Identification of NF-κB inhibitors in Qishenyiqi dropping pills for myocardial infarction treatment based on bioactivity-integrated UPLC-Q/TOF MS
Identification of NF-κB inhibitors in Qishenyiqi dropping pills for myocardial infarction treatment based on bioactivity-integrated UPLC-Q/TOF MS
复制标题
基于生物活性集成UPLC-Q/TOF MS鉴定芪参益气滴丸治疗心肌梗死中NF-κB抑制剂
DOI：
10.1002/bmc.3468
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发表时间：
2015-10-01
影响因子：
1.8
通讯作者：
Luo, Guoan
中科院分区：
文献类型：
--
作者：
Han, Yanqi;Zhou, Mengge;Luo, Guoan
芪参益气滴丸是一种规范化的治疗心肌梗死（MI）的心血管类多味药。关于QSYQ的核因子-κ B（NF-B）抑制剂的系统鉴定的知识通常是缺乏的。因此，有必要建立一种有效的方法来筛选抑制NF-B的活性成分。本研究采用大鼠冠状动脉结扎模型，观察QSYQ的心肌保护作用。检测心电图、心脏组织病理学及血清脑钠肽、心肌肌钙蛋白I、炎性细胞因子等生化指标。采用超高效液相色谱-四极杆/飞行时间质谱（UPLC-Q/TOF MS）结合NF-B荧光素酶报告基因分析系统对QSYQ中潜在的抗炎活性成分进行筛选。结果表明，强心益气汤能改善心肌梗死大鼠心功能，减轻中性粒细胞浸润，降低炎性细胞因子水平。此外，22个化合物被确定为潜在的NF-B抑制剂。结论：NF-B的失活和细胞因子的抑制可能是芪参益气汤治疗心肌梗死的主要机制。UPLC-Q/TOF MS结合生物活性人体细胞功能评价系统是筛选中药方剂中生物活性成分的一种简单有效的方法。版权所有（c）2015约翰威利父子有限公司
Qishenyiqi dropping pills (QSYQ) are a type of standardized cardiovascular multiherb medicine for the treatment of myocardial infarction (MI). Knowledge concerning the systemic identification of nuclear factor-kappa B (NF-B) inhibitors of QSYQ is generally lacking. Therefore, it is necessary to establish an effective method to screen the bioactive components of NF-B inhibition. In the present study, a rat model of coronary artery ligation was used to assess the cardioprotective effects of QSYQ. The electrocardiograms, histopathology of heart tissues and serum biochemical indicators, such as brain natriuretic peptide, cardiac troponin I and inflammatory cytokines, were measured. Subsequently, ultra-performance liquid chromatography quadrupole/time-of-flight mass spectrometry (UPLC-Q/TOF MS) combined with the NF-B luciferase reporter assay system was applied to screen the potential anti-inflammatory compounds in QSYQ. The results revealed that the administration of QSYQ could improve heart function, ameliorate neutrophil infiltration and diminish the levels of inflammatory cytokines in MI rats. Furthermore, 22 compounds were determined to be potential NF-B inhibitors. In conclusion, NF-B inactivation and cytokine suppression might be the main mechanisms of QSYQ for MI treatment. The method of UPLC-Q/TOF MS combined with a bioactive human cell functional evaluation system was proved to be a simple and effective strategy for screening bioactive compounds in traditional Chinese medicine prescriptions. Copyright (c) 2015 John Wiley & Sons, Ltd.