phytochemical-profiling-gas-chromatographymass-spectrometry-analysis

Phytochemical Profiling, Gas Chromatography&#8211;Mass Spectrometry Analysis, and <em>In Vivo</em> Activity of <em>Terminalia mantaly</em> in Rats

Synthetic drugs for inflammation, pain, and fever are effective but often cause adverse effects, increasing interest in plant-derived therapeutic ...

Bahauddin Zakariya University

Health Services Academy

Complications of diabetic foot can be prevented using a naturally occurring, efficient, and newly synthesized antimicrobial agent. The purpose of the study was to improve wound healing and antibacterial effects of quercetin and its esterified complex with 4-formyl phenyl boronic acid (4FPBA-Q) compared with phenytoin. The formation of the 4FPBA-Q complex was confirmed by thin-layer chromatography (TLC), Fourier transform infrared (FTIR) spectroscopy, and mass spectrometry (MS). The prepared 4FPBA-Q complex was used against Gram-positive bacteria along with Gram-negative bacteria, and more than 2-fold decrease in minimum inhibitory concentrations (MIC) was observed compared to pure quercetin. Scanning electron microscopic images of  and  showed their complete destruction after incubation with the 4FPBA-Q complex even after 3 h. Interestingly, wound-healing properties of the 4FPBA-Q complex in infected diabetic rats increased from 64 to 99% as compared to phenytoin, which were increased from those of noninfected diabetic rats. Furthermore, histopathological evaluations showed significantly enhanced wound healing, re-epithelialization, fibroblasts, and angiogenesis in wounds of diabetic rats after 10 days. Conclusively, reduction in the primary irritation index (PDII) and improved antibacterial and wound-healing properties render the 4FPBA-Q complex ideal for diabetic foot ulcer treatment.

Wound-Healing and Antibacterial Activity of the Quercetin-4-Formyl Phenyl Boronic Acid Complex against Bacterial Pathogens of Diabetic Foot Ulcer.

Transdermal penetration of therapeutic moieties from topical dosage forms always remains a challenge due to the presence of permeation impeding keratin which should be addressed. The purpose of the study was to formulate quercetin and 4-formyl phenyl boronic acid (QB complex) used for the preparation of nanoethosomal keratolytic gel (EF3-G). The QB complex was confirmed by Fourier transform infrared spectroscopy while skin permeation, viscosity, and epalrestat entrapment efficiency were used for the optimization of nanoethosomal gel. The keratolytic effect of the proposed nanoethosomal gel with urea (QB + EPL + U) was calculated in rat and snake skin. The spherical shape of nanoethosomes was confirmed by scanning electron microscopy. According to the findings of stability studies, viscosity decreases as temperature increases, proving their thermal stability. The negative charge of optimized EF3 with 0.7 PDI proved narrow particle size distribution with homogeneity. Optimized EF3 showed two folds increase of epalrestat permeation in highly keratinized snake skin as compared to rats' skin after 24 h. Antioxidant behaviors of EF3 (QB) > QB complex > quercetin > ascorbic acid proved reduction of oxidative stress in DPPH reduction analysis. Interestingly, the hot plate and cold allodynia test in the diabetic neuropathic rat model reduced 3-fold pain as compared to the diabetic control group which was further confirmed by in vivo biochemical studies even after the eight week. Conclusively, ureal keratolysis, primary dermal irritation index reduction, and improved loading of epalrestat render the nanoethosomal gel (EF3-G) ideal for the treatment of diabetic neuropathic pain.

Exploring the Potent Combination of Quercetin-Boronic Acid, Epalrestat, and Urea Containing Nanoethosomal Keratolytic Gel for the Treatment of Diabetic Neuropathic Pain: In Vitro and In Vivo Studies.

