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Due to this chemical diversity, several biological activities\nhave been attributed to chalcones, namely anti-diabetic, anti-inflammatory and antioxidant.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Objective:<\/jats:title>\n<jats:p>Evaluate the ability of a panel of 34 structurally related chalcones to scavenge HOCl\nand\/or suppress its production through the inhibition of human neutrophils\u2019 oxidative burst, followed\nby the establishment of the respective structure-activity relationships.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Methods:<\/jats:title>\n<jats:p>The ability of chalcones to scavenge HOCl was evaluated by fluorimetric detection of the\ninhibition of dihydrorhodamine 123 oxidation. The ability of chalcones to inhibit neutrophils\u2019 oxidative\nburst was evaluated by chemiluminometric detection of the inhibition of luminol oxidation.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Results:<\/jats:title>\n<jats:p>It was observed that the ability to scavenge HOCl depends on the position and number of\nhydroxy groups on both aromatic rings. Chalcone 5b was the most active with an IC50 value of 1.0 \u00b1\n0.1 \u03bcM. The ability to inhibit neutrophils\u2019 oxidative burst depends on the presence of a 2\u2019-hydroxy\ngroup on A-ring and on other substituents groups, e.g. methoxy, hydroxy, nitro and\/or chlorine atom(\ns) at C-2, C-3 and\/or C-4 on B-ring, as in chalcones 2d, 2f, 2j, 2i, 4b, 2n and 1d, which were the\nmost actives with IC50 values ranging from 0.61 \u00b1 0.02 \u03bcM to 1.7 \u00b1 0.2 \u03bcM.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Conclusion:<\/jats:title>\n<jats:p>The studied chalcones showed high activity at a low micromolar range, indicating their\npotential as antioxidant agents and to be used as a molecular structural scaffold for the design of new\nanti-inflammatory compounds.<\/jats:p>\n<\/jats:sec>","DOI":"10.2174\/1573406417666201230093207","type":"journal-article","created":{"date-parts":[[2020,12,31]],"date-time":"2020-12-31T04:00:50Z","timestamp":1609387250000},"page":"88-96","update-policy":"https:\/\/doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":6,"title":["Chalcones as Scavengers of HOCl and Inhibitors of Oxidative Burst: Structure-Activity Relationship Studies"],"prefix":"10.2174","volume":"18","author":[{"given":"Thaise","family":"Martins","sequence":"first","affiliation":[{"name":"LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Porto,Portugal"}]},{"given":"Vera L.M.","family":"Silva","sequence":"additional","affiliation":[{"name":"LAQV, REQUIMTE, Department of Chemistry, University of Aveiro, Aveiro,Portugal"}]},{"given":"Artur M.S.","family":"Silva","sequence":"additional","affiliation":[{"name":"LAQV, REQUIMTE, Department of Chemistry, University of Aveiro, Aveiro,Portugal"}]},{"given":"Jos\u00e9 L.F.C.","family":"Lima","sequence":"additional","affiliation":[{"name":"LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Porto,Portugal"}]},{"given":"Eduarda","family":"Fernandes","sequence":"additional","affiliation":[{"name":"LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Porto,Portugal"}]},{"given":"Daniela","family":"Ribeiro","sequence":"additional","affiliation":[{"name":"LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Porto,Portugal"}]}],"member":"965","reference":[{"key":"ref=1","doi-asserted-by":"publisher","first-page":"69","DOI":"10.1089\/152308602753625870","volume":"4","author":"Swain S.D.","year":"2002","unstructured":"Swain S.D.; Rohn T.T.; Quinn M.T.; Neutrophil priming in host defense: role of oxidants as priming agents. 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