Nuphar alkaloids with immediately apoptosis-inducing activity from Nuphar pumilum and their structural requirements for the activity
Nuphar alkaloids with immediately apoptosis-inducing activity from Nuphar pumilum and their structural requirements for the activity
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DOI：
10.1016/j.bmcl.2005.12.032
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发表时间：
2006-03-15
影响因子：
2.7
通讯作者：
Yoshikawa, M
中科院分区：
文献类型：
--
作者：
Matsuda, H;Yoshida, K;Yoshikawa, M
结果表明，水提物及其生物碱组分对人白血病细胞（U937）、小鼠黑色素瘤细胞（B16 F10）和人成纤维细胞（HT 1080）均有明显的细胞毒作用。6-羟基二聚倍半萜硫代生物碱（6-羟基硫代双胍，6，6 ′-二羟基硫代双胍，6-羟基硫代双胍B）在10 μ M的浓度下显示出显著的细胞毒活性，但缺乏6-羟基的二聚倍半萜硫代生物碱（硫代比努法里定，硫代普鲁汀B，6 ′-羟基硫代普鲁汀B，新硫代比努法里定，硫代普鲁汀B β-亚砜，和neothiobinupharidine β-亚砜）和单体倍半萜生物碱（nupharidine、7-甲氧基nupharidine和nupharolutine）显示出弱活性。接下来，使用形态学观察和DNA片段化测定（TUNEL法）来检查主要活性成分6-羟基硫代双胍胍对U937的凋亡诱导活性。在2.5-10 μ M的6-羟基硫代双胍处理后1小时内立即观察到U937的凋亡。(C)2006年由Elsevier Ltd.出版
The methanolic extract and its alkaloid fraction from the rhizomes of Nuphar pumilum showed cytotoxic effects on human leukemia cell (U937), mouse melanoma cell (B16F10), and human fibroblast (HT 1080). Dimeric sesquiterpene thioalkaloids with the 6-hydroxyl group (6-hydroxythiobinupharidine, 6,6'-dihydroxythiobinupharidine, 6-hydroxythionuphlutine B) showed substantial cytotoxic activity at a concentration of 10 mu M, but dimeric sesquiterpene thioalkaloids lacking the 6-hydroxyl group (thiobinupharidine, thionuphlutine B, 6'-hydroxythionuphlutine B, neothiobinupharidine, thionuphlutine B beta-sulfoxide, and neothiobinupharidine beta-sulfoxide) and monomeric sesquiterpene alkaloids (nupharidine, 7-epideoxynupharidine, and nupharolutine) showed weak activity. Next, apoptosis-inducing activity of a principal active constituent, 6-hydroxythiobinupharidine, on U937 was examined using morphological observation and DNA fragmentation assay (TUNEL method). Apoptosis of U937 was immediately observed within 1 h after treatment of 6-hydroxythiobinupharidine at 2.5-10 mu M. (C) 2006 Published by Elsevier Ltd.