Aldose reductase inhibitory constituents of the root of Salvia miltiorhiza Bunge.
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.
Tezuka
Y
Y
Research Institute for Wakan-Yaku (Traditional Sino-Japanese Medicines), Toyama Medical and Pharmaceutical University, Japan.
Kasimu
R
R
Basnet
P
P
Namba
T
T
Kadota
S
S
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
D004224:Diterpenes; D004365:Drugs, Chinese Herbal; D004791:Enzyme Inhibitors; C108596:danshenol A; C108597:danshenol B; D000449:Aldehyde Reductase