mechanism of BmCPV invasion but also on the anti-BmCPV mechanism of silkworm.
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[Neutralization of interleukin-17 aggravates respiratory infection induced by Chlamydia trachomatis in mice].
Beijing Da Xue Xue Bao
PUBLISHED: 08-14-2013
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To evaluate the role of interleukin-17 (IL-17) in respiratory infection with Chlamydia trachomatis in mice.
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Change of hs-CRP, sVCAM-1, NT-proBNP levels in patients with pregnancy-induced hypertension after therapy with magnesium sulfate and nifudipine.
Asian Pac J Trop Med
PUBLISHED: 08-10-2013
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To investigate the change of the hs-CRP, sVCAM-1, NT-proBNP levels of the patients with pregnancy-induced hypertension (PIH) syndrome.
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Serum tumor markers, hypoxia-inducible factor-1? HIF-1? and vascular endothelial growth factor, in patients with non- small cell lung cancer before and after intervention.
Asian Pac. J. Cancer Prev.
PUBLISHED: 07-27-2013
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To explore changes in the serum tumor makers, hypoxia-inducible factor-1? (HIF-1?) and vascular endothelial growth factor (VEGF) level and their relations in patients with non-small cell lung cancer (NSCLC) before and after intervention.
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Development of a neuromedin U-human serum albumin conjugate as a long-acting candidate for the treatment of obesity and diabetes. Comparison with the PEGylated peptide.
J. Pept. Sci.
PUBLISHED: 07-19-2013
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Neuromedin U (NMU) is an endogenous peptide implicated in the regulation of feeding, energy homeostasis, and glycemic control, which is being considered for the therapy of obesity and diabetes. A key liability of NMU as a therapeutic is its very short half-life in vivo. We show here that conjugation of NMU to human serum albumin (HSA) yields a compound with long circulatory half-life, which maintains full potency at both the peripheral and central NMU receptors. Initial attempts to conjugate NMU via the prevalent strategy of reacting a maleimide derivative of the peptide with the free thiol of Cys34 of HSA met with limited success, because the resulting conjugate was unstable?in vivo. Use of a haloacetyl derivative of the peptide led instead to the formation of a metabolically stable conjugate. HSA-NMU displayed long-lasting, potent anorectic, and glucose-normalizing activity. When compared side by side with a previously described PEG conjugate, HSA-NMU proved superior on a molar basis. Collectively, our results reinforce the notion that NMU-based therapeutics are promising candidates for the treatment of obesity and diabetes. Copyright © 2013 European Peptide Society and John Wiley & Sons, Ltd.
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A solid AND logic stimuli-responsive material with bright nondestructive performance designed by sensitive cuprophilicity.
Chem. Commun. (Camb.)
PUBLISHED: 06-28-2013
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A stimuli-responsive material with AND logic function was realized by modulating sensitive Cu-Cu interactions, which is quite different from traditional photoinduced electron transfer (PET) strategies. The obtained material not only gets rid of fluid media, but also displays nondestructive, high intensity optical signals and environmentally friendly performances.
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Effects of osmolytes on Pelodiscus sinensis creatine kinase: a study on thermal denaturation and aggregation.
Int. J. Biol. Macromol.
PUBLISHED: 05-28-2013
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The protective effect of osmolytes on the thermal denaturation and aggregation of Pelodiscus sinensis muscle creatine kinase (PSCK) was investigated by a combination of spectroscopic methods and thermodynamic analysis. Our results demonstrated that the addition of osmolytes, such as glycine and proline, could prevent thermal denaturation and aggregation of PSCK in a concentration-dependent manner. When the concentration of glycine and proline increased in the denatured system, the relative activation was significantly enhanced; meanwhile, the aggregation of PSCK during thermal denaturation was decreased. Spectrofluorometer results showed that glycine and proline significantly decreased the tertiary structural changes of PSCK and that thermal denaturation directly induced PSCK aggregation. In addition, we also built the 3D structure of PSCK and osmolytes by homology models. The results of computational docking simulations showed that the docking energy was relatively low and that the clustering groups were spread to the surface of PSCK, indicating that osmolytes directly protect the surface of the protein. P. sinensis are poikilothermic and quite sensitive to the change of ambient temperature; however, there were few studies on the thermal denaturation of reptile CK. Our study provides important insight into the protective effects of osmolytes on thermal denaturation and aggregation of PSCK.
