title: In vitro anti-inflammatory effect of picrasmalignan A by the inhibition of iNOS and COX‑2 expression in LPS‑activated macrophage RAW 264.7 cells.
abstract: Picrasma quassioides (P. quassioides) has been widely used as a traditional Chinese medicine for clearing fever and detoxification. Previous phytochemical studies have identified a novel dihydrobenzofuran-type neolignan, picrasmalignan A, isolated from the stems of P. quassioides. In the present study, the in vitro anti-inflammatory effects and molecular mechanisms of picrasmalignan A have been investigated in cultured RAW 264.7 cells, a mouse macrophage‑like cell line. A Griess assay was used to demonstrate the inhibitory effect of picrasmalignan A on the overproduction of nitric oxide (NO). An enzyme-linked immunosorbent assay was used to determine the levels of pro-inflammatory cytokines, including tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). The inhibitory effect on the enzymatic activity of cyclooxygenase 2 (COX‑2) and inducible nitric oxide synthase (iNOS) was observed by colorimetric and fluorimetric assays, respectively. Western blotting was conducted to detect the expression of iNOS and COX-2. Results showed that picrasmalignan A suppressed lipopolysaccharide-stimulated NO production and pro-inflammatory cytokine secretion, including TNF-α and IL-6, in a dose-dependent manner. It also significantly inhibited the expression and enzymatic activity of iNOS and COX-2. These results may demonstrate the anti-inflammatory mechanism of picrasmalignan A.
authors.affiliation: School of Pharmacy, Yantai University, Laishan, Yantai, Shandong 264005, P.R. China.
authors.forename: Feng
authors.initials: F
authors.lastname: Zhao
authors.forename: Lei
authors.initials: L
authors.lastname: Chen
authors.forename: Chenchen
authors.initials: C
authors.lastname: Bi
authors.forename: Menglin
authors.initials: M
authors.lastname: Zhang
authors.forename: Weihua
authors.initials: W
authors.lastname: Jiao
authors.forename: Xinsheng
authors.initials: X
authors.lastname: Yao
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D001572:Benzofurans / Q000494:pharmacology*; D015153:Blotting, Western; D002478:Cells, Cultured; D051546:Cyclooxygenase 2 / Q000737:chemistry* / Q000378:metabolism; D004797:Enzyme-Linked Immunosorbent Assay; D018836:Inflammation Mediators / Q000037:antagonists & inhibitors / Q000378:metabolism; D015850:Interleukin-6 / Q000378:metabolism; D008070:Lipopolysaccharides / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects* / Q000378:metabolism; D051379:Mice; D009569:Nitric Oxide / Q000037:antagonists & inhibitors / Q000378:metabolism; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000378:metabolism; D000093242:Interleukin-6 Inhibitors
chemical_list: D000893:Anti-Inflammatory Agents; D001572:Benzofurans; D051546:Cyclooxygenase 2; D018836:Inflammation Mediators; D015850:Interleukin-6; D008070:Lipopolysaccharides; D009569:Nitric Oxide; D052247:Nitric Oxide Synthase Type II; D014409:Tumor Necrosis Factor-alpha; D000093242:Interleukin-6 Inhibitors; C561749:picrasmalignan A; C496317:Nos2 protein, mouse; C077623:Ptgs2 protein, mouse