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尼亚齐米宁是一种从辣木叶中提取的硫代氨基甲酸盐,对抑制肿瘤启动子诱导的爱泼斯坦-巴尔病毒激活有着严格的结构要求。

Niaziminin, a thiocarbamate from the leaves of Moringa oleifera, holds a strict structural requirement for inhibition of tumor-promoter-induced Epstein-Barr virus activation.

作者信息

Murakami A, Kitazono Y, Jiwajinda S, Koshimizu K, Ohigashi H

机构信息

Department of Biotechnological Science, Faculty of Biology-Oriented Science and Technology, Japan.

出版信息

Planta Med. 1998 May;64(4):319-23. doi: 10.1055/s-2006-957442.

Abstract

Three known thiocarbamate (TC)- and isothiocyanate (ITC)-related compounds have been isolated from the leaves of Moringa oleifera, a traditional herb in southeast Asia, as inhibitors of tumor promoter teleocidin B-4-induced Epstein-Barr virus (EBV) activation in Raji cells. Interestingly, only niaziminin among 10 TCs including 8 synthetic ones showed considerable inhibition against EBV activation. The structure-activity relationships indicated that the presence of an acetoxy group at the 4'-position of niaziminin is important and indispensable for inhibition. On the other hand, among the ITC-related compounds, naturally occurring 4-[(4'-O-acetyl-alpha-L-rhamnosyloxy)benzyl]ITC and commercially available allyl- and benzyl-ITC significantly inhibited activation, suggesting that the isothiocyano group is a critical structural factor for activity.

摘要

从东南亚传统草药辣木的叶子中分离出三种已知的硫代氨基甲酸盐(TC)和异硫氰酸盐(ITC)相关化合物,作为肿瘤促进剂teleocidin B-4诱导的Raji细胞中Epstein-Barr病毒(EBV)激活的抑制剂。有趣的是,在包括8种合成化合物在内的10种TC中,只有尼亚齐米宁对EBV激活表现出显著抑制作用。构效关系表明,尼亚齐米宁4'-位上乙酰氧基的存在对抑制作用很重要且不可或缺。另一方面,在ITC相关化合物中,天然存在的4-[(4'-O-乙酰基-α-L-鼠李糖氧基)苄基]ITC以及市售的烯丙基ITC和苄基ITC显著抑制激活,这表明异硫氰基是活性的关键结构因素。

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