A Review of Dipeptidyl Peptidase-4 (DPP-4) and its potential synthetic derivatives in the management of Diabetes Mellitus

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Abstract

Dipeptidyl peptidase-4 (DPP-4) inhibitors are a type of oral medication used to treat type 2 diabetes mellitus (T2DM). They have become increasingly popular due to their effectiveness and safety in managing the condition. DPP-4 inhibitors function by inhibiting the enzyme that breaks down the incretin hormones, namely glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). These medicines efficiently raise the levels of active GLP-1 and GIP by blocking DPP-4 activity. As a result, there is an increase in the production of insulin, a decrease in the release of glucagon, and a lowering of glucose levels after a meal. Multiple clinical trials have conclusively shown that DPP-4 inhibitors effectively lower glycated hemoglobin (HbA1c) levels. Certain studies have even proved their equivalent efficacy to other anti-diabetic medications such as metformin or sulfonylureas. Furthermore, DPP-4 inhibitors possess the benefit of being weight-neutral and exhibiting a little risk of hypoglycemia. These qualities render them a compelling option for patients with type 2 diabetes mellitus who are overweight or susceptible to hypoglycemia episodes. In general, DPP-4 inhibitors are a promising therapeutic choice for the management of type 2 diabetes mellitus (T2DM), offering effective regulation of blood sugar levels with a minimal likelihood of adverse effects. Nevertheless, it is important to acknowledge some restrictions and factors to take into account, including the possibility of heightened susceptibility to pancreatitis, nasopharyngitis, and certain drug-drug combinations. Additional investigation is necessary to completely clarify the long-term safety and potential supplementary advantages of DPP-4 inhibitors.
二肽基肽酶-4 (DPP-4) 及其潜在合成衍生物在糖尿病治疗中的应用综述
二肽基肽酶-4(DPP-4)抑制剂是一种用于治疗 2 型糖尿病(T2DM)的口服药物。由于其在控制病情方面的有效性和安全性,它们越来越受欢迎。DPP-4 抑制剂通过抑制分解增量激素(即胰高血糖素样肽-1(GLP-1)和葡萄糖依赖性促胰岛素肽(GIP))的酶来发挥作用。这些药物通过阻断 DPP-4 的活性,有效提高活性 GLP-1 和 GIP 的水平。因此,胰岛素分泌增加,胰高血糖素释放减少,餐后血糖水平降低。多项临床试验证实,DPP-4 抑制剂能有效降低糖化血红蛋白(HbA1c)水平。某些研究甚至证明,其疗效与二甲双胍或磺脲类药物等其他抗糖尿病药物相当。此外,DPP-4 抑制剂还具有不影响体重和低血糖风险小的优点。这些特性使其成为体重超重或易发生低血糖的 2 型糖尿病患者的理想选择。总的来说,DPP-4 抑制剂是治疗 2 型糖尿病(T2DM)的一种很有前景的治疗选择,可有效调节血糖水平,且不良反应的可能性极低。不过,我们也必须认识到一些限制和需要考虑的因素,包括可能会增加对胰腺炎、鼻咽炎和某些药物组合的易感性。要彻底澄清 DPP-4 抑制剂的长期安全性和潜在的辅助优势,还需要进行更多的调查。
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