苦瓜中新型葫芦烷三萜类化合物及其成分的抗胆碱酯酶活性

Novel cucurbitane triterpenoids and anti-cholinesterase activities of constituents from Momordica charantia L.

作者信息

Kuanhuta Wichut, Aree Thammarat, Pornpakakul Surachai, Sawasdee Pattara

出版信息

Nat Prod Commun. 2014 Jun;9(6):765-9.

Abstract

The C-19 epimers of 5beta,19-epoxycucurbita-6,23(E),25(26)-triene-3f,19-diol (1) and 5/,19-epoxy-25-methoxycucurbita-6,23-diene-3beta,19-diol (2) along with (19R,23E)-5beta,19-epoxy-19-methoxycucurbita-6,23,25-trien-3beta-ol (3), (23E)-5beta,19-epoxycucurbita-6,23-diene-3beta,25-diol (4), ligballinol (5), charantin (6) and momordicoside K(7) were isolated from the green fruits of Momordica charantia. The (S)-epimers of 1 and 2 are the first reports in nature. The acetyl- and butyryl-cholinesterase inhibitory activities of the isolated compounds were evaluated, and 5 showed the highest activity of these compounds against butyrylcholinesterase (IC50 = 32.20 microM) with a reversible and non-competitive inhibition mode.

摘要

从苦瓜的绿色果实中分离出了5β,19 - 环氧葫芦巴 - 6,23(E),25(26) - 三烯 - 3f,19 - 二醇（1）和5/,19 - 环氧 - 25 - 甲氧基葫芦巴 - 6,23 - 二烯 - 3β,19 - 二醇（2）的C - 19差向异构体，以及(19R,23E) - 5β,19 - 环氧 - 19 - 甲氧基葫芦巴 - 6,23,25 - 三烯 - 3β - 醇（3）、(23E) - 5β,19 - 环氧葫芦巴 - 6,23 - 二烯 - 3β,25 - 二醇（4）、苦瓜醇（5）、苦瓜素（6）和苦瓜苷K（7）。1和2的(S) - 差向异构体是自然界中的首次报道。对分离出的化合物的乙酰胆碱酯酶和丁酰胆碱酯酶抑制活性进行了评估，5对丁酰胆碱酯酶表现出这些化合物中的最高活性（IC50 = 32.20 microM），其抑制模式为可逆且非竞争性。