Efficacy of the dipeptidyl peptidase IV inhibitor isoleucine thiazolidide (P32/98) in fatty Zucker rats with incipient and manifest impaired glucose tolerance

Diabetes, Obesity and Metabolism

Volumn 10, Issue 10, 2008, Pages 850-861

  Augstein, Petra ^a   Berg, S ^a   Heinke, P ^a   Altmann, S ^a   Salzsieder, E ^a   Demuth, H U ^b   Freyse, E J ^a  

^a Institut fur Diabetes 'Gerhardt Katsch'   (Germany)

^b PROBIODRUG AG   (Germany)

Author keywords

Dipeptidyl peptidase IV; Fatty Zucker rats; Glucagon like peptide 1; Ile thiazolidide; Impaired glucose tolerance; Pancreatic islets; Prediabetes; Type 2 diabetes

Indexed keywords

DIPEPTIDYL PEPTIDASE IV INHIBITOR; FATTY ACID; GLUCOSE; INCRETIN; INSULIN; ISOLEUCINE THIAZOLIDIDE; PLACEBO; TRIACYLGLYCEROL;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BODY WEIGHT; CELL VOLUME; CONTROLLED STUDY; DRUG EFFICACY; DRUG MECHANISM; DYSLIPIDEMIA; GLUCOSE BLOOD LEVEL; GLUCOSE INTOLERANCE; HYPERGLYCEMIA; HYPERINSULINEMIA; LONG TERM CARE; MALE; NONHUMAN; ORAL GLUCOSE TOLERANCE TEST; PANCREAS ISLET CELL; RAT; WEIGHT GAIN; ZUCKER DIABETIC FATTY RAT;

EID: 52249085217     PISSN: 14628902     EISSN: 14631326     Source Type: Journal    
DOI: 10.1111/j.1463-1326.2007.00813.x     Document Type: Article

References (43)

