Identification of Inhibitory Activities of Dietary Flavonoids against URAT1, a Renal Urate Re-Absorber: In Vitro Screening and Fractional Approach Focused on Rooibos Leaves.
Identification of Inhibitory Activities of Dietary Flavonoids against URAT1, a Renal Urate Re-Absorber: In Vitro Screening and Fractional Approach Focused on Rooibos Leaves.
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DOI：
10.3390/nu14030575
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发表时间：
2022-01-28
期刊：
影响因子：
5.9
通讯作者：
Suzuki H
中科院分区：
文献类型：
--
作者：
Toyoda Y;Takada T;Saito H;Hirata H;Ota-Kontani A;Tsuchiya Y;Suzuki H
高尿酸血症是一种与生活方式相关的疾病，其特征是血清尿酸水平升高，是痛风的主要危险因素；因此，人类饮食或饮食成分的降低血清尿酸的作用引起了人们的广泛关注。由于尿酸盐转运体1(URAT1)控制着尿酸从初级尿液重新吸收到血液中的大部分，抑制URAT1有助于通过增加肾脏尿酸盐的净排泄来降低血清尿酸水平。在这项研究中，我们使用基于细胞的尿酸盐转运实验来研究162种人类食用植物材料的提取物对URAT1的抑制作用。其中，我们重点研究了Rooibos茶的来源Aspalatus Linearis，以探索其有效成分。采用液-液萃取和随后的柱层析，以及用于化学表征的光谱分析，我们确定了槲皮素为URAT1抑制剂。我们还研究了23种饮食成分的URAT1抑制活性，其中包括9种黄烷醇、2种黄烷醇、2种黄酮类、2种异黄酮类、8种查尔酮和1种香豆素。在所测试的正品化合物中，菲斯汀和栎素对URAT1的抑制活性最强和次之，IC50值分别为7.5IC50M和12.6IC50MμM。虽然植物化学物质的这些影响应该在人体研究中进一步研究，但我们的发现可能会为使用营养食品促进健康提供新的线索。
Hyperuricemia, a lifestyle-related disease characterized by elevated serum urate levels, is the main risk factor for gout; therefore, the serum urate-lowering effects of human diets or dietary ingredients have attracted widespread interest. As Urate transporter 1 (URAT1) governs most urate reabsorption from primary urine into blood, URAT1 inhibition helps decrease serum urate levels by increasing the net renal urate excretion. In this study, we used a cell-based urate transport assay to investigate the URAT1-inhibitory effects of 162 extracts of plant materials consumed by humans. Among these, we focused on Aspalathus linearis, the source of rooibos tea, to explore its active ingredients. Using liquid–liquid extraction with subsequent column chromatography, as well as spectrometric analyses for chemical characterization, we identified quercetin as a URAT1 inhibitor. We also investigated the URAT1-inhibitory activities of 23 dietary ingredients including nine flavanols, two flavanonols, two flavones, two isoflavonoids, eight chalcones, and a coumarin. Among the tested authentic chemicals, fisetin and quercetin showed the strongest and second-strongest URAT1-inhibitory activities, with IC50 values of 7.5 and 12.6 μM, respectively. Although these effects of phytochemicals should be investigated further in human studies, our findings may provide new clues for using nutraceuticals to promote health.
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