This study investigates the novel application of Phenyl Boronic Acid Functionalized-Quercetin nanoparticles (PBA-Qt NPs) in the context of antibacterial and diabetic wound healing. The research reveals a multifaceted approach, encompassing physicochemical characterization, antioxidant activity, antibacterial potential, and wound healing efficacy. The purpose of the study was to improve wound healing and antibacterial effects of quercetin and its esterified nanoparticles with phenyl boronic acid (PBA-Qt) compared with phenytoin streptozotocin-induced diabetic rats as a model. PBA-Qt NPs were confirmed using TLC, SEM, and FTIR. They exhibited superior DPPH scavenging (84.2 ± 0.12 %) compared to PBA (59.00 ± 0.18 %) and quercetin (79.02 ± 0.17 %). PBA-Qt showed significant antimicrobial properties with ZOI against Gram-negative (30.34 ± 0.02) and Gram-positive bacteria (25.40 ± 0.03). The MIC for  was 1.41 ± 0.03 μg/100 μL, and for , it was 8.25 ± 0.02 μg/100 μL. The MBC against  was 4.33 ± 0.02 μg/100 μL, and for , it was 8.25 ± 0.02 μg/100 μL. PBA-Qt NPs reduced MIC for both Gram-positive and Gram-negative bacteria compared to quercetin. They enhanced wound healing by 60-99 % in infected diabetic rats, outperforming phenytoin. PBA-Qt NPs stimulated angiogenesis, tissue repair, and regeneration, improving wound closure. In diabetic and non-diabetic wounds, PBA-Qt NPs demonstrated superior wound contraction and granulation tissue formation. In conclusion, PBA-Qt nanoparticles are promising for treating diabetic chronic wounds due to reduced irritation and enhanced antibacterial and wound-healing properties.

Unlocking the potential of phenyl boronic acid functionalized-quercetin nanoparticles: Advancing antibacterial efficacy and diabetic wound healing.

Doxycycline (DX) is a drug of choice for the treatment of periodontitis, with the limitation of requiring a high dose, which may be overcome by the preparation of a targeted controlled-release hydrogel containing a newly synthesized yeast-malic acid crosslinker (YMC). YMC was synthesized  thermochemical modification of yeast with malic acid at 100-140 °C and compared with glutaraldehyde-saturated toluene (GST). Swelling capacity, acid and carboxyl content, scanning electron microscopy (SEM) imaging, Brunauer-Emmett-Teller (BET) analysis, viscosity, cross-linking density, DX loading and release behavior at pH 6.5, mucoadhesion, and antimicrobial and periodontal efficacy of the glutaraldehyde hydrogel (HGG) and YMC hydrogel (HGY) were compared. Changes from C-O (1421 cm) to C[double bond, length as m-dash]OOR (1702 cm) in the infrared spectroscopy, along with changes in the degree of substitution from 0 to 0.39, degree of esterification from 0 to 40 ± 1.5 and COOH content from 129 ± 0.5 to 290 ± 0.5 (meq. per 100 g), were found between yeast to YMC, respectively. The results revealed 1.5 times more dynamic swelling, 0.25-fold decrease in acid content, 2.3-fold increase in carboxyl content, and 1.2- and 2.1-fold increases in cross-linking density and viscosity of HGY as compared to HGG, respectively. The SEM and BET results revealed that HGY had a 2 times greater porous surface than HGG. HGY/DX was 35 ± 2% more effective in controlling periodontitis bacteria, decreased periodontal depth from 4 to 3.2 mm, and gingival index from 3 to 1 as compared to HGG/DX in patients suffering from periodontitis. HGY/DX not only serves as a tool for the controlled release of DX in periodontal pockets but also contributes to the treatment of gingival periodontitis.

A yeast-malic acid crosslinker/polyacrylic acid hydrogel containing doxycycline for the treatment of periodontitis.

The ocular bioavailability of a drug is inadequate due to physiological constraints. In this study, an ocular film of Levodopa (LD) using thiolated hemicellulose (THC) with improved mucoadhesion and permeation was made. Linseed hemicellulose (LHC) was extracted, and its esterification was done with thioglycolic acid (TGA), L cysteine (LC), and thiourea (TU). Maximum thiolation of LHC was confirmed by Ellman's test, Fourier-transformed infrared spectroscopy (FTIR), scanning electron microscopy (SEM), X-ray diffraction (XRD), thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC). Primary eye irritation tests and histopathological studies of different ocular tissues like cornea, conjunctiva, and sclera conducted on rabbit eyes exhibited nontoxic and non-irritant behavior of LHC and optimized derivative of LHC with TGA (THT-960) which was further used for the preparation of LD-containing ocular films i.e., LD-THC, LD-THT960, and LD-THT960-THC, respectively. Ascorbic acid was added to the ocular film to prevent oxidation of LD. Ex-vivo permeation studies from bovine cornea showed a 1.8fold increase in corneal permeation of LD while ocular irritancy by hen egg chorioallantoic membrane (HET-CAM) test and histopathological analysis confirmed nonirritant and nontoxic nature of THT-960. Conclusively, LD-THT960 due to improved mucoadhesion and corneal permeation of LD can be used effectively for the potential treatment of myopia.

