The regulation of inflammatory cytokine secretion in macrophage cell line by the chemical constituents of Rhus sylvestris.
In our preliminary screening study on the anti-inflammatory activity, eight triterpenes, one sterol, and one chalcone were isolated from the CH(2)Cl(2)-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 10alpha-cucurbitadienol (1), glut-5-en-3-ol (2), beta-amyrin acetate (3), beta-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), beta-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 (0-1.0microM) 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-alpha, in a mouse RAW264.7 macrophage cell line. Moreover, compounds 2, 3, 7, and 10 specifically diminished only the secretion of TNF-alpha even in 0.01microM concentrations. It is thus suggested that they are potential therapeutics of TNF-alpha-related diseases and conditions, such as transplant rejection, type II diabetes, and atherosclerosis.
Ding
Yan
Y
College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea.
Nguyen
Huu Tung
HT
Kim
Sung In
SI
Kim
Ha Won
HW
Kim
Young Ho
YH
D027926:Anacardiaceae / Q000737:chemistry*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000633:toxicity; D002460:Cell Line; D016207:Cytokines / Q000378:metabolism*; D006801:Humans; D015850:Interleukin-6 / Q000378:metabolism; D008070:Lipopolysaccharides / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects* / Q000276:immunology; D051379:Mice; D018515:Plant Leaves / Q000737:chemistry; D012855:Sitosterols / Q000737:chemistry* / Q000302:isolation & purification / Q000633:toxicity; D014315:Triterpenes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
C542899:24-hydroxycycloart-25-en-3-one; D000893:Anti-Inflammatory Agents; D016207:Cytokines; D015850:Interleukin-6; D008070:Lipopolysaccharides; D012855:Sitosterols; D014315:Triterpenes; D014409:Tumor Necrosis Factor-alpha; C025473:gamma-sitosterol