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n-Butanol soluble fraction of the water extract of Chinese toon fruit ameliorated focal brain ischemic insult in rats via inhibition of oxidative stress and inflammation.
J Ethnopharmacol
PUBLISHED: 05-01-2013
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Toona sinensis Roem. (Meliaceae; Toona sinensis; Chinese toon) is a type of arbor that is widely distributed in Asia. The fruits of Toona sinensis Roem has been traditionally recognized for treatment of cerebrovascular diseases. To evaluate the potential clinical use of the fruits of Toona sinensis Roem, we determined the dose dependence of the neuroprotective efficacy in a focal cerebral ischemic reperfusion model of rats and explored the underlying mechanisms.
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[Study of prognostic related factors of elderly patients with T/NK cell lymphoma].
Zhonghua Xue Ye Xue Za Zhi
PUBLISHED: 04-20-2013
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To analyze the prognostic related factors of elderly patients with T/NK cell lymphoma.
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Executive function in children and adolescents with posttraumatic stress disorder 4 and 12 months after the Sichuan earthquake in China.
J Child Psychol Psychiatry
PUBLISHED: 04-16-2013
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While several studies have found executive function deficits in adults and maltreated children with posttraumatic stress disorder (PTSD), there are few data on executive function in children and adolescents with PTSD related to natural disasters. The objective of this study was to test executive function changes over time in children and adolescents with PTSD after a magnitude 8.0 earthquake in Sichuan, China.
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[Practical executive function performance in high intelligence quotient children and adolescents with attention-deficit/hyperactivity disorder].
Zhonghua Yi Xue Za Zhi
PUBLISHED: 04-11-2013
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To explore the practical executive function profiles in high IQ (intelligence quotient) children and adolescents with attention deficit hyperactivity disorder (ADHD) in a Chinese sample population.
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Application of acoustic radiation force impulse imaging for the evaluation of focal liver lesion elasticity.
HBPD INT
PUBLISHED: 04-06-2013
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Acoustic radiation force impulse (ARFI) imaging is a new elastography method for the evaluation of tissue stiffness. This study aims to evaluate the performance of ARFI in noninvasive assessment of the tissue stiffness of focal liver lesion (FLL) and to explore its potential value in the differential diagnosis of FLL.
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[Development of real-time fluorescent quantitative PCR method for detecting Bombyx mori cytoplasmic polyhedrosis virus].
Bing Du Xue Bao
PUBLISHED: 04-04-2013
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A pair of specific primers were designed according to the published 118 bp conserved sequence of polyhedrin gene of Bombyx mori cytoplasmic polyhedrosis virus (BmCPV) in GenBank and a serial dilutions of a recombinant plasmid were prepared and used to generate standard curves, to establish a real-time fluorescent quantitative PCR method for detection of BmCPV. The results showed that the linear relationship between virus concentration (X) and Ct (Y) was Y = -3. 582 lgX + 38.748 with the correlation coefficient R2 = 0999. The method was very sensitive, specific and reproducible. It can be applied in the rapid detection of BmCPV and the prevalence investigation of this disease.
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Potential schistosomiasis foci in China: A prospective study for schistosomiasis surveillance and response.
Acta Trop.
