title: Isolation and identification of constituents with activity of inhibiting nitric oxide production in RAW 264.7 macrophages from Gentiana triflora.
abstract: Gentiana triflora is widely used to treat inflammation, jaundice, hepatitis, and rheumatism. In this study, three new compounds, including a benzo seven-membered ring compound, gentioxepine (1), two secoiridoid glucosides, (1S,5R,9R)-deglucosyltrifloroside (2) and (1S,5R,9R)-scabraside (3), together with seven known ones, (+)-syringaresinol (4), deglucogelidoside (5), 3,4-dihydro-1H,6H,8H-naphtho[1,2-c:4,5-c',d']dipyrano-1,8-dione (6), deglucoscabraside (7), 2-hydroxy-3-O-β-D-glucosyloxy benzoic acid methyl ester (8), gentiolactone (9), and trifloroside (10), were isolated from the ethanol extract of Gentiana triflora. Their structures were mainly confirmed on the basis of NMR, MS, IR, CD, and UV spectral evidences. Inhibiting activities of nitric oxide production of eight of the compounds isolated, as well as gentiopicroside, were evaluated in the macrophage cell line RAW 264.7. The results show that the three new compounds and compound 7 could significantly suppress lipopolysaccharide-induced production of NO, with IC50s of 2.2 µM, 37.5 µM, 17.6 µM and 6.9 µM, respectively. Among them, compounds 1, 3, and 7 showed stronger inhibitory activity than that of the clinically used drug indometacin. Other tested compounds exerted moderate inhibiting activities.
authors.affiliation: Pharmaceutical Informatics Institute, Zhejiang University, Zijingang Campus, Hangzhou, PR China. wangsf@zju.edu.cn
authors.forename: Shufang
authors.initials: S
authors.lastname: Wang
authors.forename: Yimin
authors.initials: Y
authors.lastname: Xu
authors.forename: Wei
authors.initials: W
authors.lastname: Jiang
authors.forename: Yufeng
authors.initials: Y
authors.lastname: Zhang
mesh_terms: D000818:Animals; D002460:Cell Line; D030012:Gentiana / Q000737:chemistry*; D008264:Macrophages / Q000187:drug effects* / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D009569:Nitric Oxide / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D013057:Spectrum Analysis
chemical_list: D010936:Plant Extracts; D009569:Nitric Oxide