期刊
PLANTA MEDICA
卷 78, 期 15, 页码 1683-1689出版社
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0032-1315211
关键词
Chaetomium elatum; Chaetomiaceae; azaphilones; chlorinated phenolic glycosides; caspase-3 inhibitors
资金
- Ministry of Science and Technology of China [2009CB522300, 2009ZX09302-004]
- Program for New Century Excellent Talents in University from the Ministry of Education of China [NCET-10-0120]
- China Postdoctoral Science Foundation [2012M511883]
- Fundamental Research Funds for the Central Universities [21611203]
Three new azaphilones, chaetomugilin S (1), 7,5'-bis-epi-chaetoviridin A (2), and 7-epi-chaetoviridin E (3), and two new chlorinated phenolic glycosides, globosumoside A (4) and globosumoside B (5), were isolated from the crude extract of the fungal strain Chaetomium elatum No. 89-1-3-1. Their structures were determined by detailed NMR and MS spectroscopic analyses. The absolute configurations of C-7 in chaetomugilin S (1), 7,5'-bis-epi-chaetoviridin A (2), and 7-epi-chaetoviridin E (3) were assigned by CD experiments, and the absolute configurations of 1 and 2 were established by X-ray crystallography. Compounds 1-3 are the first examples of 7R-configurated azaphilones with a chlorinated isochromen from Chaetomium spp. In addition, compounds 1-3 showed inhibitory activity in the cysteine aspartyl-specific protease-3 (caspase-3) enzymatic assay, with IC50 values of 20.6, 10.9, and 7.9 mu M, respectively.
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