Kato Eisuke, Kawakami Kazuhiro, Kawabata Jun
a Laboratory of Food Biochemistry, Division of Applied Bioscience, Graduate School of Agriculture , Hokkaido University , Kita-ku , Hokkaido , Japan Sapporo.
J Enzyme Inhib Med Chem. 2018 Dec;33(1):106-109. doi: 10.1080/14756366.2017.1396458.
Dipeptidyl peptidase 4 (DPP-4) inhibitors are used for the treatment of type-2 diabetes mellitus. Various synthetic inhibitors have been developed to date, and plants containing natural DPP-4 inhibitors have also been identified. Here, 13 plant samples were tested for their DPP-4 inhibitory activity. Macrocarpals A-C were isolated from Eucalyptus globulus through activity-guided fractionation and shown to be DPP-4 inhibitors. Of these, macrocarpal C showed the highest inhibitory activity, demonstrating an inhibition curve characterised by a pronounced increase in activity within a narrow concentration range. Evaluation of macrocarpal C solution by turbidity, nuclear magnetic resonance spectroscopy and mass spectrometry indicated its aggregation, which may explain the characteristics of the inhibition curve. These findings will be valuable for further study of potential small molecule DPP-4 inhibitors.
二肽基肽酶4（DPP-4）抑制剂用于治疗2型糖尿病。迄今为止，已开发出多种合成抑制剂，同时也鉴定出了含有天然DPP-4抑制剂的植物。在此，对13个植物样本进行了DPP-4抑制活性测试。通过活性导向分级分离从蓝桉中分离出大果桉醇A-C，结果表明它们是DPP-4抑制剂。其中，大果桉醇C表现出最高的抑制活性，其抑制曲线的特征是在狭窄的浓度范围内活性显著增加。通过浊度、核磁共振光谱和质谱对大果桉醇C溶液进行评估，结果表明其发生了聚集，这可能解释了抑制曲线的特征。这些发现对于进一步研究潜在的小分子DPP-4抑制剂具有重要价值。
