摘要
为研究太子参内生真菌Aspergillus terreus TZS-201607所产的次级代谢产物,利用硅胶柱层析、Sephadex LH-20凝胶柱层析、反相柱层析及半制备高效液相色谱等技术,从其PDB培养基发酵产物的乙酸乙酯萃取物中分离纯化得到16个单体化合物。利用波谱学方法结合文献数据分析分别鉴定为柄曲霉素(1)、5-甲氧基柄曲霉素(2)、variecoxanthone A(3)、chryxanthone A(4)、6,8-di-O-methylaverufin(5)、6,8-di-O-methylnidurufin(6)、6,8,1′-tri-O-methyl averantin(7)、(22E,24R)-ergosta-7,9(11),22-trien-3β-ol(8)、(22E,24R)-ergosta-4,6,8(14),22-trtraen-3-one(9)、(22E,24R)-3β,5α-dihydroxy-ergosta-7,22-dien-6-one(10)、(22E,24R)-3β,5α,9α-trihydroxy-ergosta-7,22-diene-6-one(11)、(22E,24R)-3α-ureido-ergosta-4,6,8(14),22-tetraene(12)、(22E,24R)-ergosta-7,22-dien-3β,5α,6β-triol(13)、(22E,24R)-5α,8α-epidioxyergosta-6,22-dien-3β-ol(14)、demethylincisterol A3(15)和(17R)-17-methylincisterol(16)。化合物1~7、12、14~16为首次从A.terreus中分离得到。体外抗肿瘤活性测试显示,化合物6、7和14对人肿瘤细胞株A549、BT-549、HeLa和THP-1表现出较强的细胞毒活性(IC50<10μM)。
The secondary metabolites of the endophytic fungus Aspergillus terreus TZS-201607 isolated from Pseudostellaria heterophylla were fully studied.A total of 16 compounds were isolated from the EtOAc extracts of the PDB culture broth by means of chromatographic techniques,including silica gel,Sephadex LH-20 gel,reversed-phase and semi-preparative HPLC column chromatography.Their structures were identified as sterigmatocystin(1),5-methoxysterigmatocystin(2),variecoxanthone A(3),chryxanthone A(4),6,8-di-O-methylaverufin(5),6,8-di-O-methylnidurufin(6),6,8,1′-tri-O-methyl averantin(7),(22E,24R)-ergosta-7,9(11),22-trien-3β-ol(8),(22E,24R)-ergosta-4,6,8(14),22-trtraen-3-one(9),(22E,24R)-3β,5α-dihydroxy-ergosta-7,22-dien-6-one(10),(22E,24R)-3β,5α,9α-trihydroxy-ergosta-7,22-diene-6-one(11),(22E,24R)-3α-ureido-ergosta-4,6,8(14),22-tetraene(12),(22E,24R)-ergosta-7,22-dien-3β,5α,6β-triol(13),(22E,24R)-5α,8α-epidioxyergosta-6,22-dien-3β-ol(14),demethylincisterol A3(15),and(17R)-17-methylincisterol(16),by spectroscopic analysis and by comparison with previously reported literatures.Compounds 1-7,12,and 14-16 were isolated from the fungus A.terreus for the first time.The cytotoxicity of compounds 1-16 against A549,BT-549,HeLa,HepG2,MCF-7,and THP-1 cell lines was evaluated.Compounds 6,7,and 14 showed strong inhibitory activity against A549,BT-549,HeLa,and THP-1 cell lines,respectively(IC50<10μM).
作者
胡晓峰
柴海全
贾林川
邵露
刘晓晓
陈野
HU Xiao-feng;CHAI Hai-quan;JIA Lin-chuan;SHAO Lu;LIU Xiao-xiao;CHEN Ye(Qingdao Hospital of Traditional Chinese Medicine,Qingdao 266071,China)
出处
《天然产物研究与开发》
CAS
CSCD
2021年第7期1156-1164,共9页
Natural Product Research and Development
基金
山东省中医药科技发展计划(2019-0590)。