D-24851衍生物YB-N12抗肿瘤作用的实验研究

Effect of D-24851 derivate YB-N12 of Antitumor

【目的】研究D-24851衍生物YB-N12体内外抗肿瘤作用。【方法】采用MTT、流式细胞检测方法和实体肉瘤S180小鼠体内给药法,测定了YB-N12对体外和体内肿瘤细胞增殖的影响。【结果】MTT法发现YB-N12对HeLa、A-549、KB、SKOV3等肿瘤细胞均具抑制作用,IC50为1.8～3.28μmol/L。流式细胞仪检测到HeLa细胞周期中G2+M期细胞的比例明显增加。连续腹腔注射YB-N12[50mg·(kg·d)-1,100mg·(kg·d)-1]10d,对小鼠肉瘤S180的生长抑制率分别为35.2%和44.4%。【结论】D-24851衍生物YB-N12在体内体外均具有抑制肿瘤增殖作用。

~： [ Objective] To study the Antitumor effects of the derivate of D-24851 （YB-N12） in vitro and in vivo. [Methods] YB-N12 induced morphological changes by MTr, flow cytometry and Inhibition of tumor growth in vivo by YB-N12. [Results] MTr assay showed the potent cytotoxic effect on human galactophore cancer. Flow cytometric analysis of HeLa cells appeared to YB-N12 can blocked the tumer cells at G2 ＋ M phase and arrested the following cell eirle. Intraperitoneal injection of YB-N12 [50 rag＂ （kg＇d）-t and 100 mg＂ （kg＇d）-1 ] was performed every day. Mouse S180 sarcoma was sensitive to YB-N12, 50mg/kg and 100mg/kg YB-N12 treatment resulted in 35.2% and 44.4% （ P 〈 0.01） inhibition of tumor growth compared with untreated control. [Coochusions] YB-N12 could obviously inhibit the growth of Hela cell in vitro and S180 cameus in vivo.