Methyl brevifolincarboxylate, a novel influenza virus PB2 inhibitor from Canarium Album (Lour.) Raeusch.,Chemical Biology & Drug Design

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Methyl brevifolincarboxylate, a novel influenza virus PB2 inhibitor from Canarium Album (Lour.) Raeusch.
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2020-06-09 , DOI: 10.1111/cbdd.13740
Fangzhao Chen ₁ , Luoping Yang ₁ , Lingyan Zhai ₁ , Yingna Huang ₁ , Feimin Chen ₁ , Wenjun Duan ₁ , Jie Yang ₁

Affiliation

Methyl brevifolincarboxylate (MBC) was isolated from ethyl acetate extract of Canarium album (Lour.) Raeusch. The structure was identified, and the effect on influenza A virus infection was evaluated. MBC exhibited inhibitory activity against influenza virus A/Puerto Rico/8/34 (H1N1) and A/Aichi/2/68 (H3N2) with IC₅₀ values of 27.16 ± 1.39 μM and 33.41 ± 2.34 μM. Mechanism studies indicated that MBC inhibited the replication of influenza A virus by targeting PB2 cap‐binding domain. Our results demonstrated MBC was a potent PB2 cap‐binding inhibitor and represented as a new type of promising lead compound for the development of anti‐influenza virus drugs from natural products.

中文翻译：

Methyl brevifolincarboxylate，一种来自 Canarium Album (Lour.) Raeusch 的新型流感病毒 PB2 抑制剂。

从Canarium album (Lour.) Raeusch 的乙酸乙酯提取物中分离出短叶黄素羧酸甲酯 (MBC) 。确定了结构，并评估了对甲型流感病毒感染的影响。MBC 对流感病毒 A/Puerto Rico/8/34 (H1N1) 和 A/Aichi/2/68 (H3N2) 表现出抑制活性，IC ₅₀值为 27.16 ± 1.39 μM 和 33.41 ± 2.34 μM。机制研究表明，MBC 通过靶向 PB2 帽结合域来抑制甲型流感病毒的复制。我们的结果表明 MBC 是一种有效的 PB2 帽结合抑制剂，是一种新型的有前途的先导化合物，用于从天然产物中开发抗流感病毒药物。

更新日期：2020-06-09

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