文献类型：期刊文献

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

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

第一作者：Zhang, Qi-li

通信作者：Zhao, L[1];Zhao, L[2];Zhao, L[3];Yang, J[4];Zhao, L[5]

机构：[1]Gansu Univ Chinese Med, Lanzhou 730000, Gansu, Peoples R China;[2]Gansu Univ Chinese Med, Dingxi Teachers Coll, Dingxi Campus, Dingxi 743000, Peoples R China;[3]Coll Gansu Prov, Key Lab Chem & Qual TCM, Lanzhou 730000, Gansu, Peoples R China;[4]Gansu Prov Engn Lab TCM Standardizat Technol & Po, Lanzhou 730000, Gansu, Peoples R China;[5]Gansu Prov Peoples Hosp, Lanzhou 730000, Gansu, Peoples R China;[6]Minist Educ, Key Lab Dunhuang Med, Lanzhou 730000, Gansu, Peoples R China

第一机构：甘肃中医药大学

通信机构：[1]corresponding author), Gansu Univ Chinese Med, Lanzhou 730000, Gansu, Peoples R China;[2]corresponding author), Coll Gansu Prov, Key Lab Chem & Qual TCM, Lanzhou 730000, Gansu, Peoples R China;[3]corresponding author), Gansu Prov Engn Lab TCM Standardizat Technol & Po, Lanzhou 730000, Gansu, Peoples R China;[4]corresponding author), Gansu Prov Peoples Hosp, Lanzhou 730000, Gansu, Peoples R China;[5]corresponding author), Minist Educ, Key Lab Dunhuang Med, Lanzhou 730000, Gansu, Peoples R China.|[10735]甘肃中医药大学;

年份：2019

卷号：11

期号：1

起止页码：108

外文期刊名：CHINESE HERBAL MEDICINES

收录：WOS:【ESCI(收录号:WOS:000457111700016)】；

基金：We sincerely thank Lanzhou University Dr. Huan-xiang Liu gave us great help in molecular docking experiments. This work was supported by the National Natural Science Foundation of China (No. 81660577, No. 21562001, and No. 81560716) and Natural Science Foundation of Gansu Province (1506RJZA036 and 148RJZA064).

语种：英文

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 (PGE 2), 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 (iNOS) 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 iNOS. 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, PGE 2, and IL-6, and the suppression of iNOS and COX-2. Therefore, gentiopicroside is a potential and selective iNOS and COX-2 inhibitor. (c) 2018 Tianjin Press of Chinese Herbal Medicines. Published by Elsevier B. V. All rights reserved.