Scientific reports · 2023
The 8-bromobaicalein inhibited the replication of dengue, and Zika viruses and targeted the dengue polymerase.
СтатьяПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод в очереди
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Boonyasuppayakorn Siwaporn, Saelee Thanaphon, Huynh Thao Nguyen Thanh, Hairani Rita, Hengphasatporn Kowit, Loeanurit Naphat, Cao Van, Vibulakhaophan Vipanee, Siripitakpong Panattida, Kaur Parveen, Chu Justin Jang Hann, Tunghirun Chairat, Choksupmanee Opas, Chimnaronk Sarin, Shigeta Yasuteru, Rungrotmongkol Thanyada, Chavasiri Warinthorn
Аннотация
Dengue and Zika viruses are mosquito-borne flaviviruses burdening millions every year with hemorrhagic fever and neurological symptoms. Baicalein was previously reported as a potential anti-flaviviral candidate and halogenation of flavones and flavanones potentiated their antiviral efficacies. Here, we reported that a chemically modified 8-bromobaicalein effectively inhibited all dengue serotypes and Zika viruses at 0.66-0.88 micromolar in cell-based system. The compound bound to dengue serotype 2 conserved pocket and inhibited the dengue RdRp activity with 6.93 fold more than the original baicalein. Moreover, the compound was mildly toxic against infant and adult C57BL/6 mice despite administering continuously for 7 days. Therefore, the 8-bromobaicalein should be investigated further in pharmacokinetics and efficacy in an animal model.