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 RelationshipABSTRACT
A new compound, 3-O-(4-O-methyl-ß-D-glucopyranosyl) xanthone (1) was isolated from the culture of Conoideocrella luteorostrata NBRC106950. The structure of 1 was mainly determined by 1H, 13C, 2D-NMR and HREIMS spectral analyses. The absolute configuration of 4-O-methylglucopyranosyl moiety was determined by the optical rotation of aqueous layer of hydrolyzed 1 as D-configuration.
Subject(s)
Hypocreales , Xanthones , Animals , Glucosides , Hypocreales/chemistry , Insecta , Molecular Structure , Xanthones/chemistryABSTRACT
We examined the immunomodulatory effect of Eriobotrya japonica seed extract (ESE) on rat allergic dermatitis elicited by repeated dinitrofluorobenzene (DNFB) application on the ear. Oral administration of ESE significantly inhibited development of allergic dermatitis based on lower ear thickness and serum immunoglobulin E (IgE) levels. Th1 cytokine interferon-gamma (IFN-gamma) and interleukin-2 (IL-2), Th2 cytokine interleukin-4 (IL-4) and interleukin-10 (IL-10) in the lesional skin were determined. Oral administration of ESE significantly decreased IL-4 while significantly increasing IL-10 in lesional skin, and the lower levels of IFN-gamma and IL-2 were reversed by oral administration of ESE. The infiltration of eosinophils in the lesional skin was decreased by oral administration of ESE. These results suggested that ESE exerts anti-allergic actions by improving the balance of Th1/Th2 in allergic dermatitis.