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黄酮类衍生物治疗肺癌的构效关系及作用机制研究进展

Research Progress on the Structure-activity Relationship and Mechanism of Flavonoid Derivatives in the Treatment of Lung Cancer.

作者信息

Yao Jiacheng, Zhu Feng, Feng Yikun, Gu Chen, Wang Tianyu, Li Xinyu, Yang Hao, Hu Xiamin, Bonnet Pierre-Antoine, Meng Xiangguo

机构信息

Graduate School, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.

Faculty of Pharmacy, Shanghai University of Medicine and Health Sciences, Shanghai 201318, China.

出版信息

Molecules. 2025 Apr 18;30(8):1827. doi: 10.3390/molecules30081827.

DOI:10.3390/molecules30081827
PMID:40333837
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12029265/
Abstract

Non-small-cell lung cancer (NSCLC) is the leading cause of cancer-related deaths worldwide. The difficulty in early diagnosis, combined with the tendency for tumor invasion and metastasis, creates significant challenges for current therapeutic approaches. Additionally, the pharmaceutical agents currently used to treat NSCLC often come with severe side effects and can lead to drug resistance. As a result, there is an urgent need to develop new therapeutic agents with fewer side effects that can effectively overcome resistance mechanisms. Flavonoids, a prominent class of natural compounds, have shown promise in preventing and treating various cancers. By structurally optimizing flavonoids, it is possible to enhance their anticancer activity and improve their pharmacokinetic properties. This article reviews the different mechanisms of action and structure-activity relationships (SARs) of flavonoid derivatives in treating NSCLC, aiming to provide a scientific foundation for developing new therapeutic agents.

摘要

非小细胞肺癌(NSCLC)是全球癌症相关死亡的主要原因。早期诊断的困难,加上肿瘤侵袭和转移的倾向,给当前的治疗方法带来了重大挑战。此外,目前用于治疗NSCLC的药物往往伴有严重的副作用,并可能导致耐药性。因此,迫切需要开发副作用较少且能有效克服耐药机制的新型治疗药物。黄酮类化合物是一类重要的天然化合物,在预防和治疗各种癌症方面已显示出前景。通过对黄酮类化合物进行结构优化,可以增强其抗癌活性并改善其药代动力学性质。本文综述了黄酮类衍生物在治疗NSCLC中的不同作用机制和构效关系(SARs),旨在为开发新型治疗药物提供科学依据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/119c6591dc15/molecules-30-01827-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/0a649d775039/molecules-30-01827-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/77882ef51ddc/molecules-30-01827-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/77420690d552/molecules-30-01827-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/7a27d48404c6/molecules-30-01827-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/3676844dca86/molecules-30-01827-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/119c6591dc15/molecules-30-01827-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/0a649d775039/molecules-30-01827-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/77882ef51ddc/molecules-30-01827-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/77420690d552/molecules-30-01827-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/7a27d48404c6/molecules-30-01827-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/3676844dca86/molecules-30-01827-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d640/12029265/119c6591dc15/molecules-30-01827-g006.jpg

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本文引用的文献

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Org Biomol Chem. 2025 Feb 12;23(7):1574-1580. doi: 10.1039/d4ob01759e.
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Exploring the 3,5-Dibromo-4,6-dimethoxychalcones and Their Flavone Derivatives as Dual α-Glucosidase and α-Amylase Inhibitors with Antioxidant and Anticancer Potential.探索3,5-二溴-4,6-二甲氧基查尔酮及其黄酮衍生物作为具有抗氧化和抗癌潜力的双α-葡萄糖苷酶和α-淀粉酶抑制剂。
Antioxidants (Basel). 2024 Oct 17;13(10):1255. doi: 10.3390/antiox13101255.
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Trends in Cancer Incidence and Potential Associated Factors in China.
中国癌症发病率的变化趋势及潜在相关因素。
JAMA Netw Open. 2024 Oct 1;7(10):e2440381. doi: 10.1001/jamanetworkopen.2024.40381.
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Recent Advances in Targeted Cancer Therapy: Are PDCs the Next Generation of ADCs?靶向癌症治疗的最新进展:PDCs 是否是下一代 ADC 药物?
J Med Chem. 2024 Jul 25;67(14):11469-11487. doi: 10.1021/acs.jmedchem.4c00106. Epub 2024 Jul 9.
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MOFs for next-generation cancer therapeutics through a biophysical approach-a review.通过生物物理方法用于下一代癌症治疗的金属有机框架材料——综述
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