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Simultaneous Screening and Analysis of Anti-inflammatory and Antiproliferative compounds from Euphorbia maculata Combining Bio-affinity Ultrafiltration with Multiple Drug Targets

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Journal of Analysis and Testing 2022年第2期6卷 98-110页

作者： Tojofaniry Fabien Rakotondrabe Min-Xia Fan Yong-Li Zhang Ming-Quan Guo CAS Key Laboratory of Plant Germplasm Enhancement and Specialty Agriculture Wuhan Botanical GardenChinese Academy of SciencesWuhan 430074China University of Chinese Academy of Sciences Beijing 100049China Sino-Africa Joint Research Center Chinese Academy of SciencesWuhan 430074China Innovation Academy for Drug Discovery and Development Chinese Academy of SciencesShanghai 201203China

Euphorbia maculata has long been used for managing different impairments in Asian ***,its antioxidant,anti-inflammatory and antiproliferative potentialities,along with its potential bioactive compounds remain *** this context,a bio-a ffinity ultrafiltration strategy was developed to fish out ligand candidates against Cycloxygenase-2(COX-2),Topoisomerase I(Topo I),and TopoisomeraseⅡ(TopoⅡ).Thereafter,lead compounds activities were assessed in silico and in vitro for ascertaining the screening results and forecasting its corresponding *** a result,the *** ethyl acetate(EMEA)fraction showed interesting COX-2 inhibition activity with an IC 50 value of 0.67±0.09μg/mL,as well as good growth inhibitions for three malignant cell *** chemical fingerprinting was also conducted to enable a tentative identification of 17 compounds,among which,11 were assessed as ligand candidates to COX-2,8 compounds to Topo I,and 10 compounds to TopoⅡ.Dihydromyricetin and quercetin-3-O-arabinoside were revealed to be multipotent compounds which exerted good a ffinity to the three targeted enzymes,and also supported with their molecular docking simulations and in vitro assay *** interrelationship between ***’s associated activities(antioxidant,anti-inflammatory and antiproliferative)was revealed with the corresponding multipotent phytochemical active components from this *** also provided a useful direction for its empirical traditional use and further explorations in the near future.

关键词： Euphorbia maculata Antioxidant Anti-infl ammatory Antiproliferative UF-UPLC-QTOF-MS/MS multipotent compounds

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