title: Practical synthesis and biological evaluation of bergenin analogs.
abstract: Here, we describe the practical synthesis and biological properties of bergenin and its structural analogs. Synthetic bergenin compounds were prepared by acylation of bergenin. These compounds were then evaluated for suppression of lipopolysaccharide-induced nitric oxide (NO) generation in cultured cells and anti-narcotic effects on morphine-dependent mice. We found that bergenin derivatives showed potent anti-inflammatory activity (suppression of NO generation) at concentrations ranging from 20 to 30 μmin vitro, and bergenin derivatives (10-20 mg/kg) exhibited significant anti-narcotic effects on morphine dependence in mice. These results suggest the potential utility of bergenin and its analogs as anti-narcotic agents and the design of more potent anti-inflammatory compounds.
authors.affiliation: Department of Neuroscience, TIDRC and Medical Research Institute, School of Medicine, Ewha Womans University, Seoul 158-710, South Korea.
authors.forename: Jae-Chul
authors.initials: JC
authors.lastname: Jung
authors.forename: Eunyoung
authors.initials: E
authors.lastname: Lim
authors.forename: Seung Hwan
authors.initials: SH
authors.lastname: Kim
authors.forename: Nam Soo
authors.initials: NS
authors.lastname: Kim
authors.forename: Mankil
authors.initials: M
authors.lastname: Jung
authors.forename: Seikwan
authors.initials: S
authors.lastname: Oh
mesh_terms: D000215:Acylation; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001578:Benzopyrans / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D060326:Chemistry Techniques, Synthetic; D008070:Lipopolysaccharides / Q000378:metabolism; D051379:Mice; D008810:Mice, Inbred C57BL; D017628:Microglia / Q000166:cytology; D009021:Morphine Dependence / Q000188:drug therapy*; D009569:Nitric Oxide / Q000378:metabolism*; D019966:Substance-Related Disorders
chemical_list: D000893:Anti-Inflammatory Agents; D001578:Benzopyrans; D008070:Lipopolysaccharides; D009569:Nitric Oxide; C006741:bergenin