二半乳糖基二酰基甘油的合成及其对人羊毛甾醇合酶的结构抑制活性。

Synthesis of digalactosyl diacylglycerols and their structure-inhibitory activity on human lanosterol synthase.

作者信息

Tanaka Rie, Sakano Yuichi, Nagatsu Akito, Shibuya Masaaki, Ebizuka Yutaka, Goda Yukihiro

机构信息

National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-Ku, Tokyo 158-8501, Japan.

出版信息

Bioorg Med Chem Lett. 2005 Jan 3;15(1):159-62. doi: 10.1016/j.bmcl.2004.10.013.

DOI:10.1016/j.bmcl.2004.10.013

PMID:15582431

Abstract

Digalactosyl and monogalactocyl diacylglycerols (DGDG and MGDG), which were identified as anti-hyperlipemia active components in Colocasia esculenta (Taro), were synthesized. The inhibitory activity of DGDG, MGDG and related compounds on human lanosterol synthase was evaluated as anti-hyperlipemic activity. DGDG with two myristoyl groups at both sn-1 and sn-2 positions and with an oleoyl group at the sn-1 position showed the most potent activity.

摘要

已合成了二半乳糖基二酰基甘油和单半乳糖基二酰基甘油（DGDG和MGDG），它们被鉴定为芋头中的抗高血脂活性成分。评估了DGDG、MGDG及相关化合物对人羊毛甾醇合酶的抑制活性作为抗高血脂活性。在sn-1和sn-2位均带有两个肉豆蔻酰基且在sn-1位带有一个油酰基的DGDG显示出最强的活性。