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通过上调三磷酸腺苷结合盒超家族 G 成员 2 对高尿酸血症小鼠的降尿酸和肾脏保护作用。

Hypouricaemic and nephroprotective effects of in hyperuricemic mice by up-regulating ATP-binding cassette super-family G member 2.

机构信息

Guangdong Provincial Key Laboratory of Microbial Safety and Health and State Key Laboratory of Applied Microbiology Southern China, Guangdong Institute of Microbiology, Guangdong Academy of Sciences, Guangzhou, China.

Guangdong Yuewei Edible Fungi Technology Co., Guangzhou, China.

出版信息

Pharm Biol. 2021 Dec;59(1):275-286. doi: 10.1080/13880209.2021.1885450.

Abstract

CONTEXT

F.A.Wolf (Polyporaceae) dispels dampness and promotes diuresis implying hypouricaemic action.

OBJECTIVE

To examine hypouricaemic action of .

MATERIALS AND METHODS

Ethanol extract (PCE) was prepared by extracting the sclerotium of with ethanol, and the water extract (PCW) was produced by bathing the remains with water. PCE and PCW (50, 100 and 200 mg/kg, respectively) were orally administered to hyperuricemic Kunming mice ( = 8) to examine its hypouricaemic effect. Also, molecular docking was performed.

RESULTS

showed excellent hypouricaemic action, decreasing the serum uric acid of hyperuricaemia (HUA) control (526 ± 112 μmol/L) to 178 ± 53, 153 ± 57 and 151 ± 62 μmol/L ( < 0.01) by PCE and 69 ± 23, 63 ± 15 and 62 ± 20 μmol/L ( < 0.01) by PCW, respectively. According to SCrs, BUNs and H&E staining, PCE and PCW partially attenuated renal dysfunction caused by HUA. They presented no negative effects on ALT, AST and ALP activities. They elevated ABCG2 (ATP-binding cassette super-family G member 2) mRNA and protein expression in comparison to HUA control. In molecular docking, compound , , , and were predicted as the top bioactives of against HUA, which even presented better scores than the positive compound, oestrone 3-sulfate.

DISCUSSION AND CONCLUSIONS

This paper demonstrated the hypouricaemic and nephroprotective effects of in hyperuricemic mice by up-regulating ABCG2. These results may be useful for the development of a hypouricaemic agent.

摘要

背景

FAWolf(多孔菌科)祛湿利尿,具有降尿酸作用。

目的

研究 FAWolf 的降尿酸作用。

材料与方法

采用乙醇提取 FAWolf 菌核得到乙醇提取物(PCE),用水提取剩余物得到水提取物(PCW)。将 PCE 和 PCW(分别为 50、100 和 200mg/kg)灌胃给药于高尿酸血症昆明小鼠(n=8),观察其降尿酸作用。同时进行分子对接。

结果

PCE 可显著降低高尿酸血症(HUA)模型小鼠的血清尿酸水平,分别降至 178±53、153±57 和 151±62μmol/L(P<0.01),PCW 可将模型小鼠的血清尿酸水平分别降至 69±23、63±15 和 62±20μmol/L(P<0.01)。根据 SCrs、BUNs 和 H&E 染色结果,PCE 和 PCW 可部分减轻 HUA 引起的肾功能障碍。它们对 ALT、AST 和 ALP 活性没有不良影响。与 HUA 对照组相比,它们均能提高 ABCG2(ATP 结合盒超家族 G 成员 2)mRNA 和蛋白表达。分子对接结果表明,化合物 、 、 、 和 被预测为 FAWolf 抗 HUA 的潜在生物活性成分,其得分甚至优于阳性对照物雌酮 3-硫酸盐。

讨论与结论

本文通过上调 ABCG2 证实了 FAWolf 对高尿酸血症小鼠的降尿酸和肾保护作用。这些结果可能有助于开发降尿酸药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6ed/7928048/6a5e024ad14c/IPHB_A_1885450_F0001_C.jpg

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