Antitumor activity of cynanauriculoside A and its effect of apoptosis induction in tumor cells
Antitumor activity of cynanauriculoside A and its effect of apoptosis induction in tumor cells
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发表时间：
2009
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通讯作者：
Zhang Ru-song
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作者：
Zhang Ru-song
目的研究白首乌苷A（cynanauriculoside A，CA）的体外抗肿瘤作用及其诱导肿瘤细胞凋亡的作用。和HO-8910细胞的体外抑瘤作用;细胞凋亡的检测采用瑞氏-姬姆萨染色和流式细胞术（FCM）结果CA对3种肿瘤细胞株均有一定的细胞毒作用，IC 50在100 ~ 1000 μ g/ml范围内，对正常细胞的毒性作用为100 ~ 1000 μ g/ml。结果表明，在80 mg/L浓度下，40、50和160 mg/kg IG对S180荷瘤小鼠的肿瘤生长有明显的抑制作用，抑制率分别为20.0%、28.0%和48.1%。CA诱导MCF-7细胞明显凋亡（P0.01）并伴有明显的形态学改变，如胞浆收缩和核染色质浓缩，100 mg/L CA对体外培养8d的大鼠皮层神经元无毒性。结论CA在体内外均具有明显的抗肿瘤作用，并有一定的诱导肿瘤细胞凋亡作用，这可能是CA抗肿瘤作用的机制之一。
Objective To investigate the antitumor effect of cynanauriculoside A(CA) isolated from the root of Cynanchum auriculatum and its effect of apoptosis induction in tumor cells.Methods CA was evaluated for its cytotoxicity in vitro against MCF-7,BEL-7402,and HO-8910 cells by determining MTT assay and its antitumor effects in vivo on S180 tumor-bearing mice by calculating tumor-inhibited rate.Measures of apoptosis including Wright′s-Giemsa staining and flow cytometry(FCM) assay were involved to explore the mechanism.And the toxcity of CA on normal cells was also evaluated on in vitro cultured rat cortical neurons.Results CA showed a definite cytotoxicity to three tumor cell lines with IC50 in the range of 35.68—39.78 mg/L.And it significantly inhibited the tumor growth of S180 tumor-bearing mice at the dose of 40,50,and 160 mg/kg by ig administrated,the inhibitory rates were 20.0%,28.0%,and 48.1%,respectively.At the concentration of 80 mg/L,CA induced obvious apoptosis in MCF-7 cells(P0.01) associated with marked morphological changes such as cytoplasm contraction and nuclear chromatin condensation,while it showed no toxcity to rat cortical neurons cultured 8 d in vitro at the concentration of 100 mg/L.Conclusion CA has significant antitumor effect in vitro[WTBZ] and in vivo,and has moderate effect of inducing tumor cells apoptosis,which may be one of the mechanisms of CA antitumor activity.