从海洋海绵Xestospongia cf. vansoesti中分离出四氢异喹啉生物碱salsolinol作为蛋白酶体抑制剂。

Isolation of salsolinol, a tetrahydroisoquinoline alkaloid, from the marine sponge Xestospongia cf. vansoesti as a proteasome inhibitor.

作者信息

Nagasawa Yumiko, Ueoka Reiko, Yamanokuchi Rumi, Horiuchi Naoki, Ikeda Tsuyoshi, Rotinsulu Henki, Mangindaan Remy E P, Ukai Kazuyo, Kobayashi Hisayoshi, Namikoshi Michio, Hirota Hiroshi, Yokosawa Hideyoshi, Tsukamoto Sachiko

机构信息

Graduate School of Pharmaceutical Sciences, Kumamoto University, Kumamoto, Japan.

出版信息

Chem Pharm Bull (Tokyo). 2011;59(2):287-90. doi: 10.1248/cpb.59.287.

DOI:10.1248/cpb.59.287

PMID:21297314

Abstract

Salsolinol (1), a tetrahydroisoquinoline alkaloid, was isolated from the marine sponge Xestospongia cf. vansoesti collected in Indonesia as a proteasome inhibitor, along with three salsolinol derivatives, norsalsolinol (2), cis-4-hydroxysalsolinol (3), and trans-4-hydroxysalsolinol (4). Compounds 1 and 2 inhibited the chymotrypsin-like activity of the proteasome with IC(50) values of 50 and 32 µg/ml, respectively, but 3 and 4 showed no inhibitory effect even at 100 µg/ml.

摘要

从印度尼西亚采集的海洋海绵类皮海绵（Xestospongia cf. vansoesti）中分离出了四氢异喹啉生物碱索索林醇（1），它是一种蛋白酶体抑制剂，同时还分离出了三种索索林醇衍生物，即去甲索索林醇（2）、顺式-4-羟基索索林醇（3）和反式-4-羟基索索林醇（4）。化合物1和2对蛋白酶体的类胰凝乳蛋白酶活性具有抑制作用，其半数抑制浓度（IC50）值分别为50和32 μg/ml，但化合物3和4即使在浓度为100 μg/ml时也未显示出抑制作用。