Insulinotropic and antidiabetic effects of 17β-estradiol and the GPR30 agonist G-1 on human pancreatic islets

Endocrinology

Volumn 152, Issue 7, 2011, Pages 2568-2579

  Kumar, Rajesh ^a   Balhuizen, Alexander ^a   Amisten, Stefan ^a   Lundquist, Ingmar ^a,b   Salehi, Albert ^a  

^a LUND UNIVERSITY   (Sweden)

^b LUND UNIVERSITY   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIESTROGEN; APOPTOSIS INHIBITOR; CASPASE 3; CYCLIC AMP; ESTRADIOL; ESTROGEN RECEPTOR; G PROTEIN COUPLED RECEPTOR 30; GLUCAGON; INSULIN; LIPOCORTIN 5; PANCREAS HORMONE; PHOSPHATIDYLINOSITOL; SOMATOSTATIN;

APOPTOSIS; ARTICLE; CELL SURVIVAL; CONFOCAL MICROSCOPY; CONTROLLED STUDY; FEMALE; HORMONE RELEASE; HUMAN; INSULIN LIKE ACTIVITY; INSULIN RELEASE; LIPID HYDROLYSIS; MALE; NON INSULIN DEPENDENT DIABETES MELLITUS; PANCREAS ISLET; PANCREAS ISLET BETA CELL; POLYMERASE CHAIN REACTION; PRIORITY JOURNAL; PROTEIN EXPRESSION; SEX DIFFERENCE; WESTERN BLOTTING;

APOPTOSIS; CELL SURVIVAL; CYCLOPENTANES; DIABETES MELLITUS, TYPE 2; ESTRADIOL; ESTROGEN ANTAGONISTS; FEMALE; GENE EXPRESSION REGULATION; HUMANS; HYPERGLYCEMIA; HYPOGLYCEMIC AGENTS; INSULIN; ISLETS OF LANGERHANS; MALE; MOLECULAR TARGETED THERAPY; OLIGONUCLEOTIDE ARRAY SEQUENCE ANALYSIS; ORGAN CULTURE TECHNIQUES; QUINOLINES; RECEPTORS, ESTROGEN; RECEPTORS, G-PROTEIN-COUPLED; RNA, MESSENGER; SECOND MESSENGER SYSTEMS; SEX CHARACTERISTICS;

EID: 79959457594     PISSN: 00137227     EISSN: 00137227     Source Type: Journal    
DOI: 10.1210/en.2010-1361     Document Type: Article

References (39)

