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Articles by Santosh G. Tupe in JoVE
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Development of Metarhizium anisopliae as a Mycoinsecticide: From Isolation to Field Performance
Santosh G. Tupe1, Ejaj K. Pathan1, Mukund V. Deshpande1
1Biochemical Sciences Division, CSIR-National Chemical Laboratory
Here, we report the different stages involved in the knowledge-based development of an effective mycoinsecticide, including the isolation, identification, screening, and selection of the "best-fit" entomopathogenic fungus, Metarhizium anisopliae, for the control of insect pests in agriculture.
Other articles by Santosh G. Tupe on PubMed
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Effect of Different Dietary Zinc Levels on Hepatic Antioxidant and Micronutrients Indices Under Oxidative Stress Conditions
Metabolism: Clinical and Experimental.
Nov, 2010 |
Pubmed ID: 20359724 Dietary zinc (Zn) status exerts a powerful influence on the degree of oxidative damage caused by free radicals. We examined the effect of dietary Zn variations with oxidative stress (OS) treatment on antioxidant status, liver function, and status of vitamins in male Wistar rats. Oxidative stress was generated by intraperitoneal injections of tert-butyl hydroperoxide; and dietary Zn variations done were Zn deficient, normal, and excess, with 8, 30, and 60 mg Zn per kilogram diet, respectively. After 21-day dietary regimen, the animals were killed; and plasma aspartate aminotransferase, alanine aminotransferase, hepatic antioxidant enzymes (catalase, superoxide dismutase, glutathione peroxidase), Zn, reduced glutathione, lipid peroxidation (LPO), and hepatic riboflavin, nicotinic acid, and ascorbic acid estimations were done. The alanine aminotransferase and aspartate aminotransferase levels were elevated in rats with OS and Zn-deficient diet, which were restored to normal levels with excess dietary Zn. Hepatic antioxidant enzymes and reduced glutathione levels were significantly decreased with concomitant increase in LPO due to OS induction in animals with Zn-deficient diet. Corresponding enhanced enzyme activities, higher hepatic Zn, and lowered LPO were observed in animals with normal- and excess-Zn diet. A dose-dependent increase in hepatic nicotinic acid accumulation was observed as the dietary Zn level increased from deficient to excess; however, there was no influence on riboflavin and ascorbic acid status. The results suggest that Zn may have a therapeutic potential in treatment of oxidative liver damage along with enhanced nicotinic acid absorption.
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Dietary Nicotinic Acid Supplementation Improves Hepatic Zinc Uptake and Offers Hepatoprotection Against Oxidative Damage
The British Journal of Nutrition.
Jun, 2011 |
Pubmed ID: 21262064 We examined the effect of dietary nicotinic acid (NA) variations before and after oxidative stress (OS) treatment on the antioxidant defence system, function and morphology of the liver along with Zn status in rats. OS was generated by three intraperitoneal injections of tert-butyl hydroperoxide in the first week for the pre-exposure group and in the third week for the post-exposure group, respectively. These groups were further divided into subgroups and fed on a diet with marginally deficient Zn (10 mg Zn/kg diet) and NA variations as NA deficient, normal and excess with 10, 30 and 1000 mg NA/kg diet, respectively. Aspartate aminotransferase and alanine aminotransferase levels were elevated in rats with OS coupled with the Zn- and NA-deficient diet, which decreased towards normal with excess dietary NA. Excess NA supplementation in the OS pre-exposure group resulted in nearly preserved hepatic architecture with normal hepatocytes, whereas maximum tissue destruction was evident in the post-exposure group with NA deficiency. Dose-dependent improvement in the antioxidant defence system, enhanced reduced glutathione levels, lowered lipid peroxidation and higher hepatic Zn levels were observed with NA supplementation. The effect was more prominent in the pre-exposure group. In conclusion, dietary NA supplementation improves hepatic Zn uptake and results in hepatoprotection against OS-induced damage in rats.
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Hybrid Molecules of Carvacrol and Benzoyl Urea/thiourea with Potential Applications in Agriculture and Medicine
Bioorganic & Medicinal Chemistry Letters.
