Instituto Universitario de Bio-Orgánica "Antonio González", Universidad de La Laguna, 38320, La Laguna, Tenerife, Spain.
Facultad de Ciencias Químicas, Campus UNA, 2169, San Lorenzo, Paraguay.
Naunyn Schmiedebergs Arch Pharmacol. 2018 Jan;391(1):9-16. doi: 10.1007/s00210-017-1432-x. Epub 2017 Oct 23.
Procedures to characterize drugs that can be obtained from plant extracts or combinatorial chemistry are tedious, and they consume considerable resources (e.g., animals) and time. Thus, we have looked for a way to streamline this process. We describe here a novel system for the pre-characterization of drugs based on liquid chromatography coupled to biological detection using perifused or perfused organs. This novel system allows the on-line detection of pharmacologically active substances in hydrosoluble mixtures from vegetal extracts or combinatorial chemistry libraries. Depending on the volume of drug solution and concentration of the samples, the procedure can work through either medium pressure liquid chromatography or HPLC, and it enables the fingerprints of drugs to be assessed based on their contractile activity on combinations of different isolated tissues. As an example, we show how the system can identify active fractions from an extract of Stevia rebaudiana Bertoni, an activity that was later associated with rebaudioside N. Coupling liquid chromatography to biological detection offers a rapid way to focus attention on active products in complex samples, mostly from hydrosoluble species, helping to considerably reduce the time and cost of the pre-characterization of drugs.
从植物提取物或组合化学中获得的药物的特征描述过程繁琐，需要消耗大量资源（如动物）和时间。因此，我们一直在寻找简化该过程的方法。我们在这里描述了一种新的基于液相色谱和生物检测的药物预特征描述系统，该系统使用灌流或灌注器官。这种新系统允许在线检测来自植物提取物或组合化学文库的水溶性混合物中具有药理活性的物质。根据药物溶液的体积和样品的浓度，可以通过中压液相色谱或 HPLC 进行该过程，并且可以根据不同分离组织组合的收缩活性来评估药物的指纹。例如，我们展示了该系统如何识别甜菊叶提取物中的活性部分，这种活性后来与甜菊苷 N 相关联。将液相色谱与生物检测相结合，为关注复杂样品（主要是水溶性物种）中的活性产物提供了一种快速方法，有助于大大缩短药物预特征描述的时间和成本。
