文献类型：期刊文献

中文题名：Anti-inflammatory activities of gentiopicroside against iNOS and COX-2 targets

英文题名：Anti-inflammatory activities of gentiopicroside against iNOS and COX-2 targets

作者：Qi-li Zhang[1,2,3,4,5];Jian Zhang[1,3,4];Peng-fei Xia[1,3,4];Xue-jing Peng[1,3,4];Hai-long Li[1];Hua Jin[1];Yang Li[1];Jie Yang[6];Lei Zhao[1,3,4,6]

第一作者：Qi-li Zhang

机构：[1]Gansu University of Chinese Medicine;[2]Dingxi Campus of Gansu University of Chinese Medicine, Dingxi Teachers College;[3]Key Laboratory of Chemistry and Quality for TCM of the College of Gansu Province;[4]Gansu Province Engineering Laboratory for TCM Standardization Technology and Popularization;[5]Key Laboratory of Dunhuang Medicine, Ministry of Education;[6]Gansu Province People's Hospital

第一机构：甘肃中医药大学

年份：2019

卷号：11

期号：1

起止页码：108

中文期刊名：Chinese Herbal Medicines

外文期刊名：中草药（英文版）

收录：CSTPCD

基金：supported by the National Natural Science Foundation of China (No.81660577, No.21562001, and No.81560716);Natural Science Foundation of Gansu Province (1506RJZA036 and 148RJZA064)

语种：英文

中文关键词：anti-inflammatory;activity;cyclooxygenase-2;gentiopicroside;inducible;nitric;oxide;synthase;inflammation;target

外文关键词：anti-inflammatory activity;cyclooxygenase-2;gentiopicroside;inducible nitric oxide synthase;inflammation target

摘要：Objective: To isolate high-purity gentiopicroside from the Chinese herbal Gentiana officinalis and investigate its anti-inflammatory activity against iNOS and COX-2 targets.Methods: The purity and structures of gentiopicroside were determined by HPLC, IR, NMR, and MS. The anti-inflammatory effects of gentiopicroside were investigated by in vivo, in vitro, and molecular experiments.Results: In vitro experiment results showed that gentiopicroside inhibited nitric oxide(NO), prostaglandin E2(PGE2), and interleukin-6(IL-6) production in mouse macrophages RAW 264.7 stimulated by lipopolysaccharide. In vivo experiment found that xylene-induced mouse ear swelling was inhibited by gentiopicroside with an inhibition rate of 34.17%. Molecular docking of cyclooxygenase-2(COX-2) and inducible nitric oxide synthase(i NOS) with gentiopicroside showed that hydrogen bonds(H-bonds) were formed between the sugar fragments in gentiopicroside structure with Tyr355, Ser353, Leu352, Ser530,Arg120, and His90 of COX-2, and Glu377, Asp382, Tyr373, Tyr347, Gln263, Asn370, and Gly371 of i NOS.Thus, gentiopicroside had a lower docking score and displayed satisfactory anti-inflammatory activities.Conclusion: These results suggested that the mechanism of anti-inflammatory activity of gentiopicroside was associated with the downregulation of inflammatory cytokines, such as NO, PGE2, and IL-6, and the suppression of iNOS and COX-2. Therefore, gentiopicroside is a potential and selective iNOS and COX-2 inhibitor.
Objective: To isolate high-purity gentiopicroside from the Chinese herbal Gentiana officinalis and investigate its anti-inflammatory activity against iNOS and COX-2 targets.Methods: The purity and structures of gentiopicroside were determined by HPLC, IR, NMR, and MS. The anti-inflammatory effects of gentiopicroside were investigated by in vivo, in vitro, and molecular experiments.Results: In vitro experiment results showed that gentiopicroside inhibited nitric oxide(NO), prostaglandin E2(PGE2), and interleukin-6(IL-6) production in mouse macrophages RAW 264.7 stimulated by lipopolysaccharide. In vivo experiment found that xylene-induced mouse ear swelling was inhibited by gentiopicroside with an inhibition rate of 34.17%. Molecular docking of cyclooxygenase-2(COX-2) and inducible nitric oxide synthase(i NOS) with gentiopicroside showed that hydrogen bonds(H-bonds) were formed between the sugar fragments in gentiopicroside structure with Tyr355, Ser353, Leu352, Ser530,Arg120, and His90 of COX-2, and Glu377, Asp382, Tyr373, Tyr347, Gln263, Asn370, and Gly371 of i NOS.Thus, gentiopicroside had a lower docking score and displayed satisfactory anti-inflammatory activities.Conclusion: These results suggested that the mechanism of anti-inflammatory activity of gentiopicroside was associated with the downregulation of inflammatory cytokines, such as NO, PGE2, and IL-6, and the suppression of iNOS and COX-2. Therefore, gentiopicroside is a potential and selective iNOS and COX-2 inhibitor.