Abstract
Conventionally, benzophenone-type molecules are beneficial for alleviating the UV exposure of humans. More importantly, various compounds with this skeleton have demonstrated various biological activities. In this paper, we report the anti-hyperuricemic effect of the benzophenone compound 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid (HMS). Preliminarily, its molecular docking score and xanthine oxidase (XOD) inhibition suggested a good anti-hyperuricemic effect. Then, its anti-hyperuricemic effect, primary mechanisms and general toxicity were examined on a hyperuricemic mouse model which was established using potassium oxonate and hypoxanthine together. HMS demonstrated a remarkable anti- hyperuricemic effect which was near to that of the control drugs, showing promising perspective. General toxicity was assessed and it showed no negative effects on body weight growth and kidney function. Moreover, anti-inflammatory action was observed for HMS via spleen and thymus changes. Its anti-hyperuricemic mechanisms may be ascribed to its inhibition of XOD and its up-regulation of organic anion transporter 1 (OAT1) and down-regulation of glucose transporter 9 (GLUT9).
Highlights
Due to their significant absorption of ultraviolet radiation (UV), UV filters extensively dominate sunscreen formulations in many products, such as cosmetics, plastics, packages and films [1] and are even utilized as DNA photosensitizers and photocatalysts [2]
In comparison to the positive control oxypurinol which is almost buried in the inner active tunnel of xanthine oxidase (XOD), hydroxy-4-methoxybenzophenone-5-sulfonic acid (HMS)’s two cyclic moieties were buried into the inner tunnel and its two substituents attached to one aromatic moiety sited and occupied the outer tunnel
2018, 2671 active tunnel of XOD, HMS’s two cyclic moieties were buried into the inner tunnel and its two substituents attached to one aromatic moiety sited and occupied the outer tunnel
Summary
Due to their significant absorption of ultraviolet radiation (UV), UV filters extensively dominate sunscreen formulations in many products, such as cosmetics, plastics, packages and films [1] and are even utilized as DNA photosensitizers and photocatalysts [2]. The most important ones are benzophenone-type chemicals, since ultraviolet (UV) irradiation can excite them to undergo an ultrafast conversion from singlet to triplet states, which is the very property that is exploited in some of the above applications. Due to their unique and typical photochemical properties, they serve as archetypal systems for investigating the fundamental photochemistry of aromatic ketones [3]. Molecules 2018, 23, x FOR PEER REVIEW exploited in some of the above applications Besides the main benefit of benzophenone-type chemicals of alleviating alleviating human human UV exposure, are alsoconsidered consideredasasendocrine endocrine disruptors [1,4]
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