目的 研究長(zhǎng)柱重樓總皂苷（PCT3）的體內(nèi)外抗腫瘤活性及ig一次性給藥的急性毒性。方法 采用改良MTT法檢測(cè)PCT3對(duì)人結(jié)直腸癌（HCT-116）細(xì)胞和人胃癌（SGC-7901）細(xì)胞增殖的影響，計(jì)算半數(shù)抑制濃度（IC₅₀）。ig一次性給予小鼠1.646、2.352、3.360、4.800 g/kg PCT3進(jìn)行急性毒性測(cè)試。建立小鼠皮下肝癌（H22）模型，分別ip順鉑2 mg/kg（陽(yáng)性對(duì)照）、生理鹽水（陰性對(duì)照）；ig給予0.5% CMC-Na（溶劑對(duì)照）、30、90、270 mg/kg PCT3，連續(xù)給藥9 d，檢測(cè)小鼠腫瘤、體質(zhì)量抑制率，肝、脾、腎、胸腺系數(shù)。結(jié)果 與陰性對(duì)照組比較，PCT3對(duì)HCT-116和SGC-7901細(xì)胞增殖有明顯的抑制作用（P<0.05、0.01），IC₅₀分別為7.6、5.9 μg/mL。大劑量PCT3可致動(dòng)物腹瀉及活動(dòng)抑制，半數(shù)致死量（LD₅₀）為1.985 5 mg/kg。與溶劑對(duì)照組比較，PCT3對(duì)小鼠體質(zhì)量無(wú)顯著影響；270 mg/kg PCT3對(duì)H22腫瘤發(fā)揮顯著抑制作用（P<0.05），抑制率為26.8%；對(duì)各臟器系數(shù)均無(wú)顯著影響；與陰性對(duì)照組比較，順鉑顯著抑制腫瘤和體質(zhì)量的增長(zhǎng)（P<0.01），抑制率分別達(dá)81.4%和37.4%；對(duì)肝臟、脾臟、胸腺系數(shù)均發(fā)揮顯著抑制作用（P<0.05、0.01）。結(jié)論 順鉑抑瘤率明顯高于PCT3，但其顯著抑制小鼠的體質(zhì)量和肝臟、脾臟、胸腺系數(shù)，PCT3在體內(nèi)外具有一定的抗腫瘤活性，且毒性較低，其活性及作用機(jī)制有待進(jìn)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.

云南省科技廳-昆明醫(yī)科大學(xué)應(yīng)用基礎(chǔ)研究聯(lián)合專項(xiàng)項(xiàng)目（2014FB011）；云南省教育廳科學(xué)研究基金重點(diǎn)項(xiàng)目（2014Z060）