摘要:目的 研究蒙药瑞香狼毒炮制前后的体外细胞毒性和抗肿瘤活性.方法 利用石油醚、醋酸乙酯和正丁醇分别萃取获得瑞香狼毒药材生品、奶制品、煎膏制品的各溶剂提取物,再通过萃取、分离纯化方法分别获得瑞香狼毒的9个单体化合物、总蛋白质和6个相对分子质量不同的蛋白质组分(Pr.1~Pr.6).将各溶剂提取物及单体化合物制成浓度为2.0 mg/ml的溶液,总蛋白质制成浓度分别为0.5、1.0、2.0、4.0、6.0、8.0 mg/ml的系列溶液,各蛋白质组分制备成浓度均为10mg/ml的溶液,分别作为样品溶液,采用MTT法分别测定各样品对人肝癌SMMC-7721细胞、狗肾MDCK细胞的生长抑制作用.结果 瑞香狼毒总蛋白质抗肿瘤活性和细胞毒性作用随其浓度增加而增强,其中4个蛋白质组分呈现较强的抗肿瘤活性,其活性由强至弱依次为Pr.4≥Pr.6≥Pr.3=Pr.2,3个蛋白质组分具有细胞毒性,其毒性由强至弱依次为Pr.4≥Pr.3≥Pr.1.瑞香狼毒单体化合物中,西瑞香素、狼毒色原酮、异狼毒素呈现不同程度的抗肿瘤活性,而狼毒色原酮、异狼毒素同时具有较弱的细胞毒性.除石油醚和多糖提取物外,瑞香狼毒药材生品各溶剂提取物均呈现不同程度的抗肿瘤活性和细胞毒性,并呈药物剂量依赖性;而炮制后,在保留一定程度抗肿瘤活性的基础上,其相应各溶剂提取物的细胞毒性均降低.结论 瑞香狼毒的细胞毒性主要源自多成分的协同作用,其蛋白质可能是瑞香狼毒的主要毒性位点之一,而炮制方法可降低瑞香狼毒药材的毒性且保留其生物活性.%Objective To study in vitro antitumor activitity and cytotoxicity of Stellera chamaejasme L..Methods Various solvent extracts were obtained from raw materials of Stellera chamaejasme L, dairy products, and decoction products using petroleum ether, ethyl acetate and n-butanol. Through extraction, separation, and purification, 9 monomer compounds, total protein and 6 protein fractions with different molecular weight (Pr.l ~ Pr.6) were acquired from Stellera chamaejasme L. The solvent extracts and the monomer compounds were made of the concentration of 2.0 mg/ml solution, and the total protein concentrations were 0.5, 1.0, 2.0, 4.0, 6.0, 8.0 mg/ml. The concentration of the protein fractions were prepared as 10 mg/ml of the solution. MTT assay were used to detect the inhibitory effect of proliferation of human hepatoma SMMC-7721 cells, canine kidney MDCK cells by the samples.Results Antitumor activity and Cytotoxicity of total protein from Stellera chamaejasme L. Increased with the rise in the concentration, of which four protein components showing more potent anti-tumor activity and its activity from strong to weak were Pr.4 > Pr.6 3= Pr.3 = Pr.2, and 3 components showed cytotoxic and its effect from strong to weak were Pr.4 ≥Pr.3 ≥ Pr.l. Of monomer compounds from Stellera chamaejasme L, Daphnoretin, Stellera chamaejasme chromone, different chamaejasmine exhibited various degrees of antitumor activity while Stellera chamaejasme chromone, different chamaejasmine had weaker cytotoxicity. Except the petroleum ether and polysaccharide extracts, various solvent extracts from raw materials of Stellera chamaejasme L. Showed varying degrees of antitumor activity and cytoxicity in a dose-dependent manner. After processing, cytotoxicity of the corresponding solvent extracts decreased while retaining some antitumor activity.Conclusions Cell activities of Stellera chamaejasme L. Are mainly derived from the synergy of multiple components. The protein may be one of the main toxic sites ofStellera chamaejasme L. Processing reduces the toxicity ofStellera chamaejasme L.