Gainche Maël, Ogeron Clémence, Ripoche Isabelle, Senejoux François, Cholet Juliette, Decombat Caroline, Delort Laetitia, Berthon Jean-Yves, Saunier Etienne, Caldefie Chezet Florence, Chalard Pierre
Clermont Auvergne INP, Université Clermont Auvergne, CNRS, ICCF, F-63000 Clermont-Ferrand, France.
Université Clermont-Auvergne, INRA, UNH, Unité de Nutrition Humaine, CRNH Auvergne, F-63000 Clermont-Ferrand, France.
Molecules. 2021 Mar 30;26(7):1939. doi: 10.3390/molecules26071939.
is a plant commonly used for the treatment of several pathologies, such as diarrhoea, ulcers, pain, stomach aches, fevers, and gout. Our study focused on the use of for the treatment of gout disease. We first studied the chemical composition of a methanolic extract of the aerial parts and demonstrated its xanthine oxidase (XO) inhibitory activity. Then, we performed a fractionation and evaluated the most XO inhibitory active fractions by UV measurement. Purification of some fractions allowed the determination of the inhibitory activity of pure compounds. We demonstrated that spiraeoside, a glycosylated flavonoid, possesses an activity around 25 times higher than allopurinol, used as a reference in the treatment of gout disease. In order to easily and quickly identify potent inhibitors in complex matrix, we developed a complementary strategy based on an HPLC method and an Effect Directed Assay (EDA) method combining HPTLC and biochemical assays. The HPLC method, capable of determining compounds exhibiting interactions with the enzyme, could be an efficient strategy for evaluating potent enzyme inhibitors in a complex mixture. This strategy could be applied for quantitative assays using LC/MS experiments.
是一种常用于治疗多种病症的植物，如腹泻、溃疡、疼痛、胃痛、发烧和痛风。我们的研究聚焦于其用于治疗痛风疾病。我们首先研究了地上部分甲醇提取物的化学成分，并证明了其黄嘌呤氧化酶（XO）抑制活性。然后，我们进行了分馏，并通过紫外测量评估了XO抑制活性最强的部分。对一些部分的纯化使得能够确定纯化合物的抑制活性。我们证明了绣线菊苷，一种糖基化黄酮，其活性比用作痛风疾病治疗参考的别嘌呤醇高约25倍。为了在复杂基质中轻松快速地鉴定强效抑制剂，我们基于一种HPLC方法和一种将HPTLC与生化分析相结合的效应导向分析（EDA）方法开发了一种互补策略。能够确定与酶有相互作用的化合物的HPLC方法，可能是评估复杂混合物中强效酶抑制剂的有效策略。该策略可应用于使用LC/MS实验的定量分析。
