合成和生物评估的复星甲基衍生物
Elizabeth Fragopoulou1, Katerina Gkotsi1, Filio Petsini1
1Department of Nutrition and Dietetics, Harokopio University, 70 Eleftheriou Venizelou Avenue Kallithea, 17676 Athens, Greece.
Molecules (Basel, Switzerland)
|July 29, 2023
概括
复星的甲索基衍生物显示出增强的抗血小板和抗癌性质. 4'-甲基衍生物表现出优异的抗血小板活性,而其他衍生物对特定癌症细胞系表现出强大的抗瘤作用.
科学领域:
- 药理学和药物化学 药理学和药物化学
- 自然产品衍生品 自然产品衍生品
- 癌症生物学 癌症生物学
背景情况:
- Resveratrol是一种天然的stilbene,具有有益的健康效果,但其生物可用性较差.
- 为了提高生物可用性和药理活性,正在探索resveratrol衍生物.
- 关于复星衍生物对血小板功能的影响的数据有限.
研究的目的:
- 合成新的白醇甲基衍生物.
- 评估这些衍生物的抗血小板活性.
- 评估它们对癌细胞的抗增殖作用.
主要方法:
- 合成的复星甲基衍生物.
- 使用由PAF,ADP和TRAP刺激的富血小板血 (PRP) 测试了抗血小板活性.
- 评估了针对PC-3和HCT116癌细胞系的抗瘤活性.
- 为结构分析而进行的形研究.
主要成果:
- 一些甲基衍生物显示出与白醇相比的可比或增强的抗血小板活性.
- 4种extquotesingle-methoxy衍生物显示出明显更高的抗血小板功效,对TRAP诱导的聚合.
- 特定衍生物 (3-MRESV,3,4 extquotesingle-DMRESV,TMRESV) 在PC-3和HCT116细胞中表现出强大的抗瘤活性.
- 在分析中,发现了4种extquotesingle-methoxy衍生物和Vorapaxar之间的结构相似性.
结论:
- 复星甲衍生物提供了改善的抗血小板和抗癌作用.
- 4 extquotesingle-methoxy衍生物是一种有前途的抗血小板剂候选物.
- 这些衍生物在各种疾病中具有治疗应用的潜力.
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