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热带水果山竹中的黄烷酮作为抗癌剂的潜力:体外和体内诱导 caspase 依赖的细胞凋亡。

Potential of xanthones from tropical fruit mangosteen as anti-cancer agents: caspase-dependent apoptosis induction in vitro and in mice.

机构信息

Department of Biochemistry, Faculty of Medicine, Srinakharinwirot University, Bangkok, Thailand.

出版信息

Appl Biochem Biotechnol. 2010 Oct;162(4):1080-94. doi: 10.1007/s12010-009-8903-6. Epub 2010 Jan 26.

DOI:10.1007/s12010-009-8903-6
PMID:20101528
Abstract

The pericarp of mangosteen (Garcinia mangostana L.) is rich in various xanthones that are known to possess unique biological activities. In this work, we characterized the anti-proliferative and cytotoxic activities of mangosteen xanthones both in vitro and in mice. In vitro analysis with a human colorectal adenocarcinoma cell line, COLO 205, showed that mangosteen xanthones not only inhibit the proliferation of target cells but also induce their death by apoptosis that involves the activation of the caspase cascade. In vivo analysis using a mouse subcutaneous tumor model with COLO 205 cells showed that, at relatively low doses, the growth of tumors was repressed upon intratumoral administration of mangosteen xanthones. When a higher dose of mangosteen xanthones was administered, the size of tumors was reduced gradually, and, in some mice, the disappearance of tumors was seen. Histopathological evaluation and biochemical analysis of tumors that received mangosteen xanthones indicate the induction of apoptosis in tumors, which resulted in the repression of their growth and the reduction of their sizes. These results demonstrate the potential of mangosteen xanthones to serve as anti-cancer agents for the chemotherapy of cancer.

摘要

山竹果皮富含多种据称具有独特生物活性的呫吨酮。本工作旨在研究山竹果呫吨酮的体外抗增殖和细胞毒性作用及其在小鼠体内的作用。体外分析采用人结直肠腺癌细胞系 COLO 205,结果表明山竹果呫吨酮不仅能抑制靶细胞增殖,还能通过涉及半胱天冬酶级联激活的细胞凋亡诱导其死亡。体内分析采用 COLO 205 细胞皮下肿瘤模型,结果表明,山竹果呫吨酮瘤内给药时,在相对较低剂量下即可抑制肿瘤生长。当给予较高剂量的山竹果呫吨酮时,肿瘤大小逐渐缩小,并且在一些小鼠中,肿瘤消失。接受山竹果呫吨酮的肿瘤的组织病理学评价和生化分析表明,肿瘤发生了凋亡,从而抑制了肿瘤的生长并减小了肿瘤的体积。这些结果表明,山竹果呫吨酮具有作为癌症化疗抗癌剂的潜力。

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