Polygonum cuspidatum, compared with baicalin and berberine, inhibits inducible nitric oxide synthase and cyclooxygenase-2 gene expressions in RAW 264.7 macrophages.
Polygonum cuspidatum water extract (PCWE) was shown to be a potent inhibitor of lipopolysaccharide (LPS)-induced expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). PCWE was compared to baicalin isolated from Scutellaria baicalensis Georgi and berberine of Coptidis rhizoma and Phellodendri cortex, for their effects on LPS-induced nitric oxide (NO) production and iNOS and COX-2 gene expressions in RAW 264.7 macrophages. Both PCWE and the compounds inhibited LPS-induced NO production in a concentration-dependent manner without a cytotoxicity. The decrease in NO production was in parallel with the inhibition of LPS-induced iNOS gene expression by PCWE and the compounds. In contrast, iNOS enzyme activity was not inhibited by PCWE and two agents. In addition, only PCWE inhibited LPS-induced prostaglandin E2 (PGE2) production and COX-2 gene expression without affecting COX-2 enzyme activity, while baicalin or berberine did not. Furthermore, N-nitro-L-arginine (NLA) and N-nitro-L-arginine methyl ester (L-NAME) pretreatment enhanced LPS-induced iNOS protein expression, which was inhibited by these PCWE and two agents, although LPS-induced COX-2 protein expression was not affected by NLA and L-NAME. PCWE inhibited PGE2 production and COX-2 protein expression in NLA/LPS or L-NAME/LPS-co-treated RAW 264.7 cell, however, baicalin or berberine did not. From the results, it was concluded that co-treatment with NOS inhibitors and PCWE effectively blocks acute production of NO and inhibits expression of iNOS and COX-2 genes.
Kim
Kyung-Woon
KW
Molecular and Cellular Glycobiology Unit, Department of Biological Science, Sungkyunkwan University, Chunchun-Dong 300, Suwon City, Kyunggi-Do 440-746, South Korea.
Ha
Ki-Tai
KT
Park
Cheol-Soo
CS
Jin
Un-Ho
UH
Chang
Hyen Wook
HW
Lee
In-Seon
IS
Kim
Cheorl-Ho
CH
D000818:Animals; D001599:Berberine / Q000008:administration & dosage / Q000494:pharmacology*; D000089042:Coptis chinensis; D051546:Cyclooxygenase 2 / Q000235:genetics / Q000378:metabolism; D015232:Dinoprostone / Q000096:biosynthesis; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000494:pharmacology*; D045468:Fallopia japonica / Q000737:chemistry*; D005419:Flavonoids / Q000008:administration & dosage / Q000494:pharmacology*; D015870:Gene Expression / Q000187:drug effects*; D008070:Lipopolysaccharides; D008264:Macrophages / Q000201:enzymology; D051379:Mice; D019331:NG-Nitroarginine Methyl Ester / Q000494:pharmacology; D009569:Nitric Oxide / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II / Q000235:genetics / Q000378:metabolism; D019335:Nitroarginine / Q000494:pharmacology; D032102:Phellodendron / Q000737:chemistry; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology; D031364:Scutellaria baicalensis / Q000737:chemistry
D004365:Drugs, Chinese Herbal; D004791:Enzyme Inhibitors; D005419:Flavonoids; D008070:Lipopolysaccharides; D010936:Plant Extracts; D001599:Berberine; D019335:Nitroarginine; D009569:Nitric Oxide; C038044:baicalin; C107393:Coptidis rhizoma extract; D052247:Nitric Oxide Synthase Type II; D051546:Cyclooxygenase 2; D015232:Dinoprostone; D019331:NG-Nitroarginine Methyl Ester