Virtual Screening of candidate Bio-actives from selected medicinal plants against rilpivirine resistance in HIV

E3S Web of Conferences
2024.0

Abstract

HIV, the causative virus of AIDS, has posed a severe threat to global health for an extensive period. Recent statistics show the magnitude of this challenge, with approximately 2.4 million people in India living with HIV, along with 41.97 thousand deaths which were reported in 2021. In the face of this on-going crisis, patients have relied heavily on anti-retroviral therapies, among which Rilpivirine stands out as a key treatment option, particularly for individuals exhibiting low viral loads. However, the efficacy of Rilpivirine diminishes significantly in patients against high viral loads of HIV-1C, leading to the emergence of drug-resistant strains. Consequently, there exists an urgent need to identify and develop more potent therapeutic agents to combat HIV infection. To address this, we performed an in-silicon investigation, utilizing virtual screening tools to explore potential alternative drugs to Rilpivirine for HIV treatment. Our methodology involved mining data from reputable sources such as the PubChemand Zinc databases to identify compounds with potential antiretroviral activity. We subjected these compounds to screening using the SwissADME tool, evaluating their pharmacokinetic characteristics and adherence to Lipinski's rule of five. Compounds demonstrating favourable properties, as indicated by zero violations in OSIRIS Property Explorer, were then prioritized for further analysis. The structural frameworks of Rilpivirine protein-ligand complexes, both native (7Z2D) and mutant (7Z2E) variants, were procured from the Protein Data Bank (PDB). Further, ligand molecules' structural configurations were sourced from databases such as PubChem and Corinasoftware. Employing molecular docking simulations facilitated by HDOCK docking software, the binding affinities of these ligands against the receptor protein-ligand complexes were studied, from which, Schumannificine emerged as the most promising candidate, exhibiting the most stable binding interactions.In summation, out of 65 phytochemicals, our comprehensive investigation underscores the potential of Schumannificine (CID: 184890), an alkaloid compound derived from the Schumanniophytonmagnificum plant as a novel and viable therapeutic option for HIV patients. © The Authors.

Knowledge Graph

Similar Paper

Virtual Screening of candidate Bio-actives from selected medicinal plants against rilpivirine resistance in HIV
E3S Web of Conferences 2024.0
In Search of a Novel Anti-HIV Drug:  Multidisciplinary Coordination in the Discovery of 4-[[4-[[4-[(1E)-2-Cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, Rilpivirine)
Journal of Medicinal Chemistry 2005.0
Molecular docking and dynamics studies for the identification of Nipah virus glycoprotein inhibitors from Indian medicinal plants
Journal of Biomolecular Structure and Dynamics 2023.0
Rubrisandrins A and B, Lignans and Related Anti-HIV Compounds from <i>Schisandra rubriflora</i>
Journal of Natural Products 2006.0
Novel natural non-nucleoside inhibitors of HIV-1 reverse transcriptase identified by shape- and structure-based virtual screening techniques
European Journal of Medicinal Chemistry 2019.0
Structure-Based Virtual Screening for the Discovery of Natural Inhibitors for Human Rhinovirus Coat Protein
Journal of Medicinal Chemistry 2008.0
Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus
Journal of Medicinal Chemistry 2016.0
Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus
Bioorganic &amp; Medicinal Chemistry Letters 2017.0
Niruriside, a New HIV REV/RRE Binding Inhibitor from <i>Phyllanthus niruri</i>
Journal of Natural Products 1996.0
Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant <i>Justicia gendarussa</i>
Journal of Natural Products 2017.0