利用受体配体亲和技术筛选黄芩中血管紧张素转换酶2和二肽基肽酶4抑制剂  

Study on screening angiotensin converting enzyme 2 and dipeptidyl peptidase 4 inhibitors in baical skullcap root by receptor-ligand affinity technique

作　　者：康健斌[1] 张语迟[2] KANG Jianbin;ZHANG Yuchi(Department of Pharmacy,Changchun Hospital of Traditional Chinese Medicine,Changchun 130052,China;National and Local Joint Engineering Laboratory of Separation,Purifi cation and Activity Screening Technology of Natural Drugs,Changchun Normal University,Changchun 130032,China)

机构地区：[1]长春市中医院药剂科,长春130052 [2]长春师范大学天然药物分离纯化及活性筛选技术国家地方联合工程实验室,长春130032

出　　处：《长春中医药大学学报》2024年第8期859-863,共5页Journal of Changchun University of Chinese Medicine

基　　金：中央本级重大增减支项目(2060302)。

摘　　要：目的筛选中药黄芩中血管紧张素转换酶2(ACE2)和二肽基肽酶4(DPP-4)抑制剂。方法以ACE2和DPP-4作为靶蛋白,利用受体配体亲和超滤和液质联用技术,对黄芩中与ACE2和DPP-4亲和的化合物进行筛选和分析,以筛选具有同时抑制ACE2和DPP-4的化合物。结果从黄芩中筛选出了5,7,2′,6′-4羟基黄酮、5,7,2′,5′-4羟基-8,6′-二甲氧基黄酮、白杨素-7-O-葡萄糖醛酸苷、黄芩素-6-O-葡萄糖醛酸苷、千层纸素A-7-O-葡萄糖醛酸苷、汉黄芩苷、白杨素、千层纸素A,可以同时亲和抑制ACE2和DPP-4,具有潜在的抗新型冠状病毒的作用。结论从黄芩中筛选出与新型冠状病毒肺炎有关的靶蛋白抑制剂,具备潜在开发价值。Objective To screen the inhibitors of angiotensin converting enzyme 2(ACE2)and dipeptidyl peptidase 4(DPP-4)from baical skullcap root.Methods ACE2 and DPP4 were used as the target proteins,the compounds in baical skullcap root that were compatible with ACE2 and DPP4 were screened and analyzed by receptor-ligand affinity ultrafiltration and liquid chromatographymass spectrometry,in order to screen compounds that could simultaneously inhibit ACE2 and DPP-4.Results 5,7,2′,6′-4 hydroxyfl avone,5,7,2′,5′-4 hydroxy-8,6′-dimethoxyfl avone,chrysin-7-O-glucuronide,baicalein-6-O-glucuronide,oroxylin A-7-O-glucuronide,wogonoside,chrysin,oroxylin A were screened from baical skullcap root,and their affi nity and inhibition towards ACE2 and DPP-4 coexisted,and they had potential anti novel coronavirus effect.Conclusion The target protein inhibitors related to novel coronavirus pneumonia screened from baical skullcap root have potential development value.

关 键 词：受体配体亲和 血管紧张素转换酶2 二肽基肽酶4 抑制剂 

分 类 号：R917[医药卫生—药物分析学]