Author(s):
1. Salman Zafar:
Institute of Chemical Sciences, University of Peshawar,Peshawar- 25120,Pakistan
2. Muhammad Iqbal Choudhary:
Institute of Chemical Sciences, University of Peshawar,Peshawar- 25120,Pakistan
Abstract:
Biotransformation represents a valuable strategy for the generation ofstructurally diverse libraries of bioactive molecules. The present studyinvestigated the microbial transformation of dihydrotestosterone (DHT) with theobjective of identifying potential cholinesterase inhibitors. Employing wholecellcultures of Macrophomina phaseolina and Gibberella fujikuroi, eightstructurally distinct derivatives were obtained. Transformation by M. phaseolinayielded two previously characterized metabolites, while six known compoundswere produced via transformation with G. fujikuroi. Among these metabolites,three exhibited significant and selective inhibitory activities against the butyrylcholinesterase (BChE) enzyme. Furthermore, molecular docking simulationsdemonstrated strong concordance with experimental results, providing theoreticalvalidation and mechanistic insights into enzyme ligand interactions. Given thecentral role of cholinesterase inhibition in the therapeutic management ofAlzheimer’s disease (AD), these preliminary findings, corroborated by in silicoanalyses, offer promising leads for the development of more potent and selectivecholinesterase inhibitors as potential candidates in AD treatment.
Page(s):
76-76
DOI:
DOI not available
Published:
Journal: 4th International Conference of Sciences “Revamped Scientific Outlook of 21st Century, 2025” , November 12,2025, Volume: 1, Issue: 1, Year: 2025
Keywords:
dihydrotestosterone
,
Alzheimers Disease
,
Molecular dockingsimulation
,
Butyrylcholinesterase inhibition
,
Microbial transformation
References:
References are not available for this document.
Citations
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