Inhibitors of aldose reductase and advanced glycation end-products formation from the leaves of Stelechocarpus cauliflorus R.E. Fr.
Two dihydroflavonol glycosides, engeletin and astilbin, were isolated from an EtOAc extract of the leaves of Stelechocarpus cauliflorus R.E. Fr. (Annonaceae). The inhibitory activity of engeletin against a recombinant human aldose reductase (IC50 value=1.16 microM) was twice that of quercetin as a positive control (2.48 microM), and 23 times greater than that of astilbin (26.7 microM). Engeletin inhibited the enzyme uncompetitively. Astilbin was about as potent as the positive control, quercetin, in its inhibition of advanced glycation end-products formation. These flavonoids displayed therapeutic potential in the prevention and treatment of diabetic complications.
Wirasathien
L
L
Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.
Pengsuparp
T
T
Suttisri
R
R
Ueda
H
H
Moriyasu
M
M
Kawanishi
K
K
D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D029061:Annonaceae / Q000737:chemistry*; D044948:Flavonols / Q000737:chemistry / Q000494:pharmacology; D017127:Glycation End Products, Advanced / Q000037:antagonists & inhibitors*; D006027:Glycosides / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018515:Plant Leaves / Q000737:chemistry*
D044948:Flavonols; D017127:Glycation End Products, Advanced; D006027:Glycosides; D010936:Plant Extracts; C522936:engeletin; C099069:astilbin; D000449:Aldehyde Reductase