Schistosomiasis, a parasitic disease caused by Schistosoma species such as S. haematobium, S. mansoni, and S. japonicum, poses a significant global health burden. The thioredoxin glutathione reductase (TGR) enzyme, crucial for maintaining the parasite's redox balance and preventing oxidative stress, has been identified as a promising target for anti-schistosomal drug development. This study aims to identify potential TGR inhibitors from Azadirachta indica phytochemicals using molecular modeling approaches. We screened 60 compounds derived from A. indica bark and leaves through molecular docking to assess their binding affinity, followed by the evaluation of binding-free energies for the most promising candidates. Drug-likeness and pharmacokinetic properties were assessed, and molecular dynamics simulations were conducted to explore the conformational stability of the protein-ligand complexes. Our findings revealed that several A. indica compounds exhibited significantly lower docking scores (up to -9.669 kcal/mol) compared to the standard drug praziquantel (-4.349 kcal/mol). Notably, Isorhamnetin, Isomargolonone, Nimbaflavone, Quercetin, and Nimbionol demonstrated strong interactions with TGR, although Isorhamnetin showed potential mutagenicity. Further binding free energy calculations and molecular dynamics simulations confirmed the stability of Isomargolonone, Nimbionol, and Quercetin as potential TGR inhibitors. In conclusion, these findings suggest that Isomargolonone, Nimbionol, and Quercetin warrant further experimental validation as promising candidates for anti-schistosomal therapy.

Download full-text PDF

Source
http://dx.doi.org/10.1007/s12013-024-01577-2DOI Listing

Publication Analysis

Top Keywords

azadirachta indica
8
thioredoxin glutathione
8
glutathione reductase
8
potential tgr
8
tgr inhibitors
8
promising candidates
8
molecular dynamics
8
dynamics simulations
8
isomargolonone nimbionol
8
nimbionol quercetin
8

Similar Publications

Hospital surfaces are often contaminated with multidrug-resistant pathogenic bacteria that cause healthcare-associated infections and lead to increased mortality and morbidity. There is a need for new alternative antibacterial agents to overcome antibiotic resistance. Azadirachta indica and Simmondsia chinensis have been found to possess antibacterial activity and medicinal value.

View Article and Find Full Text PDF

Introduction: Silver nanoparticles (AgNPs) derived from natural sources have garnered significant attention due to their unique properties and eco-friendly production methods. With lung cancer remaining a major global health issue, there is a continuous need for novel and effective therapeutic approaches beyond conventional treatments such as chemotherapy, immunotherapy, and targeted therapies.

Objective: This study aims to synthesize AgNPs using plant extracts from Gymnema sylvestre, Moringa oleifera, and Azadirachta indica and to evaluate their anticancer activity, particularly their effects on gene expression in A549 lung cancer cells.

View Article and Find Full Text PDF

Evaluation of the Effect of Applying Chitosan, Neem, Tulsi, Aloe vera, and Chlorhexidine Solutions on the Shear Bond Strength of Composite to Dentin.

J Dent (Shiraz)

December 2024

Postgraduate Student, Dept. of Operative Dentistry, Biomaterials Research Center, School of Dentistry, Shiraz University of Medical Sciences, Shiraz, Iran.

Statement Of The Problem: Dentin adhesion is challenging and needs modifications. Newly introduced nature-derived materials may be a useful solution in improving dentin adhesion. The use of natural antimicrobial agents for pretreating prepared dentin surfaces before restoration has become of interest.

View Article and Find Full Text PDF

The current study was designed to investigate the effect of A. indica (Neem) leaf extracts (ethanolic and aqueous) in yeast-induced pyrexia and acetic acid-induced writhing in rat models to evaluate the antipyretic and analgesic biomarkers and its phytochemical screening with computational analysis. For the antipyretic activity model 60 albino rats (160-200g) of either sex were divided into 4 groups and all groups were injected with yeast to induce pyrexia.

View Article and Find Full Text PDF

This study aimed to determine the chemical composition of ginger Zingiber officinale Roscoe (Zingiberaceae) and soursop Annona muricata Linn (Annonaceae) oils, formulate stable emulsions of these oils separately, as well as neem oil Azadirachta indica A. Juss (Meliaceae), and evaluate the insecticidal activity of these emulsions against Duponchelia fovealis Zeller, 1847 (Lepidoptera: Crambidae). Each stable emulsion contained an oil phase containing ginger, soursop, or neem oil, a fruit polyalcohol-based emulsifier, ethanol, or water.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!