1. American Diabetes Association. Diagnosis and classification of diabetes mellitus. Diabetes Care 2006; 29 (Suppl. 1): S43-S48.
2. CDC Diabetes Program: NaNional diabetes fact sheet: national estimates on diabetes [article online], 2003. Available from URL: www.cdc.gov/ diabetes/pubs/factsheet.htm. 2003.
3. Haffner SM, Agostino RD Jr, Saad MF et al. Carotid artery atherosclerosis in type-2 diabetic and nondiabetic subjects with and without symptomatic coronary artery disease (The Insulin Resistance Atherosclerosis Study). Am J Cardiol 2000; 85: 1395-1400.
4. Caballero AE. Endothelial dysfunction, inflammation, and insulin resistance: A focus on subjects at risk for type 2 diabetes. Curr Diab Rep 2004; 4: 237-246.
5. Tuomilehto J. Counterpoint: Evidence-based prevention of type 2 diabetes: The power of lifestyle management. Diabetes Care 2007; 30: 435-438.
6. Inzucchi SE, Sherwin RS. The prevention of type 2 diabetes mellitus. Endocrinol Metab Clin North Am 2005; 34: 199-219, viii.
7. Younis N, Soran H, Farook S. The prevention of type 2 diabetes mellitus: recent advances. QJM 2004; 97: 451-455.
8. Wajchenberg BL. β-cell failure in diabetes and preservation by clinical treatment. Endocr Rev 2007; 28: 187-218.
9. Drucker DJ, Nauck MA. The incretin system: Glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 2006; 368: 1696-1705.
10. Holst JJ. Glucagon-like peptide-1: From extract to agent. The Claude Bernard Lecture, 2005. Diabetologia 2006; 49: 253-260.
11. Demuth HU, McIntosh CH, Pederson RA. Type 2 diabetes - therapy with dipeptidyl peptidase IV inhibitors. Biochim Biophys Acta 2005; 1751: 33-44.
12. Ahren B. Vildagliptin: An inhibitor of dipeptidyl peptidase-4 with antidiabetic properties. Expert Opin Investig Drugs 2006; 15: 431-442.
13. Ahren B, Holst JJ, Martensson H, Balkan B. Improved glucose tolerance and insulin secretion by inhibition of dipeptidyl peptidase IV in mice. Eur J Pharmacol 2000; 404: 239-245.
14. McIntosh CH, Demuth HU, Kim SJ, Pospisilik JA, Pederson RA. Applications of dipeptidyl peptidase IV inhibitors in diabetes mellitus. Int J Biochem Cell Biol 2006; 38: 860-872.
15. Pospisilik JA, Ehses JA, Doty T, McIntosh CH, Demuth HU, Pederson RA. Dipeptidyl peptidase IV inhibition in animal models of diabetes. Adv Exp Med Biol 2003; 524: 281-291.
16. Li X, Zhang L, Meshinchi S et al. Islet microvasculature in islet hyperplasia and failure in a model of type 2 diabetes. Diabetes 2006; 55: 2965-2973.
17. Janssen SW, Hermus AR, Lange WP et al. Progressive histopathological changes in pancreatic islets of Zucker diabetic fatty rats. Exp Clin Endocrinol Diabetes 2001; 109: 273-282.
18. Berthiaume N, Mika AK, Zinker BA. Development of insulin resistance and endothelin-1 levels in the Zucker fatty rat. Metabolism 2003; 52: 845-849.
19. Apweiler R, Freud P. Development of glucose intolerance in obese (fa/fa) Zucker rats. Horm Metab Res 1993; 25: 521-524.
20. Ziegler B, Hahn HJ, Ziegler M. Insulin recovery in pancreas and host organs of islet grafts. Exp Clin Endocrinol 1985; 85: 53-60.
21. Weibel ER. Stereological principles for morphometry in electron microscopic cytology. Int Rev Cytol 1969; 26: 235-302.
22. Wargent E, Stocker C, Augstein P et al. Improvement of glucose tolerance in Zucker diabetic fatty rats by long-term treatment with the dipeptidyl peptidase inhibitor P32/98: Comparison with and combination with rosiglitazone. Diabetes Obes Metab 2005; 7: 170-181.
23. Dunger A, Lucke S, Besch W, Hahn HJ. The rat pancreatic B-cell during pregnancy and after delivery. Int J Feto-Maternal Med 1990; 2: 55-61.
24. Besch W, Woltanski KP, Keilacker H et al. Measurement of insulin in human sera using a new RIA kit. 1. Insulin determination in the absence of insulin antibodies - conventional assay and micro modification. Exp Clin Endocrinol 1987; 90: 264-270.
25. Ahren B, Pacini G, Foley JE, Schweizer A. Improved meal-related beta-cell function and insulin sensitivity by the dipeptidyl peptidase-IV inhibitor vildagliptin in metformin-treated patients with type 2 diabetes over 1 year. Diabetes Care 2005; 28: 1936-1940.
26. Pospisilik JA, Martin J, Doty T et al. Dipeptidyl peptidase IV inhibitor treatment stimulates beta-cell survival and islet neogenesis in streptozotocin-induced diabetic rats. Diabetes 2003; 52: 741-750.
27. Ahren B, Gomis R, Standl E, Mills D, Schweizer A. Twelve- and 52-week efficacy of the dipeptidyl peptidase IV inhibitor LAF237 in metformin-treated patients with type 2 diabetes. Diabetes Care 2004; 27: 2874-2880.
28. Nauck MA, Meininger G, Sheng D, Terranella L, Stein PP. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, compared with the sulfonylurea, glipizide, in patients with type 2 diabetes inadequately controlled on metformin alone: A randomized, double-blind, non-inferiority trial. Diabetes Obes Metab 2007; 9: 194-205.
29. Pospisilik JA, Stafford SG, Demuth HU et al. Long-term treatment with the dipeptidyl peptidase IV inhibitor P32/98 causes sustained improvements in glucose tolerance, insulin sensitivity, hyperinsulinemia, and beta-cell glucose responsiveness in VDF (fa/fa) Zucker rats. Diabetes 2002; 51: 943-950.
30. Sudre B, Broqua P, White RB et al. Chronic inhibition of circulating dipeptidyl peptidase IV by FE 999011 delays the occurrence of diabetes in male Zucker diabetic fatty rats. Diabetes 2002; 51: 1461-1469.
31. Raz I, Hanefeld M, Xu L, Caria C, Williams-Herman D, Khatami H. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus. Diabetologia 2006; 49: 2564-2571.
32. Ahren B, Landin-Olsson M, Jansson PA, Svensson M, Holmes D, Schweizer A. Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes. J Clin Endocrinol Metab 2004; 89: 2078-2084.
33. McIntosh CH, Demuth HU, Pospisilik JA, Pederson R. Dipeptidyl peptidase IV inhibitors: How do they work as new antidiabetic agents? Regul Pept 2005; 128: 159-165.
34. Pauly RP, Demuth HU, Rosche F et al. Improved glucose tolerance in rats treated with the dipeptidyl peptidase IV (CD26) inhibitor Ile-thiazolidide. Metabolism 1999; 48: 385-389.
35. Pederson RA, White HA, Schlenzig D, Pauly RP, McIntosh CH, Demuth HU. Improved glucose tolerance in Zucker fatty rats by oral administration of the dipeptidyl peptidase IV inhibitor isoleucine thiazolidide. Diabetes 1998; 47: 1253-1258.
36. Reimer MK, Holst JJ, Ahren B. Long-term inhibition of dipeptidyl peptidase IV improves glucose tolerance and preserves islet function in mice. Eur J Endocrinol 2002; 146: 717-727.
37. Pospisilik JA, Stafford SG, Demuth HU, McIntosh CH, Pederson RA. Long-term treatment with dipeptidyl peptidase IV inhibitor improves hepatic and peripheral insulin sensitivity in the VDF Zucker rat: A euglycemic-hyperinsulinemic clamp study. Diabetes 2002; 51: 2677-2683.
38. Meier JJ, Gethmann A, Gotze O et al. Glucagon-like peptide 1 abolishes the postprandial rise in triglyceride concentrations and lowers levels of non-esterified fatty acids in humans. Diabetologia 2006; 49: 452-458.
39. Taskinen MR. Diabetic dyslipidaemia: From basic research to clinical practice. Diabetologia 2003; 46: 733-749.
40. Monnier L, Lapinski H, Colette C. Contributions of fasting and postprandial plasma glucose increments to the overall diurnal hyperglycemia of type 2 diabetic patients: Variations with increasing levels of HbA(1c). Diabetes Care 2003; 26: 881-885.
41. Shiraiwa T, Kaneto H, Miyatsuka T et al. Postprandial hyperglycemia is a better predictor of the progression of diabetic retinopathy than HbA1c in Japanese type 2 diabetic patients. Diabetes Care 2005; 28: 2806-2807.
42. Service FJ, O'Brien PC. The relation of glycaemia to the risk of development and progression of retinopathy in the Diabetic Control and Complications Trial. Diabetologia 2001; 44: 1215-1220.
43. Home P. Contributions of basal and post-prandial hyperglycaemia to micro- and macrovascular complications in people with type 2 diabetes. Curr Med Res Opin 2005; 21: 989-998.