Inhibitory effect of rhetsinine isolated from Evodia rutaecarpa on aldose reductase activity.
Aldose reductase inhibitors have considerable potential for the treatment of diabetic complications, without increased risk of hypoglycemia. Search for components inhibiting aldose reductase led to the discovery of active compounds contained in Evodia rutaecarpa Bentham (Rutaceae), which is the one of the component of Kampo-herbal medicine. The hot water extract from the E. rutaecarpa was subjected to distribution or gel filtration chromatography to give an active compound, N2-(2-methylaminobenzoyl)tetrahydro-1H-pyrido[3,4-b]indol-1-one (rhetsinine). It inhibited aldose reductase with IC(50) values of 24.1 microM. Furthermore, rhetsinine inhibited sorbitol accumulation by 79.3% at 100 microM. These results suggested that the E. rutaecarpa derived component, rhetsinine, would be potentially useful in the treatment of diabetic complications.
Kato
A
A
Department of Hospital Pharmacy, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan. kato@med.u-toyama.ac.jp
Yasuko
H
H
Goto
H
H
Hollinshead
J
J
Nash
R J
RJ
Adachi
I
I
D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D002243:Carbolines / Q000302:isolation & purification / Q000494:pharmacology*; D048909:Diabetes Complications / Q000188:drug therapy; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D004912:Erythrocytes / Q000187:drug effects*; D032086:Evodia / Q000737:chemistry*; D005260:Female; D005638:Fruit; D006801:Humans; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology*; D013012:Sorbitol / Q000378:metabolism*
D002243:Carbolines; D004791:Enzyme Inhibitors; C539930:N2-(2-methylaminobenzoyl)tetrahydro-1H-pyrido(3,4-b)indol-1-one; D010936:Plant Extracts; D013012:Sorbitol; D000449:Aldehyde Reductase