title: Constituents of PG201 (Layla(®)), a multi-component phytopharmaceutical, with inhibitory activity on LPS-induced nitric oxide and prostaglandin E2 productions in macrophages.
abstract: Fourteen compounds, coumarin (1), demethylsuberosin (2), xanthotoxin (3), psoralen (4), decursinol (5), decursin (6), decursinol angelate (7), chikusetsusaponin IVa (8), chikusetsusaponin IVa methyl ester (9), ethyl caffeate (10), syringaresinol (11), cnidilide (12), farnesol (13), and linoleic acid (14), were isolated from phytopharmaceutical PG201 (Layla(®)) by activity-guided fractionation utilizing inhibitory activity on nitric oxide (NO) production in vitro. The isolates 1-14 were evaluated for their inhibitory activity on LPS-induced NO and prostaglandin E2 (PGE2) productions in RAW 264.7 cells. All the compounds except 14 displayed suppressive effects on LPS-induced NO and PGE2 production with IC50 values ranging from 8 to 60 μM. Among these, compound 10 showed the most potent inhibitory effect on NO production from RAW 264.7 cells with an IC50 value of 8.25 μM. Compounds 2, 9, and 10 exhibited high inhibitory effects on PGE2 production with the IC50 values of 9.42, 7.51, and 6.49 μM, respectively. These findings suggest that compounds 2, 9, and 10 are the potential anti-inflammatory active constituents of PG201 and further study may be needed to explain their mechanism of action.
authors: College of Pharmacy, Kyung Hee University, Seoul, 130-701, Republic of Korea.
authors: Hyun Ji
authors: HJ
authors: Kim
authors: College of Pharmacy, Kyung Hee University, Seoul, 130-701, Republic of Korea.
authors: Hye Mi
authors: HM
authors: Kim
authors: Department of Life and Nanopharmaceutical Science, Kyung Hee University, Seoul, 130-701, Republic of Korea.
authors: Byeol
authors: B
authors: Ryu
authors: College of Pharmacy, Kyung Hee University, Seoul, 130-701, Republic of Korea.
authors: Woo-Seok
authors: WS
authors: Lee
authors: College of Pharmacy, Kyung Hee University, Seoul, 130-701, Republic of Korea.
authors: Ji-Sun
authors: JS
authors: Shin
authors: College of Pharmacy, Kyung Hee University, Seoul, 130-701, Republic of Korea. ktlee@khu.ac.kr.|Department of Life and Nanopharmaceutical Science, Kyung Hee University, Seoul, 130-701, Republic of Korea. ktlee@khu.ac.kr.
authors: Kyung-Tae
authors: KT
authors: Lee
authors: College of Pharmacy, Kyung Hee University, Seoul, 130-701, Republic of Korea. dsjang@khu.ac.kr.|Department of Life and Nanopharmaceutical Science, Kyung Hee University, Seoul, 130-701, Republic of Korea. dsjang@khu.ac.kr.
authors: Dae Sik
authors: DS
authors: Jang
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology*; D015232:Dinoprostone / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D007249:Inflammation / Q000378:metabolism / Q000517:prevention & control*; D008070:Lipopolysaccharides / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects* / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D009569:Nitric Oxide / Q000378:metabolism*; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D010946:Plants, Medicinal; D000067996:RAW 264.7 Cells
chemical_list: D000893:Anti-Inflammatory Agents; D008070:Lipopolysaccharides; D010936:Plant Extracts; C476094:herbal extract PG201; D009569:Nitric Oxide; D015232:Dinoprostone
keywords: Constituents; Layla®; Nitric oxide; PG201; Phytopharmaceutical; Prostaglandin E2