Zhang Jianjun, Zhao Min, Wu Fan, Shi Zheng, Xie Rui
Department of Pharmacy, The First Affiliated Hospital of Zhejiang Chinese Medical University (Zhejiang Provincial Hospital of Traditional Chinese Medicine), Hangzhou, China.
J Enzyme Inhib Med Chem. 2025 Dec;40(1):2551970. doi: 10.1080/14756366.2025.2551970. Epub 2025 Sep 2.
The quest for effective and safe treatments for diabetes mellitus has led to the exploration of natural metabolites as potential α-glucosidase inhibitors. This study delves into the inhibition mechanism of wedelolactone against α-glucosidase and its hypoglycaemic activity. Activity assay results discovered that wedelolactone functioned as a mixed-type inhibitor, with an IC of 39.12 ± 2.54 μM, surpassing the potency of the standard drug acarbose. Employing multi-spectra methods, our findings indicated that wedelolactone binding induced conformation changes in α-glucosidase to attenuate its enzymatic activity, as evidenced by fluorescence quenching, synchronous fluorescence, 3D fluorescence, CD spectra, and ANS assay. Molecular docking studies provided insights into the specific interactions between wedelolactone and α-glucosidase. Collectively, these results laid the groundwork for the potential application of wedelolactone as a natural therapeutic agent in diabetes management.
对糖尿病有效且安全治疗方法的探索促使人们研究天然代谢产物作为潜在的α-葡萄糖苷酶抑制剂。本研究深入探讨了水飞蓟宾对α-葡萄糖苷酶的抑制机制及其降血糖活性。活性测定结果发现，水飞蓟宾作为一种混合型抑制剂，IC值为39.12±2.54μM，超过了标准药物阿卡波糖的效力。采用多光谱方法，我们的研究结果表明，水飞蓟宾的结合会引起α-葡萄糖苷酶的构象变化，从而减弱其酶活性，荧光猝灭、同步荧光、三维荧光、圆二色谱和ANS测定都证明了这一点。分子对接研究揭示了水飞蓟宾与α-葡萄糖苷酶之间的具体相互作用。这些结果共同为水飞蓟宾作为糖尿病管理中的天然治疗剂的潜在应用奠定了基础。
