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从[来源未提及]中分离得到的三种新香豆素及其对猪流行性腹泻病毒（PEDV）的抑制活性。

Three new coumarins from and their porcine epidemic diarrhea virus (PEDV) inhibitory activity.

作者信息

Yang Jun-Li, Dhodary Basanta, Quy Ha Thi Kim, Kim Jinwoong, Kim Eunhee, Oh Won Keun

机构信息

Korea Bioactive Natural Material Bank, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.

Choong Ang Vaccine Laboratory, 59-3 Hwaam-dong, Yuseong-gu, Daejeon 305-348, Republic of Korea.

出版信息

Tetrahedron. 2015 Jul 8;71(28):4651-4658. doi: 10.1016/j.tet.2015.04.092. Epub 2015 Apr 30.

DOI:10.1016/j.tet.2015.04.092
PMID:32287428
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7111744/
Abstract

Swine based agro-industries throughout the world are in big threat of new PEDV infection due to lack of efficient prophylactic defenses as well as dependable curing agents. Bioactivity-guided fractionation of a methanol soluble extract from radix of led to the isolation of three new (-) together with 10 known coumarins (-). The structures of new isolates (-) were established by extensive spectroscopic analysis and their absolute configurations were assigned based on ECD spectra calculation and analysis. Among all isolates, compound  revealed strongest inhibitory effect on PEDV replication. Quantitative real-time PCR data showed inhibitory effect of on genes responsible for synthesis of PEDV vital structural proteins (GP6 nucleocapsid, GP2 spike, and GP5 membrane) in a dose-dependent manner. Also, compound demonstrated the inhibitory effect on PEDV GP6 nucleocapsid and GP2 spike protein synthesis as analyzed by western blotting. This study represents a new class of chemical entities for developing anti-PEDV agents.

摘要

由于缺乏有效的预防性防御措施以及可靠的治疗药物，全球以猪为基础的农业产业面临新型猪流行性腹泻病毒（PEDV）感染的巨大威胁。对某植物根甲醇提取物进行生物活性导向的分离，得到了3个新的（-）以及10个已知的香豆素（-）。通过广泛的光谱分析确定了新分离物（-）的结构，并基于电子圆二色光谱（ECD）计算和分析确定了它们的绝对构型。在所有分离物中，化合物对PEDV复制表现出最强的抑制作用。定量实时PCR数据显示，对负责PEDV重要结构蛋白（GP6核衣壳、GP2刺突和GP5膜）合成的基因具有剂量依赖性抑制作用。此外，通过蛋白质免疫印迹分析表明，化合物对PEDV GP6核衣壳和GP2刺突蛋白的合成也有抑制作用。本研究代表了一类用于开发抗PEDV药物的新型化学实体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/49d2/7111744/5f6a156a7856/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/49d2/7111744/ef1e486a1e5e/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/49d2/7111744/5f6a156a7856/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/49d2/7111744/ef1e486a1e5e/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/49d2/7111744/5f6a156a7856/gr1.jpg

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