鉴定,选和全面评估使用素生产的hirudo中的新型血栓抑制
Xiaoyu Chai1, Fulu Pan1, Qianqian Wang1
1Department of Chemistry of Traditional Chinese Medicine, School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
Frontiers in pharmacology
|December 6, 2024
概括
希鲁多水解剂 (HHS) 显示出有前途的血栓抑制潜力,其中一种特定的 (P1) 显示出显著的抗凝效应. 对于抗血栓性药物开发,建议进一步优化P1.
科学领域:
- 生物化学 生物化学
- 药理学 药理学是指药理学的学科.
- 药用化学 医学化学
背景情况:
- 血抑制是管理心血管疾病 (CVD) 的关键策略.
- 口服和蛋白质药物的疗效受到胃肠道消化系统的限制.
- 希鲁多提取物有可能成为抗血栓剂的来源.
研究的目的:
- 评估素产生的化酸盐 (HHS) 的阻血栓的特性.
- 开发一种全面的查和评估方法,用于血栓激素抑制剂.
- 识别和描述来自HHS的强血栓抑制 (TIPs).
主要方法:
- 在体外评估hirudo提取物和HHS血栓抑制活性.
- 纳米LC-MS/MS与用于TIP查的化分析相结合.
- 在体外的抗凝剂测定 (APTT,TT,PT) 和血小板聚合抑制.
- 用UV-Vis光谱和分子动力学模拟来研究TIP-血栓相互作用.
主要成果:
- HHS保留了60-75%的血栓抑制活性.
- 在HHS中发现了90种;Asn-Asp-Leu-Trp-Asp-Gln-Gly-Leu-Val-Ser-Gln-Asp-Leu (P1) 是最强大的TIP.
- P1表现出显著的血栓抑制 (IC<50>: 2,425.5 ± 109.7 μM),剂量取决于延长的血栓时间,并减少了血小板聚合.
- 光谱和模拟数据证实P1与血栓结合.
结论:
- HHS代表了发现和评估抗血栓化合物的宝贵来源.
- 鉴定的P1显示了结构优化和进一步临床前评估的潜力.
- 这项研究为查和验证新型血栓激素抑制剂提供了坚实的框架.
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