Inhibition of vertebrate squalene epoxidase by isoprenyl gallates and phenylalkyl gallates.
Galloy esters with 'substrate-like' isoprenoid or phenylalkyl side chains were newly synthesized and tested for the enzyme inhibition activities toward recombinant rat squalene epoxidase. Isoprenyl gallates (4-6) showed good inhibition (IC50 = 1.5 5.1 microM), as potent as previously reported substrate analogues, while phenylalkyl gallates (7-10) were moderate inhibitors of the enzyme (IC50 = 12-61 microM).
Abe
I
I
University of Shizuoka, School of Pharmaceutical Sciences, Yida, Japan. abei@ys7.u-shizuoka-ken.ac.jp
Kashiwagi
Y
Y
Noguchi
H
H
D000818:Animals; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D005707:Gallic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry / Q000379:methods; D010105:Oxygenases / Q000037:antagonists & inhibitors*; D051381:Rats; D050603:Squalene Monooxygenase
D004791:Enzyme Inhibitors; D005707:Gallic Acid; D010105:Oxygenases; D050603:Squalene Monooxygenase