注射用多西他赛磺丁基-<i>β</i>-环糊精包合物的体外抗肿瘤作用

林娜; 刘晶; 丁亚军; 吴华

注射用多西他赛磺丁基-β-环糊精包合物的体外抗肿瘤作用

In vitro antitumor effect of the sulfobutyl-β-cyclodextrin inclusion of docetaxel for injection

摘要

摘要: 为了评价注射用多西他赛磺丁基-β-环糊精包合物（ML061）对各种体外培养肿瘤细胞的细胞毒性作用，本研究选取MDA-MB-435、MDA-MB-435s、NCI-H446、HO-8910、Bcap-37、KB、SMMC-7721、HT-29、SW480、LS-174t、SGC-7901、MCF-7、A549、NCI-H460等14个肿瘤细胞株，分别用不同质量浓度（200，20，2，0.2，0.02，0.002，0.000 2，0.000 02 μg/mL）ML061处理肿瘤细胞72 h，用MTT法测定细胞活力，并计算药物对各肿瘤细胞的半数抑制浓度IC₅₀。结果发现，ML061可抑制多种体外培养的肿瘤细胞株的活力，且这种抑制作用呈剂量依赖性。与阳性对照药市售多西他赛注射液奥名润相比，在选取的14个肿瘤细胞株中，ML061对Bcap-37、MDA-MB-435、MDA-MB-435s、NCI-H446和SW480的IC₅₀小于0.1 μg/mL。ML061对人卵巢癌Bcap-37、人结肠癌SW480、人小细胞肺癌NCI-H446、人乳腺癌MDA-MB-435及MDA-MB-435s等肿瘤细胞株的体外抑制作用较强。总之，ML061抑制多种体外培养的肿瘤细胞增殖，与阳性对照药奥名润相同，以Bcap-37、SW480、NCI-H446和MDA-MB-435s这4个细胞株较为敏感，而MDA-MB-435对ML061的敏感性高于奥名润。

Abstract: To evaluate the in vitro cytotoxicity of the sulfobutyl-β-cyclodextrin inclusion of docetaxel for injection (ML061) on various tumor cell lines,14 tumor cell lines including MDA-MB-435,MDA-MB-435s,NCI-H446,HO-8910,Bcap-37,KB,SMMC-7721,HT-29,SW480,LS-174t,SGC-7901,MCF-7,A549 and NCI-H460 were used for the treatment with ML061 at different concentrations (200,20,2,0.2,0.02,0.002,0.000 2,0.000 02 μg/mL) for 72 h,then the cell proliferation was evaluated by MTT method,and finally IC₅₀ was calculated.It was found that ML061 selectively inhibited the proliferation of a variety of tumor cell lines in vitro,with a certain in vitro killing effect on the 14 tumor cell lines in a dose-dependent trend.It was found that among the 14 tumor cell lines,the IC₅₀ values of Bcap-37,MDA-MB-435,MDA-MB-435s,NCI-H446 and SW480 were less than 0.1 μg/mL(being sensitive to ML061).Compared with the positive control Aomingrun,ML061 had stronger in vitro inhibition effect on human ovarian cancer Bcap-37,human colon cancer SW480,human small cell lung cancer NCI-H446,human breast cancer MDA-MB-435 and MDA-MB- 435s.In conclusion,ML061 inhibits the proliferation of a variety of tumor cell lines in vitro,of which Bcap-37,SW480,NCI-H446 and MDA-MB-435s cell lines are as sensitive as Aomingrun,but MDA-MB-435 is more sensitive to ML061 than Aomingrun.

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