YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
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Improvement of Cardiovascular Dysfunction in Diabetic Rat by KST221085

당뇨병성 심혈관합병증에 대한 KST221085의 개선효과

  • 정이숙 (아주대학교 의과대학 생리학교실) ;
  • 한호규 (한국과학기술연구원) ;
  • 이수환 (아주대학교 의과대학 생리학교실) ;
  • 백은주 (아주대학교 의과대학 생리학교실) ;
  • 문창현 (아주대학교 의과대학 생리학교실)
  • Published : 2001.06.01
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Abstract

The present study was conducted to evaluate the effect of KST221085, a newly synthesized antidiabetic agent, on the hearts from streptozotocin (STZ)-induced diabetic rats. In isolated diabetic hearts, left ventricular developed pressure (LVDP), heart rate (HR) and coronary flow rate (CFR) were decreased compared to normal control, indicating cardiovascular dysfunction in diabetic heart. The treatment with 10 $\mu$M KST221085 remarkably improved the diabetes-induced contractile impairment, without any influence on HR. Reduced coronary flow in diabetic heart was also significantly increased by treatment with 10 $\mu$M KST221085. In isolated aorta from diabetic rat, treatment with 10 $\mu$M KST221085 increased endothelium-dependent relaxation, suggesting that KST221085 can improve the impaired endothelial function in diabetic aorta. Our results suggest that KST221085 treatment can improve the cardiovascular dysfunction in STZ-induced diabetic rats.

Keywords

References

  1. Joslin's Diabetes Mellitus Diabetes mortality from vital statistics Entmacher, P. S.;Marble, A.(ed.)
  2. Diabetes Metab. Rev. v.37 Cardiovascular disease and hypertension in diabetes mellitus Jarrett, R. J.
  3. Diabetologia v.34 Incidence of macrovascular disease in diabetes mellitus. The London cohort of the WHO, multinational study of vascular disease in diagetics Morrish, N. J.;Stevens, L. K.;Fuller, J. H.;Keen, H.;Jarrett, R. J.
  4. Biochem. Biophys. Res. commun v.258 Thiazolidinediones down-regulate plasminogen activator inhibitor type 1 expression in human vascular endothelial cells;A possible role for PPARgamma in endothelial function Kato K.;Satoh H.;Endo Y.;Yamada D.;Midorikawa S.;Sato W.;Mizuno K.;Fujita T.;Tsukamoto K.;Watanabe T.
  5. Nippon Rinsho v.58 Cardiovascular effects of the thiazolidinedione troglitazone Yamada K.;Kuzuya H.;Nakano T.
  6. J. Med. Chem. v.41 Substituted tetrahydropyrrolo[2,1-b] oxazol-5(6H)-ones and Tetra-hydropyrrolo[2,1-b]thiazol-5-(6H)-ones as Hypoglycemic Agents Aicher T.D.;Balkan B.;Bell P.A.;Brand L. J.;Cheon S. H.;Deems R. O. Fell J. B.;Fillers W. S.;Fraser T. D.;Gao J.;Knorr D. D.;Kahle G. G.;Leone C. L.; Nadelson J.;Simpson R.;Smith H. C.
  7. J. Cardiovasc. Pharmacol. v.16 Profile of cromakalim in the treatment of myocardial ischemia in isolated rat hearts and anesthetized dogs Grover, G. J.;Dzwonczy, S.;Parham, C. S.
  8. Eur. J. Pharmacol. v.191 Reduction of ischemic damage in isolated rat hearts by the potassium channel opener RP 53891 Grover, G. J.;Dzwonczy, S.;Sleph, P. G.
  9. Am. J. Physiol. v.267 Insulin's effect on protein kinase C and diacylglycerol induced by diabetes and glucose in vascular tissues Inoguchi T.;Xia P.;Kunisaki M.;Higashi S.;Feener E. P.;King G. L.
  10. J. Clin. Invest. v.83 Differential regulation of protein kinase C and (Na, K)-adenosine triphosphate activities by elevated glucose levels in retinal capillary endothelial cells Lee, T. S.;MacGregor, L. C.;Fluharty, S. J.;king, G. L.
  11. Trends Cardiovase. Med. v.5 Diversity of the protein kinase C gene family implications for cardiovascular disease Harrington, E. O.;Ware, J. A.
  12. Jpn. J. Pharmacol. v.33 Effect of gliclazide on prostaglandin I2 formation in normal and streptozotocin-induced diabetic animals Fujitani, B.;Maeda, J.;Tsuboi, T.;Kadokawa, T.;Shimizu, M.
  13. J. Clin. Invest. v.85 Elevated glucose promotes generation of endothelium-derived vasoconstrictor prostanoids in rabbit aorta Tesfamariam, B.;Brown, M. L.;Deykin, D.;Cohen, R. A.
  14. 보건복지부 보고서 (HMP-98-D-4-0042) Thiaxolidinedione 및 oxaxolidine 유도체의 합성 및 항당뇨병성 활성에 관한 연구 천승훈
  15. Jpn. J. Physiol. v.49 Protein kinase C inhibitors abolish the increased resistance of diabetic rat heart to ischemia-reperfusion injury Moon C. H.;Jung Y. S.;Lee S. H.;Baik E. J.