1. Mathis D, Vence L, Benoist C 2001 β-Cell death during progression to diabetes. Nature 414:792-798
2. Robertson RP, Harmon J, Tran PO, Tanaka Y, Takahashi H 2003 Glucose toxicity in β-cells: type 2 diabetes, good radicals gone bad, and the glutathione connection. Diabetes 52:581-587
3. Hess RA 2003 Estrogen in the adult male reproductive tract: a review. Reprod Biol Endocrinol 1:52
4. Wild S, Roglic G, Green A, Sicree R, King H 2004 Global prevalence of diabetes. Diabetes Care 27:1047-1053
5. Louet JF, LeMay C, Mauvais-Jarvis F 2004 Antidiabetic actions of estrogen: insight from human and genetic mouse models. Curr Atheroscler Rep 6:180-185 (Pubitemid 38898916)
6. Fissore F, Fortunati N, Comba A, Fazzari A, Gaidano G, Berta L, Frairia R 1994 The receptor-mediated action of sex steroid binding protein (SBP, SHBG): accumulation of cAMP in MCF-7 cells under SBP and estradiol treatment. Steroids 59:661-667 (Pubitemid 24359341)
7. Filardo EJ, Quinn JA, Frackelton Jr AR, Bland KI 2002 Estrogen action via the G protein-coupled receptor, GPR30: stimulation of adenylyl cyclase and cAMP-mediated attenuation of the epidermal growth factor receptor-to-MAPK signaling axis. Mol Endocrinol 16:70-84
8. Mårtensson UE, Salehi SA, Windahl S, Gomez MF, Swärd K, Daszkiewicz- Nilsson J, Wendt A, Andersson N, Hellstrand P, Grände PO, Owman C, Rosen CJ, Adamo ML, Lundquist I, Rorsman P, Nilsson BO, Ohlsson C, Olde B, Leeb-Lundberg LM 2009 Deletion of the G protein-coupled receptor 30 impairs glucose tolerance, reduces bone growth, increases blood pressure, and eliminates estradiol- stimulated insulin release in female mice. Endocrinology 150: 687-698
9. 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
10. Bologa CG, Revankar CM, Young SM, Edwards BS, Arterburn JB, Kiselyov AS, Parker MA, Tkachenko SE, Savchuck NP, Sklar LA, Oprea TI, Prossnitz ER 2006 Virtual and biomolecular screening converge on a selective agonist for GPR30. Nat Chem Biol 2:207-212
11. Wade GN, Blaustein JD, Gray JM, Meredith JM 1993 ICI 182,780: a pure antiestrogen that affects behaviors and energy balance in rats without acting in the brain. Am J Physiol Regul Integr Comp Physiol 265:R1392-R1398
12. Tremblay A, Tremblay GB, Labrie C, Labrie F, Giguère V 1998 EM-800, a novel antiestrogen, acts as a pure antagonist of the transcriptional functions of estrogen receptors α and β. Endocrinology 139:111-118
13. Heding L 1966 A simplified insulin radioimmunoassay method. In: Donato L, Milhaud G, Sirchis J eds. Labelled proteins in tracer studies. Brussels: Euratom; 345-350
14. Ahrén B, Lundquist, I 1982 Glucagon immunoreactivity in plasma from normal and dystrophic mice. Diabetologia 4:258-263
15. Panagiotidis G, Salehi AA, Westermark P, Lundquist I 1992 Homologous islet amyloid polypeptide: effects on plasma levels of glucagon, insulin and glucose in the mouse. Diabetes Res Clin Pract 18:167-171 (Pubitemid 23032607)
16. Amisten S, Braun OO, Bengtsson A, Erlinge D 2008 Gene expression profiling for the identification of G-protein coupled receptors in human platelets. Thromb Res 122:47-57 (Pubitemid 351601841)
17. Pfaffl MW 2001 A new mathematical model for relative quantification in real-time RT-PCR. Nucleic Acids Res 29:e45
18. Ramakers C, Ruijter JM, Deprez RH, Moorman AF 2003 Assumption- free analysis of quantitative real-time polymerase chain reaction (PCR) data. Neurosci Lett 339:62-66 (Pubitemid 36263221)
19. Jonsson A, Isomaa B, Tuomi T, Taneera J, Salehi A, Nilsson P, Groop L, Lyssenko V 2009 A variant in the KCNQ1 gene predicts future type 2 diabetes and mediates impaired insulin secretion. Diabetes 58:2409-2413
20. Bradford MM 1976 A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 72:248-254
21. Meidute Abaraviciene S, Lundquist I, Galvanovskis J, Flodgren E, Olde B, Salehi A 2008 Palmitate-induced β-cell dysfunction is associated with excessive NO production and is reversed by thiazolidinedione- mediated inhibition of GPR40 transduction mechanisms. PLoS ONE 3:e2182
