秦岭特色药用植物桃儿七内生真菌代谢产物的分离鉴定及生物活性研究

Isolation, Identification, and Biological Activity of Metabolites from Endophytic Fungi of Qinling Characteristic Pharmaceutical Plant Sinopodophyllum hexandrum(Royle) Ying

以秦岭无病害健康桃儿七内生烟色拟盘多毛孢菌为研究对象,采用萃取法从菌丝中分离活性代谢产物,并对其结构进行鉴定,采用3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐(MTT)比色法检测了代谢产物的细胞毒活性,采用Ellman光度法检测了代谢产物的乙酰胆碱酯酶抑制活性,并检测了代谢产物的α-葡萄糖苷酶抑制活性。结果表明,在桃儿七内生烟色拟盘多毛孢菌代谢产物中分离并鉴定了10个萜类化合物,其中化合物1-1、1-2、1-3和1-4为新化合物。化合物1-3、1-4和1-8对A549、HeLa和HepG2细胞均表现出明显的细胞毒活性;化合物1-3对乙酰胆碱酯酶表现出较强的抑制活性;化合物1-1、1-2、1-3和1-4对α-葡萄糖苷酶均未表现出明显的抑制活性。表明,基于桃儿七内生烟色拟盘多毛孢菌分离出具有抗肿瘤活性和乙酰胆碱酯酶抑制活性的萜类化合物,为桃儿七内生真菌用于抗肿瘤及治疗阿尔兹海默病新药开发提供了新思路。

Taking the endophytic Trichospora fumigata of Qinling healthy Sinopodophyllum hexandrum(Royle) Ying as a research object, we isolated the active metabolits from mycelia by an extraction method, and identified their structures.Moreover, we evaluated the cytotoxic activity of the metabolits by 3-(4,5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide(MTT) colorimetric method, evaluated acetylcholinesterase inhibitory activity of the metabolits by Ellman photometric assay, and evaluated α-glucosidase inhibitory activity of the metabolits.The results show that 10 terpenoids are isolated and identified from the endophytic Trichospora fumigata of Sinopodophyllum hexandrum(Royle) Ying, among which, compounds 1-1,1-2,1-3,and 1-4 are new compounds.Compounds 1-3,1-4,and 1-8 show significant cytotoxic activity against A549,HeLa, and HepG2 cells, compound 1-3 show strong acetylcholinesterase inhibitory activity, while compounds 1-1,1-2,1-3,1-4 show no α-glucosidase inhibitory activity.The terpenoids with antitumor activity and acetylcholinesterase inhibitory activity can be isolated from the endophytic Trichospora fumigata of Sinopodophyllum hexandrum(Royle) Ying, which provides a new idea for the development of new drugs for anti-tumor and treatment of Alzheimer′s disease by using the endophytic fungi of Sinopodophyllum hexandrum(Royle) Ying.