【摘要】 目的观察刺果紫玉盘素J(calamistrin J,Cal-J)的体内外抗肿瘤活性及其选择性。方法MTT法观察不同质量浓度的Cal-J对人非小细胞肺癌NCI-H460细胞、人肝癌HepG2细胞、人宫颈癌HeLa细胞、人结肠癌Lovo细胞、肉瘤S180细胞5种肿瘤细胞系和正常人胚肺成纤维细胞(HELF)增殖的影响,Hoechst33258染色后在荧光显微镜下观察Lovo细胞凋亡的形态变化。在S180荷瘤小鼠进行整体抑瘤实验,计算Cal-J的抑瘤率。结果Cal-J对NCI-H460、HepG2、HeLa、HELF、S180、Lovo等6种细胞的增殖均有不同程度的抑制作用,其IC50依次为>100、(91±4)、(60.5±2.4)、(39.3±1.7)、(38±4)、(25±4)μg/mL。其中对Lovo细胞株抑制作用最强,且呈剂量、时间双重依赖性。Cal-J作用48h后,荧光显微镜下可见Lovo细胞核固缩,染色质凝聚等典型凋亡形态学特征。Cal-J对荷瘤小鼠S180移植瘤的生长有明显的抑制作用,Cal-J高、中、低(90、30、10mg/kg)剂量组的抑瘤率分别为51%、30%、17%,作用呈剂量依赖性。结论Cal-J对体外培养的多种人类肿瘤细胞和人胚肺成纤维细胞具有不同程度的细胞毒性作用,其中对人结肠癌Lovo细胞作用最强,并具有诱导细胞凋亡的作用。Cal-J还可抑制荷瘤小鼠S180移植瘤的生长。更多还原

【Abstract】 Objective To observe the anti-tumor activity of calamistrin J(Cal-J) in vivo and in vitro and their selectivity.Methods The inhibitory effect of Cal-J at various concentrations on growth of five kinds of tumor cell lines(NCI-H 460,HepG2,HeLa,Lovo,and S180) and normal human embryonic lung fibroblast(HELF) was determined by MTT assay.The morphological changes of the Lovo apoptosis were observed by fluorescence microscope with Hoechst 33258 staining.The inhibitory effect of Cal-J on the growth of tumor was observed with the models of transplanted sarcoma 180(S180) in Kunming mice and the inhibitory rate of Cal-J on tumor growth was calculated.Results Cal-J had different inhibitory intensities on the six kinds of cell lines.They were NCI-H460,HepG2,HeLa,HELF,S180,and Lovo.Their IC50(μg/mL) were >100,(91±4),(60.5±2.4),(39.3±1.7),(38±4),and(25±4) μg/mL,respectively.Among them Cal-J had the strongest inhibitory effect on Lovo cells and it was observed in a dose-and time-dependent manner.Lovo cells treated by Cal-J could be observed typically morphological changes through fluorescence microscope,including cell shrinkage with a condensed cytoplasm,chromatin condensation,etc.Cal-J could obviously inhibit the growth of S180 in mice and showed a dose-effect relationship.The inhibitory rate of Cal-J(90,30,and 10 mg/kg) were 51%,30%,and 17%,respectively.Conclusion Cal-J has different inhibitory intensities on several tumor cells and HELF cells in vivo,among which the inhibitory effect on Lovo cells is the strongest and also significantly induce apoptosis of Lovo cells.Cal-J can also has a marked inhibitory effect on the growth of S180 after administered to the tumor-bearing mice.更多还原