Lin Jing, Wang Xi
Department of Pharmacology, School of Pharmacy, Fujian Medical University, Fuzhou 350004, China.
Yao Xue Xue Bao. 2011 Apr;46(4):390-4.
Synergistic antitumor effects of HB (berberine alpha-hydroxy-beta-decanoylethyl sulfonate, houttuyn berberine) with HCPT (hydroxycamptothecine), and its correlative mechanism were studied in vitro. MTT assay was employed to determine the cytotoxicity of HB combined with HCPT in tumor cells culture in vitro, IC50 and combination index (CI value) were used to evaluate the synergistic effects. The supercoiled DNA relaxation mediated by topoisomerase I & II was measured by agarose gel electrophoresis assay, and influence of HB was detected. The results showed that HB could inhibit the proliferation of tumor cells (SGC-7901, SW1116 and SW480) in vitro, and the inhibition ratio was increased, IC50 was reduced when combining with HCPT. CI value of the two drugs was less than 1 in HepG2, SW480, SGC-7901 and SW1116 cells. The lowest value was 0.447, 0.626, 0.161 and 0.178 in these tumor cells, respectively, further indicating HB has synergistic action with HCPT on suppressing tumor proliferation. The agarose gel electrophoresis assay showed HB can inhibit topoisomerase I & II activity of SW480 cells at the concentration of 2.0-8.0 mg x L(-1). HCPT is a typical inhibitor of topoisomerase I , the synergistic action between HCPT and HB on suppressing tumor proliferation is perhaps related to the congenerous inhibition of topoisomerase.
研究了黄连素α-羟基-β-癸酰乙基磺酸盐（小檗碱）（HB）与羟基喜树碱（HCPT）的体外协同抗肿瘤作用及其相关机制。采用MTT法测定HB与HCPT联合作用于体外培养肿瘤细胞的细胞毒性，用半数抑制浓度（IC50）和联合指数（CI值）评价协同效应。通过琼脂糖凝胶电泳法检测拓扑异构酶I和II介导的超螺旋DNA松弛情况，检测HB的影响。结果表明，HB能体外抑制肿瘤细胞（SGC-7901、SW1116和SW480）的增殖，与HCPT联合时抑制率增加，IC50降低。在HepG2、SW480、SGC-7901和SW1116细胞中，两种药物的CI值均小于1。在这些肿瘤细胞中最低值分别为0.447、0.626、0.161和0.178，进一步表明HB与HCPT在抑制肿瘤增殖方面具有协同作用。琼脂糖凝胶电泳分析表明，HB在浓度为2.0 - 8.0 mg·L-1时可抑制SW480细胞的拓扑异构酶I和II活性。HCPT是拓扑异构酶I的典型抑制剂，HCPT与HB在抑制肿瘤增殖方面的协同作用可能与拓扑异构酶的同类抑制有关。
