Abstract

Microorganisms and plants can be important sources of many compounds with potential pharmaceutical applications. Extraction of these matrices is one of the ways of identifying the presence of inhibitory active substances against enzymes whose high activity leads to serious human diseases including cancer, Parkinson's or Crohn's diseases. The isolation and purification of inhibitors are time-consuming and expensive steps in the analysis of the crude extract and therefore, it is necessary to find a fast, efficient, and inexpensive method for screening extracts of interest. TLC-Bioautography combines the separation of the extract on a thin layer with its subsequent biological analysis. TLC-Bioautography methods have been developed for several classes of enzymes including oxidoreductases, hydrolases and isomerases, and there is a potential for developing functional methods for other classes of enzymes. This review summarizes known TLC-Bioautography methods and their applications for determining the presence of enzyme inhibitors in extracts and compares the effectiveness of different methodological approaches. It also indicates the current state and perspective of the development of TLC-Bioautography and its possible future applications.

摘要

微生物和植物可能是许多具有潜在药物应用的化合物的重要来源。提取这些基质是识别酶的抑制活性物质存在的方法之一，这些酶的高活性会导致严重的人类疾病，包括癌症、帕金森病或克罗恩病。抑制剂的分离和纯化是粗提物分析中耗时且昂贵的步骤，因此，有必要找到一种快速、有效且廉价的方法来筛选感兴趣的提取物。TLC-Bioautography 将提取物在薄层上的分离与随后的生物分析相结合。TLC-Bioautography 方法已开发用于几类酶，包括氧化还原酶、水解酶和异构酶，并且有可能为其他类别的酶开发功能方法。本综述总结了已知的 TLC-Bioautography 方法及其在确定提取物中酶抑制剂存在方面的应用，并比较了不同方法的有效性。它还表明了 TLC-Bioautography 的发展现状和前景及其未来可能的应用。