title: [Studies on collagenase inhibitors. IV. Inhibitors of bacterial collagenase in Coptidis rhizoma].
abstract: A hot aqueous extract of Coptidis Rhizoma had an inhibitory effect on the bacterial collagenase from Clostridium histolyticum. Active principles were isolated by silica gel column chromatography from the CHCl3 extract. Consequently, two inhibitors obtained were identified with the chloride of berberine and coptisine. The concentrations of the berberine and coptisine in the assay mixture to give 50% inhibition (IC50) were 0.73 mM and 0.16 mM, respectively. The type of inhibition by coptisine chloride was shown to be a mixture type from Lineweaver-Burk plots. Tetrahydroberberine, a reduction product of berberine chloride, had no inhibitory effect. This result suggests that the quaternary nitrogen of the alkaloids plays an important role in inhibitory activity.
authors.affiliation: Department of Pharmacology, Kohno Clinical Medicine Research Institute, Tokyo, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Tanaka
authors.forename: K
authors.initials: K
authors.lastname: Metori
authors.forename: S
authors.initials: S
authors.lastname: Mineo
authors.forename: M
authors.initials: M
authors.lastname: Hirotani
authors.forename: T
authors.initials: T
authors.lastname: Furuya
authors.forename: H
authors.initials: H
authors.lastname: Matsumoto
authors.forename: T
authors.initials: T
authors.lastname: Satoh
authors.forename: S
authors.initials: S
authors.lastname: Kobayashi
mesh_terms: D001599:Berberine / Q000031:analogs & derivatives* / Q000302:isolation & purification / Q000494:pharmacology*; D004365:Drugs, Chinese Herbal / Q000032:analysis*; D003012:Microbial Collagenase / Q000037:antagonists & inhibitors*
chemical_list: D004365:Drugs, Chinese Herbal; C034384:coptisine; D001599:Berberine; D003012:Microbial Collagenase