海南粗榧内生真菌F127发酵液的次级代谢产物研究

对海南粗榧(Cephalotaxus hainanensis Li.)内生真菌F127发酵液化学组分进行研究。用多种色谱技术对F127代谢产物进行分离纯化,以LC-MS、ESI-MS和超导核磁共振分析鉴定化合物结构,最后采用MTT法测定化合物的抗肿瘤活性。从海南粗榧内生真菌F127的发酵液中分离得到5个单体化合物,分别鉴定为oblongolide T(1)、sorbicillin(2)、邻苯二甲酸二丁酯(3)、phomopsolide B(4)、6,8-二羟基-3-甲基-3,4-二氢异香豆素(5),且化合物1、4、5对肿瘤细胞K562、NB4、HL-60、Hep G-2和Lovo表现出不同抑制活性。化合物4对5株肿瘤细胞均表现出抑制活性,对K562、NB4、HL-60抑制效果显著,IC50值分别为3.35、0.014和0.16μg/m L,对Hep G-2和Lo Vo只有温和抑制作用;化合物1对K562、NB4、HL-60抑制作用良好,IC50值分别为51.82、54.25和29.31μg/m L;化合物5对NB4和Hep G-2则具有一定抑制活性;化合物2和3对测试细胞株未表现出抑制活性。5个化合物均是首次从海南粗榧内生真菌中分离得到,并首次报道了化合物1、4对K562、NB4、HL-60的优良细胞毒活性,为进一步研究海南粗榧内生真菌中的活性天然产物奠定了基础。

Secondary Metabolites of Endophyte F127 from Cephalotaxus hainanensis Li.

To study the chemical constituents of the endophyte F127 of Cephalotaxus hainanensis Li.,the constituents were isolated and purified by multi-chromatography,and their structure were elucidated by spectroscopic analyses including LC-MS,ESI-MS,1H NMR and 13C NMR.Meanwhile,the cyctotoxic activities were evaluated by MTT assay.Five known metabolites including oblongolide T(1),sorbicillin(2),dibutylphthalate(3),phomopsolide B(4) and one 3,4-dihydroisocomnarin(5) were isolated from the broth of the endophyte F127.And compound 1,4,5 exhibited different cyototoxic activities against K562,NB4,HL-60,HepG-2 and LoVo.Compound 4 showed cytotoxic activities against 5 tumor cell lines in vitro,which significantly inhibiting K562,NB4,HL-60 cells with IC5o of 3.35,0.014 and 0.16 μg/mL,and moderately inhibiting HepG-2 and LoVo.Compound 1 exhibited good cytotoxic activites aginst K562,NB4,HL-60 cells as well,with IC5o of 51.82,54.25 and 29.31 μg/mL.Moderate cytotoxic activites aginst NB4 and HepG-2 were alsso observed for compound 5.The rest of the founds showed no substantial effect against the tumor cells.The five compounds were all the first time isolated from the endophytes from C.hainanensis Li..And the significant cytotoxic activtities against to K562,NB4,HL-60 of compound 1 and 4 was reported for the first time,which laid the foundation of studying the bioactive natural products from endophytes from C.hainanensis Li..