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从微花苘麻中分离出的抗呼吸道病毒成分。

Antiviral constituents against respiratory viruses from Mikania micrantha.

机构信息

Department of Biology and Biochemistry and Institute of Chinese Medicine, The Chinese University of Hong Kong, Shatin, Hong Kong, People's Republic of China.

出版信息

J Nat Prod. 2009 May 22;72(5):925-8. doi: 10.1021/np800542t.

Abstract

Phytochemical investigation of the dried aerial parts of Mikania micrantha led to the isolation of a new sesquiterpene, 3beta-acetoxy-1,10-epoxy-4-germacrene-12,8;15,6-diolide (1), along with six known constituents: 1,10-epoxy-4-germacrene-12,8;15,6-diolide (2), dihydromikanolide (3), potassium mikanin 3-sulfate (4), mikanin (5), alpinetin (6), and ergosta-7,22-dien-3beta-ol (7). Their structures were elucidated by spectroscopic methods, and the molecular structures and stereochemistry of sesquiterpene lactones 1-3 were revealed by single-crystal X-ray analysis. Compound 2 showed moderate activity against respiratory syncytial virus (IC(50) = 37.4 uM) and parainfluenza type 3 virus (IC(50) = 37.4 uM) with a therapeutic index (TI) of 16.0 for both compounds. Compound 4, the main component of M. micrantha, exhibited inhibitory activity against parainfluenza type 3 virus with IC(50) (19.7 uM) and TI (24.0) values comparable to those of ribavirin, serving as a positive control.

摘要

对薇甘菊干燥地上部分的植物化学研究导致了一种新的倍半萜的分离,3β-乙酰氧基-1,10-环氧-4-愈创木烯-12,8;15,6-二醇内酯(1),以及六个已知的成分:1,10-环氧-4-愈创木烯-12,8;15,6-二醇内酯(2),二氢愈创木内酯(3),钾米卡宁 3-硫酸盐(4),米卡宁(5),白杨素(6)和麦角甾-7,22-二烯-3β-醇(7)。它们的结构通过光谱方法阐明,并且倍半萜内酯 1-3 的分子结构和立体化学通过单晶 X 射线分析揭示。化合物 2 对呼吸道合胞病毒(IC50 = 37.4 μM)和副流感 3 型病毒(IC50 = 37.4 μM)表现出中等活性,两者的治疗指数(TI)均为 16.0。4 号化合物,薇甘菊的主要成分,对副流感 3 型病毒具有抑制活性,IC50(19.7 μM)和 TI(24.0)值与利巴韦林相当,作为阳性对照。

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