典型文献
Inhibition of drug-metabolizing enzymes by Jingyin granules:implications of herb-drug interactions in antiviral therapy
文献摘要：
Jingyin granules,a marketed antiviral herbal medicine,have been recommended for treating H1N1 influenza A virus infection and Coronavirus disease 2019(COVID-19)in China.To fight viral diseases in a more efficient way,Jingyin granules are frequently co-administered in clinical settings with a variety of therapeutic agents,including antiviral drugs,anti-inflammatory drugs,and other Western medicines.However,it is unclear whether Jingyin granules modulate the pharmacokinetics of Western drugs or trigger clinically significant herb-drug interactions.This study aims to assess the inhibitory potency of the herbal extract of Jingyin granules(HEJG)against human drug-metabolizing enzymes and to clarify whether HEJG can modulate the pharmacokinetic profiles of Western drug(s)in vivo.The results clearly demonstrated that HEJG dose-dependently inhibited human CES1 A,CES2A,CYPs1 A,2A6,2C8,2C9,2D6,and 2E1;this herbal medicine also time-and NADPH-dependently inhibited human CYP2C19 and CYP3A.In vivo tests showed that HEJG significantly increased the plasma exposure of lopinavir(a CYP3A-substrate drug)by 2.43-fold and strongly prolonged its half-life by 1.91-fold when HEJG(3g/kg)was co-administered with lopinavir to rats.Further investigation revealed licochalcone A,licochalcone B,licochalcone C and echinatin in Radix Glycyrrhizae,as well as quercetin and kaempferol in Folium Llicis Purpureae,to be time-dependent CYP3A inhibitors.Collectively,our findings reveal that HEJG modulates the pharmacokinetics of CYP substrate-drug(s)by inactivating CYP3A,providing key information for both clinicians and patients to use herb-drug combinations for antiviral therapy in a scientific and reasonable way.
文献关键词：
中图分类号：
作者姓名：
Feng Zhang;Wei Liu;Jian Huang;Qi-long Chen;Dan-dan Wang;Li-wei Zou;Yong-fang Zhao;Wei-dong Zhang;Jian-guang Xu;Hong-zhuan Chen;Guang-bo Ge
作者机构：
Institute of Interdisciplinary Integrative Medicine Research,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China;Institute of Liver Diseases,Shuguang Hospital,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China;Pharmacology and Toxicology Division,Shanghai Institute of Food and Drug Control,Shanghai 201203,China;SPH Xing Ling Sci.&Tech.Pharmaceutical Co.,Ltd,Shanghai 201703,China
文献出处：
引用格式：
[1]Feng Zhang;Wei Liu;Jian Huang;Qi-long Chen;Dan-dan Wang;Li-wei Zou;Yong-fang Zhao;Wei-dong Zhang;Jian-guang Xu;Hong-zhuan Chen;Guang-bo Ge-.Inhibition of drug-metabolizing enzymes by Jingyin granules:implications of herb-drug interactions in antiviral therapy)[J].中国药理学报（英文版）,2022(04):1072-1081
A类：
Jingyin,HEJG,CES2A,CYPs1,2C8,lopinavir,Llicis,Purpureae
B类：
Inhibition,metabolizing,enzymes,by,granules,implications,interactions,antiviral,therapy,marketed,herbal,have,been,recommended,treating,H1N1,influenza,infection,Coronavirus,China,To,fight,diseases,more,efficient,way,are,frequently,administered,settings,variety,therapeutic,agents,including,drugs,inflammatory,other,medicines,However,unclear,whether,pharmacokinetics,trigger,clinically,This,study,aims,assess,inhibitory,potency,extract,against,human,clarify,profiles,vivo,results,clearly,demonstrated,that,dose,dependently,inhibited,CES1,2A6,2C9,2D6,2E1,this,also,NADPH,CYP2C19,CYP3A,tests,showed,significantly,increased,plasma,exposure,substrate,fold,strongly,prolonged,its,half,life,when,3g,was,rats,Further,investigation,revealed,licochalcone,echinatin,Radix,Glycyrrhizae,well,quercetin,kaempferol,Folium,inhibitors,Collectively,our,findings,modulates,inactivating,providing,key,information,both,clinicians,patients,use,combinations,scientific,reasonable
AB值：
0.485174
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