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目的:测定药用拟层孔菌子实体的石油醚粗提物、乙酸乙酯粗提物和甲醇粗提物的总三萜及总甾醇含量;研究3种粗提物及从乙酸乙酯粗提物中分离得到的三萜类单体化合物的体内抗肿瘤活性。探讨其抗肿瘤活性与总三萜和总甾醇含量的关系。方法:通过分光光度法测定3种粗提物的总三萜和总甾醇含量。通过H22荷瘤小鼠移植模型的体内抗肿瘤实验,观察该真菌子实体的石油醚提取物、乙酸乙酯提取物、甲醇提取物及三萜类单体化合物的抗肿瘤活性进行评价。结果:乙酸乙酯粗提物中总三萜含量和总甾醇含量最高,石油醚次之。从乙酸乙酯层分离得到5个单体化合物:去氢齿孔酮酸,3-酮基-去氢硫色多孔菌酸,去氢齿孔酸,阿里红酸A和阿里红酸C。在体内实验中,乙酸乙酯层抑瘤率效果最佳,当浓度达到1 000mg·kg~(-1)时抑瘤率为64.65%,与阳性药5-氟尿嘧啶(5-Fu)的抑瘤率(59.98%)接近,并且免疫器官指数均有一定的变化。单体化合物2(3-酮基-去氢硫色多孔菌酸)抑瘤率为75.13%,与阳性药物CTX(81.76%)抑瘤率接近,比阳性药5-Fu高。其余4种单体化合物也有一定作用效果。结论:乙酸乙酯提取物及这5种单体化合物能有效抑制肿瘤的生长,并且对机体的免疫力有较好的促进作用,该5种单体化合是药用拟层孔菌子实体的抗肿瘤活性成分,药用拟层孔菌的抗肿瘤活性成分可能是三萜类化合物。
OBJECTIVE: To determine the total triterpene and total sterol content of petroleum ether crude extract, ethyl acetate crude extract and methanol crude extract from the fruiting body of Pseudotsugar, and to study three crude extracts and crude extracts from ethyl acetate In vivo antitumor activity of triterpene monomer compounds isolated from. To investigate the relationship between antitumor activity and total triterpene and total sterol content. Methods: The total triterpene and total sterol contents of three crude extracts were determined by spectrophotometry. The antitumor activity of petroleum ether extract, ethyl acetate extract, methanol extract and triterpene monomer of the fungal fruiting body was evaluated by in vivo anti-tumor experiment in H22 tumor-bearing mouse transplantation model. Results: The total triterpene content and the total sterol content in the crude ethyl acetate extract were the highest, followed by petroleum ether. Five monomeric compounds were isolated from the ethyl acetate layer: deprotonated ketoacid, 3-keto-dehydroascorbic acid, dehydropermacetic acid, alginic acid A and alginic acid C. In vivo experiments, ethyl acetate inhibition rate of the best results, when the concentration reached 1 000mg · kg -1 (-1) inhibition rate was 64.65%, and the positive drug 5-fluorouracil (5-Fu) inhibition Rate (59.98%) close to, and immune organ index have certain changes. The inhibitory rate of monomeric compound 2 (3-keto-dehydro-sulfur polysilicic acid) was 75.13%, which was close to that of positive drug CTX (81.76%) and higher than the positive drug 5-Fu. The remaining four kinds of monomer compounds also have some effect. Conclusion: The ethyl acetate extract and the five kinds of monomeric compounds can effectively inhibit the growth of the tumor and promote the immunity of the organism. The five kinds of monomer compounds are anti-drug Tumor active ingredient, the anti-tumor active ingredient of medicinal pinopod may be triterpenoids.