黄癸素对肿瘤细胞增殖的抑制作用  

Antitumor effects of berberine α-hydroxy β-decanoylethyl sulfonate in vitro

作　　者：林菁[1] 彭华毅[1] 王希[1] 陈小英[1] 陈文斌[1] 

机构地区：[1]福建医科大学药学院药理系,福州350004

出　　处：《中药药理与临床》2011年第1期20-23,共4页Pharmacology and Clinics of Chinese Materia Medica

基　　金：福建省科技计划项目2005KD50

摘　　要：目的：研究黄癸素对体外培养肿瘤细胞的抑制作用,探讨其对肿瘤细胞的促凋亡作用。方法：台盼蓝排染法检测黄癸素、盐酸小檗碱对HL-60和K562细胞生长的抑制作用,MTT法检测黄癸素、鱼腥草素对贴壁生长的肿瘤细胞株的影响,计算IC50;Hoechst 33258染色观察形态改变、比色法检测caspase活性,用于分析细胞凋亡。结果：黄癸素对14株肿瘤细胞均有不同程度的抑制作用,对HL-60、K562、SGC-7901、B16、SW480、MGC80-3、U2OS、SW1116细胞（按IC50由低至高顺序）具有显著抑制,IC50为6.8816.52μg/ml,其中对HL-60、K562的IC50与盐酸小檗碱相近;对AGS、TE-11、HepG2细胞的IC50分别为23.47、27.82和28.50μg/ml;而SMMC-7721、SW1990和PANC-1细胞对黄癸素的敏感性相对较低,IC50分别为51.10、41.34和77.37μg/ml。以核固缩为特征的凋亡细胞增加,caspase-3、caspase-8活性增强,显示黄癸素对K562细胞具有促凋亡作用。结论：黄癸素具有显著的抑制肿瘤细胞活性,其作用谱较广,可促进K562细胞凋亡。Objective： Berberine α-hydroxy β-decanoylethyl sulfonate（HB） is an ion pair compound of berberine and houttuyfonate.This study is to investigate the antitumor activity of HB in vitro,and its induction of cell apoptosis.Methods： The cytotoxicity of HB,berberine or houttuyfonate were determined by Trypan blue dye exclusion test（in HL-60 and K562 cells）or MTT assay（in the other twelwe tumor cell lines）.Morphological change examined by Hoechst 33258 dyeing,caspase activity evaluated by microplate reader,were employed to observe the cell apoptosis.Results： HB could significantly inhibit the proliferation in vitro of most of the tumor cell lines in the test.The IC 50 were 6.8816.52 μg/ml for the cell lines-HL-60,K562,SGC-7901,B16,SW480,MGC80-3,U2OS,SW1116（listed in ascending order of IC 50）,and 23.47,27.82,28.50 μg/ml for AGS,TE-11,HepG2 respectively.HB showed relatively low effect on SMMC-7721,SW1990 and PANC-1 cells（IC 50 were respectively 51.10,41.34 and 77.37 μg/ml）.The inhibitory activity of HB was similar to that of Ber in HL-60 and K562 cells.Karyopyknosis,and caspase3,caspase 8 activity increase were detected in K562 cells of HB groups,indicating its effect of inducing apoptosis.Conclusion： HB has significant and broad-spectrum antitumor activities in vitro,and can induce apoptosis of K562 cell.

关 键 词：黄癸素 小檗碱 肿瘤细胞株 IC50 凋亡 

分 类 号：R285[医药卫生—中药学]