[Bioactive constituents inhibiting TNF-alpha production in fresh rhizome of Pinellia ternata].

To study the bioactive constituents of the fresh rhizome of Pinellia ternata, and provide the scientific basis for quality control. Various chromatographic techniques were used to separate and purify the chemical constituents, and their chemical structures were determined on the basis of physical-chemical properties and spectroscopic analysis. The inhibitory effects of the isolated compounds on tumor necrosis factor (TNF)-alpha production in the peritoneal macrophages of mice stimulated with lipopolysaccharide (LPS) were assayed in vitro by microplate colorimetric method. Nine compounds were isolated and identified as (E)-p-coumaryl alcohol (1), 3, 4-dihydroxycinnamyl alcohol (2), ferulic acid (3), lariciresinol (4), erythro-guaiacylglycerol-beta-O-4'-sinapyl ether (5), dehydrodiconiferyl alcohol (6) , isolariciresinol (7) , sachaliside 1 (8) and coniferin (9). The inhibitory effect of compounds 1, 2, 3, 8, and 9 were 24.1% , 57.6% , 40.2% , 82.7% , and 62.0% , respectively, against the TNF-alpha production in the peritoneal macrophages of mice stimulated with LPS at a concentration of 10(-5) mol L(-1) in vitro. The compounds 1, 2 and 4-8 from genera Pinellia Ten. and compound 9 from P. ternata were isolated for the first time. The compounds 1, 2, 8 and 9 were phenylpropanoids, and 4-7 were lignanoids. The anti-inflammatory effects of the rhizome of P. ternata might relate at the least to compounds 1, 2, 3, 8 and 9.