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具有组蛋白去乙酰化酶抑制活性的牛蒡子苷元衍生物的设计、合成及活性评价

Design, synthesis and activity evaluation of arctigenin derivatives with HDAC inhibition activity.

作者信息

Jiang Xinyue, Yan Yuchao, Yang Huali, Cheng Maosheng, Dou Deqiang, Liu Yang

机构信息

Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University Shenyang 110016 P.R. China

Department of Chinese Medicine Chemistry, Liaoning University of Traditional Chinese Medicine Dalian 116000 P.R. China

出版信息

RSC Adv. 2024 Mar 20;14(13):9314-9325. doi: 10.1039/d4ra00050a. eCollection 2024 Mar 14.

DOI:10.1039/d4ra00050a
PMID:38510486
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10951978/
Abstract

Arctigenin, a natural product with diverse pharmacological activities, can inhibit cell proliferation and survival and has shown promising potential in cancer research. In this study, we designed a series of arctigenin derivatives with HDAC inhibitory activity based on the synergistic effects between HDAC inhibitors and arctigenin. Among them, compound B7 exhibited significantly higher antiproliferative activity in the MV411 cell line compared to the positive control, tucidinostat. Additionally, enzymatic activity testing was performed with compound B7. Further mechanistic studies indicated that compound B7 induced apoptosis through the Caspase-3 pathway in MV411 cells and enhanced histone acetylation levels in the MV411 cell line. These findings highlight the broad potential application of these arctigenin derivatives in cancer therapy.

摘要

牛蒡子苷元是一种具有多种药理活性的天然产物，能够抑制细胞增殖和存活，在癌症研究中显示出了有前景的潜力。在本研究中，基于组蛋白去乙酰化酶（HDAC）抑制剂与牛蒡子苷元之间的协同作用，我们设计了一系列具有HDAC抑制活性的牛蒡子苷元衍生物。其中，化合物B7在MV411细胞系中表现出比阳性对照图西司他更高的抗增殖活性。此外，对化合物B7进行了酶活性测试。进一步的机制研究表明，化合物B7通过半胱天冬酶-3途径诱导MV411细胞凋亡，并提高了MV411细胞系中的组蛋白乙酰化水平。这些发现突出了这些牛蒡子苷元衍生物在癌症治疗中的广泛潜在应用。

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本文引用的文献

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