在Tenacissoside G和paclitaxel之间评估P-glycoprotein介导的草药相互作用
Jiudong Hu1,2, Yujie Hu2, Lingyan Xu2
1College of Food Science and Technology, Shanghai Ocean University, Shanghai, China.
Biomedical chromatography : BMC
|August 17, 2024
概括
泰纳西索G (Tsd-G) 通过抑制P-glycoprotein (P-gp) 在老鼠中延长了帕克利塔塞尔 (PTX) 循环时间. 这表明Tsd-G可能会与PTX调解草药相互作用,影响疗效和安全性.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物新陈代谢 药物新陈代谢
- 自然产品 化学 化学
背景情况:
- P-glycoprotein (P-gp) 中介草药相互作用 (HDIs),影响药物的有效性和安全性.
- 来自Marsdenia tenacissima的tenacissoside G (Tsd-G) 具有抗癌性质. 这是一种抗癌物质.
研究的目的:
- 在大鼠中研究Tsd-G对帕克利塔塞尔 (PTX) 的药理动力学影响.
- 探索P-gp在TsdG和PTX之间调解HDI中的潜在作用.
主要方法:
- 鼠接受了Tsd-G (20-60毫克/公斤) 或对照组7天,随后是静脉注射PTX (6毫克/公斤).
- 血PTX度使用超高性能液体染色学-并联质谱法 (UHPLC-MS/MS) 来量化.
- 分析了TsdG对P-gp的结合和表达抑制.
主要成果:
- 使用Tsd-G显著延长了PTX的平均停留时间.
- Tsd-G通过键与P-gp稳定结合.
- Tsd-G抑制了大鼠肝中的P-gp表达.
结论:
- Tsd-G与PTX呈现草药相互作用,可能由P-gp调解.
- Tsd-G对P-gp的抑制可能会改变PTX的药理动力学,影响其治疗潜力和安全性.
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