Journal
CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 64, Issue 7, Pages 988-990Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.c16-00220
Keywords
Trypanosoma brucei brucei; depsipeptide; nortriterpenoid; Ophiocordyceps coccidiicola
Funding
- Ministry of Education, Culture, Sports, Science and Technology (MEXT) of Japan-Senryaku project [S0891078]
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During the search for new antitrypanosomal drug leads, four antitrypanosomal compounds, of three depsipeptides and one nortriterpenoid, were isolated from cultures of the mutant strain IU-3 of the insect pathogenic fungus Ophiocordyceps coccidiicola NBRC 100683. Their structures were identified by the analysis of high resolution-electron ionization (HR-EI)-MS and HR-FAB-MS, and H-1- and C-13-NMR spectra, including extensive two dimensional (2D)-heteronuclear NMR experiments, and comparison with literature data for destruxin A (1), destruxin B (2), destruxin E chlorohydrin (3) and helvolic acid (4). Compounds 1-4 showed in vitro antitrypanosomal activity against Trypanosome brucei brucei GUTat3.1 with IC50 values of 0.33, 0.16, 0.061 and 5.08 mu g/mL, respectively.
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