摘要
目的探索山茶花内生真菌Paraconiothyrium brasiliense次生代谢产物化学成分及降糖作用。方法使用硅胶柱色谱、薄层色谱(TLC)及高效液相色谱(HPLC)等分离纯化真菌发酵后的乙酸乙酯部位提取物,根据波谱方法与文献数据对比进行结构表征。采用pNPG法对分离得到的化合物进行降糖活性筛选,并用分子对接的手段进一步研究化合物对α-葡萄糖苷酶的抑制作用。结果从真菌发酵后的乙酸乙酯部位提取物中分离得到11个已知化合物,并检测了降糖活性。化合物6对α-葡萄糖苷酶有抑制活性,IC50为(15.48±11.82)。分子对接表明,化合物6结合能为-6.5 kJ/mol。结论化合物1~5、7~11为首次从真菌Paraconiothyrium brasiliense中分离得到,其中化合物6对α-葡萄糖苷酶有较强的抑制作用。
Objective To study the chemical composition of the endophytic fungus Paraconiothyrium brasiliense from camellia sp.and their hypoglycemic effects.Methods The ethyl acetate extracts were separated and purified by silica gel column chromatography,thin layer chromatography(TLC),and high performance liquid chromatography(HPLC).The structures of the obtained compounds were characterized according to spectroscopic methods or by comparison with relevant literature data.The hypoglycemic activity of the isolated compounds was screened by pNPG method,and the inhibitory mechanism ofα-glucosidase was further studied by molecular docking method.Results Eleven known compounds were isolated from the ethyl acetate extract after fungal fermentation.The glucose-lowering activity assay indicated that compound 6 had an inhibitory activity onα-glucosidase with IC50 value of(15.48±11.82).Molecular docking assay showed that the binding energy of compound 6 was-6.5 kJ/mol.Conclusion Compounds 1~5,7~11 are isolated for the first time from the fungus Paraconiothyrium brasiliense.Compound 6 shows a moderate inhibitory effect onα-glucosidase.
作者
冼小雅
赵苗
梁琳
闫梦麒
周先丽
梁成钦
XIAN Xiaoya;ZHAO Miao;LIANG Lin;YAN Mengqi;ZHOU Xianli;LIANG Chengqin(College of Pharmacy,Guilin Medical University,Guilin 541199,China;College of Intelligent Medicine&Biotechnology,Guilin Medical University,Guilin 541199,China)
出处
《华夏医学》
CAS
2024年第3期54-62,共9页
Acta Medicinae Sinica
基金
国家自然科学基金项目(81860621)。
关键词
山茶花内生真菌
次生代谢产物
降糖活性
Paraconiothyrium Brasiliense
fungus
secondary metabolites
hypoglycemic activity
