Screening and separation of natural anticancer active ingredients related to phospholipase C

IF 2.8 3区 工程技术 Q2 CHEMISTRY, ANALYTICAL
Na Liu, Zili Yue, Shuang Hu, Rongrong Xing, Runqin Wang, Li Yang, Xuan Chen
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Abstract

Based on the specific binding of drug molecules to cell membrane receptors, a screening and separation method for active compounds of natural products was established by combining phospholipase C (PLC) sensitized hollow fiber microscreening by a solvent seal with high-performance liquid chromatography technology. In the process, the factors affecting the screening were optimized. Under the optimal screening conditions, we screened honokiol (HK), magnolol (MG), negative control drug carbamazepine, and positive control drug amentoflavone, the repeatability of the method was tested. The PLC activity was determined before and after the screening. Experimental results showed that the sensitization factors of PLC of HK and MG were 61.0 and 48.5, respectively, and amentoflavone was 15.0, carbamazepine could not bind to PLC. Moreover, the molecular docking results were consistent with this measurement, indicating that HK and MG could be combined with PLC, and they were potential interacting components with PLC. This method used organic solvent to seal the PLC greatly ensuring the activity, so this method had the advantage of integrating separation, and purification with screening, it not only exhibited good reproducibility and high sensitivity but was also suitable for screening the active components in natural products by various targets in vitro.

筛选和分离与磷脂酶 C 有关的天然抗癌活性成分。
基于药物分子与细胞膜受体的特异性结合,将溶剂密封的磷脂酶 C(PLC)敏化中空纤维微筛技术与高效液相色谱技术相结合,建立了一种天然产物活性化合物的筛选和分离方法。在此过程中,对影响筛选的因素进行了优化。在优化的筛选条件下,我们筛选了本诺可醇(HK)、木兰醇(MG)、阴性对照药卡马西平和阳性对照药门冬酰胺黄酮,并测试了该方法的重复性。在筛选前后测定了 PLC 活性。实验结果表明,HK和MG对PLC的敏化系数分别为61.0和48.5,门黄酮为15.0,卡马西平不能与PLC结合。此外,分子对接结果与该测定结果一致,表明HK和MG可与PLC结合,是PLC的潜在相互作用成分。该方法采用有机溶剂封闭PLC,极大地保证了PLC的活性,具有集分离、纯化和筛选于一体的优点,不仅重现性好、灵敏度高,而且适用于体外多靶点筛选天然产物中的活性成分。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Journal of separation science
Journal of separation science 化学-分析化学
CiteScore
6.30
自引率
16.10%
发文量
408
审稿时长
1.8 months
期刊介绍: The Journal of Separation Science (JSS) is the most comprehensive source in separation science, since it covers all areas of chromatographic and electrophoretic separation methods in theory and practice, both in the analytical and in the preparative mode, solid phase extraction, sample preparation, and related techniques. Manuscripts on methodological or instrumental developments, including detection aspects, in particular mass spectrometry, as well as on innovative applications will also be published. Manuscripts on hyphenation, automation, and miniaturization are particularly welcome. Pre- and post-separation facets of a total analysis may be covered as well as the underlying logic of the development or application of a method.
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