Huang Dan, Ding Yan, Li Yan, Zhang Wenming, Fang Weishuo, Chen Xiaoguang
Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, China.
Cancer Lett. 2006 Feb 28;233(2):289-96. doi: 10.1016/j.canlet.2005.03.019. Epub 2005 Sep 9.
Oleanolic acid (3beta-hydroxy-olea-12-en-28-oic acid, OA) exists widely in plant kingdom and possesses various pharmacological activities. In recent years, it was found that it had marked anti-tumor effects and exhibited cytotoxic activity towards many cancer cell lines in culture. In this article, the anti-tumor and differentiation-inducing effects of a derivative of OA modified at C-3, 3-oxo oleanolic acid (3-oxo-olea-12-en-28-oic acid, 3-oxo-OA, 3-7-1) was reported. In vitro, 3-7-1 were found to inhibit significantly the growth of cancer cells derived from different tissues. And 3-7-1 had inhibitory effect on melanoma in vivo. This selection may relate to the differentiation induced by 3-7-1. The inhibition of 3-7-1 on B16-BL6 suggests that 3-7-1 may be a useful anti-cancer agent for melanoma.
齐墩果酸（3β-羟基-齐墩果-12-烯-28-酸，OA）广泛存在于植物界，并具有多种药理活性。近年来，发现它具有显著的抗肿瘤作用，对多种培养的癌细胞系表现出细胞毒活性。本文报道了在C-3位修饰的OA衍生物3-氧代齐墩果酸（3-氧代-齐墩果-12-烯-28-酸，3-oxo-OA，3-7-1）的抗肿瘤和诱导分化作用。在体外，发现3-7-1能显著抑制源自不同组织的癌细胞生长。并且3-7-1在体内对黑色素瘤有抑制作用。这种作用可能与3-7-1诱导分化有关。3-7-1对B16-BL6的抑制作用表明3-7-1可能是一种对黑色素瘤有效的抗癌剂。
