【摘要】 目的研究瘿花甲素(rosthorin A)体内外抗肿瘤活性及其作用机制。方法采用改良MTT法测试rosthorin A对S180细胞株增殖的影响;以荷S180肉瘤小鼠为模型,检测rosthorin A对荷瘤小鼠肉瘤重量、体重的影响;通过流式细胞术检测rosthorin A对S180细胞株和肉瘤组织细胞周期的影响。结果Rosthorin A对S180细胞株的IC50值为2.69 mg·L-1。小鼠经腹腔注射rosthorin A的LD50为83.20mg·kg-1。与溶剂对照组相比,rosthorin A在2~8 mg·kg-1内对荷S180肉瘤小鼠肿瘤生长无抑制作用(P>0.05),但可使S180细胞株和S180肉瘤组织细胞G0/G1期所占比例增多。结论 Rosthorin A对S180细胞株体外有较强的细胞毒活性,可通过阻滞细胞由G0/G1期进入S期抑制细胞增殖,体内在实验剂量范围内对荷S180肉瘤小鼠无抑瘤作用。更多还原

【Abstract】 Objective To determine the antitumor activity and mechanism of a diterpenoid compound rosthorin A from Isodon xerophilus. Methods Modified MTT assay was used to test the effect of rosthorin A on the proliferation of S180 tumor cell strain. The influence on tumor growth in mice with transplanted sarcoma(S180) was observed. The cell cycle of S180 cell lines and mouse sarcoma(S180) was analysed with Flow Cytometry. Results The IC50 of rosthorin A in S180 cell lines was 2.69 mg·L-1. Through intraperitoneal injection, the LD50 of rosthorin A in mice was 83.20 mg·kg-1. Compared with the solvent control group, there was no obvious difference(P > 0.05) in the inhibitory rate of tumor with rosthorin A at 2-8 mg·kg-1. But the cell cycle at G0/G1 phase of S180 was increased. Conclusion Rosthorin A has an obvious effect on inhibiting S180 cell proliferation in vitro and the mechanism might stop at the G0/G1 phase, but has no obvious antitumor activity for mouse transplanted sarcoma.更多还原