Selective apoptosis-inducing activity of crinum-type Amaryllidaceae alkaloids

被引:98
作者
McNulty, James
Nair, Jerald J.
Codina, Carles
Bastida, Jaume
Pandey, Siyaram
Gerasimoff, Jenny
Griffin, Carly
机构
[1] McMaster Univ, Dept Chem, Hamilton, ON L8S 4M1, Canada
[2] Univ Barcelona, Fac Farm, Dept Nat Prod, E-08028 Barcelona, Spain
[3] Univ Windsor, Dept Chem & Biochem, Windsor, ON N9B 3P4, Canada
基金
加拿大自然科学与工程研究理事会;
关键词
amaryllidaceae; apoptosis-induction; anticancer agent; alkaloid;
D O I
10.1016/j.phytochem.2007.01.006
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The selective apoptosis-inducing activity of Amaryllidaceae alkaloids belonging to the crinane-type is reported. A mini-library of natural and synthetic crinane alkaloids was assembled. Biological screening indicated crinamine 4 and haemanthamine 9 to be potent inducers of apoptosis in tumour cells at micromolar concentrations. Structure-activity relationships demonstrated the requirement for both an alpha-C2 bridge and a free hydroxyl at the C-11 position as pharmacophoric requirements for this activity. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1068 / 1074
页数:7
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