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用于痛风性关节炎的蜘蛛香药理学基础:其提取物、馏分和成分的抗高尿酸血症和抗炎作用。

Pharmacological basis for use of Lychnophora trichocarpha in gouty arthritis: anti-hyperuricemic and anti-inflammatory effects of its extract, fraction and constituents.

机构信息

Laboratório de Plantas Medicinais, Escola de Farmácia, Universidade Federal de Ouro Preto, Ouro Preto, Minas Gerais 35400-000, Brazil.

出版信息

J Ethnopharmacol. 2012 Aug 1;142(3):845-50. doi: 10.1016/j.jep.2012.06.012. Epub 2012 Jun 23.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

The ethanolic extract of Lychnophora trichocarpha Spreng. is used in Brazilian folk medicine to treat bruise, pain and inflammatory diseases.

AIM OF THE STUDY

The present study aimed at investigating whether ethanolic extract of L. trichocarpha, its ethyl acetate fraction and its main bioactive compounds could be useful to treat gouty arthritis by countering hyperuricemia and inflammation.

MATERIALS AND METHODS

L. trichocarpha ethanolic extract (LTE), ethyl acetate fraction from ethanolic extract (LTA) and isolated compounds were evaluated for urate-lowering activity and liver xanthine oxidase (XOD) inhibition in oxonate-induced hyperuricemic mice. Anti-inflammatory activity in monosodium urate crystal-induced paw oedema, an experimental model of gouty arthritis, was also investigated.

RESULTS

Crude ethanolic extract and its ethyl acetate fraction showed significant urate-lowering effects. LTE was also able to significantly inhibit liver xantine oxidase (XOD) activity in vivo at the dose of 250mg/kg. Luteolin, apigenin, lupeol, lychnopholide and eremantholide C showed the anti-hyperuricemic activities among tested compounds. Apigenin also showed XOD inhibitory activity in vivo. Luteolin, lychnopholide, lupeol and eremantholide C, in turn, did not shown significant inhibitory activity towards this enzyme, indicating that this mechanism is not likely to be involved in urate-lowering effects of those compounds. LTE, LTA, lupeol, β-sitosterol, lychnopholide, eremantholide, luteolin and apigenin were also found to inhibit monosodium urate crystals-induced paw oedema in mice.

CONCLUSIONS

Ethanolic extract of Lychnophora trichocarpha and some of its bioactive compounds may be promising agents for the treatment of gouty arthritis since they possesses both anti-hiperuricemic and anti-inflammatory properties.

摘要

民族药理学相关性

巴西民间医学用 Lychnophora trichocarpha Spreng 的乙醇提取物治疗瘀伤、疼痛和炎症性疾病。

研究目的

本研究旨在探讨 Lychnophora trichocarpha 的乙醇提取物、其乙酸乙酯部分及其主要生物活性化合物是否可通过对抗高尿酸血症和炎症来治疗痛风性关节炎。

材料和方法

评估 Lychnophora trichocarpha 乙醇提取物(LTE)、乙醇提取物的乙酸乙酯部分(LTA)和分离化合物对黄嘌呤氧化酶(XOD)在氧嗪酸钾诱导的高尿酸血症小鼠中的尿酸降低活性和肝抑制作用。还研究了在单钠尿酸盐晶体诱导的爪肿胀(痛风性关节炎的实验模型)中的抗炎活性。

结果

粗乙醇提取物及其乙酸乙酯部分显示出显著的降尿酸作用。LTE 还能够在 250mg/kg 剂量下显著抑制体内黄嘌呤氧化酶(XOD)的活性。木樨草素、芹菜素、羽扇豆醇、lychnopholide 和 eremantholide C 是在所测试的化合物中表现出抗高尿酸血症活性的化合物。芹菜素在体内也表现出 XOD 抑制活性。木樨草素、lychnopholide、羽扇豆醇和 eremantholide C 则对这种酶没有显示出显著的抑制活性,表明这种机制不太可能参与这些化合物的降尿酸作用。LTE、LTA、羽扇豆醇、β-谷甾醇、lychnopholide、eremantholide、木樨草素和芹菜素也被发现可抑制单钠尿酸盐晶体诱导的小鼠爪肿胀。

结论

Lychnophora trichocarpha 的乙醇提取物及其一些生物活性化合物可能是治疗痛风性关节炎的有前途的药物,因为它们具有抗高尿酸血症和抗炎作用。

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