Antitumor effect of orlistat, a fatty acid synthase inhibitor, is via activation of caspase-3 on human colorectal carcinoma-bearing animal

被引：93

作者：

Chuang, Hui-Yen ^{[1
]}

Chang, Ya-Fang ^{[1
]}

Hwang, Jeng-Jong ^{[1
]}

机构：

[1] Natl Yang Ming Univ, Dept Biomed Imaging & Radiol Sci, Taipei 112, Taiwan

来源：

BIOMEDICINE & PHARMACOTHERAPY | 2011年 / 65卷 / 04期

关键词：

Fatty acid synthase; Human colorectal carcinoma; Orlistat; BREAST-CANCER CELLS; PROSTATE-CANCER; LIPID RAFTS; FOOD-INTAKE; APOPTOSIS; EXPRESSION; PATHWAY; OA-519; MODEL; PROGRESSION;

D O I：

10.1016/j.biopha.2011.02.016

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

100103 [病原生物学]; 100218 [急诊医学];

摘要：

We established a HT-29/tk-luc human colorectal carcinoma-bearing animal model for the study of the inhibition effect and mechanism of orlistat, a fatty acid synthase (FASN) inhibitor. The results showed that orlistat caused cell cycle arrest at G1 phase, and triggered apoptosis through caspase-3 activation. The tumor inhibition effect of orlistat may also due to the inhibition of fatty acid synthesis without altering FASN activity. The tumor size of orlistat-treated mice in vivo was significantly smaller than that of the controls with 55% inhibition. The therapeutic efficacy was further confirmed with the bioluminescent imaging and nuclear molecular imaging with (131)I-FIAU/gamma scintigraphy and (11)C-acetate/microPET. We suggest that FASN is a potential target for the treatment of human colorectal carcinoma. (C) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：286 / 292

页数：7

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