Fei Fuhuan, Sun Huanmei, Cheng Xixi, Liu Jiajun, Wang Jing, Li Qian, Zhang Yajun
Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, College of Life Sciences, Northwest University, Xi'an, 710069 China.
Chin Med. 2018 Sep 24;13:49. doi: 10.1186/s13020-018-0207-8. eCollection 2018.
San-ao decoction (SAD) has been widely used in Chinese medicine against respiratory diseases, such as asthma and rhinallergosis. The bioactive compounds for such pharmacological action remain unknown.
We developed a methodology to isolate the bioactive compounds of SAD. The assay involved the immobilization of beta 2-adrenoceptor ( -AR) onto magnetic fine particles, the capture of target compounds by the immobilized receptor, the identification of the receptor bound compounds by reversed-phase high-performance liquid chromatography coupled with tandem mass spectrometry.
Vicenin, shaftoside, isoshaftoside, liquiritin apioside and isoliquiritin apioside were identified as -AR ligands in SAD extract. The binding of these compounds to -AR occurred on serine, serine and phenylalanine of the receptor.
The developed methodology has high stability and specificity for recognizing and isolating target compounds. It is an alternative method for rapidly screening bioactive compounds of immobilized receptor from Chinese prescriptions.
三拗汤已在中国医学中广泛用于治疗呼吸系统疾病，如哮喘和鼻变态反应。这种药理作用的生物活性化合物尚不清楚。
我们开发了一种分离三拗汤生物活性化合物的方法。该测定包括将β2 -肾上腺素能受体（β-AR）固定在磁性细颗粒上，通过固定化受体捕获目标化合物，通过反相高效液相色谱-串联质谱法鉴定与受体结合的化合物。
在三拗汤提取物中，异荭草苷、轴皮苷、异轴皮苷、甘草苷元芹糖糖苷和异甘草苷元芹糖糖苷被鉴定为β-AR配体。这些化合物与β-AR的结合发生在受体的丝氨酸、丝氨酸和苯丙氨酸上。
所开发的方法在识别和分离目标化合物方面具有高稳定性和特异性。它是一种从中药方剂中快速筛选固定化受体生物活性化合物的替代方法。
