没药中环阿尔廷烷型三萜的生物转化研究

目的:对爱伦堡没药中分离获得的环阿尔廷-24-烯-1α,2α,3β-三醇开展生物转化研究,以期获得抗肿瘤活性好、结构新颖的环阿尔廷烷型三萜衍生物。方法:采用马铃薯培养基,将底物加入到14株菌株培养液中,27.8℃培养7 d,以TLC检测产物,筛选具有转化能力的菌株;选择微紫青霉开展制备级转化试验,27.8℃培养10d,乙酸乙酯萃取后,硅胶柱色谱分离纯化转化产物,以质谱、核磁共振波谱确定其结构,并采用MTT法测定其对人前列腺癌细胞株生长抑制作用。结果:微紫青霉对底物进行了转化,获得了两个新的环阿尔廷烷型三萜,产率为21.15%;产物对人前列腺癌细胞PC3和DU145具有生长抑制作用,IC50值为14.5和27.8μmol/L。结论:环阿尔廷烷型三萜能被微紫青霉生物转化,产生两个新的羟基化衍生物。

Biotransformation of Cycloartane-Type Triterpenoid from Myrrh

Objective:To study the biotransformation of cycloartan-24-ene-1α,2α,3β-triol isolated from myrrh and find new anti-tumor bioactive cycloartane-type derivatives.Methods:Fourteen microbial strains were cultured in potato medium at 27.8 ℃ for 7 days.The strain of Penicillium janthinellum was selected for preparative transform assay,and cultured in potato medium at 27.8 ℃ for 10 days.The medium was extracted by EtOAc,and then EtOAc layer was purified by the silica gel column chromatography.The product was structurally elucidated by MS and NMR spectra,and their anti-proliferative effects against human prostate cancer PC3 and DU145 cells were evaluated using MTT assay.Results:The substrate was transformed to two new hydroxyl substituted triterpenoids,with a yield of 21.15%;The products displayed anti-proliferative effect against PC3 and DU145 cells with IC50 values of 14.5 μmol/L and 27.8 μmol/L,respectively.Conclusion:Cycloartane-type triterpenoid can be bio-transformed by Penicillium janthinellum,and leading to the isolation of two new hydroxyl substituted derivatives.