[1]刘艳 田秀标 韩颖.GLP-1受体激动剂呈葡萄糖依赖性刺激胰岛β细胞胰岛素分泌的机制[J].国际内分泌代谢杂志,2015,(01):66-69.[doi:10.3760/cma.j.issn.1673-4157.2015.01.017]
　Liu Yan*,Tian Xiubiao,Han Ying..Mechanism of GLP-1 receptor agonists in the stimulation of insulin secretion of islet β cell in a glucose-dependent manner[J].International Journal of Endocrinology and Metabolism,2015,(01):66-69.[doi:10.3760/cma.j.issn.1673-4157.2015.01.017]
点击复制

GLP-1受体激动剂呈葡萄糖依赖性刺激胰岛β细胞胰岛素分泌的机制()
分享到：

《国际内分泌代谢杂志》[ISSN:1673-4157/CN:12-1383/R]

卷:
期数:
2015年01
页码:
66-69
栏目:
小论坛
出版日期:
2015-01-20

文章信息/Info

Title:
Mechanism of GLP-1 receptor agonists in the stimulation of insulin secretion of islet β cell in a glucose-dependent manner
作者:
刘艳 田秀标 韩颖
300070 天津医科大学研究生院(刘艳); 300280 天津海滨人民医院内分泌科(刘艳,田秀标, 韩颖)
Author(s):
Liu Yan*; Tian Xiubiao; Han Ying.
*Graduate School of Tianjin Medical University, Tianjin 300070,China
关键词:
β细胞;  抗糖尿病药物;  GLP-1;  胰岛素分泌;  2型糖尿病
Keywords:
β cells;  Anti diabetic drugs;  GLP-1;  Insulin secretion;  Type 2 diabetes mellitus
DOI:
10.3760/cma.j.issn.1673-4157.2015.01.017
摘要:
2型糖尿病的主要治疗目标是控制高血糖,然而传统的治疗药物如胰岛素和磺脲类药物在降低血糖的同时也可以出现低血糖。因此,应在一定的血糖范围内自我调整用药量,避免出现低血糖。低血糖会造成身心障碍,同时可引起心血管事件。因此临床用药应最大限度的降低低血糖风险。胰高血糖素样肽-1受体激动剂呈葡萄糖依赖性的刺激胰岛素分泌,在胰岛素剂量很小或者缺乏,以及血糖浓度不高时,胰高血糖素样肽-1受体激动剂则不会刺激或很少刺激胰岛素分泌。
Abstract:
The aim to treat type 2 diabetes is to control the high blood glucose. However, the traditional drugs such as insulin and sulfonylureas can not only lower the blood glucose, but also cause hypoglycemia.Therefore, the drug dosage should be adjusted frequently in order to maintain the blood glucose in a certain range and to avoid hypoglycemia. Hypoglycemia can cause physical and mental disorders, as well as cardiovascular events. Therefore, great efforts should be made in clinical medication to reduce the risk of hypoglycemia. Glucagon-like peptide -1 receptor agonists can stimulate the secretion of insulin in a blood glucose-dependent manner. When the insulin dose is very low or deficient, or the concentration of blood glucose is not high, glucagon like peptide-1 receptor agonists will not or rarely stimulate insulin secretion.

参考文献/References:

