1株药用红树内生真菌Talaromyces flavus TGGP34次级代谢产物及其活性研究

Study on the secondary metabolites and bioactivities of a medicinal mangrove endophytic fungus Talaromyces flavus TGGP34

目的研究1株药用红树老鼠簕(Acanthus ilicifolius L.)来源内生真菌篮状菌属的Talaromyces flavus TGGP34的次级代谢产物及其抗菌活性。方法利用正相硅胶柱层析、Sephadex LH-20凝胶柱层析、半制备高效液相色谱(HPLC)等色谱分离方法,对TGGP34发酵产物的乙酸乙酯粗浸膏进行系统分离纯化;利用核磁共振波谱(NMR)、质谱(MS)等方法并结合文献报道数据确定化合物结构,并对其抗菌活性进行测定。结果从内生真菌T. flavus TGGP34中分离得到9个化合物,包括4个甾醇类化合物β-sitosterol(1)、24-methylcholesta-7,22-diene-3β,5α,6β-triol(2)、3β,15β-dihydroxyl-(22E,24R)-ergosta-5,8(14),22-trien-7-one(3)、ganodermaside B(4),3个内酯类化合物dehydroisopenicillide(5)、penicillide(6)、purpactin A(7),2个二酮哌嗪类化合物cyclo-(S-Pro-R-Val)(8)和cyclo-(L-Pro-L-Leu)(9),其中化合物3对3株致病菌金黄色葡萄球菌(Staphylococcus aureus)、表皮葡萄球菌(Staphylococcus epidermidis)和白色念珠菌(Candida albicans)表现出明显的抑制活性,其MIC值分别为12.5、12.5和6.25μg/mL。结论化合物1~4为首次从篮状菌属(Talaromyces sp.)中分离得到;化合物3具有显著的抗菌活性,具有重要的研究和潜在开发价值。

Objective To study the secondary metabolites and biological activities of the endophytic fungus Talaromyces flavus TGGP34 derived from Acanthus ilicifolius L. Methods The isolated compounds were separated by normal phase silica gel, Sephadex LH-20, semi-preparative HPLC column chromatography,thin layer chromatography and so on. And their structures were identified by 1 D NMR, MS, other spectral analysis methods and comparison with literature data. They were also tested for their antibacterial activity.Results Nine known compounds were isolated from the endophytic fungus T. flavus TGGP34, including four sterols β-sitosterol(1), 24-methylcholesta-7,22-diene-3β,5α,6β-triol(2), 3β,15β-dihydroxyl-(22 E,24 R)-ergosta-5,8(14), 22-trien-7-one(3), ganodermaside B(4), three lactones dehydroisopenicillide(5), penicillide(6),purpactin A(7), and two diketopiperazines cyclo-(S-Pro-R-Val)(8) and cyclo(L-Pro-L-Leu)(9). Compound 3 showed antibacterial activity against three pathogenic bacteria Staphylococcus aureus, Staphylococcus epidermidis and Candida albicans, with the MIC values of 12.5, 12.5 and 6.25μg/mL, respectively. Conclusion Compounds 1~4 were isolated from the genus Talaromyces sp. for the first time, and compound 3 showed significant antibacterial activity, and had important research and potential development value.