PUBLISHED: 04-03-2013
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Schistosomiasis japonica was endemic in 12 provinces (including municipalities and autonomous regions) in the Peoples Republic of China (PR China). Despite the tremendous decrease of schistosomiasis incidence after almost 60 years of control, the distribution of snail-breeding sites has not been reduced significantly. In order to verify current transmission risks and identify the potential establishment of new foci of schistosomiasis driven by environmental changes, we conducted surveillance in selected risk areas of three provinces: Jiangsu, Anhui and Shandong from 2008 to 2010 in addition to routine snail surveillance. We investigated populations and possible reservoirs in sentinel sites and report that the total number of new acute cases did not diminish further in spite of ongoing control activities. In Anhui Province the local count compared to the national count was 43% (19/44) in 2008, 33% (25/75) in 2009 and 40% (17/42) in 2010. In all, 31.58km(2) areas of snail breeding sites were newly detected nationwide through the year 2008-2010, of which the proportion of Anhui was 42% (5.03/11.98) in 2008, 95% (8.39/8.79) in 2009 and 79% (8.52/10.81) in 2010. Sentinel surveillance showed eight, nine and five confirmed cases of acute schistosomiasis in mobile populations (fishermen, migrant workers) in 2008, 2009 and 2010, respectively. All these cases were detected in Chaohu County, which must therefore be deemed an area at risk. We conclude that continuous surveillance with an emphasis on snails must be enhanced in potential risk areas in PR China.
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[Clinical value of inferior vena caval filter insertion under color Doppler flow imaging guidance through the right internal jugular vein].
Nan Fang Yi Ke Da Xue Xue Bao
PUBLISHED: 03-27-2013
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To explore the efficacy and feasibility of color Doppler flow imaging (CDFI)-guided inferior vena caval filter (IVCF) insertion through the right internal jugular vein for prevention of pulmonary embolism in patients with deep venous thrombosis (DVT).
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Antifeedant activity of spin-labeled derivatives of deoxypodophyllotoxin against Brontispa longissima larvae.
Nat Prod Commun
PUBLISHED: 03-22-2013
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To continue our search for natural product-based compounds for the control of Brontispa longissima larvae, eight spin-labeled podophyllotoxin derivatives (4a-h) and the intermediates 2 and 3 were tested for their insect antifeedant activity against third-instar larvae of B. longissima. Among all the tested compounds, 4a, 4c, 2 and 3 showed pronounced antifeedant activities with AFC50 values of 0.16, 0.31, 0.15 and 0.28 mg/mL, respectively. The different antifeedant activity ranges of these compounds indicated that variation of the structures of L-amino acids in these compounds markedly affected the activity profiles of this compound class, and some important SAR information has been revealed from it.
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Retrograde approach for the recanalization of coronary chronic total occlusion: collateral selection and collateral related complication.
Chin. Med. J.
PUBLISHED: 03-20-2013
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The retrograde approach through collaterals has been applied in the treatment of chronic total occlusion (CTO) lesions during percutaneous recanalization of coronary arteries. This study was to investigate the success rate of recanalization and collateral related complications in patients when using the retrograde approach.
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Design, synthesis and bioactivity evaluation of novel benzophenone hydrazone derivatives.
Pest Manag. Sci.
PUBLISHED: 03-09-2013
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Benzophenone hydrazone derivatives are among the most important classes of synthetic insecticides. In an effort to discover new molecules with good insecticidal/acaricidal activities, a series of novel benzophenone hydrazone N-acylated thiourea and urea derivatives was synthesized and bioassayed.
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Comparison of the neural differentiation potential of human mesenchymal stem cells from amniotic fluid and adult bone marrow.
Cell. Mol. Neurobiol.
PUBLISHED: 03-01-2013
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Human mesenchymal stem cells (MSCs) are considered a promising tool for cell-based therapies of nervous system diseases. Bone marrow (BM) has been the traditional source of MSCs (BM-MSCs). However, there are some limitations for their clinical use, such as the decline in cell number and differentiation potential with age. Recently, amniotic fluid (AF)-derived MSCs (AF-MSCs) have been shown to express embryonic and adult stem cell markers, and can differentiate into cells of all three germ layers. In this study, we isolated AF-MSCs from second-trimester AF by limiting dilution and compared their proliferative capacity, multipotency, neural differentiation ability, and secretion of neurotrophins to those of BM-MSCs. AF-MSCs showed a higher proliferative capacity and more rapidly formed and expanded neurospheres compared to those of BM-MSCs. Both immunocytochemical and quantitative real-time PCR analyses demonstrated that AF-MSCs showed higher expression of neural stemness markers than those of BM-MSCs following neural stem cell (NSC) differentiation. Furthermore, the levels of brain-derived growth factor and nerve growth factor secreted by AF-MSCs in the culture medium were higher than those of BM-MSCs. In addition, AF-MSCs maintained a normal karyotype in long-term cultures after NSC differentiation and were not tumorigenic in vivo. Our findings suggest that AF-MSCs are a promising and safe alternative to BM-MSCs for therapy of nervous system diseases.
