吲哚衍生物的结构修饰及其抗乳腺癌作用研究进展  

Research progress on structural modifications of indole derivatives and anti-breast cancer effects

作　　者：方玉秋 王薪淇 齐学洁[1] 段莉莉 琚辉[1] FANG Yuqiu;WANG Xinqi;QI Xuejie;DUAN Lili;JU Hui(School of Traditional Chinese Medicine,Tianjin University of Traditional Chinese Medicine,Tianjin Key Laboratory of Therapeutic Substance of Traditional Chinese Medicine,Tianjin 301617,China)

机构地区：[1]天津中医药大学中药学院,天津市中药功效物质研究重点实验室,天津301617

出　　处：《药物评价研究》2024年第2期419-429,共11页Drug Evaluation Research

基　　金：天津市教育委员会重点项目(2022ZD041)。

摘　　要：吲哚是平面杂环分子,对乳腺癌、肺癌、结肠癌等具有广泛的抗癌活性,在药物设计中发挥重要作用。从吲哚-3-甲醇及其代谢产物3,3′-二吲哚甲烷的结构修饰、吲哚骨架结构修饰、氧化吲哚衍生物及氮杂吲哚衍生物的结构修饰入手,并综合吲哚衍生物对Lumina型乳腺癌、三阴性乳腺癌、人表皮生长因子受体2(HER-2)过表达型乳腺癌的影响,从细胞水平、乳腺癌相关蛋白、受体、经典通路、体内外药理模型建立以及相关指标的变化等方面对其抗乳腺癌作用进行系统综述,以期为抗乳腺癌新药研发提供依据。Indole,a planar heterocyclic molecule,plays an important role in drug design due to its extensive anti-cancer activity against breast cancer,lung cancer and colon cancer.In this paper,the structure modification of indole-3-methanol(I3C) and its metabolite 3,3′-diindolemethane(DIM),the structure modification of indole skeleton structure,the structure modification of oxidized indole derivatives and azaindole derivatives were studied.In addition,the effects of indole derivatives on Luminal type breast carcinoma,human epidermal growth factor receptor 2(HER-2) overexpression type breast carcinoma and triple negative breast cancer(TNBC) were summarized.The anti-breast cancer effects of indole derivatives were systematically reviewed from the aspects of cell level,breast cancer-related proteins,receptors,classical pathways,establishment of pharmacological models in vivo and in vitro,and changes of related indexes,to provide theoretical basis for the research of indole derivatives in the field of antibreast cancer drug innovation.

关 键 词：吲哚-3-甲醇 吲哚 氧化吲哚 氮杂吲哚 乳腺癌 人表皮生长因子受体2(HER-2) 

分 类 号：R285.5[医药卫生—中药学]