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、5.9 μg/mL。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 detect the antitumor activity of total saponins form Paris forrestii (PCT3) in vitro and in vivo and its acute toxicity by disposable ig administration.Methods The inhibitory effect of PCT3 on proliferation of human colorectal cancer cells (HCT-116) and human gastric cancer cells (SGC-7901) was detected by modified MTT assay, and the half inhibition concentration (IC₅₀) was calculated. Acute toxicity test of PCT3 at doses of 1 646, 2 352, 3 360 and 4 800 mg/kg was performed by ig administration in mice. Mouse model of hepatocellular carcinoma (H22) was established with sc injection, and the mice were respectively ip given cisplatin 2 mg/kg (positive control), normal saline (negative control), ig given 0.5% CMC-Na (solvent control), 30, 90 and 270 mg/kg PCT3 continuously for 9 d, and the inhibitory rate of tumor, body weight, liver, spleen, kidney and thymus coefficients were detected.Results PCT3 had significant inhibitory effect on the proliferation of HCT-116 and SGC-7901 cells, with IC₅₀ values of 7.6 and 5.9 μg/mL, respectively. PCT3 induced animal diarrhea and activity inhibition in mice, the half lethal dose (LD₅₀) was 1985.5 mg/kg. Compared with solvent control group, PCT3 had no significant effect on body weight of mice; 270 mg/kg PCT3 had a significant inhibitory effect on H22 tumor mass (P<0.05), the inhibitory rate was 26.8%; There was no significant effect on the organ coefficient; compared with negative control group, cisplatin significantly inhibited the tumor growth and body weight (P<0.01), the inhibitory rates were 81.4% and 37.4% respectively; The liver, spleen and thymus coefficients were also significantly inhibited (P<0.05, 0.01).Conclusion The tumor inhibitory rate of cisplatin is significantly higher than that of PCT3, but it also significantly inhibits mice body weight and liver, spleen, thymus coefficients. PCT3 shows obvious antitumor activity in vitro and in vivo, and the toxicity is not remarkable. It could be a potential antitumor agent in the future.

云南省科技厅-昆明医科大学应用基础研究联合专项项目（2014FB011）；云南省教育厅科学研究基金重点项目（2014Z060）