Improvement of vascular function by acute and chronic treatment with the GPR30 agonist G1 in experimental diabetes mellitus

PLoS ONE

Volumn 7, Issue 6, 2012, Pages

  Li, Zi lin ^a,c   Liu, Jin cheng ^a   Liu, Shui bing ^b   Li, Xiao qiang ^b   Yi, Ding hua ^a   Zhao, Ming gao ^b  

^a FOURTH MILITARY MEDICAL UNIVERSITY   (China)

^b FOURTH MILITARY MEDICAL UNIVERSITY   (China)

^c PLA 452 Hospital   (China)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLCHOLINE; CHEMOKINE RECEPTOR AGONIST; ENDOTHELIAL NITRIC OXIDE SYNTHASE; G PROTEIN COUPLED RECEPTOR 30; G1 (DRUG); GLUCOSE; N(G) NITROARGININE METHYL ESTER; NITRIC OXIDE; PHENYLEPHRINE; UNCLASSIFIED DRUG; ANTIDIABETIC AGENT; G PROTEIN COUPLED RECEPTOR; GPR30 PROTEIN, RAT; INSULIN;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BLOOD VESSEL FUNCTION; CONTROLLED STUDY; DIABETES MELLITUS; DOSE RESPONSE; DRUG MECHANISM; ENDOTHELIUM; ENDOTHELIUM CELL; ENZYME ACTIVITY; ENZYME PHOSPHORYLATION; FEMALE; NONHUMAN; OVARIECTOMY; RAT; THORACIC AORTA; VASOCONSTRICTION; VASODILATATION; ANIMAL; BLOOD; BODY WEIGHT; DRUG EFFECT; DRUG POTENTIATION; EXPERIMENTAL DIABETES MELLITUS; GLUCOSE BLOOD LEVEL;

RATTUS;

ANIMALS; BLOOD GLUCOSE; BODY WEIGHT; DIABETES MELLITUS, EXPERIMENTAL; FEMALE; HYPOGLYCEMIC AGENTS; INSULIN; NITRIC OXIDE; OVARIECTOMY; RATS; RECEPTORS, G-PROTEIN-COUPLED;

EID: 84861865685     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0038787     Document Type: Article

References (36)

