前列腺细胞膜色谱-液相色谱-质谱法筛选钩藤有效成分。

PubMed ID
G H
发表日期 年月

原始出处 色谱科学杂志
Journal of chromatographic science
作者 He  Jianyu  Han  Shengli  Yang  Fangfang  Zhou  Nan  Wang  Sicen 

文献标题 前列腺细胞膜色谱-液相色谱-质谱法筛选钩藤有效成分。
Prostate cell membrane chromatography-liquid chromatography-mass spectrometry for screening of active constituents from Uncaria rhynchophylla.
Prostate cell membrane chromatography-liquid chromatography-mass spectrometry for screening of active constituents from Uncaria rhynchophylla.

文献摘要

钩藤是一种传统的中药,用于治疗高血压和癫痫等抽搐性疾病。采用大鼠前列腺细胞膜色谱-液相色谱-质谱联用技术(LC-MS)对大鼠前列腺细胞膜色谱进行了研究。钩藤提取物。发现了4个化合物(corynoxine、isorhynchophyline、isocorynoxeine和rhynchophyline)。竞争结合实验结果表明,这四种化合物在一个共同的结合位点上直接竞争,并以类似坦索罗辛的方式与α1A肾上腺素能受体(α1A-AR)相互作用。用大鼠前列腺细胞膜色谱法(CMC)测定了四种化合物与α1A-AR结合的亲和常数。最后在大鼠尾动脉上进行药效学实验。这种CMC-LC-MS联用系统通过筛选天然药物,寻找新的靶向受体的药理活性分子,为药物的发现提供了一种手段。


Uncaria rhynchophylla is a traditional Chinese medicinal herb used to treat hypertension and convulsive disorders such as epilepsy. Rat prostate cell membrane chromatography combined with liquid chromatography-mass spectrometry (LC-MS) was used to identify active constituents from U. rhynchophylla extracts. Four compounds (corynoxeine, isorhynchophylline, isocorynoxeine and rhynchophylline) were discovered. Competitive binding assay results indicated that the four compounds were in direct competition at a single common binding site and interacted with α1A adrenergic receptors (α1A-AR) in a manner similar to tamsulosin. Affinity constant values of the four compounds binding with α1A-AR were also measured using rat prostate cell membrane chromatography (CMC). Finally, their pharmacodynamic effects were tested on rat caudal arteries. This CMC combined LC-MS system offers a means of drug discovery by screening natural medicinal herbs for new pharmacologically active molecules targeting specific receptors.

Uncaria rhynchophylla is a traditional Chinese medicinal herb used to treat hypertension and convulsive disorders such as epilepsy. Rat prostate cell membrane chromatography combined with liquid chromatography-mass spectrometry (LC-MS) was used to identify active constituents from U. rhynchophylla extracts. Four compounds (corynoxeine, isorhynchophylline, isocorynoxeine and rhynchophylline) were discovered. Competitive binding assay results indicated that the four compounds were in direct competition at a single common binding site and interacted with α1A adrenergic receptors (α1A-AR) in a manner similar to tamsulosin. Affinity constant values of the four compounds binding with α1A-AR were also measured using rat prostate cell membrane chromatography (CMC). Finally, their pharmacodynamic effects were tested on rat caudal arteries. This CMC combined LC-MS system offers a means of drug discovery by screening natural medicinal herbs for new pharmacologically active molecules targeting specific receptors.


获取全文 10.1093/chromsci/bms188