Synthesis and cytotoxicity evaluation of 3-amino-2-hydroxypropoxygenistein derivatives

• 来源期刊: 中国天然药物
• 学科: 医学
• 年，卷（期）: 2017,（11）
• 页码范围: 871-880
• 页数: 10页
• 分类号: R282|R965
• 语种: 英文
• DOI: 10.3724/SP.J.1009.2017.00871

摘要

Soy isoflavones exhibit various biological activities,such as antioxidant,anti-tumor,anti-inflammatory,and cardiovascular protective effects.The present study was designed to investigate the effects of sixteen synthesized 3-amino-2-hydroxypropoxy genistein derivatives on cell proliferation and activation of Nrf2 (Nuclear factor erythroid 2-related factor 2)/ARE (antioxidant response elements) pathway in human cancer cell lines.Most of the tested compounds exerted greater cytotoxic activity than genistein,as measured by MTT assay.Moreover,compound 8c showed the highest ARE-luciferase reporter activity among the test compounds.It strongly promoted Nrf2 nuclear translocation and up-regulated the expression of total Nrf2 and downstream targets NQO-1 and HO-1 at protein level.The present study may provide a basis for the application of isoflavone derivatives as Nrf2/ARE pathway inducers for cancer therapy and cancer prevention.