[Bioactive constituents inhibiting TNF-alpha production in fresh rhizome of Pinellia ternata].
OBJECTIVE
To study the bioactive constituents of the fresh rhizome of Pinellia ternata, and provide the scientific basis for quality control.


METHODS
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.


RESULTS
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.


CONCLUSIONS
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.
Han
Mei-hua
MH
State Key Laboratory of Natural and Biomimetic Drugs, Department of Natural Medicine, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.
Yang
Xiu-wei
XW
Zhong
Guo-yue
GY
Zhang
Ming
M
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000302:isolation & purification / Q000494:pharmacology; D002478:Cells, Cultured; D002934:Cinnamates / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D003373:Coumaric Acids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D005663:Furans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D017705:Lignans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D017737:Macrophages, Peritoneal / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D030021:Pinellia / Q000737:chemistry*; D010946:Plants, Medicinal / Q000737:chemistry; D027343:Rhizome / Q000737:chemistry*; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002934:Cinnamates; D003373:Coumaric Acids; D005663:Furans; D017705:Lignans; D014409:Tumor Necrosis Factor-alpha; C060282:lariciresinol; C004999:ferulic acid; C016316:coniferin