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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。
OBJECTIVE: To study the biotransformation of cycloarten-24-ene-1α, 2α, 3β-triol isolated from myrrh in Ehrenberg, in order to obtain the antitumor activity, novel cycloarterine triterpene derivative. Methods: The medium was added to 14 strains of culture medium with potato medium and cultured at 27.8 ℃ for 7 days. The products were screened by TLC and the strains with transformation ability were screened. Penicillium chrysogenum was selected to carry out preparation-grade transformation test. 27.8 ℃ After cultured for 10 days, extracted with ethyl acetate, the products were separated and purified by silica gel column chromatography. Their structures were confirmed by mass spectrometry and nuclear magnetic resonance spectroscopy. The inhibitory effects on the growth of human prostate cancer cell lines were determined by MTT assay. Results: The substrate was transformed by Penicillium purpurogenum, and two new ring-shaped argentine-type triterpenes were obtained with the yield of 21.15%. The product had the growth inhibition effect on human prostate cancer cells PC3 and DU145 with IC50 value of 14.5 and 27.8 μmol / L. CONCLUSION: Cycloalkane-type triterpenoids can be bioconverted by Penicillium violaceum to produce two new hydroxylated derivatives.