Evaluating Cepharanthine Analogues as Natural Drugs Against SARS-CoV-2

    November 2021 in “ FEBS Open Bio
    Atsushi Hijikata, Clara Shionyu‐Mitsuyama, Setsu Nakae, Masafumi Shionyu, Motonori Ota, Shigehiko Kanaya, Takatsugu Hirokawa, Shogo Nakajima, Koichi Watashi, Tsuyoshi Shirai
    TLDR Cepharanthine analogues, especially tetrandrine, show potential for treating COVID-19.
    The study evaluated cepharanthine (CEP) analogues as potential natural drugs against SARS-CoV-2, using in silico docking simulations and in vitro infection assays. CEP showed potent activity in inhibiting SARS-CoV-2 infection, with IC50 and IC90 values of 1.90 µm and 4.46 µm, respectively, outperforming other analogues like tetrandrine (TET). The study suggested that CEP and TET might interact with human lysosomal membrane proteins but did not show a strong preference for specific targets. The diphenyl ester moiety was identified as a potential pharmacophore, and the study highlighted the challenge of drug-induced phospholipidosis, suggesting modifications to CEP derivatives to reduce adverse effects while maintaining efficacy.
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