一种巨孔毛细管电泳法,用于从复杂的天然药物混合物中发现瘤向成分
Nurmuhammat Kehriman1, Tao Huang2, Chunsu Liang2
1Department of Pharmaceutical Analysis, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, China; Department of Pharmacy, Jiangbei Campus of The First Affiliated Hospital of Army Medical University (No. 958 Hospital of PLA Army), Chongqing, 400020, China.
一种新型的巨孔毛细血管电泳 (MFCE) 方法可以直接监测瘤组织-化合物相互作用. 这种技术可以快速识别天然药物中的强效抗瘤化合物,加速抗癌药物发现.
科学领域:
- 药理学 药理学是指药理学的学科.
- 分析化学 分析化学
- 生物化学 生物化学
背景情况:
- 传统的查天然药物中的抗瘤化合物是低效的,缺乏生理相关性.
- 现有的方法耗时,劳动密集,可复制性差,无法模拟体内条件.
研究的目的:
- 开发和验证一个巨孔毛细血管电泳 (MFCE) 方法,用于直接监测瘤组织与化合物相互作用.
- 为了快速定性和定量分析复杂的天然产品混合物和瘤组织之间的相互作用.
- 促进新型多向抗癌化合物的发现.
主要方法:
- 建立了一个巨孔毛细血管电泳 (MFCE) 系统,使用瘤组织作为在巨孔上固定的相互作用阶段.
- 应用MFCE与CE-MS/MS和LC-MS/MS相结合,用于化合物-组织相互作用的定性和定量分析.
- 使用非线性染色学量化结合动力学参数,并通过体外和体内试验验证实结果.
主要成果:
- MFCE成功地确定了Aidi注射和A549瘤组织之间的相互作用化合物,与之前的研究一致.
- 对艾菲蜂蜜膏提取物的分析确定了与HT-29瘤组织相互作用的多种化合物.
- 鉴定的化合物在细胞活力测定和异种移植模型中表现出强烈的抗瘤活性.
结论:
- MFCE提供了一种快速,可靠和可重复的策略,用于直接监测瘤组织与化合物相互作用.
- 该方法准确量化结合动力学,并验证已识别的化合物的生物相关性.
- MFCE为从天然药物中有效发现多向抗癌剂奠定了基础.
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