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Identification and synthesis of quinolizidines with anti-influenza a virus activity.

ABSTRACT: Influenza A virus infection causes a contagious respiratory illness that poses a threat to human health. However, there are limited anti-influenza A therapeutics available, which is further compounded by the emergence of drug resistant viruses. In this study, Sophora quinolizidine alkaloids were identified as a new class of anti-influenza A virus agents. Among the tested Sophora alkaloids, dihydroaloperine exhibited the most potent activity with an EC50 of 11.2 ?M. The potency of the quinolizidine alkaloids was improved by approximately 5-fold with chemical modifications on the aloperine molecule. These compounds were effective against an H1N1 influenza A virus that was resistant to the two antiflu drugs oseltamivir and amantadine. The identification of the quinolizidine alkaloids as effective and novel anti-influenza A agents may aid in the development of new therapeutics.

SUBMITTER: Dang Z

PROVIDER: S-EPMC4137370 | biostudies-literature | 2014 Aug

REPOSITORIES: biostudies-literature

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Identification and synthesis of quinolizidines with anti-influenza a virus activity.

Dang Zhao Z Jung Katherine K Zhu Lei L Lai Weihong W Xie Hua H Lee Kuo-Hsiung KH Huang Li L Chen Chin-Ho CH

ACS medicinal chemistry letters 20140630 8

Influenza A virus infection causes a contagious respiratory illness that poses a threat to human health. However, there are limited anti-influenza A therapeutics available, which is further compounded by the emergence of drug resistant viruses. In this study, Sophora quinolizidine alkaloids were identified as a new class of anti-influenza A virus agents. Among the tested Sophora alkaloids, dihydroaloperine exhibited the most potent activity with an EC50 of 11.2 μM. The potency of the quinolizidi ...[more]

PMID: 25147619

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