Sep, 2012 |
Pubmed ID: 22850211 Benzoyl phenyl urea, a class of insect growth regulator's acts by inhibiting chitin synthesis. Carvacrol, a naturally occurring monoterpenoid is an effective antifungal agent. We have structurally modified carvacrol (2-methyl-5-[1-methylethyl] phenol) by introducing benzoylphenyl urea linkage. Two series of benzoylcarvacryl thiourea (BCTU, 4a-f) and benzoylcarvacryl urea (BCU, 5a-f) derivatives were prepared and characterized by elemental analysis, IR, (1)H and (13)C NMR and Mass spectroscopy. Derivatives 4b, 4d, 4e, 4f and 5d, 5f showed comparable insecticidal activity with the standard BPU lufenuron against Dysdercus koenigii. BCTU derivatives 4c, 4e and BCU 5c showed good antifungal activity against phytopathogenic fungi viz. Magnaporthe grisae, Fusarium oxysporum, Dreschlera oryzae; food spoilage yeasts viz. Debaromyces hansenii, Pichia membranifaciens; and human pathogens viz. Candida albicans and Cryptococcus neoformans. Compounds 5d, 5e and 5f showed potent activity against human pathogens. Moderate and selective activity was observed for other compounds. All the synthesized compounds were non-haemolytic. These compounds have potential application in agriculture and medicine.
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Antifungal Dimeric Chalcone Derivative Kamalachalcone E from Mallotus Philippinensis
Natural Product Research.
2014 |
Pubmed ID: 24099509 From the red coloured extract (Kamala) prepared through acetone extraction of the fresh whole uncrushed fruits of Mallotus philippinensis, one new dimeric chalcone (1) along with three known compounds 1-(5,7-dihydroxy-2,2,6-trimethyl-2H-1-benzopyran-8-yl)-3-phenyl-2-propen-1-one (2), rottlerin (3) and 4'-hydroxyrottlerin (4) were isolated. The structure of compound 1 was elucidated by 1D and 2D NMR analyses that included HSQC, HMBC, COSY and ROESY experiments along with the literature comparison. Compounds 1-4 were evaluated for antifungal activity against different human pathogenic yeasts and filamentous fungi. The antiproliferative activity of the compounds was evaluated against Thp-1 cell lines. Compounds 1 and 2 both exhibited IC50 of 8, 4 and 16 μg/mL against Cryptococcus neoformans PRL518, C. neoformans ATCC32045 and Aspergillus fumigatus, respectively. Compound 4, at 100 μg/mL, showed 54% growth inhibition of Thp-1 cell lines.
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Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation
ACS Medicinal Chemistry Letters.
Nov, 2015 |
Pubmed ID: 26617963 Known morpholine class antifungals (fenpropimorph, fenpropidin, and amorolfine) were synthetically modified through silicon incorporation to have 15 sila-analogues. Twelve sila-analogues exhibited potent antifungal activity against different human fungal pathogens such as Candida albicans, Candida glabrata, Candida tropicalis, Cryptococcus neoformans, and Aspergillus niger. Sila-analogue 24 (fenpropimorph analogue) was the best in our hands, which showed superior fungicidal potential than fenpropidin, fenpropimorph, and amorolfine. The mode of action of sila-analogues was similar to morpholines, i.e., inhibition of sterol reductase and sterol isomerase enzymes of ergosterol synthesis pathway.
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Ultrasound- and Molecular Sieves-Assisted Synthesis, Molecular Docking and Antifungal Evaluation of 5-(4-(Benzyloxy)-substituted Phenyl)-3-((phenylamino)methyl)-1,3,4-oxadiazole-2(3H)-thiones
Molecules (Basel, Switzerland).
May, 2016 |
Pubmed ID: 27171073 A novel series of 5-(4-(benzyloxy)substituted phenyl)-3-((phenyl amino)methyl)-1,3,4-oxadiazole-2(3H)-thione Mannich bases 6a-o were synthesized in good yield from the key compound 5-(4-(benzyloxy)phenyl)-1,3,4-oxadiazole-2(3H)-thione by aminomethylation with paraformaldehyde and substituted amines using molecular sieves and sonication as green chemistry tools. The antifungal activity of the new products was evaluated against seven human pathogenic fungal strains, namely, Candida albicans ATCC 24433, Candida albicans ATCC 10231, Candida glabrata NCYC 388, Cryptococcus neoformans ATCC 34664, Cryptococcus neoformans PRL 518, Aspergillus fumigatus NCIM 902 and Aspergillus niger ATCC 10578. The synthesized compounds 6d, 6f, 6g, 6h and 6j exhibited promising antifungal activity against the tested fungal pathogens. In molecular docking studies, derivatives 6c, 6f and 6i showed good binding at the active site of C. albicans cytochrome P450 enzyme lanosterol 14 α-demethylase. The in vitro antifungal activity results and docking studies indicated that the synthesized compounds have potential antifungal activity and can be further optimized as privileged scaffolds to design and develop potent antifungal drugs.
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