title: Aldose reductase inhibitory constituents of the root of Salvia miltiorhiza Bunge.
abstract: The constituents of the MeOH extract of Salvia miltiorhiza BUNGE, which showed strong aldose reductase (AR) inhibitory activity, were examined, and two new abietane-type diterpenoids, danshenol A (1) and danshenol B (2), were isolated together with six known ones: dihydrotanshimme I (3), cryptotanshinone (4), tanshinone I (5), tanshinone IIA (6), (-)-danshexinkun A (7), and sugiol (8). Among them, 4, 5, and 8 were weak AR inhibitors with IC50 from 4.80 to > 10.0 microM, while 1, 2, 3, 6, and 7 were strong inhibitors (IC50 from 0.10 to 1.75 microM). Danshenol A (1), the strongest inhibitor, had IC50 of 0.10 microM which is comparable to that of epalrestat in clinical use. Moreover, from a consideration of IC50, and yield of each compound, it was concluded that tanshinone IIA (6) is the major active constituent of the MeOH extract and danshenol A (I) and (-)danshexinkun A(7) are the minor ones.
authors.affiliation: Research Institute for Wakan-Yaku (Traditional Sino-Japanese Medicines), Toyama Medical and Pharmaceutical University, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Tezuka
authors.forename: R
authors.initials: R
authors.lastname: Kasimu
authors.forename: P
authors.initials: P
authors.lastname: Basnet
authors.forename: T
authors.initials: T
authors.lastname: Namba
authors.forename: S
authors.initials: S
authors.lastname: Kadota
mesh_terms: D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D000818:Animals; D004224:Diterpenes / Q000302:isolation & purification* / Q000494:pharmacology; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D018517:Plant Roots / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar
chemical_list: D004224:Diterpenes; D004365:Drugs, Chinese Herbal; D004791:Enzyme Inhibitors; C108596:danshenol A; C108597:danshenol B; D000449:Aldehyde Reductase