目的:研究苍耳子65%乙醇提取液的乙酸乙酯、正丁醇和水萃取物对大鼠肝脏的毒性作用,为探讨苍耳子的毒性成分提供实验依据。方法:苍耳子碎粉22kg,用8倍量乙醇浸泡6h回流加热提取2h,共提取2次,合并提取液,减压回收乙醇至无醇味,浓缩,浓缩液用石油醚萃取,回收石油醚;依次用乙酸乙酯、正丁醇萃取,回收有机溶剂,水层减压干燥。取苍耳子干燥乙酸乙酯萃取物4.8g,正丁醇萃取物24g和水萃取物56g,各加含3%吐温-80生理盐水2000mL,分别配成浓度为0.0024、0.0120和0.0280g/mL的混悬液。将SPF级雄性大鼠40只随机分成4组,每组10只。3个给药组大鼠分别用乙酸乙酯、正丁醇和水萃取物的混悬液2.5mL灌胃,2次/d(剂量分别为每天0.06g/kg、0.3g/kg、0.7g/kg),空白对照组给予等体积的吐温80生理盐水灌胃,2次/d,均连续灌胃28d。观察给药后大鼠外观、饮食和活动情况;并于给药前和给药开始后7、14、21、28d称体重。第29天检测血清丙氨酸氨基转移酶(ALT)、天冬氨酸氨基转移酶(AST)、碱性磷酸酶(AKP)、总胆红素(TBil)和直接胆红素(DBil)的水平;之后,处死大鼠,计算肝脏指数,并进行肝脏组织学形态观察。结果:水萃取物组大鼠给药后7d皮毛无光泽,活动及摄食量减少。正丁醇和水萃取物组大鼠给药后14、21d出现皮毛枯黄,精神萎靡,28d出现竖毛,倦卧少动。乙酸乙酯萃取物组大鼠未见明显改变。正丁醇萃取物组大鼠给药开始后21、28d体重分别为(240.6±24.1)和(255.1±21.3)g,水萃取物组大鼠给药开始后14、21、28d体重分别为(214.4±20.5)、(230.7±21.2)和(239.1±18.5)g,均明显低于同时间点空白对照组大鼠体重[分别为(251.7±27.2)、(280.7±38.2)和(306.2±36.5)g,(P<0.05,P<0.01)]。正丁醇萃取物组AST为(112.6±24.3)U/L,明显高于空白对照组[(79.9±20.4)U/L,P<0.01];水萃取物组ALT、AST和AKP分别为(51.1±3.9)、(112.9±16.6)和(198.4±41.8)U/L,明显高于空白对照组[(44.3±6.2)、(79.9±20.4)和(152.2±39.9)U/L,(P<0.01,P<0.05)];正丁醇萃取物组和水萃取物组肝脏指数分别为4.71±0.89和5.80±0.64,明显高于空白对照组3.14±0.33(P<0.01)。各给药组大鼠的TBil和DBil值有所增加,但与空白对照组比较差异无统计学意义(P>0.05)。光镜观察可见正丁醇萃取物和水萃取物组大鼠肝细胞间隙增大、细胞核溶解、炎细胞浸润等病理改变。结论:苍耳子乙醇提取液的正丁醇萃取物及水萃取物对大鼠具有明显肝毒性作用。 Objective: To study the toxic effects of ethyl acetate, n-butanol and water extracts of 65% ethanol extract of Xanthium sib on rat liver, and to provide an experimental basis for exploring the toxic components of Xanthium ssp. Method: Xanthium smashed powder 22kg, soaked with 8 times the amount of ethanol 6h reflux heating extraction 2h, extracted a total of 2 times, the combined extract, vacuum recovery of ethanol until no alcohol taste, concentrated, the concentrate was extracted with petroleum ether, oil recovery Ether; followed by ethyl acetate, n-butanol extraction, recovery of organic solvent, the aqueous layer was dried under reduced pressure. Xanthium fruiting dry ethyl acetate extract 4.8g, n-butanol extract 24g and water extract 56g, each containing 3% Tween -80 saline 2000mL, dubbed the concentration of 0.0024,0.0120 and 0.0280g / mL of suspension. 40 SPF male rats were randomly divided into 4 groups of 10. The rats in the three administration groups were orally administered 2.5 mL of ethyl acetate, n-butanol and water extract respectively, twice a day (the dosage was 0.06g / kg, 0.3g / kg, 0.7g / kg). The blank control group was given an equal volume of Tween 80 saline, 2 times / d, were fed continuously for 28 days. The appearance, diet and activity of the rats were observed after administration. Body weight was weighed before administration and on the 7th, 14th, 21st and 28th days after administration. The serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (AKP), total bilirubin (TBil) and direct bilirubin After that, the rats were sacrificed, the liver index was calculated, and the morphology of the liver was observed. Results: The skin extracts of rats in water extract group were dull on day 7 after administration, and their activities and food consumption decreased. N-butanol and water extract group 14 and 21 days after administration, the fur appeared yellow, apathetic, vertical hair on 28d, tired and lying less. Ethyl acetate extract group rats no significant change. The weights of rats in n-butanol extracts group were (240.6 ± 24.1) and (255.1 ± 21.3) g at 21 and 28 days after the beginning of administration, respectively. The body weights at 14, 21 and 28 days after administration of water extract group were ( 214.4 ± 20.5), (230.7 ± 21.2) and (239.1 ± 18.5) g, respectively, were significantly lower than those of the blank control rats at the same time points (251.7 ± 27.2, 280.7 ± 38.2 and 306.2 ± 36.5, ) g, (P <0.05, P <0.01)]. The AST in the n-butanol extract group was (112.6 ± 24.3) U / L, which was significantly higher than that in the blank control group (79.9 ± 20.4 U / L, P <0.01) 51.1 ± 3.9, 112.9 ± 16.6 and 198.4 ± 41.8 U / L, respectively, which were significantly higher than those in the blank control group [(44.3 ± 6.2), (79.9 ± 20.4) and (152.2 ± 39.9) <0.01, P <0.05). The liver index of n-butanol extract group and water extract group were 4.71 ± 0.89 and 5.80 ± 0.64, respectively, which were significantly higher than those of the blank control group (3.14 ± 0.33, P <0.01). The TBil and DBil values ​​of rats in each group were increased, but there was no significant difference compared with the blank control group (P> 0.05). Light microscopy showed n-butanol extract and water extract group increased liver cell gap, nuclear lysis, inflammatory cell infiltration and other pathological changes. CONCLUSION: The n-butanol extract and water extract of Xanthium sibiricum ethanol extract have obvious hepatotoxicity in rats.