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Effects of Sargassum fusiforme polysaccharides on antioxidant activities and intestinal functions in mice.
Int. J. Biol. Macromol.
PUBLISHED: 02-20-2013
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Sargassum fusiforme is a kind of brown algae that has been widely consumed not only as food, but also as herbal medicine for thousands of years. The purpose of this study was to investigate the antioxidant activities and intestinal functions of polysaccharides extracted from S. fusiforme (SFP) in normal and cyclophosphamide-induced immunosuppressed mice. The experiment was performed on six groups of ICR mice, which treated with cyclophosphamide (CY, 200 mg/kg) or different dosages of SFP for 14 days. The results showed that administration of SFP was able to overcome the immunosuppression, and significantly increased the spleen index and antioxidant activities in mice (P<0.05). It also remarkably improved the numbers of jejunal intraepithelial lymphocytes (IELs) and goblet cells in immunosuppressed mice (P<0.05). For normal mice, SFP increased both thymus index and intestinal function parameters such as villus length/crypt depth ratio and intestinal IELs and goblet cells (P<0.05). The results suggested that SFP, possessing pronounced antioxidant activities, may play an important role in the improvement of intestinal function in mice. This might be one of the possible mechanisms of SFP for the immunomodulatory effects.
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Silver pyroarsonates obtained from Ag(I)-mediated in situ condensation of aryl arsonate ligands under solvothermal conditions.
Inorg Chem
PUBLISHED: 02-06-2013
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Four new layered silver(I) organoarsonates, namely, [Ag(3)(L(3))(CN)] (1) (H(2)L(3) = (PhAsO(2)H)(2)O), [Ag(3)(L(4))(CN)] (2) (H(2)L(4) = (2-NO(2)-C(6)H(4)-AsO(2)H)(2)O), [Ag(3)(HL(5))(H(2)L(5))] (3) (H(3)L(5) = 3-NO(2)-4-OH-C(6)H(3)-AsO(3)H(2)) and [Ag(2)(HL(5))] (4), were synthesized under solvothermal conditions. During the preparations of 1 and 2, condensation of organoarsonate ligands (H(2)L(1) = Ph-AsO(3)H(2); H(2)L(2) = 2-NO(2)-C(6)H(4)-AsO(3)H(2)) and the decomposition of acetonitrile molecules to cyanide anions occurred. Single crystals of H(2)L(4) ligand and compounds 1-4 were isolated, and their crystal structures have been determined by single crystal X-ray diffraction studies. In 1, the one-dimensional (1D) chains based on Ag(I) ions and {L(3)}(2-) anions are further interconnected by CN(-) into two-dimensional (2D) layers. In 2, adjacent Ag(I) ions within the silver(I) organoarsonate layer are further bridged by ?(4)-CN(-) anions with very short Ag···Ag contacts. In 3, the hexanuclear {Ag(6)O(12)} clusters are interconnected by bridging organoarsonate ligands into a silver(I) arsonate hybrid layer. In 4, the right-handed {Ag(4)O(4)} chains are further interconnected by organoarsonate ligands as well as additional Ag-O-Ag bridges into a novel silver(I) arsonate layer. Compounds 1 and 2 display red and orange-red emissions, respectively, which may be assigned to be an admixture of ligand-to-metal charge transfer (LMCT) and metal-centered (4d-5s/5p) transitions perturbed by Ag(I)···Ag(I) interactions. Upon cooling from room temperature to 10 K, compound 1 exhibits interesting temperature-dependent emissions.
