Influenza a Virus Inhibition: Evaluating Computationally Identified Cyproheptadine Through In Vitro Assessment

Influenza is still a chronic global health threat, inducing a sustained search for effective antiviral therapeutics. Computational methods have played a pivotal role in developing small molecule therapeutics. In this study, we applied a combined in silico and in vitro approach to explore the potential anti-influenza activity of cyproheptadine, a clinically used histamine H1 receptor antagonist. Virtual screening based on the average quasivalence number (AQVN) and electron-ion interaction potential (EIIP) descriptors suggests similarities between cyproheptadine and several established anti-influenza agents. The subsequent ligand-based pharmacophore screening of a focused H1 antagonist library was aligned with the bioinformatics prediction, and further experimental in vitro evaluation of cyproheptadine demonstrated its anti-influenza activity. These findings provide proof of concept for cyproheptadine's in silico-predicted antiviral potential and underscore the value of integrating computational predictions with experimental validation. The results of the current study provide a preliminary proof of concept for the predicted anti-influenza potential based on computational analysis and emphasize the utility of integrating in silico screening with experimental validation in the early stages of drug repurposing efforts.

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Publication Details

Journal
International Journal of Molecular Sciences
Published
2025-06-21
DOI
https://doi.org/10.3390/ijms26135962
Primary Topic
Computational Drug Discovery Methods
Type
article
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article

Influenza a Virus Inhibition: Evaluating Computationally Identified Cyproheptadine Through In Vitro Assessment

Natalya Bukreyeva, Andrej Perdih, Slobodan Paessler, Milan Senćanski et al.
International Journal of Molecular Sciences
Computational Drug Discovery Methods
article

Influenza a Virus Inhibition: Evaluating Computationally Identified Cyproheptadine Through In Vitro Assessment

Natalya Bukreyeva, Andrej Perdih, Slobodan Paessler, Milan Senćanski, Veljko Veljković, Kristina Stevanović, Bruno Botta, Vladimir Perović, Ayub Darji, Draginja Radošević, Sanja Glišić, Sergi López-Serrano, Mattia Mori, Junki Maruyama
article en

Abstract

Influenza is still a chronic global health threat, inducing a sustained search for effective antiviral therapeutics. Computational methods have played a pivotal role in developing small molecule therapeutics. In this study, we applied a combined in silico and in vitro approach to explore the potential anti-influenza activity of cyproheptadine, a clinically used histamine H1 receptor antagonist. Virtual screening based on the average quasivalence number (AQVN) and electron-ion interaction potential (EIIP) descriptors suggests similarities between cyproheptadine and several established anti-influenza agents. The subsequent ligand-based pharmacophore screening of a focused H1 antagonist library was aligned with the bioinformatics prediction, and further experimental in vitro evaluation of cyproheptadine demonstrated its anti-influenza activity. These findings provide proof of concept for cyproheptadine's in silico-predicted antiviral potential and underscore the value of integrating computational predictions with experimental validation. The results of the current study provide a preliminary proof of concept for the predicted anti-influenza potential based on computational analysis and emphasize the utility of integrating in silico screening with experimental validation in the early stages of drug repurposing efforts.

International Journal of Molecular SciencesVol. 26(13)
University of Siena (IT), Universitat Autònoma de Barcelona (ES), University of Ljubljana (SI), Universitat Pompeu Fabra (ES), Barcelona Biomedical Research Park (ES), University of Belgrade (RS), Biomed Protection (United States) (US), Centre de Recerca en Sanitat Animal (ES), National Institute of Chemistry (SI), The University of Texas Medical Branch at Galveston (US), Sapienza University of Rome (IT)
Openalex Percentile: Top 84%
Computational Drug Discovery Methods
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