China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Biotechnology, Tianjin University of Science & Technology, Tianjin 300457, China.
Centre de recherche de Gif-sur-Yvette, Institut de Chimie des Substances Naturelles, UPR 2301, CNRS, Avenue de la Terrasse, 91198 Gif-sur-Yvette, France.
Molecules. 2021 Feb 15;26(4):1024. doi: 10.3390/molecules26041024.
Our previous study found that desmethylxanthohumol () inhibited α-glucosidase in vitro. Recently, further investigations revealed that dehydrocyclodesmethylxanthohumol () and its dimer analogue rottlerone () exhibited more potent α-glucosidase inhibitory activity than . The aim of this study was to synthesize a series of rottlerone analogues and evaluate their α-glucosidase and DPP-4 dual inhibitory activity. The results showed that compounds and irreversibly and potently inhibited α-glucosidase (IC = 0.22 and 0.12 μM) and moderately inhibited DPP-4 (IC = 23.59 and 26.19 μM), respectively. In addition, compounds and significantly promoted glucose consumption, with the activity of at 0.2 μM being comparable to that of metformin at a concentration of 1 mM.
我们之前的研究发现去甲黄腐醇（）在体外抑制α-葡萄糖苷酶。最近的进一步研究表明，脱氢环去甲黄腐醇（）及其二聚体类似物罗特酮（）比表现出更强的α-葡萄糖苷酶抑制活性。本研究旨在合成一系列罗特酮类似物，并评价它们对α-葡萄糖苷酶和 DPP-4 的双重抑制活性。结果表明，化合物和不可逆地、有效地抑制α-葡萄糖苷酶（IC=0.22 和 0.12 μM），适度抑制 DPP-4（IC=23.59 和 26.19 μM）。此外，化合物和显著促进葡萄糖消耗，化合物在 0.2 μM 时的活性与浓度为 1mM 的二甲双胍相当。
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