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咖啡渣中的咖啡酸作为 MMP-9 和 DPP-4 酶的双重抑制剂。

Caffeic Acid in Spent Coffee Grounds as a Dual Inhibitor for MMP-9 and DPP-4 Enzymes.

机构信息

Research Group of Computer-Aided Drug Design and Discovery of Bioactive Natural Products, Faculty of Pharmacy, Sanata Dharma University, Yogyakarta 55282, Indonesia.

Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta 55281, Indonesia.

出版信息

Molecules. 2023 Oct 19;28(20):7182. doi: 10.3390/molecules28207182.

Abstract

Type 2 diabetes mellitus and diabetic foot ulcers remain serious worldwide health problems. Caffeic acid is one of the natural products that has been experimentally proven to have diverse pharmacological properties. This study aimed to assess the inhibitory activity of caffeic acid and ethanolic extract of spent coffee grounds targeting DPP-4 and MMP-9 enzymes and evaluate the molecular interactions through 50-ns molecular dynamics simulations. This study also introduced our new version of PyPLIF HIPPOS, PyPLIF HIPPOS 0.2.0, which allowed us to identify protein-ligand interaction fingerprints and interaction hotspots resulting from molecular dynamics simulations. Our findings revealed that caffeic acid inhibited the DPP-4 and MMP-9 activity with an IC of 158.19 ± 11.30 µM and 88.99 ± 3.35 µM while ethanolic extract of spent coffee grounds exhibited an IC of 227.87 ± 23.80 µg/100 µL and 81.24 ± 6.46 µg/100 µL, respectively. Molecular dynamics simulations showed that caffeic acid interacted in the plausible allosteric sites of DPP-4 and in the active site of MMP-9. PyPLIF HIPPOS 0.2.0 identified amino acid residues interacting more than 10% throughout the simulation, which were Lys463 and Trp62 in the plausible allosteric site of DPP-4 and His226 in the active site of MMP-9.

摘要

2 型糖尿病和糖尿病足溃疡仍然是全球严重的健康问题。咖啡酸是一种已被实验证明具有多种药理特性的天然产物。本研究旨在评估咖啡酸和废咖啡渣乙醇提取物对 DPP-4 和 MMP-9 酶的抑制活性,并通过 50-ns 分子动力学模拟评估分子相互作用。本研究还介绍了我们的新版本 PyPLIF HIPPOS,PyPLIF HIPPOS 0.2.0,它允许我们识别蛋白质-配体相互作用指纹和分子动力学模拟产生的相互作用热点。我们的研究结果表明,咖啡酸对 DPP-4 和 MMP-9 的抑制活性的 IC 分别为 158.19 ± 11.30 µM 和 88.99 ± 3.35 µM,而废咖啡渣乙醇提取物的 IC 分别为 227.87 ± 23.80 µg/100 µL 和 81.24 ± 6.46 µg/100 µL。分子动力学模拟表明,咖啡酸在 DPP-4 的可能变构位点和 MMP-9 的活性位点相互作用。PyPLIF HIPPOS 0.2.0 识别了在整个模拟过程中相互作用超过 10%的氨基酸残基,它们是 DPP-4 的可能变构位点中的 Lys463 和 Trp62,以及 MMP-9 的活性位点中的 His226。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3853/10609219/1ad303a4799e/molecules-28-07182-g001.jpg

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