State Key Laboratory of Applied Microbiology Southern China, Guangdong Provincial Key Laboratory of Microbial Culture Collection and Application and Guangdong Open Laboratory of Applied Microbiology, Guangdong Institute of Microbiology, Guangzhou 510070, China.
R & D Department, Guangdong Yuewei Edible Fungi Technology Co., Guangzhou 510663, China.
Molecules. 2018 Oct 17;23(10):2671. doi: 10.3390/molecules23102671.
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).
传统上，二苯甲酮类分子有益于缓解人体的紫外线暴露。更重要的是，具有这种骨架的各种化合物已经表现出多种生物活性。在本文中，我们报告了二苯甲酮化合物 2-羟基-4-甲氧基二苯甲酮-5-磺酸（HMS）的抗高尿酸血症作用。初步研究表明，其分子对接评分和黄嘌呤氧化酶（XOD）抑制作用提示其具有良好的抗高尿酸血症作用。然后，在使用氧嗪酸钾和次黄嘌呤共同建立的高尿酸血症小鼠模型上，对其抗高尿酸血症作用、主要机制和一般毒性进行了研究。HMS 表现出显著的抗高尿酸血症作用，接近对照药物，显示出有希望的前景。对一般毒性进行了评估，结果表明其对体重增长和肾功能没有不良影响。此外，通过脾和胸腺的变化观察到 HMS 的抗炎作用。其抗高尿酸血症机制可能归因于其对 XOD 的抑制作用以及对有机阴离子转运蛋白 1（OAT1）的上调和葡萄糖转运蛋白 9（GLUT9）的下调。