22. Filardo E, Quinn J, Pang Y, Graeber C, Shaw S, Dong J, Thomas P 2007 Activation of the novel estrogen receptor G protein-coupled receptor 30 (GPR30) at the plasma membrane. Endocrinology 148: 3236-3245 (Pubitemid 46997004)
23. Kanda N, Watanabe S 2003 17β-Estradiol inhibits oxidative stressinduced apoptosis in keratinocytes by promoting Bcl-2 expression. J Invest Dermatol 121:1500-1509 (Pubitemid 38005505)
24. Kang L, Zhang X, Xie Y, Tu Y, Wang D, Liu Z, Wang ZY 2010 Involvement of estrogen receptor variant ER-α36, not GPR30, in nongenomic estrogen signaling. Mol Endocrinol 24:709-721
25. Wang Z, Zhang X, Shen P, Loggie BW, Chang Y, Deuel TF 2006 A variant of estrogen receptor-α, hER-α36: Transduction of estrogenand antiestrogen-dependent membrane-initiated mitogenic signaling. Proc Natl Acad Sci USA 103:9063-9068 (Pubitemid 43902533)
26. Yamazaki S, Katada T, Ui M 1982 α2-Adrenergic inhibition of insulin secretion via interference with cyclic AMP generation in rat pancreatic islets. Mol Pharmacol 21:648-653 (Pubitemid 12128279)
27. Leclercq-Meyer V, Herchuelz A, Valverde I, Couturier E, Marchand J, Malaisse WJ 1980 Modeof action of clonidine upon islet function: dissociated effects upon the time course and magnitude of insulin release. Diabetes 29:193-200 (Pubitemid 10129113)
28. Mandrup-Poulsen T 2001 β-Cell apoptosis: stimuli and signaling. Diabetes 50(Suppl 1):S58-S63
29. Boutros T, Chevet E, Metrakos P 2008 Mitogen-activated protein (MAP) kinase/MAP kinase phosphatase regulation: roles in cell growth, death, and cancer. Pharmacol Rev 60:261-310
30. Khoo S, Gibson TB, Arnette D, Lawrence M, January B, McGlynn K, Vanderbilt CA, Griffen SC, German MS, Cobb MH 2004 MAP kinases and their roles in pancreatic β-cells. Cell Biochemistry and Biophysics 40:191-200
31. Abaraviciene SM, Lundquist I, Salehi A 2008 Rosiglitazone counteracts palmitate-induced β-cell dysfunction by suppression of MAP kinase, inducible nitric oxide synthase and caspase 3 activities. Cell Mol Life Sci 65:2256-2265
32. Kim SJ, Nian C, Widenmaier S, McIntosh CH 2008 Glucose-dependent insulinotropic polypeptide-mediated up-regulation of β-cell antiapoptotic Bcl-2 gene expression is coordinated by cyclic AMP (cAMP) response element binding protein (CREB) and cAMP-responsive CREB coactivator 2. Mol Cell Biol 28:1644-1656
33. Szego EM, Barabás K, Balog J, Szilágyi N, Korach KS, Juhász G, Abrahám IM2006 Estrogen induces estrogen receptor α-dependent cAMP response element-binding protein phosphorylation via mitogen activated protein kinase pathway in basal forebrain cholinergic neurons in vivo. J Neurosci 26:4104-4110
34. Lenzen S, Bailey CJ 1984 Thyroid hormones, gonadal and adrenocortical steroids and the function of the islets of Langerhans. Endocr Rev 5:411-434
35. Rossini AA, Williams RM, Appel MC, Like AA 1978 Sex differences in the multiple-dose streptozotocin model of diabetes. Endocrinology 103:1518-1520 (Pubitemid 9075641)
36. Levin ER 2009 G protein-coupled receptor 30: estrogen receptor or collaborator? Endocrinology 150:1563-1565
37. Langer G, Bader B, Meoli L, Isensee J, Delbeck M, Noppinger PR, Otto C 2010 A critical review of fundamental controversies in the field of GPR30 research. Steroids 75:603-610
38. Soriano S, Ropero AB, Alonso-Magdalena P, Ripoll C, Quesada I, Gassner B, Kuhn M, Gustafsson JA, Nadal A 2009 Rapid regulation of K(ATP) channel activity by 17β-estradiol in pancreatic β-cells involves the estrogen receptor β and the atrial natriuretic peptide receptor. Mol Endocrinol 23:1973-1982
39. Nadal A, Alonso-Magdalena P, Soriano S, Ripoll C, Fuentes E, Quesada I, Ropero AB 2011 Role of estrogen receptors α, β and GPER1/ GPR30 in pancreatic β-cells. Front Biosci 16:251-260