1. Prossnitz ER, Sklar LA, Oprea TI, Arterburn JB, (2008) GPR30: a novel therapeutic target in estrogen-related disease. Trends Pharmacol Sci 29: 116 123.
2. Meyer MR, Prossnitz ER, Barton M, (2011) The G protein-coupled estrogen receptor GPER/GPR30 as a regulator of cardiovascular function. Vascul Pharmacol 55: 17 25.
3. Broughton BR, Miller AA, Sobey CG, (2010) Endothelium-dependent relaxation by G protein-coupled receptor 30 agonists in rat carotid arteries. Am J Physiol Heart Circ Physiol 298: H1055 1061.
4. Bologa CG, Revankar CM, Young SM, Edwards BS, Arterburn JB, (2006) Virtual and biomolecular screening converge on a selective agonist for GPR30. Nat Chem Biol 2: 207 212.
5. Dennis MK, Burai R, Ramesh C, Petrie WK, Alcon SN, (2009) In vivo effects of a GPR30 antagonist. Nat Chem Biol 5: 421 427.
6. Haas E, Bhattacharya I, Brailoiu E, Damjanovic M, Brailoiu GC, (2009) Regulatory role of G protein-coupled estrogen receptor for vascular function and obesity. Circ Res 104: 288 291.
7. Lindsey SH, Carver KA, Prossnitz ER, Chappell MC, (2011) Vasodilation in response to the GPR30 agonist G-1 is not different from estradiol in the mRen2.Lewis female rat. J Cardiovasc Pharmacol 57: 598 603.
8. Sharma G, Prossnitz ER, (2011) Mechanisms of estradiol-induced insulin secretion by the G protein-coupled estrogen receptor GPR30/GPER in pancreatic beta-cells. Endocrinology 152: 3030 3039.
9. Kumar R, Balhuizen A, Amisten S, Lundquist I, Salehi A, (2011) Insulinotropic and antidiabetic effects of 17beta-estradiol and the GPR30 agonist G-1 on human pancreatic islets. Endocrinology 152: 2568 2579.
10. Schalkwijk CG, Stehouwer CD, (2005) Vascular complications in diabetes mellitus: the role of endothelial dysfunction. Clin Sci (Lond) 109: 143 159.
11. Bucala R, Tracey KJ, Cerami A, (1991) Advanced glycosylation products quench nitric oxide and mediate defective endothelium-dependent vasodilatation in experimental diabetes. J Clin Invest 87: 432 438.
12. Atochin DN, Huang PL, (2010) Endothelial nitric oxide synthase transgenic models of endothelial dysfunction. 965-974 p.
13. Huang PL, Huang Z, Mashimo H, Bloch KD, Moskowitz MA, (1995) Hypertension in mice lacking the gene for endothelial nitric oxide synthase. Nature 377: 239 242.
14. Freedman JE, Sauter R, Battinelli EM, Ault K, Knowles C, (1999) Deficient platelet-derived nitric oxide and enhanced hemostasis in mice lacking the NOSIII gene. Circ Res 84: 1416 1421.
15. Huang PL, (2000) Lessons learned from nitric oxide synthase knockout animals. Semin Perinatol 24: 87 90.
16. Kuhlencordt PJ, Rosel E, Gerszten RE, Morales-Ruiz M, Dombkowski D, (2004) Role of endothelial nitric oxide synthase in endothelial activation: insights from eNOS knockout endothelial cells. Am J Physiol Cell Physiol 286: C1195 1202.
17. Lefer DJ, Jones SP, Girod WG, Baines A, Grisham MB, (1999) Leukocyte-endothelial cell interactions in nitric oxide synthase-deficient mice. Am J Physiol 276: H1943 1950.
18. Dennis MK, Field AS, Burai R, Ramesh C, Petrie WK, (2011) Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. J Steroid Biochem Mol Biol 127: 358 366.
19. Balhuizen A, Kumar R, Amisten S, Lundquist I, Salehi A, (2010) Activation of G protein-coupled receptor 30 modulates hormone secretion and counteracts cytokine-induced apoptosis in pancreatic islets of female mice. Mol Cell Endocrinol 320: 16 24.
20. Mount PF, Kemp BE, Power DA, (2007) Regulation of endothelial and myocardial NO synthesis by multi-site eNOS phosphorylation. J Mol Cell Cardiol 42: 271 279.
21. Bauer PM, Fulton D, Boo YC, Sorescu GP, Kemp BE, (2003) Compensatory phosphorylation and protein-protein interactions revealed by loss of function and gain of function mutants of multiple serine phosphorylation sites in endothelial nitric-oxide synthase. J Biol Chem 278: 14841 14849.
22. Fleming I, Busse R, (1999) Signal transduction of eNOS activation. Cardiovasc Res 43: 532 541.
23. Meyer MR, Amann K, Field AS, Hu C, Hathaway HJ, (2012) Deletion of g protein-coupled estrogen receptor increases endothelial vasoconstriction. Hypertension 59: 507 512.
24. Meyer MR, Baretella O, Prossnitz ER, Barton M, (2010) Dilation of epicardial coronary arteries by the G protein-coupled estrogen receptor agonists G-1 and ICI 182,780. Pharmacology 86: 58 64.
25. Prossnitz ER, Barton M, (2011) The G-protein-coupled estrogen receptor GPER in health and disease. Nat Rev Endocrinol.
26. Huang PL, (2009) eNOS, metabolic syndrome and cardiovascular disease. Trends Endocrinol Metab 20: 295 302.
27. Takenouchi Y, Kobayashi T, Taguchi K, Matsumoto T, Kamata K, (2009) Gender differences in endothelial function in aortas from type 2 diabetic model mice. J Pharmacol Sci 111: 91 99.
28. Skyrme-Jones RA, O'Brien RC, Luo M, Meredith IT, (2000) Endothelial vasodilator function is related to low-density lipoprotein particle size and low-density lipoprotein vitamin E content in type 1 diabetes. J Am Coll Cardiol 35: 292 299.
29. Natali A, Toschi E, Baldeweg S, Casolaro A, Baldi S, (2005) Haematocrit, type 2 diabetes, and endothelium-dependent vasodilatation of resistance vessels. Eur Heart J 26: 464 471.
30. Huang PL, (2005) Unraveling the links between diabetes, obesity, and cardiovascular disease. Circ Res 96: 1129 1131.
31. Dimmeler S, Fleming I, Fisslthaler B, Hermann C, Busse R, (1999) Activation of nitric oxide synthase in endothelial cells by Akt-dependent phosphorylation. Nature 399: 601 605.
32. Fulton D, Gratton JP, McCabe TJ, Fontana J, Fujio Y, (1999) Regulation of endothelium-derived nitric oxide production by the protein kinase Akt. Nature 399: 597 601.
33. Liu SB, Han J, Zhang N, Tian Z, Li XB, (2011) Neuroprotective effects of oestrogen against oxidative toxicity through activation of G-protein-coupled receptor 30 receptor. Clin Exp Pharmacol Physiol 38: 577 585.
34. Zhong W, Zou G, Gu J, Zhang J, (2010) L-arginine attenuates high glucose-accelerated senescence in human umbilical vein endothelial cells. Diabetes Res Clin Pract 89: 38 45.
35. Gingerich S, Kim GL, Chalmers JA, Koletar MM, Wang X, (2010) Estrogen receptor alpha and G-protein coupled receptor 30 mediate the neuroprotective effects of 17beta-estradiol in novel murine hippocampal cell models. Neuroscience 170: 54 66.
36. Chen L, Liu JC, Zhang XN, Guo YY, Xu ZH, (2008) Down-regulation of NR2B receptors partially contributes to analgesic effects of Gentiopicroside in persistent inflammatory pain. Neuropharmacology 54: 1175 1181.