Wang Yan-Yang, Zhe Hong, Zhao Ren
Department of Radiation Oncology, General Hospital of Ningxia Medical University, No,804 Shengli Str, Yinchuan, Ningxia, China.
Mol Cancer. 2014 Feb 20;13:30. doi: 10.1186/1476-4598-13-30.
Solid cancer remains a major cause of death in the world. As limited treatment options are currently available to patients with solid cancer, novel preventive control and effective therapeutic approaches are considered to be reasonable and decisive measures to combat this disease. The plant-derived triterpenoids, commonly used for medicinal purposes in many Asian countries, poses various pharmacological properties. A large number of triterpenoids exhibit cytotoxicity against a variety of cancer cells, and cancer preventive, as well as anticancer efficacy in preclinical animal models. To improve antitumor activity, some synthetic triterpenoid derivatives have been synthesized, including cyano-3,12-dioxooleana-1,9(11)- dien-28-oic (CDDO), its methyl ester (CDDO-Me), and imidazolide (CDDO-Im) derivatives. In this review, we will critically examine the current preclinical evidences of cancer preventive and therapeutic activity about one of the synthetic triterpenoids, CDDO-Me. Both in vitro and in vivo effects of this agent and related molecular mechanisms are presented.
实体癌仍然是全球主要的死亡原因。由于目前实体癌患者的治疗选择有限,新型预防控制和有效治疗方法被认为是对抗这种疾病的合理且决定性的措施。植物来源的三萜类化合物在许多亚洲国家常用于药用,具有多种药理特性。大量三萜类化合物对多种癌细胞具有细胞毒性,并在临床前动物模型中具有癌症预防和抗癌功效。为了提高抗肿瘤活性,已经合成了一些合成三萜类衍生物,包括氰基-3,12-二氧代齐墩果-1,9(11)-二烯-28-酸(CDDO)、其甲酯(CDDO-Me)和咪唑化物(CDDO-Im)衍生物。在本综述中,我们将严格审查合成三萜类化合物之一CDDO-Me的癌症预防和治疗活性的当前临床前证据。介绍了该药物的体外和体内作用以及相关分子机制。