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咖啡酸类似物作为多功能治疗剂的发现与开发

Discovery and Development of Caffeic Acid Analogs as Versatile Therapeutic Agents.

作者信息

Mou Yi, Wen Shuai, Sha Hong-Kai, Zhao Yao, Gui Li-Juan, Wang Yan, Jiang Zheng-Yu

机构信息

College of Pharmacy and Chemistry & Chemical Engineering, Taizhou University, Taizhou 225300, China.

Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.

出版信息

Pharmaceuticals (Basel). 2024 Oct 20;17(10):1403. doi: 10.3390/ph17101403.

DOI:10.3390/ph17101403
PMID:39459042
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11510674/
Abstract

Caffeic acid (CA) is a polyphenolic acid compound widely distributed in plant seeds. As natural compounds with high research interest, caffeic acid and its derivatives show good activity in the treatment of tumors and inflammation and have antibacterial properties. In recent years, caffeic acid derivatives have been studied extensively, and these derivatives fall roughly into three categories: (1) caffeic acid ester derivatives, (2) caffeic acid amide derivatives, (3) caffeic acid hybrids. These caffeic acid analogues exert mainly antibacterial and antioxidant activities. Among the caffeic acid analogues summarized in this paper, compounds and CAP10 have good activity against , and their MIC is 32 µg/mL and 13 μM, respectively. In a DPPH assay, compounds , , CS2, Phellinsin A and showed strong antioxidant activity, and their IC values are 18.6 μM, 67.85 μM, 40.29 μM, 0.29 ± 0.004 mM, 4774.37 ± 137.20 μM, respectively. Overall, compound CAP10 had the best antibacterial activity and compound had the best antioxidant activity. This paper mainly summarizes and discusses some representative caffeic acid analogs, hoping to provide better drug design strategies for the subsequent development of caffeic acid analogs.

摘要

咖啡酸（CA）是一种广泛分布于植物种子中的多酚酸化合物。作为具有高研究价值的天然化合物，咖啡酸及其衍生物在肿瘤和炎症治疗中表现出良好的活性，并具有抗菌特性。近年来，咖啡酸衍生物得到了广泛研究，这些衍生物大致可分为三类：（1）咖啡酸酯衍生物，（2）咖啡酸酰胺衍生物，（3）咖啡酸杂化物。这些咖啡酸类似物主要发挥抗菌和抗氧化活性。在本文总结的咖啡酸类似物中，化合物 和CAP10对 具有良好活性，其MIC分别为32 µg/mL和13 μM。在DPPH测定中，化合物 、 、CS2、桑黄菌素A和 表现出较强的抗氧化活性，其IC值分别为18.6 μM、67.85 μM、40.29 μM、0.29±0.004 mM、4774.37±137.20 μM。总体而言，化合物CAP10具有最佳的抗菌活性，化合物 具有最佳的抗氧化活性。本文主要总结和讨论了一些具有代表性的咖啡酸类似物，希望为咖啡酸类似物的后续开发提供更好的药物设计策略。

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