Antiviral activity of geldanamycin and its derivatives against influenza virus
Taechowisan, Thongchai; Samsawat, Tipparat; Puckdee, Winyou; Phutdhawong, Waya S..
Artículo
| IMSEAR | ID: sea-210735
Two new geldanamycin derivatives such as 17-(tryptamine)-17-demethoxygeldanamycin (2) andC17 methoxyl of geldanamycin (1). Their antiviral activity was evaluated based on influenza virus propagation inembryonated chicken eggs and viral absorption by hemagglutination (HA) inhibition test. The findings indicatedthat these compounds inhibited viral propagation at a concentration of 12.5 µg/ml. For the viral absorption, onlycompounds 2 and 3 inhibited HA at a concentration of 50 µg/ml. The solubility of compounds 2 and 3 in waterwas 290 and 306 µM, higher than that of compound 1 about 1.91 and 2.01 times, respectively. The compounds 2and 3 showed a moderate cytotoxic activity on LLC-MK2 and Vero cells with IC50 values of >200.00 µg/ml. Theseresults demonstrated the invention of tryptamine-geldanamycin hybrids to prevent influenza virus infection in viralabsorption and viral propagation steps.
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