Euphorbia maculata has long been used for managing different impairments in Asian countries.However,its antioxidant,anti-inflammatory and antiproliferative potentialities,along with its potential bioactive compounds r...Euphorbia maculata has long been used for managing different impairments in Asian countries.However,its antioxidant,anti-inflammatory and antiproliferative potentialities,along with its potential bioactive compounds remain unexplored.In 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 activities.As a result,the E.maculata 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 lines.EMEA 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 validations.The interrelationship between E.maculata’s associated activities(antioxidant,anti-inflammatory and antiproliferative)was revealed with the corresponding multipotent phytochemical active components from this work.It also provided a useful direction for its empirical traditional use and further explorations in the near future.展开更多
文摘Euphorbia maculata has long been used for managing different impairments in Asian countries.However,its antioxidant,anti-inflammatory and antiproliferative potentialities,along with its potential bioactive compounds remain unexplored.In 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 activities.As a result,the E.maculata 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 lines.EMEA 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 validations.The interrelationship between E.maculata’s associated activities(antioxidant,anti-inflammatory and antiproliferative)was revealed with the corresponding multipotent phytochemical active components from this work.It also provided a useful direction for its empirical traditional use and further explorations in the near future.
