Tyurenkov I N, Faibisovich T I, Bakulin D A
Volgograd State Medical University.
S. M. Kirov Military Medical Academy.
Probl Endokrinol (Mosk). 2023 Aug 30;69(4):61-69. doi: 10.14341/probl13257.
Diabetes mellitus (DM) is the leading cause of premature death and disability. Despite a significant number of drugs, the effectiveness of therapy aimed at normalizing the level of glycemia and preventing complications does not fully satisfy doctors and patients. Therefore, the search for new approaches for the prevention and treatment of DM and its complications continues. Significant resources are used to develop new drugs, but recently the possibility of using «old» widely available drugs with newly discovered pleiotropic properties has been substantiated. These may include preparations of gammaaminobutyric acid (GABA) and agents that directly or indirectly activate GABAergic transmission, which have a pronounced pancreatic protective effect, which has been widely discussed in foreign literature over the past 10-15 years. However, there are few such publications in the domestic literature.It has been established that the content of GABA in β-cells in patients with type 1 and type 2 diabetes is reduced and this correlates with the severity of the disease. Genetic suppression of GABA receptors causes a significant decrease in the mass of β-cells and glucose-stimulated insulin secretion, which confirms the importance of GABA in ensuring glucose homeostasis and the advisability of replenishing the GABA deficiency in DM with its additional administration. It has been established that in animals with DM, GABA suppresses apoptosis and stimulates the regeneration of β-cells, increases β-cell mass and insulin production.Experimental data have been obtained indicating a synergistic effect of GABA when combined with glucagon-like peptide-1 (GLP-1) receptor agonists, DPP-4 inhibitors and sodium-glucose cotransporter 2 (SGLT-2) inhibitors, when a more pronounced pancreoprotective effect is observed, due to decrease in oxidative and nitrosative stress, inflammation, increase in the level of Klotho protein, Nrf-2 activity and antioxidant defense enzymes, suppression of NF-kB activity and expression of pro-inflammatory cytokines. As a result, all this leads to a decrease in apoptosis and death of β-cells, an increase in β-cell mass, insulin production and, at the same time, a decrease in glucagon levels and insulin resistance.The review substantiates the feasibility of using GABA and drugs with a positive GABAeric effect in combination with new generation antidiabetic agents: GLP-1 receptor agonists, DPP-4 inhibitors and SGLT-2 inhibitors in order to increase their antidiabetic potential.The search was carried out in the databases Pubmed, eLibrary, Medline. Keywords: diabetes mellitus, gamma-aminobutyric acid, glucagon-like peptide-1, GLP-1 receptor agonists, glucose-dependent insulinotropic peptide, dipeptidyl peptidase inhibitors, sodium-glucose cotransporter 2 inhibitors. The search was carried out from 2000 to 2022, but the review presents the results studies published mainly in the last 3 years, due to the requirements of the journal for the maximum amount of work and the number of sources.
糖尿病(DM)是过早死亡和残疾的主要原因。尽管有大量药物,但旨在使血糖水平正常化并预防并发症的治疗效果并不能完全令医生和患者满意。因此,寻找预防和治疗DM及其并发症的新方法的工作仍在继续。大量资源被用于开发新药,但最近已证实使用具有新发现的多效性特性的“老”的常用药物的可能性。这些药物可能包括γ-氨基丁酸(GABA)制剂以及直接或间接激活GABA能传递的药物,它们具有显著的胰腺保护作用,在过去10至15年的国外文献中对此进行了广泛讨论。然而,国内文献中此类出版物较少。已确定1型和2型糖尿病患者β细胞中GABA的含量降低,且这与疾病的严重程度相关。对GABA受体的基因抑制会导致β细胞数量和葡萄糖刺激的胰岛素分泌显著减少,这证实了GABA在确保葡萄糖稳态中的重要性以及通过额外给药补充DM中GABA缺乏的合理性。已确定在患有DM的动物中,GABA可抑制细胞凋亡并刺激β细胞再生,增加β细胞数量和胰岛素产生。已获得实验数据表明,GABA与胰高血糖素样肽-1(GLP-1)受体激动剂、二肽基肽酶-4(DPP-4)抑制剂和钠-葡萄糖协同转运蛋白2(SGLT-2)抑制剂联合使用时具有协同作用,此时由于氧化应激和亚硝化应激、炎症的减少,Klotho蛋白水平、Nrf-2活性和抗氧化防御酶的增加,NF-κB活性和促炎细胞因子表达的抑制,观察到更显著的胰腺保护作用。结果,所有这些导致β细胞凋亡和死亡减少,β细胞数量、胰岛素产生增加,同时胰高血糖素水平和胰岛素抵抗降低。该综述证实了将GABA和具有正向GABA能作用的药物与新一代抗糖尿病药物:GLP-1受体激动剂、DPP-4抑制剂和SGLT-2抑制剂联合使用以增加其抗糖尿病潜力的可行性。检索在数据库Pubmed、eLibrary、Medline中进行。关键词:糖尿病、γ-氨基丁酸、胰高血糖素样肽-1、GLP-1受体激动剂、葡萄糖依赖性促胰岛素多肽、二肽基肽酶抑制剂、钠-葡萄糖协同转运蛋白2抑制剂。检索时间为2000年至2022年,但由于期刊对工作量和来源数量的要求,本综述呈现的主要是过去3年发表的研究结果。