Article ID Journal Published Year Pages File Type
1372248 Bioorganic & Medicinal Chemistry Letters 2009 4 Pages PDF
Abstract

In our preliminary screening study on the anti-inflammatory activity, eight triterpenes, one sterol, and one chalcone were isolated from the CH2Cl2-soluble extract of the stems and leaves of Rhus sylvestris Siebold and Zucc (Anacardiaceae). On the basis of their spectroscopic data, these compounds were identified as 10α-cucurbitadienol (1), glut-5-en-3-ol (2), β-amyrin acetate (3), β-amyrin (4) and lupeol (5), cycloart-24-en-3-one (6), cycloart-25-en-3,24-dione (7), 24-hydroxycycloart-25-en-3-one (8), β-sitosterol (9), and 2′-hydroxy-4,4′-dimethoxychalcone (10). All of them were isolated from this plant for the first. Furthermore, the compounds in non-cytotoxic concentrations (0–1.0 μM) were tested for their ability to block inflammatory cytokine secretion in the presence of LPS in the murine RAW264.7 macrophage cell line. Among the compounds that were tested, compounds 8 and 9 reduced the LPS-induced secretion of IL-6, as well as TNF-α, in a mouse RAW264.7 macrophage cell line. Moreover, compounds 2, 3, 7, and 10 specifically diminished only the secretion of TNF-α even in 0.01 μM concentrations. It is thus suggested that they are potential therapeutics of TNF-α-related diseases and conditions, such as transplant rejection, type II diabetes, and atherosclerosis.

Graphical abstractBioassay-guided fractionation of the CH2Cl2-soluble extract led to the isolation of 10 compounds. Compounds 8 and 9 reduced the LPS-induced secretion of IL-6 and TNF-α in a RAW264.7 cell line.Figure optionsDownload full-size imageDownload as PowerPoint slide

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Physical Sciences and Engineering Chemistry Organic Chemistry
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