壮药赤苍藤防治高尿酸血症和痛风的药效物质基础和作用机制研究

In recent years, hyperuricemia and gout have gradually become a common and frequently occurring disease that seriously threatens people's health. Nowadays, clinical drugs of treat hyperuricemia and gout have certain toxic and side effects. Erythropalum scandens Bl. is a Olacaceae plant, it is widely used to treat hyperuricemia, gout, arthritis, urethritis and kidney stone by Zhuang people. It's twigs can be eaten. It is a highly development value medicinal and edible plants. Our research team has experimentally confirmed that the extract of Erythropalum scandens decrease the level of serum uric acid by inhibiting xanthine oxidase, so as to achieve the effect of treatment of hyperuricemia, the effect is superior to allopurinol. In order to develop Erythropalum scandens better, the chemical constituents were isolated and identified by chromatographic analysis and spectral analysis.After chemical constituents fingerprints of Erythropalum scandens were established and the blood components of Erythropalum scandens was analyzed by the method of UHPLC-Q-TOF/MS. Based on this, the main active components of Erythropalum scandens and potential target groups were predicted by network pharmacology method, then confirmed by animal pharmacological experiments to reveal effective substantive basis and molecular mechanism of Erythropalum scandens to treat hyperuricemia and gout.This study will provide a theoretical basis for further clinical application of Erythropalum scandens.

近年来，高尿酸血症和痛风已逐渐成为严重威胁人们健康的常见多发病，目前治疗的药物以具有一定毒副作用的西药为主。壮药赤苍藤（Erythropalum scandens Bl.）为铁青树科植物，壮族人们将其广泛用于治疗高尿酸血症、痛风、关节炎、尿道炎、肾结石等症，具有较好疗效；其嫩枝可以食用，是具有极高开发价值的药食同源植物。本研究小组已实验证实赤苍藤提取物通过抑制嘌呤氧化酶降低血尿酸的形成，从而达到治疗高尿酸血症的作用，效果优于别嘌呤醇。为了更好地开发壮药赤苍藤，本研究采用色谱分析法和光谱分析法分离鉴定赤苍藤的化学成分，采用UHPLC-Q-TOF/MS技术建立其指纹图谱和分析其入血成分，在此基础上采用网络药理学方法筛选赤苍藤治疗高尿酸血症和痛风的主要活性成分群和潜在靶标群，并通过动物药理实验进一步验证，揭示赤苍藤治疗高尿酸血症和痛风的药效物质基础和作用机制，为赤苍藤进一步临床应用奠定理论基础。

近年来，高尿酸血症和痛风已逐渐成为严重威胁人们健康的常见多发病，目前治疗的药物以具有一定毒副作用的西药为主。壮药赤苍藤（Erythropalum scandens Bl.）.为铁青树科植物，壮族人们将其广泛用于治疗高尿酸血症、痛风、关节炎、尿道炎、肾结石等症，具有较好疗效；其嫩枝可以食用，是具有极高开发价值的药食同源植物。项目前期实验证实赤苍藤提取物通过抑制嘌呤氧化酶降低血尿酸的形成，从而达到治疗高尿酸血症的作用，效果优于别嘌呤醇。本项目采用电感耦合等离子体质谱法检测赤苍藤茎中元素的含量，采用色谱分析法分离纯化出15种化合物，并运用质谱和核磁共振等光谱学方法确定10种化合物，其中1种为新化合物，7种化合物首次从该植物中得到，初步确定其中4种化合物入血。通过体内外活性实验，以及分子对接方法，初步确定赤苍藤治疗高尿酸血症和痛风的药效物质基础为糖苷类化化合物、生物碱类化合物和多糖，其作用机制是抑制XOD的酶的活性，上调OAT1和下调URAT1和GLUT9，抑制尿酸的生成和重吸收，促进尿酸排放。并在此基础上建立赤苍藤颗粒的制备工艺，发现赤苍藤具有保护肝脏和心血管内皮的活性，为赤苍藤作为新资源提供理论基础，为临床应用提供了实验依据。项目共发表论文3篇，申请专利2项，专利授权1项，科技成果登记1项。