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Chem Pharm Bull (Tokyo) ; 64(7): 988-90, 2016.
Article in English | MEDLINE | ID: mdl-27373660

ABSTRACT

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 (1)H- and (13)C-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 Trypanosoma brucei brucei GUTat3.1 with IC50 values of 0.33, 0.16, 0.061 and 5.08 µg/mL, respectively.


Subject(s)
Antiprotozoal Agents/pharmacology , Ascomycota/chemistry , Trypanosoma brucei brucei/drug effects , Antiprotozoal Agents/chemistry , Antiprotozoal Agents/metabolism , Ascomycota/metabolism , Dose-Response Relationship, Drug , Molecular Conformation , Parasitic Sensitivity Tests , Structure-Activity Relationship
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