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Comparative effects of quercetin, luteolin, apigenin and their related polyphenols on uric acid production in cultured hepatocytes and suppression of purine bodies‐induced hyperuricemia by rutin in mice
Cytotechnology ( IF 2.2 ) Pub Date : 2021-02-02 , DOI: 10.1007/s10616-021-00452-9
Shin-Ichi Adachi 1 , Mifuyu Oyama 2 , Shinji Kondo 1 , Kazumi Yagasaki 1
Affiliation  

Hyperuricemia, the high uric acid (UA) state in blood, has been accepted as an important risk factor for gout. The liver is a main factory of UA production. In the present study, we have examined the effects of three kinds of flavonol and flavones as typical aglycons, i.e., quercetin, luteolin, apigenin, their glycosides and related compounds, on UA productivity in cultured hepatocytes, adopting allopurinol as the positive control drug. Quercetin, luteolin, diosmetin (4′-O-methylluteolin) and apigenin at 10, 30 and 100 μM as well as allopurinol at 0.1, 0.3 and 1 μM dose-dependently and significantly decreased UA production in the hepatocytes, when compared with 0 μM (control). Both rutin (quercetin-3-O-rutinoside) and quercitrin (quercetin-3-O-ramnoside) significantly reduced UA production in the hepatocytes at 100 μM. Luteolin glycosides such as orientin (luteolin-8-C-glucoside) and isoorientin (luteolin-6-C-glucoside) exerted no influences on it even at 100 μM. Likewise, apigenin glycosides such as vitexin (apigenin-8-C-glucoside) and isovitexin (apigenin-6-C-glucoside) showed no inhibitory effect on it, while apigetrin (apigenin-7-O-glucoside) significantly reduced it at 100 μM. In model mice with purine bodies-induced hyperuricemia, allopurinol completely suppressed the hyperuricemia at a dose of 10 mg/kg body weight. Rutin suppressed significantly the hyperuricemia at a dose of 300 mg/kg body weight, while vitexin showed no significant effect up to 300 mg/kg body weight. Thus, rutin (O-glycoside) is demonstrated to be hypouricemic in both cultured hepatocytes and model mice with recently contrived purine bodies-induced hyperuricemia.



中文翻译:

槲皮素、木犀草素、芹菜素及其相关多酚对培养肝细胞尿酸产生及芦丁抑制小鼠嘌呤体诱导的高尿酸血症的影响比较

高尿酸血症,即血液中的高尿酸 (UA) 状态,已被认为是痛风的重要危险因素。肝脏是UA生产的主要工厂。在本研究中,我们以别嘌醇为阳性对照药物,考察了槲皮素、木犀草素、芹菜素及其苷类和相关化合物三种黄酮醇和黄酮类化合物作为典型苷元对培养肝细胞尿酸产量的影响。与 0 μM 相比,10、30 和 100 μM 的槲皮素、木犀草素、薯蓣草素(4'- O-甲基木犀草素)和芹菜素以及 0.1、0.3 和 1 μM 的别嘌呤醇剂量依赖性地显着降低肝细胞中 UA 的产生(控制)。芦丁 (quercetin-3- O -rutinoside) 和槲皮素 (quercetin-3- O-ramnoside) 在 100 μM 时显着降低肝细胞中 UA 的产生。木犀草素糖苷如荭草素(luteolin-8- C - glucoside)和异荭草素(luteolin-6- C - glucoside)即使在100μM时也对其没有影响。同样,芹菜素(apigenin-8- C -glucoside )和异牡荆素(apigenin-6- C -glucoside)等芹菜素苷对其没有抑制作用,而芹菜素(apigenin-7- O-葡萄糖苷)在 100 μM 时显着降低。在嘌呤体诱导的高尿酸血症模型小鼠中,别嘌醇在 10 mg/kg 体重的剂量下完全抑制了高尿酸血症。芦丁在 300 mg/kg 体重的剂量下显着抑制高尿酸血症,而牡荆素在 300 mg/kg 体重的剂量下没有显着效果。因此,芦丁(O-糖苷)在培养的肝细胞和最近设计的嘌呤体诱导的高尿酸血症模型小鼠中均被证明具有降尿酸作用。

更新日期:2021-02-02
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