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.
Authors
- Natalya Bukreyeva
- Andrej Perdih (ORCID: https://orcid.org/0000-0002-6645-9231)
- Slobodan Paessler (ORCID: https://orcid.org/0000-0002-2213-9551)
- Milan Senćanski (ORCID: https://orcid.org/0000-0002-7296-3223)
- Veljko Veljković (ORCID: https://orcid.org/0000-0002-1980-0927)
- Kristina Stevanović (ORCID: https://orcid.org/0009-0002-7066-426X)
- Bruno Botta (ORCID: https://orcid.org/0000-0001-8707-4333)
- Vladimir Perović (ORCID: https://orcid.org/0000-0002-3700-6452)
- Ayub Darji (ORCID: https://orcid.org/0000-0002-0967-3303)
- Draginja Radošević (ORCID: https://orcid.org/0000-0002-3284-7201)
- Sanja Glišić (ORCID: https://orcid.org/0000-0001-5691-1055)
- Sergi López-Serrano (ORCID: https://orcid.org/0000-0002-0968-7713)
- Mattia Mori (ORCID: https://orcid.org/0000-0003-2398-1254)
- Junki Maruyama (ORCID: https://orcid.org/0000-0003-0088-4793)
Institutions
- 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)
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
- Field-Weighted Citation Impact
- 0.00