木本曼陀罗内生真菌Diaporthe phaseolorum MBM-21的次级代谢产物研究  

Study on the secondary metabolites of endophytic fungus Diaporthe phaseolorum MBM-21 from Brugmansia arborea

作　　者：陈育伍 刘博 王晓晴 牟越 郝艳琦 王雅[2] 孙奕[1] CHEN Yu-wu;LIU Bo;WANG Xiao-qing;MU Yue;HAO Yan-qi;WANG Ya;SUN Yi(Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences,Beijing 100700,China;College of Life Science and Engineering,Lanzhou University of Technology,Lanzhou 730050,China)

机构地区：[1]中国中医科学院中药研究所,北京100700 [2]兰州理工大学生命科学与工程学院,甘肃兰州730050

出　　处：《中国药物化学杂志》2023年第12期914-921,共8页Chinese Journal of Medicinal Chemistry

基　　金：中国中医科学院科技创新工程项目(CI2021A04514)。

摘　　要：目的对木本曼陀罗内生真菌Diaporthe phaseolorum MBM-21的次级代谢产物进行研究。方法采用多种色谱法对Diaporthe phaseolorum MBM-21次级代谢产物进行分离,并结合理化性质及波谱解析等方法进行结构鉴定。采用MTT法测定单体化合物对非小细胞肺癌细胞A549和人宫颈癌细胞HeLa的细胞毒性。结果与结论从木本曼陀罗内生真菌Diaporthe phaseolorum MBM-21的次级代谢产物中分离得到12个化合物,分别鉴定为RKS-1778(1)、cytochalasin H(2)、cytochalasin U(3)、18-desoxycytochalasin C(4)、phomoxanthone A(5)、(22E,24R)-3β,5α,9α-trihydroxyergosta-7,22-diene-6-one(6)、stigmasta-7,22-diene-3β,5α,6α-triol(7)、cyclic(phenylpropane-pro)dipeptide(8)、brevinamide F(9)、N-acetyltryptamine(10)、3-isobutyl-pyrroline-2,5-dione cyclic(leuc-pro)dipeptide(11)和2-acetylamino-benzoic acid(12)。化合物2、4、5、7对A549细胞具有显著的细胞毒性,IC50值分别为1.16、9.86、7.12、7.23μmol·L^(-1);化合物2、4、5对HeLa细胞显示出较强的细胞毒性,IC50值分别为2.23、5.43、3.15μmol·L^(-1)。To study the antitumor activity of secondary metabolites of the Diaporthe fungus Diaporthe phaseolorum MBM-21,twelve compounds were isolated and purified by reverse phase ODS,repeated silica gel column chromatography and high performance liquid chromatography(HPLC).These compounds were identified as RKS-1778(1),cytochalasin H(2),cytochalasin U(3),18-desoxycytochalasin C(4),phomoxanthone A(5),(22E,24R)-3β,5α,9α-trihydroxyergosta-7,22-diene-6-one(6),stigmasta-7,22-diene-3β,5α,6α-triol(7),cyclic(phenylpropane-pro)dipeptide(8),brevinamide F(9),N-acetyltryptamine(10),3-isobutyl-pyrroline-2,5-dione cyclic(leuc-pro)dipeptide(11)and 2-acetylamino-benzoic acid(12).Compounds 2,4,5 and 7 exhibited strong cytotoxicity against human non-small cell lung cancer A549 cell line with IC50 values of 1.16,9.86,7.12 and 7.23μmol·L^(-1),respectively.Compounds 2,4 and 5 showed strong cytotoxicity against HeLa cell line with the IC50 values of 2.23,5.43 and 3.15μmol·L^(-1),respectively.

关 键 词：木本曼陀罗 内生真菌 双孢菌属 次级代谢产物 细胞毒性 

分 类 号：R284[医药卫生—中药学]