Thiolated hemicellulose containing mucoadhesive and permeation-enhancing ocular films of levodopa for potential treatment of myopia.

Visceral bleeding poses a significant threat, requiring effective management through positively charged chitosan. This study aimed to address the limitations of chitosan-based hemostatic hydrogels by synthesizing a modified maleic anhydride complex of chitosan (MAC). Biocompatibility, biodegradability, and non-toxicity made MAC a suitable candidate for super porous hydrogels (SPHs) used in hemostatic applications. Graft polymerization synthesized MAC, confirmed via Fourier transform infrared spectroscopy, demonstrating superior antioxidant activity compared to chitosan and maleic anhydride. SPHs were prepared using MAC alone and with N, N-methylene bisacrylamide (MBA) as crosslinkers. MAC exhibited higher water absorbency and pH-dependent swelling than the MBA-chitosan complex. Drug loading and entrapment efficiency varied with the drug-to-SPH ratio. In vitro drug release studies showed sustained release (SR) with SPHs-MAC following zero-order kinetics and SPHs-MBA following Korsmeyer-Peppas. SPHs-MAC gelled more rapidly with temperature changes, and MAC hydrogels showed larger antimicrobial zones of inhibition (28±2).In vivo hemostasis studies revealed rapid hemostatic effects with MACL-H, reducing blood loss to 78.5 ± 1.5 mg in iver rat models. MAC hydrogels significantly lowered blood loss in rat tail amputation models compared to controls. This formulation demonstrates strong potential for effective visceral bleeding management.

Chitosan/Maleic anhydride and Itaconic acid super porous hydrogels, containing levofloxacin for the treatment of visceral bleeding.

Corrigendum to "Thiolated hemicellulose containing mucoadhesive and permeation-enhancing ocular films of levodopa for potential treatment of myopia" [Int. J. Biol. Macromol. 309 (2025) 142901].

[This retracts the article DOI: 10.1016/j.heliyon.2023.e23452.].

Retraction notice to "Unlocking the potential of phenyl boronic acid functionalized-quercetin nanoparticles: Advancing antibacterial efficacy and diabetic wound healing" [Heliyon 10 (2024) e23452].

Article	Year
Wound-Healing and Antibacterial Activity of the Quercetin-4-Formyl Phenyl Boronic Acid Complex against Bacterial Pathogens of Diabetic Foot Ulcer. ACS omega\| PubMed ID: 35874257	2022
Exploring the Potent Combination of Quercetin-Boronic Acid, Epalrestat, and Urea Containing Nanoethosomal Keratolytic Gel for the Treatment of Diabetic Neuropathic Pain: In Vitro and In Vivo... Molecular pharmaceutics\| PubMed ID: 37246527	2023
Unlocking the potential of phenyl boronic acid functionalized-quercetin nanoparticles: Advancing antibacterial efficacy and diabetic wound healing. Heliyon\| PubMed ID: 38169972	2024
A yeast-malic acid crosslinker/polyacrylic acid hydrogel containing doxycycline for the treatment of periodontitis. RSC advances\| PubMed ID: 39139228	2024
Thiolated hemicellulose containing mucoadhesive and permeation-enhancing ocular films of levodopa for potential treatment of myopia. International journal of biological macromolecules\| PubMed ID: 40203929	2025
Chitosan/Maleic anhydride and Itaconic acid super porous hydrogels, containing levofloxacin for the treatment of visceral bleeding. Anais da Academia Brasileira de Ciencias\| PubMed ID: 40366923	2025
Corrigendum to "Thiolated hemicellulose containing mucoadhesive and permeation-enhancing ocular films of levodopa for potential treatment of myopia" [Int. J. Biol. Macromol. 309 (2025) 14290... International journal of biological macromolecules\| PubMed ID: 40973517	2025
Retraction notice to "Unlocking the potential of phenyl boronic acid functionalized-quercetin nanoparticles: Advancing antibacterial efficacy and diabetic wound healing" [Heliyon 10 (2024) e... Heliyon\| PubMed ID: 41216508	2025

Hafiz Muhammad Usman Abid

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