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Characterization of a New Antienterovirus D68 Compound Purified from Avocado.
ACS Infectious Diseases ( IF 4.0 ) Pub Date : 2020-06-22 , DOI: 10.1021/acsinfecdis.0c00404
Minetaro Arita 1 , Hiroyuki Fuchino 2 , Hitomi Kawakami 2 , Masami Ezaki 2 , Nobuo Kawahara 2
Affiliation  

One of the major challenges in development of antienterovirus (EV) drugs is in the safety of the drug. Here, we attempted to identify anti-EV compounds from an edible plant extract library and found potent antienterovirus D68 (EV-D68) activity in avocado (Persea americana). The purified identity is determined as 2R,4R-(12Z,15Z)-heneicosa-12,15-diene-1,2,4-triol, named avoenin. Avoenin shows an EC50 of 2.0 μM for EV-D68 (Fermon) infection with CC50 of >150 μM in RD cells by targeting the uncoating step of EV-D68 infection. Resistant mutations of EV-D68 (VP3-V24I, S173P, and S180G) to avoenin confer cross-resistance to pleconaril, an uncoating inhibitor of EV-D68. The inhibitory effect of avoenin is substantially specific to EV-D68 among the EVs. This work reveals avoenin as the identity of anti-EV-D68 activity in avocado and offers insights into development of a novel and effective strategy to overcome EV-D68 infection and its related respiratory diseases.

中文翻译:

从鳄梨中纯化的新抗肠病毒D68化合物的表征。

抗肠病毒(EV)药物开发的主要挑战之一是药物的安全性。在这里,我们尝试从可食用植物提取物文库中鉴定抗EV化合物,并在鳄梨(Persea americana)中发现了有效的抗肠道病毒D68(EV-D68)活性。纯化的身份确定为2 R,4 R-(12 Z,15 Z)-heneicosa-12,15-二烯-1,2,4-三醇,称为avoenin。Avoenin对CC 50的EV-D68(Fermon)感染的EC 50为2.0μM通过靶向EV-D68感染的脱膜步骤,在RD细胞中获得> 150μM的抗性。EV-D68(VP3-V24I,S173P和S180G)对avoenin的抗性突变赋予对pleconaril的交叉抗性,pleconaril是EV-D68的脱膜抑制剂。在电动汽车中,avoenin的抑制作用基本上对EV-D68具有特异性。这项工作揭示了avoenin是鳄梨中抗EV-D68活性的特征,并为开发克服EV-D68感染及其相关呼吸系统疾病的新颖有效策略提供了见识。
更新日期:2020-08-14
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