[1] Inzucchi SE, Bergenstal RM, Buse JB, et al. Management of hyperglycemia in type 2 diabetes: a patient-centered approach: position statement of the American Diabetes Association(ADA)and the European Association for the Study of Diabetes(EASD)[J].Diabetes Care,2012,35(6):1577-1596.
[2] Pettersson B, Rosenqvist U, Deleskog A, et al. Self-reported experience of hypoglycemia among adults with type 2 diabetes mellitus(Exhype)[J]. Diabetes Res Clin Pract,2011,92(1):19-25.
[3] Johnston SS, Conner C, Aagren M, et al. Evidence linking hypoglycemic events to an increased risk of acute cardiovascular events in patients with type 2 diabetes[J].Diabetes Care,2011,34:1164-1170.
[4] Yakubovich N, Gerstein HC. Serious cardiovascular outcomes in diabetes: the role of hypoglycemia[J].Circulation,2011,123(3):342-348.
[5] Montrose-Rafizadeh C, Egan JM, Roth J. Incretin hormones regulate glucose-dependent insulin secretion in RIN 1046-38 cells: mechanisms of action[J].Endocrinology,1994,135(2):589-594.
[6] G?ke R, Wagner B, Fehmann HC,et al. Glucose-dependency of the insulin stimulatory effect of glucagon-like peptide-1(7-36)amide on the rat pancreas[J].Res Exp Med(Berl),1993,193(2):97-103.
[7] Qualmann C, Nauck MA, Holst JJ,et al. Insulinotropic actions of intravenous glucagon-like peptide-1(GLP-1)
[7-36 amide] in the fasting state in healthy subjects[J].Acta Diabetol,1995,32(1):13-16.
[8] Degn KB, Brock B, Juhl CB, et al. Effect of intravenous infusion of exenatide(synthetic exendin-4)on glucose-dependent insulin secretion and counterregulation during hypoglycemia[J]. Diabetes,2004,53(9):2397-2403.
[9] Bergenstal RM, Wysham C, MacConell L, et al. Efficacy and safety of exenatide once weekly versus sitagliptin or pioglitazone as an adjunct to metformin for treatment of type 2 diabetes(DURATION-2): a randomised trial[J].Lancet,2010,376(9739):431-439.
[10] Russell-Jones D, Cuddihy RM, Hanefeld M, et al. Efficacy and safety of exenatide once weekly versus metformin, pioglitazone, and sitagliptin used as monotherapy in drug-naive patients with type 2 diabetes(DURATION-4): a 26-week double-blind study[J].Diabetes Care, 2012,35(2):252-258.
[11] Apovian CM, Bergenstal RM, Cuddihy RM, et al. Effects of exenatide combined with lifestyle modification in patients with type 2 diabetes[J]. Am J Med,2010,123(5):468.e9-468.e17.
[12] Liutkus J, Rosas Guzman J, Norwood P, et al. A placebo-controlled trial of exenatide twice-daily added to thiazolidinediones alone or in combination with metformin[J].Diabetes Obes Metab,2010,12(12):1058-1065.
[13] Blevins T, Pullman J, Malloy J, et al. DURATION-5: exenatide once weekly resulted in greater improvements in glycemic control compared with exenatide twice daily in patients with type 2 diabetes[J]. Clin Endocrinol Metab,2011,96(5):1301-1310.
[14] Drucker DJ, Buse JB, Taylor K, et al. Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority study[J].Lancet,2008,372(9645):1240-1250.
[15] Pencek R, Brunell SC, Li Y,et al.Use of concomitant glucose-lowering therapies and associated treatment results observed in clinical trials of exenatide twice-daily[J].Endocr Pract,2012,18(2):227-237.
[16] Blevins T, Han J, Nicewarner D, et al. Exenatide is non-inferior to insulin in reducing HbA1c: an integrated analysis of 1423 patients with type 2 diabetes[J].Postgrad Med,2010,122(3):118-128.
[17] Rorsman P, Renstr?m E. Insulin granule dynamics in pancreatic β cells[J].Diabetologia,2003,46(8):1029-1045.
[18] Rorsman P, Eliasson L, Renstr?m E, et al. The cell physiology of biphasic insulin secretion[J].News Physiol Sci,2000,15(2):72-77.
[19] Barg S, Eliasson L, Renstr m E, et al. A subset of 50 secretory granules in close contact with L-type Ca2+ channels accounts for first-phase insulin secretion in mouse β cells[J].Diabetes,2002,51(Suppl 1):S74-S82.
[20] Chepurny OG, Leech CA, Kelley GG,et al. Enhanced Rap1 activation and insulin secretagogue properties of an acetoxymethyl ester of an Epac-selective cyclic AMP analog in rat INS-1 cells: studies with 8-pCPT-2’-O-Me-cAMP-AM[J].Biol Chem,2009,284(16):10728-10736.
[21] Kelley GG, Chepurny OG, Schwede F, et al. Glucose-dependent potentiation of mouse islet insulin secretion by Epac activator 8-pCPT-2’-O-Me-cAMP-AM[J].Islets,2009,1(3):260-265.
[22] Seino S, Takahashi H, Fujimoto W, et al. Roles of cAMP signalling in insulin granule exocytosis[J].Diabetes Obes Metab,2009,11(Supp14):180-188.
[23] Kang G, Leech CA, Chepurny OG, et al. Role of the cAMP sensor Epac as a determinant of KATP channel ATP sensitivity in human pancreatic β-cells and rat INS-1 cells[J].J Physiol,2008,586(5):1307-1319.
[24] MacDonald PE, Wheeler MB. Voltage-dependent K+ channels in pancreatic β cells: role, regulation and potential as therapeutic targets[J]. Diabetologia,2003, 46(8): 1046-1062.
[25] Suga S, Kanno T, Nakano K, et al. GLP-1(7-36)amide augments Ca2+ current through L-type Ca2+ channel of rat pancreatic beta-cell in a cAMP-dependent manner[J].Diabetes,1997,46(11):1755-1760.
[26] Kang G, Chepurny OG, Rindler MJ, et al. A cAMP and Ca2+ coincidence detector in support of Ca2+-induced Ca2+ release in mouse pancreatic β cells[J]. J Physiol,2005, 566: 173-188.
[27] Kang G, Holz GG. Ampli cation of exocytosis by Ca2+-induced Ca2+ release in INS-1 pancreatic β cells[J].J Physiol,2003,546(Pt 1): 175-189.
[28] Eliasson L, Ma X, Renstr?m E, et al. SUR1 regulates PKA-independent cAMP-induced granule priming in mouse pancreatic β-cells[J].J Gen Physiol,2003, 121(3): 181-197.
[29] Kemp DM, Habener JF. Synergistic effect of dimethyl sulfoxide on glucagon-like peptide 1(GLP-1)-stimulated insulin secretion and gene transcription in INS-1 cells: characterization and implications[J].Biochem Pharmacol,2002,64(4):689-697.

相似文献/References:

[1]袁扬,孙子林.PANDER与β细胞凋亡[J].国际内分泌代谢杂志,2007,(04):253.
[2]崔巍,施秉银.内质网应激介导β细胞生存/死亡的研究进展[J].国际内分泌代谢杂志,2007,(04):256.
[3]王登,贾正平,李茂星,等.糖皮质激素与2型糖尿病[J].国际内分泌代谢杂志,2014,(02):118.[doi:10.3760/cma.j.issn.1673-4157.2014.02.014]
　Wang Deng*,Jia Zhengping,Li Maoxing,et al.Glucocorticoid and type 2 diabetes mellitus[J].International Journal of Endocrinology and Metabolism,2014,(01):118.[doi:10.3760/cma.j.issn.1673-4157.2014.02.014]
[4]曹雯,范尧夫,孙洪平,等.逆转2型糖尿病:梦想还是现实?[J].国际内分泌代谢杂志,2020,40(05):315.[doi:10.3760/cma.j.cn121383-20191110-11015]
　Cao Wen,Fan Yaofu,Sun Hongping,et al.Reversing type 2 diabetes mellitus: dreams or reality?[J].International Journal of Endocrinology and Metabolism,2020,40(01):315.[doi:10.3760/cma.j.cn121383-20191110-11015]

更新日期/Last Update: 2015-01-20