The 8-bromobaicalein inhibited the replication of dengue, and Zika viruses and targeted the dengue polymerase

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,...

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Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2023
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10039358/
https://www.ncbi.nlm.nih.gov/pubmed/36966240
http://dx.doi.org/10.1038/s41598-023-32049-x
Descripción
Sumario: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.

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