期刊
PHYTOCHEMISTRY
卷 83, 期 -, 页码 79-86出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.phytochem.2012.06.004
关键词
Entandrophragma cylindricum; Cameroonian medicinal plant; Sapelenin; Anti-inflammatory; Cytotoxic
资金
- Dortmunder Gambrinus Fellowship
- International Foundation of Science [F/4893-1]
- German Academic Exchange Service (DAAD) initiative Welcome to Africa
- Ministry of Innovation, Science, Research and Technology of the State of North Rhine-Westphalia, Germany
- German Research Foundation (DFG)
Four acyclic triterpene derivatives named sapelenins G-J (1-4), along with eight known compounds, sapelenins A-D, ekeberin D2 (5), (+)-catechin and epicatechin, and anderolide G, were isolated from the stem bark of the Cameroonian medicinal plant, Entandrophragma cylindricum Sprague, on the basis of bioassay-guided fractionation. Their structures were determined by means of high-resolution mass spectrometry and NMR spectroscopic data, as well as by comparison with the literature values of their analogs. The absolute configurations of the compounds (1-4) were assigned by the modified Mosher's method in conjunction with NOESY experiments and chemical modifications. The anti-inflammatory activities of the sapelenins were evaluated by assessing their ability to suppress or inhibit the secretion of cytokine interleukin-17 (IL-17) by human peripheral blood mononuclear cells (PBMC) stimulated with phytohemagglutinin (PHA). The cytotoxicity of these compounds on PMBCs was further assessed for correctly interpreting their anti-inflammatory responses. The tested compounds demonstrated moderate to significant anti-inflammatory activities by suppressing the secretion of IL-17 by PHA-stimulated human PBMCs. One of them, sapelenin G (1), showed high potency in suppressing the secretion of IL-17 by PBMCs comparable to reference cyclosporine A, without causing any cytotoxic effects (negligible), and deserves further considerations towards developing an effective anti-inflammatory drug. (C) 2012 Elsevier Ltd. All rights reserved.
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