The marine algal-derived endophytic fungus Aspergillus wentii EN-48 produces the potential anti-tumor agent asperolide A, a tetranorlabdane diterpenoid active against lung cancer. However, the fermentation yield of as...The marine algal-derived endophytic fungus Aspergillus wentii EN-48 produces the potential anti-tumor agent asperolide A, a tetranorlabdane diterpenoid active against lung cancer. However, the fermentation yield of asperolide A was very low and only produced in static cultures. Static fermentation conditions of A. wentii EN-48 were optimized employing response surface methodology to enhance the production of asperolide A. The optimized conditions resulted in a 13.9-fold yield enhancement, which matched the predicted value, and the optimized conditions were successfully used in scale-up fermentation for the production of asperolide A. Exogenous addition of plant hormones (especially 10 pmol/L methyl jasmonate) stimulated asperolide A production. To our knowledge, this is first optimized production of an asperolide by a marine-derived fungus. The optimization is effective and valuable to supply material for further anti-tumor mechanism studies and preclinical evaluation of asperolide A and other norditerpenoids.展开更多
Nine prenylated and geranylated xanthones were synthesized in two steps with total yields ranging from 11%to 36%.All of the compounds were first reported.Then,the antitumor,anti-tyrosinase,anti-pancreatic lipase,antif...Nine prenylated and geranylated xanthones were synthesized in two steps with total yields ranging from 11%to 36%.All of the compounds were first reported.Then,the antitumor,anti-tyrosinase,anti-pancreatic lipase,antifungal and antibacterial activities of all or part of compounds 1–9 were evaluated.Compound 9 exhibited clear antitumor activity,and its cytotoxicity against MCF-7 and MDA-MB-231 cells was stronger compared with cisplatin.Compounds 1–4 and 6–7 also exhibited certain activity other than the antitumor activity described above.These results demonstrated that compounds 1–4,6–7 and 9 were very promising leads for further structural modification.展开更多
基金Supported by the National Natural Science Foundation of China(NSFC,Nos.31200042,31570038)the NSFC-Shandong Joint Fund for Marine Science Research Centers(No.U1406402)
文摘The marine algal-derived endophytic fungus Aspergillus wentii EN-48 produces the potential anti-tumor agent asperolide A, a tetranorlabdane diterpenoid active against lung cancer. However, the fermentation yield of asperolide A was very low and only produced in static cultures. Static fermentation conditions of A. wentii EN-48 were optimized employing response surface methodology to enhance the production of asperolide A. The optimized conditions resulted in a 13.9-fold yield enhancement, which matched the predicted value, and the optimized conditions were successfully used in scale-up fermentation for the production of asperolide A. Exogenous addition of plant hormones (especially 10 pmol/L methyl jasmonate) stimulated asperolide A production. To our knowledge, this is first optimized production of an asperolide by a marine-derived fungus. The optimization is effective and valuable to supply material for further anti-tumor mechanism studies and preclinical evaluation of asperolide A and other norditerpenoids.
基金Leading Project of Fujian Provincial Department of Science and Technology(Grant No.2018Y0072)。
文摘Nine prenylated and geranylated xanthones were synthesized in two steps with total yields ranging from 11%to 36%.All of the compounds were first reported.Then,the antitumor,anti-tyrosinase,anti-pancreatic lipase,antifungal and antibacterial activities of all or part of compounds 1–9 were evaluated.Compound 9 exhibited clear antitumor activity,and its cytotoxicity against MCF-7 and MDA-MB-231 cells was stronger compared with cisplatin.Compounds 1–4 and 6–7 also exhibited certain activity other than the antitumor activity described above.These results demonstrated that compounds 1–4,6–7 and 9 were very promising leads for further structural modification.