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具有强大抗病毒作用的牡荆素类黄酮糖苷类化合物存在于榕树叶中。

Potent antiviral flavone glycosides from Ficus benjamina leaves.

机构信息

Department of Virology and Developmental Genetics, Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer-Sheva, Israel.

出版信息

Fitoterapia. 2012 Mar;83(2):362-7. doi: 10.1016/j.fitote.2011.11.014. Epub 2011 Dec 3.

DOI:10.1016/j.fitote.2011.11.014
PMID:22155188
Abstract

Crude ethanol extracts from Ficus benjamina leaves strongly inhibit Herpes Simplex Virus 1 and 2 (HSV-1/2) as well as Varicella Zoster Virus (VZV) cell infection in vitro. Bioassay-guided fractionation of the crude extract demonstrated that the most efficient inhibition of HSV-1 and HSV-2 was obtained with the flavonoid fraction. The present study was aimed to further isolate, purify and identify substances with potent antiviral activity from the flavonoid fraction of F. benjamina extracts. Flavonoids were collected from the leaf ethanol extracts through repeated purification procedure and HPLC analysis. The antiviral activity of each substance was then evaluated in cell culture. Three known flavone glycosides, (1) quercetin 3-O-rutinoside, (2) kaempferol 3-O-rutinoside and (3) kaempferol 3-O-robinobioside, showing highest antiviral efficiency were selected and their structure was determined by spectroscopic analyses including NMR and mass spectrometry (MS). These three flavones were highly effective against HSV-1 reaching a selectivity index (SI) of 266, 100 and 666 for compound 1, 2 and 3, respectively, while the SI of their aglycons, quercetin and kaempferol amounted only in 7.1 and 3.2, respectively. Kaempferol 3-O-robinobioside showed similar SI to that of acyclovir (ACV), the standard anti-HSV drug. Although highly effective against HSV-1 and HSV-2, these flavone glycosides did not show any significant activity against VZV.

摘要

榕树叶的粗乙醇提取物强烈抑制单纯疱疹病毒 1 和 2(HSV-1/2)以及水痘带状疱疹病毒(VZV)细胞感染体外。生物测定指导的粗提物的分馏表明,HSV-1 和 HSV-2 的最有效抑制是用黄酮类化合物获得的。本研究旨在从榕树叶提取物的黄酮类化合物中进一步分离、纯化和鉴定具有强抗病毒活性的物质。黄酮类化合物从叶乙醇提取物中通过重复的纯化程序和 HPLC 分析收集。然后在细胞培养中评估每种物质的抗病毒活性。三种已知的黄酮苷,(1)槲皮素 3-O-芸香糖苷,(2)山奈酚 3-O-芸香糖苷和(3)山奈酚 3-O-新橙皮糖苷,显示出最高的抗病毒效率,通过包括 NMR 和质谱(MS)在内的光谱分析确定其结构。这三种黄酮类化合物对 HSV-1 非常有效,化合物 1、2 和 3 的选择性指数(SI)分别达到 266、100 和 666,而它们的糖苷,槲皮素和山奈酚的 SI 仅为 7.1 和 3.2。山奈酚 3-O-新橙皮糖苷对 ACV(阿昔洛韦)的抗病毒活性与标准抗病毒药物相似。尽管对 HSV-1 和 HSV-2 非常有效,但这些黄酮苷对 VZV 没有显示出任何显著的活性。

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