PDF(Pubmed)
Abstract：
Dipeptidyl peptidase 4 (DPP4) inhibitors, commonly known as gliptins, have been an integral part of the treatment of type 2 diabetes mellitus (T2DM) for several years. Despite their remarkable efficacy in lowering glucose levels and their compatibility with other hypoglycemic drugs, recent studies have revealed adverse effects, prompting the search for improved drugs within this category, which has required the use of animal models to verify the hypoglycemic effects of these compounds. Currently, in many countries the use of mammals is being significantly restricted, as well as cost prohibitive, and alternative in vivo approaches have been encouraged. In this sense, Drosophila has emerged as a promising alternative for several compelling reasons: it is cost-effective, offers high experimental throughput, is genetically manipulable, and allows the assessment of multigenerational effects, among other advantages. In this study, we present evidence that diprotin A, a DPP4 inhibitor, effectively reduces glucose levels in Drosophila hemolymph. This discovery underscores the potential of Drosophila as an initial screening tool for novel compounds directed against DPP4 enzymatic activity.
摘要：
二肽基肽酶4（DPP4）抑制剂，通常被称为gliptins，多年来一直是2型糖尿病（T2DM）治疗的重要组成部分。尽管它们在降低葡萄糖水平方面具有显着的功效，并且与其他降血糖药物兼容，最近的研究揭示了副作用，促使在这一类别中寻找改进的药物，这需要使用动物模型来验证这些化合物的降血糖作用。目前,在许多国家，哺乳动物的使用受到了极大的限制，以及成本过高，和替代体内方法受到鼓励。在这个意义上,果蝇已成为一种有希望的替代品，有几个令人信服的原因：它具有成本效益，提供高实验吞吐量，是基因可操纵的，并允许评估多代效应，在其他优势中。在这项研究中,我们提供的证据表明二丙肽A,一种DPP4抑制剂，有效降低果蝇血淋巴的葡萄糖水平。这一发现强调了果蝇作为针对DPP4酶活性的新型化合物的初始筛选工具的潜力。
