钟剑锋 谢宇宝 蔡汇明 何家豪 杨咏祺 陈晓珺 崔明筠 朱钦昌 付开聪 贺震旦

【摘 要】 目的：秦盾祛痛风胶囊（TFCAP）是哈尼族降尿酸民族药制剂，已在当地中医院用于痛风的治疗，极具潜力和应用前景，但缺乏现代科学证据及机制研究。本研究检测该药的黄嘌呤氧化酶抑制活性和细胞毒性，对其降尿酸机理进行初步探讨，为其应用提供实验支撑和依据。方法：用纯水和乙醇分别提取TFCAP，利用紫外分光光度法建立黄嘌呤氧化酶活性评价模型，检测TFCAP水提物和醇提物及成分标准品降尿酸活性;使用cck8试剂检测该药对不同细胞株的细胞毒性;对醇提物进行HPLC分析。结果：TFCAP水提物的黄嘌呤氧化酶抑制作用较低;TFCAP醇提物对黄嘌呤氧化酶的IC50为（338.3±50.9） μg/mL，对实验所用不同细胞CC50在1.3～2.2 mg/mL之间;建立了醇提物的HPLC指纹图谱。结论：TFCAP醇提物具有良好的黄嘌呤氧化酶抑制活性，是其临床发挥降尿酸作用的可能机制之一，且体外细胞毒性较小，安全性良好。

【关键词】 痛风;哈尼族;黄嘌呤氧化酶;细胞毒性

【中图分类号】R285.5 【文献标志码】 A 【文章编号】1007-8517（2021）13-0033-06

Abstract：Objective Qindunqutongfeng Capsule （TFCAP） is a traditional medicine derived from Hani nationality using for urate-lowering therapy. It has been used in the treatment of gout in the local Chinese medicine hospital. Although with great application prospects in urate-lowering therapy，TFCAP lacks modern scientific evidence and mechanism research. To provide experimental support for the application of TFCAP，this study examines the xanthine oxidase inhibitory activity and cytotoxicity of TFCAP，and preliminarily investigates its mechanism. Methods TFCAP was extracted with pure water and ethanol respectively，and in vitro xanthine oxidase activity evaluation model was applied by using UV spectrophotometry to evaluate the xanthine oxidase inhibitory activity of TFCAP water and ethanol extract; CCK-8 reagent was used to detect the cytotoxicity of TFCAP ethanol extract and component standards on several cell lines; the fingerprint chromatography of TFCAP was determined by HPLC.Result The inhibitory effect of TFCAP water extract on xanthine oxidase is low; The IC50 of the ethanol extract of TFCAP on xanthine oxidase is （338.3±50.9） μg/mL，the CC50 on different cells used in the experiment is between 1.3～2.2 mg/mL; the fingerprint chromatography for ethanol extract of TFCAP was well established. Conclusion TFCAP ethanol extract has low cytotoxicity，and possesses inhibitory activity against xanthine oxidase，which may be one of the possible mechanisms for its urate-lowering effect.

Keywords：Gout; Hani nationality;Xanthine oxidase;Cytotoxicity

痛風是常见多发的代谢性风湿病，我国痛风发病率约为1%～3%[1]，痛风临床表现为高尿酸血症，常与多种疾病伴发，严重者易导致肾衰竭危及生命[2]。尿酸由黄嘌呤氧化酶催化黄嘌呤生成 [3]，尿酸催化生成过程中还会产生大量超氧阴离子和过氧化氢等自由基，与细胞损伤、炎症等密切相关[4]。因此，抑制黄嘌呤氧化酶的活性是痛风药物研究的一个重要靶点。临床常见的黄嘌呤氧化酶抑制剂主要有别嘌呤醇和非布索坦，但都伴有严重的副作用[5-6]，寻找毒副作用小的中药活性成分具有重要的意义和研究前景。……