去氢木香内酯在内生真菌Y0液体发酵中的生物转化研究

Biotransformation of Denydcrostus Lactone in the Liquid Fermentation Broth of Endogenous Fungi Y0

目的去氢木香内酯在内生真菌Y0液体发酵中的生物转化。方法对内生真菌Y0纯化培养,采用色谱法及波谱技术对转化产物进行分离及结构鉴定,并采用MTT法评价其对结肠癌SW620细胞的毒性。利用网络药理学相关数据库获取化合物1、2以及结肠癌SW620细胞靶点信息,对化合物与结肠癌SW620细胞结合能较强的靶点做进一步的分子对接。结果去氢木香内酯在Y0菌液中转化得到2个化合物,分别鉴定为(1S,3S,5S,6S,7S,11S)-3-hydroxyl-11,13-dihydrodehydrocostuslactone和(1S,3S,5S,6S,7S,11R)-3-hydroxyl-11,13-dihydrodehydrocostuslactone。化合物1和2对结肠癌SW620细胞的IC50分别为(42.82±8.32)μg/mL,(29.23±7.17)μg/mL。化合物1和2与结肠癌SW620细胞均有结合靶点。结论化合物1和2为愈创木烷型倍半萜类化合物,化合物1与化合物2对SW620细胞毒性相比,化合物2的细胞毒性更强。

Objective To investigate the biotransformation of dehydrocostlactone in the liquid fermentation of endogenic fungus Y0.Methods The endophytic fungus of Y0 were purified and cultured,and then the transformed products were isolated and identified by chromatographic and spectral techniques.The toxicity to SW620 cells was evaluated by MTT assay.The targets information of two compounds and colon cancer SW620 cells was obtained by using online pharmacologic database.Further molecular docking of the compounds with targets with strong binding energy of colon cancer SW620 cells was performed.Results Two compounds were obtained by the way of biotransformation from dehydrocostlactone in endogenic fungus Y0 and identified as(1S,3S,5S,6S,7S,11S)-3-hydroxl-11,13dihydrodehydrocostuslactone and(1S,3S,5S,6S,7S,11R)-3-hydroxyl-11,13-dihydrodehydrocostusl actone.The IC50 of compounds 1 and 2 against coloncancer cell SW620 were(42.82±8.32)μg/mL and(29.23±7.17)μg/mL.Compounds 1 and 2 have binding targets to colon cancer SW620 cells.Conclusion Compounds 1 and 2 are guaiacane sesquiterpenoids.Compound 1 was more cytotoxic to SW620 cells than compound 2.