In vitro aldose reductase inhibitory activity of some flavonyl-2,4-thiazolidinediones

Das-Evcimen N., Bozdag-Dundar O., Sarika M., Ertan R.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.23, sa.3, ss.297-301, 2008 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 23 Sayı: 3
  • Basım Tarihi: 2008
  • Doi Numarası: 10.1080/14756360701475282
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.297-301
  • Anahtar Kelimeler: 2,4-thiazolidinediones, flavone derivatives, antidiabetic, aldose reductase, inhibition, DIABETIC COMPLICATIONS, HYPOGLYCEMIC ACTIVITY, FLAVONE DERIVATIVES, POLYOL PATHWAY, AGENT CS-045, COMMUNICATION, PREVENTION, POTENT, CT-112, NIDDM
  • Ankara Üniversitesi Adresli: Evet

Özet

Aldose reductase (AR) is implicated to play a critical role in diabetes and cardiovascular complications because of the reaction it catalyzes. AR enzyme appears to be the key factor in the reduction of glucose to sorbitol. Synthesis and accumulation of sorbitol in cells due to AR activity is the main cause of diabetic complications, such as diabetic cataract, retinopathy, neuropathy and nephropathy. Aldose reductase inhibitors have been found to prevent sorbitol accumulation in tissues. Numerous compounds have been prepared in order to improve the pharmacological prophile of inhibition of aldose reductase enzyme. In this study, seventeen flavonyl-2,4-thiazolidinediones (flavonyl-2,4-TZD) (Ia-e, IIa-e and IIIa-g) were tested for their ability to inhibit rat kidney AR. Compound Ib showed the highest inhibitory activity (88.69 +/- 1.46%) whereas Ia, IIa, IIIa, IIIb also showed significant inhibitory activity (49.26 +/- 2.85, 67.29 +/- 1.09, 71.11 +/- 1.95, 64.86 +/- 1.21%, respectively).