You Position: Home > Paper
Synthesis of 8-alkyl-13-bromo-berberine hydrochloride derivatives and their effect on proliferation of human HepG2 cell line
( views:239, downloads:0 )
- Author:
- No author available
- Journal Title:
- CHINESE TRADITIONAL AND HERBAL DRUGS
- Issue:
- 11
- DOI:
- No doi available
- Key Word:
- 盐酸小檗碱;烷基化;溴代;细胞毒性
Abstract： 目的 为了进一步提高小檗碱的抗肿瘤活性,对小檗碱进行了烷基化,为开发新抗肿瘤药物奠定基础.方法 以盐酸小檗碱为起始原料,经格氏试剂烷基化及溴代反应,合成-系列8-烷基-13-溴代-盐酸小檗碱,经UV、IR、1H-NMR和元素分析进行结构鉴定.用四甲基偶氮唑盐(MTT)法观测产物对人肝癌细胞HepG2增殖能力的影响.结果 发现该细胞对目标产物的敏感性与碳链长度有很大关系,其中8-辛基-13-溴代盐酸小檗碱对该细胞的敏感性最强,在浓度为32 μg/mL时抑制率为96.82%,IC50为3.33μg/mL.结论 从IC50可知在8个碳原子以内,随着溴代小檗碱侧链的增长,抗癌活性增强.
- [1]谭宇蕙,陈冠林,郭淑杰,等.小檗碱对人胃癌MGC-803细胞生长抑制及诱导凋亡的作用[J].2001,(1).
- [2]陈冠林,陈蔚文,谭宇蕙,等.盐酸小檗碱诱导人胃癌MGC-803细胞凋亡的研究[J].2000,(5).
- [3]K S, Chang.Down-regulation of c-Ki-ras2 gene expression associated with morphologic differentiation in human embryonal carcinoma cells treated with berberine.[J].1991,90(1).
- [4]Kosfalova D,Drimal J,Kettmann V,etc.In vitro cytotoxicity of berberine against HeLa and L1210 cancer cell lines.[J].2004,59(7).
- [5]章涛,李苌清,杨俊卿,等.小檗碱抑制人乳腺癌MDA-MB-231细胞增殖及其与过氧化物酶体增殖物激活受体γ的关系[J].2009,(2).
- [6]H L, Wu,C Y, Hsu,W H, Liu,etc.Berberine-induced apoptosis of human leukemia HL-60 cells is associated with down-regulation of nucleophosmin/B23 and telomerase activity.[J].1999,81(6).
- [7]Chin-Wen Chi,Yue-Fang Chang,Tsurn-Waan Chao,etc.Flowcytometric analysis of the effect of Berberine on the expression of glucocorticoid receptors in human hepatoma HepG2 cells[J].1994,54(26).
- [8]M L, Sethi.Enzyme inhibition VI: Inhibition of reverse transcriptase activity by protoberberine alkaloids and structure-activity relationships.[J].1983,72(5).
- [9]B, Gatto,M M, Sanders,C, Yu,etc.Identification of topoisomerase I as the cytotoxic target of the protoberberine alkaloid coralyne.[J].1996,56.
- [10]Jantova S,Cipak L,Cernakova M,etc.Effect of berberine on proliferation, cell cycle and apoptosis in HeLa and L1210 cells.[J].2003,55(8).
- [11]Sanders MM,Mao Y,Wu HY,etc.Selective cytotoxicity of topoisomerase-directed protoberberines against glioblastoma cells.[J].1998,56(9).
- [12]林菁.小檗碱对K562细胞生长的抑制作用[J].1996,(4).
- [13]Kuo, C. L.,Chou, C. C.,Yung, B. Y.-M..Berberine complexes with DNA in the berberine-induced apoptosis in human leukemic HL-60 cells[J].1995,93(2).