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首页> 外文期刊>Biomedical Chromatography: An International Journal Devoted to Research in Chromatographic Methodologies and Their Applications in the Biosciences >A rapid assay to screen adenosine deaminase inhibitors from Ligustri Lucidi Fructus against metabolism of cordycepin utilizing ultra‐high‐performance liquid chromatography–tandem mass spectrometry
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A rapid assay to screen adenosine deaminase inhibitors from Ligustri Lucidi Fructus against metabolism of cordycepin utilizing ultra‐high‐performance liquid chromatography–tandem mass spectrometry

机译：利用超高效液相色谱 - 串联质谱法从Ligustri Lucidi植物筛选腺苷脱氨酶抑制剂的快速试验。利用超高效液相色谱 - 串联质谱法

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Abstract Cordycepin has recently received increased attention owing to its extensive pharmacological activity. Adenosine deaminase (ADA) is widely distributed in mammalian blood and tissues; as a result, cordycepin is quickly metabolized upon entering into the body and converted into the inactive metabolite 3′‐deoxyinosine, thus limiting its activity when administered alone. We herein present a novel ultra‐high‐performance liquid chromatography–tandem mass spectrometry (UHPLC–MS/MS) method for screening ADA inhibitors against the metabolism of cordycepin. Cordycepin and 3′‐deoxyinosine were chosen as substrate and product, respectively. A proper separation was achieved for all analytes within 3?min. 3′‐Deoxyinosine was quantified in the presence or absence of potential ADA inhibitors to evaluate ADA activity. The assay can simultaneously determine substrate and product, with the endogenous substance and ADA inhibitors added not interfering in its activity. After optimizing the enzymatic incubation and UHPLC–MS/MS conditions, K m and V max values for ADA deamination of cordycepin were 95.18?±?7.85?μ m and 363.90?±?12.16?μmol/min/unit, respectively. Oleanolic acid and ursolic acid from Ligustri Lucidi Fructus were chosen as ADA inhibitors with half maximal inhibitory concentration values of 21.82?±?0.39 and 18.41?±?0.14 μ m , respectively. A non‐competitive inhibition model was constructed and this assay can be used to screen other potential ADA inhibitors quickly and accurately.
机译：摘要冬虫夏素最近受到其广泛的药理学活动的增加。腺苷脱氨酶（ADA）广泛分布在哺乳动物血液和组织中;结果，在进入体内迅速地代谢并转化成活性代谢物3'-脱氧糖苷，因此在单独施用时限制其活性。我们本文提出了一种新型超高效液相色谱 - 串联质谱（UHPLC-MS / MS）方法，用于筛选ADA抑制剂免受冬虫夏素的代谢。选择冬虫夏蛋白和3'-脱氧苷分别作为底物和产物。在3？min内的所有分析物中达到了适当的分离。在存在或不存在潜在的ADA抑制剂中量化3'-脱氧苷，以评估ADA活性。测定可以同时测定底物和产品，内源性物质和ADA抑制剂在其活性中添加不干扰。优化酶促培养和UHPLC-MS / MS条件后，冬虫氏蛋白萜素的ADA脱胺的K m和v Max值分别为95.18Ω·α±7.85Ω·ηm和363.90？±12.16Ω·μmol/ min /单位。选择来自Ligustri Lucidi果肉的葡聚糖酸和尿酸酸作为ADA抑制剂，半最大抑制浓度值为21.82≤0.39和18.41？±0.14μm。构建了非竞争性抑制模型，该测定可用于快速准确地筛选其他潜在的ADA抑制剂。

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