川皮苷对小鼠黑色素瘤试验性转移的抑制作用及相关机制  

Inhibition and Related Mechanism of Nobiletin in Experimental Metastasis of Melanoma Cells in Mice

作　　者：王光凤[1] 肖璘[1] 周自桂 郭彦飞 刘全海[1] 

机构地区：[1]上海医药工业研究院,上海200437 [2]南京神州佳美药物研究有限公司,江苏南京210016

出　　处：《中国医药工业杂志》2006年第10期689-693,共5页Chinese Journal of Pharmaceuticals

摘　　要：采用小鼠肺高转移黑色素瘤细胞K111尾静脉注射肺转移模型,研究川皮苷的抗肿瘤转移作用,并在体外试验中研究其对K111细胞分泌明胶酶MMP2和MMP9的影响。结果表明,川皮苷对试验性小鼠黑色素瘤肺转移有较好的抑制作用,剂量为32mg/kg时抑制率47.3%。明胶酶谱法检测结果表明,川皮苷125和62.5μmol/L对MMP2和MMP9的分泌均表现抑制作用,表达率为对照组的30%和50%。定量PCR试验表明,用125μmol/L川皮苷处理的K111细胞,MMP2和MMP9的mRNA水平均低于对照组。提示川皮苷可在转录水平抑制MMP2和MMP9的表达,并对小鼠试验性转移模型有抑制作用。The anti-metastasis effect of nobiletin was investigated using experimental lung metastasis model mice by injection of melanoma cells K111 from caudal vein. The influence of nobiletin on amount of gelatinases MMP2 and MMP9 secreted by K111 cells in vitro was also tested. The results showed that nobiletin could effectively inhibit the experimental lung metastasis of melanoma cells, the inhibition rate against metastasis was 47.3 % at 32mg/kg. The results of gelatin zymography showed that the secretion of the MMP2 and MMP9 was decreased at the drug concentration of 125 and 62.5μmol/L, the expression rates of the two groups were about 30% and 50%, compared with the control. Real time PCR assay demonstrated that mRNA level of MMP2 and MMP9 in K111 cells treated with 125μmol/L nobiletin was also lower than that of the control. The results indicated that nobiletin could down-regulate the expression of MMP2 and MMP9 at transcriptional level and metastasis as well in mice model.

关 键 词：川皮苷 基质金属蛋白酶 抗肿瘤转移 

分 类 号：R944.9[医药卫生—药剂学]