Hypouricemic effect of Grifola frondosa on hyperuricemic mice and virtual screening of bioactives by 3D QSAR pharmacophore modeling
Hypouricemic effect of Grifola frondosa on hyperuricemic mice and virtual screening of bioactives by 3D QSAR pharmacophore modeling
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DOI：
10.1016/j.jff.2017.11.049
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发表时间：
2018
影响因子：
5.6
通讯作者：
T. Yong;Yizhen Xie;Shaodan Chen;Diling Chen;Jiyan Su;C. Jiao;Huiping Hu;Chun Xiao
中科院分区：
文献类型：
--
作者：
T. Yong;Yizhen Xie;Shaodan Chen;Diling Chen;Jiyan Su;C. Jiao;Huiping Hu;Chun Xiao
灰树花在亚洲已被开发为治疗代谢性疾病的草药和美味的食物。水提物和醇提物均有明显的降尿作用，使血尿酸水平从高尿酸血症对照组的240molo l/L(P<； .01)降低到30、60和120 μmg/kg剂量组的170、169和153 moL/L，50、100和200 μmg/kg的水提物组分别降至169、168和156 摩尔/L，与正常对照组(159 μm ol/L)相似。ELISA法分析表明，GFW和GFE对URAT1蛋白有抑制作用，而不是对黄嘌呤氧化酶(XOD)的抑制作用。成功建立了URAT1的3D-QSAR药效团模型。其中4个化合物得到了充分的鉴定和图谱，值得进一步研究。综上所述，海藻是开发功能食品的一个很有前途的候选者。
Grifola frondosa(GF) has been exploited as herb medicine for metabolic diseases and also as tasty food in Asia. Water (GFW) and ethanol (GFE) extracts produced remarkable hypouricemic effects, thereby decreasing the levels of serum uric acid from 240 μmol/L (hyperuricemia control,P< .01) to 170, 169, and 153 μmol/L for GFW at doses of 30, 60, and 120 mg/kg and to 169, 168, and 156 μmol/L for GFE at 50, 100, and 200 mg/kg correspondingly, which were similar to the normal control (159 μmol/L). ELISA analysis demonstrated the inhibitory effects of GFW and GFE on URAT1 protein rather than xanthine oxidase (XOD). The 3D-QSAR pharmacophore model for URAT1 was established successfully. Four compounds were identified and mapped adequately, deserving further study. Taken together,G. frondosais a promising candidate for the development of functional foods.