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The developmental trajectories of executive function of children and adolescents with Attention Deficit Hyperactivity Disorder.
Res Dev Disabil
PUBLISHED: 01-30-2013
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This study examined the developmental trajectories of executive function (EF) of children and adolescents with Attention Deficit Hyperactivity Disorder (ADHD) in Han Chinese. Five hundred and fifteen children and adolescents with ADHD and 249 healthy controls took part in this study. All of them were administered four EF tests capturing inhibition, working memory, shifting and planning components. The participants were further divided into four age groups, 7-8, 9-10, 11-12, and 13-15 years old, respectively, for developmental trajectories comparison. The performance of the typical developing children and adolescents aged 7-15 were reported to get stable at age 11-12 for inhibition, working memory and planning, and kept developing till age 13-15 for shifting. For inhibition and shifting, participants with ADHD displayed similar performance to the healthy controls who were 2 years younger whereas they did poorer than the healthy controls of their same age. And at age 13-15, such poorer performance disappeared for inhibition but maintained for shifting. No significant differences were found between participants with and without ADHD in working memory and planning across all age groups. The current findings suggested, compared with healthy controls, Han Chinese children and adolescents with ADHD displayed delayed developmental trajectories on inhibition and shifting, whereas they showed similar trend of development on working memory and planning.
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The association between hepatitis B virus infection and disease activity, synovitis, or joint destruction in rheumatoid arthritis.
Clin. Rheumatol.
PUBLISHED: 01-23-2013
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The prevalence of chronic hepatitis B virus (HBV) infection in China is high. Four percent of patients with HBV infection can present with polyarthritis and positive rheumatic factor similar to rheumatoid arthritis (RA). Here, we investigated the association between HBV infection and serological, radiological, or histological disease status in RA. According to HBV infection status, 223 consecutive hospitalized Chinese patients with RA were divided into the groups of chronic HBV infection, past HBV infection, and no HBV infection. Clinical data and hand radiographs were collected. Synovium was obtained by closed-needle biopsy, and serial tissue sections were stained immunohistochemically for HBV surface antigen (HBsAg) and cluster of differentiation (CD) markers. (1) The prevalence of HBsAg positivity and chronic hepatitis B in RA was consistent with the age-matched general Chinese population (11.2 vs. 8.7 %, 1.7 vs. 1.0 %, respectively, P?>?0.05). (2) Clinical parameters, disease activity score in 28 joints, or Sharp scores showed no significant difference among the three groups in 206 RA or 140 treatment-naïve patients, both with active disease (all P?>?0.05). (3) Synovial immunohistochemical staining showed negative HBsAg in ten RA patients with HBV carrier status and ten RA patients with past HBV infection. Except for higher subintimal CD3+ cell density in the past HBV infection group, Krenns synovitis score, mean densities of subintima positive-staining cells (CD20, CD38, CD79a, and CD68), and CD34+ microvessel counts showed no significant difference among RA patients with HBV carrier status, past HBV infection, or no HBV infection (all P?>?0.05). Chronic HBV infection may have no significant effect on disease activity, synovitis, or joint destruction in RA.
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Design, synthesis and potent cytotoxic activity of novel podophyllotoxin derivatives.
Bioorg. Med. Chem.
PUBLISHED: 01-18-2013
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Twenty new acyl thiourea derivatives of podophyllotoxin and 4-demethylepipodophyllotoxin were prepared and screened for their cytotoxicity against four human tumor cell lines, A-549, DU-145, KB, and KBvin. With IC50 values of 0.098-1.13 ?M, compounds 13b, 13c, and 13o displayed much better cytotoxic activity than the control etoposide. Most importantly, 13b and 13o exhibited promising cytotoxicity against the drug resistant tumor cell line KBvin with IC50 values of 0.098 and 0.13 ?M, respectively, while etoposide lost activity completely. Structure-activity relationship (SAR) correlations of the new derivatives have been established. Compounds 13b and 13o merit further development as a new generation of epipodophyllotoxin-derived antitumor clinical trial candidates.
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