药用拟层孔菌子实体提取物的抗肿瘤活性研究

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。

Anti-tumor Activity of Extracts from Fruiting Body of Fomitopsis officinalis

Objective:To determine the total triterpenes and total sterol content in petroleum ether extract, EtOAc extract, and MeOH extract of the fruiting body of Fomitopsis officinali, and study the anti-tumor activity of three kinds of crude extracts and triterpene monomer compounds isolated from EtOAc extract, and explore the relationship between its anti-tumor activity and the content of total triterpenes and total sterol content. Method:Total terpene and sterol content in three crude extracts was determined by spectrophotometric method. Based on the in vivo anti-tumor experiment in H22 tumor-burdened transplantation mice models, the petroleum ether extract, EtOAc extract, and MeOH extract of the fruiting body as well as triterpene monomer compounds were observed and evaluated for anti-tumor activity. Result:The total triterpenes and total sterol content is the highest in EtOAc extract, followed by petroleum ether extract. Five monomer compounds were isolated and obtained from EtOAc extract:dehydroeburiconic acid, 3-keto-dehydrosulphurenic acid, dehydroeburicoic acid, fomlactone A and fomlactone C. In the in vivo experiment, EtOAc fraction has the best anti-tumor activity, and when its concentration reached 1000 mg·kg^-1,its anti-tumor rate was 64.65%, closed to the positive drug 5-fluorouracil (anti-tumor rate of 59.98%), and the immune organ indexes also had some changes. The anti-tumor rate of compound 2(3-keto-dehydrosulfurenic acid) was 75.13%, closed to the positive drug CTX (anti-tumor rate of 81.76%), highter than positive drug 5-Fu. The other four kinds of monomer compounds all had a certain effect on the tumor. Conclusion:EtOAc extract and five monomer compounds can effectively inhibit tumor growth, and can improve the body's immune system. These five monomer compounds are the effective anti-tumor ingredients of the fruiting body of F. officinali, and the active anti-tumor ingredient may be triterpene compounds in F. officinalis.