本文關鍵詞： Microbial transformation Mortierella ramanniana Gibberella fujikuroi Diterpenoid Ingenane Hydroxylation　出處：《Chinese Journal of Natural Medicines》2016年12期 　論文類型：期刊論文

【摘要】：The regio- and stereo-selective hydroxylations of two ingenane diterpenoids, 20-deoxyingenol(1) and 13-oxyingenol dodecanoat(2), by the filamentous fungi Mortierella ramanniana and Gibberella fujikuroi were investigated in the present study. Four undescribed metabolites(3 6) of substrate 1 and two undescribed metabolites(7 and 8) of substrate 2 were isolated. All the lites were identified as hydroxylated ingenane derivatives by extensive NMR and HR-ESI-MS data analyses. All the biotransformed compounds and the substrates were evaluated for their cytotoxicities against three human cancer cell lines, including human colon cancer Caco-2, breast cancer MCF-7, and adriamycin(ADM)-resistant MCF-7/ADM cell lines. All ingenane alcohols(1, and 3 6) displayed no significant cytotoxic activities. The substrate 13-oxyingenol dodecanoat(2) showed moderate cytotoxicity with IC50 values being 35.59 ± 5.37 μmol·L~(-1)(Caco-2), 24.04 ± 4.70 μmol·L~(-1)(MCF-7), and 22.24 ± 5.19 μmol·L~(-1)(MCF-7/ADM). However, metabolites 7 and 8 displayed no significant cytotoxicity. These results indicated that the hydroxylation at the C~(-1)3 aliphatic acid ester of substrate 2 can significantly reduce the cytotoxic activity.
[Abstract]:The regio- and stereo-selective hydroxylations of two ingenane diterpenoids1) and 13-oxyingenol dodecanoat2, by the filamentous fungi Mortierella ramanniana and Gibberella fujikuroi were investigated in the present study. Four undescribed metabolites(3 6) of substrate 1 two undescribed metabolites(7 and 8. Evaluated for their cytotoxicities against three human cancer cell lines. including human colon cancer Caco-2, breast cancer MCF-7, and adriamycin(ADM)-resistant MCF-7/ADM cell lines. All ingenane alcohol 1, and 3) displayed no cytotoxic activities. The substrate substrate 13-oxyol doanoat2) showed moderate cytotoxicity IC50 values IC50 values values values 鹵5.37 渭 values values values 鹵5.37 渭 #en4aco-2n, 24.04 鹵4.70 渭 #en3C3F-7F-7F, #en322.24 鹵5.19 mol -1F-711# significant significant These significant These These These. That the hydroxylation at the aliphatic acid ester of substrate 2 can significantly reduce the cytotoxic activity.
【作者單位】： Department
【分類號】：R915

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