保肝药物利加隆抑制脑胶质瘤细胞生长

水飞蓟素是一种类黄酮，它的抗癌作用已在很多肿瘤细胞系中得到确认。Kim KW等的体外试验和体内试验均证实：水飞蓟素抑制了脑胶质瘤的生长，可以作为一种潜在的抗恶性胶质瘤制剂。上海东方医院神经外科魏社鹏

Silibinin Inhibits Glioma Cell Proliferation via Ca(2+)/ROS/MAPK-Dependent Mechanism In Vitro and Glioma Tumor Growth In Vivo

Kim KW, Choi CH, Kim TH, Kwon CH, Woo JS, Kim YK.

Neurochem Res. 2009 Mar 5

Department of Neurosurgery, College of Medicine, Pusan National University, Pusan, 602-739, Korea.

Anticancer activity of silibinin, a flavonoid, has been demonstrated in various cancer cell types. However, the underlying mechanism and in vivo efficacy in glioma were not elucidated. The present study was undertaken to determine the effect of silibinin on glioma cell proliferation in vitro and to examine whether silibinin inhibits tumor growth in vivo. Silibinin resulted in inhibition of proliferation in a dose- and time-dependent manner, which was largely attributed to cell death. Silibinin induced a transient increase in intracellular Ca(2+) followed by an increase in reactive oxygen species (ROS) generation. The silibinin-induced cell death was prevented by EGTA, calpain inhibitor and antioxidants (N-acetylcysteine and Trolox). Western blot analysis showed that silibinin also induced ROS-dependent activation of extracellular signal-regulated kinase, p38 kinase, and c-Jun N-terminal kinase. Inhibitors of these kinases prevented the silibinin-induced cell death. Silibinin caused caspase activation and the silibinin-induced cell death was prevented by caspase inhibitors. Glioma cell migration was also decreased by silibinin treatment. Oral administration of silibinin in animals with subcutaneous U87MG glioma cells reduced tumor volume. Subsequent tumor tissue analysis showed a decrease in Ki-67 positive cells, an increase in TUNEL-positive cells, and caspase activation. These results indicate that silibinin induces a caspase-dependent cell death via Ca(2+)/ROS/MAPK-mediated pathway in vitro and inhibits glioma growth in vivo. These data suggest that silibinin may serve as a potential therapeutic agent for malignant human gliomas.

 

水飞蓟素

通用名称：水飞蓟素

英文名称：Silibinin

中文别名：西里马灵、西利马林、治肝快

所属类别：消化系统药物/肝胆疾病辅助用药/治疗肝炎辅助用药

【药理】

本品有明显的保护及稳定肝细胞膜的作用；对四氯化碳、硫代乙酰胺、毒蕈素、鬼笔碱、猪屎豆硷等肝脏毒物引起的各种 类型肝损伤具有不同程度的保护和治疗作用，并对四氯化碳所引起的丙氨酸氨基转移酶的升高有一定的阻止作用。临床应用表明，本品可改善肝功能，使谷丙转氨 酶、胆红素下降，且可改善乏力、腹胀、肝区痛等症状以及增进食欲。

【适应症】

适用于慢性迁延性肝炎、慢性活动性肝炎、初期肝硬化、肝中毒等病的治疗。临床试用于

急、慢性肝炎患者，症状、体征、肝功能均有明显改善。

【用法用量】

口服:2片／次,3次／日。 3个月为一疗程。

每片含水飞蓟素35毫克或38.5毫克。

肌注：水飞蓟宾邻苯二甲酸单酯钠, 25-50毫克/次。

【不良反应】

个别患者用药后有头昏、恶心等。

【相关商品名】

利肝隆   利肝素  利加隆