目的研究长柱重楼总皂苷(PCT3)的体内外抗肿瘤活性及ig一次性给药的急性毒性。方法采用改良MTT法检测PCT3对人结直肠癌(HCT-116)细胞和人胃癌(SGC-7901)细胞增殖的影响,计算半数抑制浓度(IC50)。ig一次性给予小鼠1.646、2.352、3.360、4.800 g/kg PCT3进行急性毒性测试。建立小鼠皮下肝癌(H22)模型,分别ip顺铂2 mg/kg(阳性对照)、生理盐水(阴性对照);ig给予0.5%CMC-Na(溶剂对照)、30、90、270 mg/kg PCT3,连续给药9 d,检测小鼠肿瘤、体质量抑制率,肝、脾、肾、胸腺系数。结果与阴性对照组比较,PCT3对HCT-116和SGC-7901细胞增殖有明显的抑制作用(P<0.05、0.01),IC50分别为7.6、5.9μg/m L。大剂量PCT3可致动物腹泻及活动抑制,半数致死量(LD50)为1.985 5 mg/kg。与溶剂对照组比较,PCT3对小鼠体质量无显著影响;270 mg/kg PCT3对H22肿瘤发挥显著抑制作用(P<0.05),抑制率为26.8%;对各脏器系数均无显著影响;与阴性对照组比较,顺铂显著抑制肿瘤和体质量的增长(P<0.01),抑制率分别达81.4%和37.4%;对肝脏、脾脏、胸腺系数均发挥显著抑制作用(P<0.05、0.01)。结论顺铂抑瘤率明显高于PCT3,但其显著抑制小鼠的体质量和肝脏、脾脏、胸腺系数,PCT3在体内外具有一定的抗肿瘤活性,且毒性较低,其活性及作用机制有待进一步研究。 Objective To study the antitumor activity of PCT-3 in vitro and in vivo and the acute toxicity of ig single-dose administration. Methods The effect of PCT3 on the proliferation of human colorectal cancer (HCT-116) and human gastric carcinoma (SGC-7901) cells was detected by modified MTT method. The half inhibitory concentration (IC50) was calculated. ig once to mice 1.646,2.352,3.360,4.800 g / kg PCT3 acute toxicity test. The model of H22 mice was established by intraperitoneal injection of cisplatin 2 mg / kg ip (positive control) and saline (negative control) respectively; ig 0.5% CMC-Na (solvent control), 30,90,270 mg / kg PCT3, continuous administration of 9 d, detection of tumor in mice, body mass inhibition rate, liver, spleen, kidney, thymus coefficient. Results Compared with the negative control group, PCT3 significantly inhibited the proliferation of HCT-116 and SGC-7901 cells (P <0.05, 0.01) with IC50 of 7.6 and 5.9 μg / mL, respectively. High dose PCT3 can cause diarrhea and activity inhibition, with a LD50 of 1.985 5 mg / kg. Compared with the solvent control group, PCT3 had no significant effect on the body weight of mice; 270 mg / kg PCT3 had a significant inhibitory effect on H22 tumor (P <0.05), and the inhibition rate was 26.8% Compared with the negative control group, cisplatin significantly inhibited the growth of tumors and body weight (P <0.01), and the inhibitory rates were 81.4% and 37.4%, respectively. Cisplatin significantly inhibited the hepatic, splenic and thymus parameters (P <0.05, 0.01 ). CONCLUSION: The inhibitory rate of cisplatin is significantly higher than that of PCT3, but it significantly inhibits the body weight, liver, spleen and thymus of mice, and PCT3 has anti-tumor activity in vitro and in vivo, and its toxicity is low. Its activity and mechanism needs to be treated. further research.