An efficient approach to probe bioactive components of herbal patches by 2D-carbon microfiber fractionation and multi-chamber membrane separation electrophoresis: Spatholobus suberectus Dunn as a case
Lei Yang , Haiyan Cui , Meiyu Cui , Yu Qiu , Miao Shao , Yuwei Zhu , Yonglong Liu , Donatella Nardiello , Maurizio Quinto , Hai-Bo Shang , Huwei Liu , Donghao Li
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引用次数: 0
Abstract
Herbal patches are widely used in clinics for their good curative effects. However, due to the complexity of plant matrices and the extremely low content of transdermal components, the individuation of their effective bioactive compounds represents a challenge: there is then a great need for an efficient method to reveal the bioactive ingredients of herbal patches. In this work, a wide-screening approach is proposed to an individuation of transdermal bioactive components in herbal patches obtained by Spatholobus suberectus Dunn (S. suberectus). Using a two-dimensional microscale carbon fiber/active carbon fiber system combined with a quadrupole time-of-flight high-resolution mass spectrometry (2DµCFs-QTOF-HRMS), a rapid and comprehensive analysis, lasting only 5 min, allowed the identification of 45 distinct polar components within S. suberectus extracts. Among these, 30 components exhibited a transdermal penetration estimated at values higher than 10 %. The key target, predicted by bioinformatics, was prostaglandin-endoperoxide synthase 2 (PTGS2). From the transdermal components of S. suberectus, four potential inhibitors of PTGS2 (protocatechuic acid, isoliquiritigenin, medicarpin, and catechin) were screened by multi-chamber membrane separation electrophoresis (MCMSE). The presence of binding pockets and action sites for medicarpin, isoliquiritigenin, and catechin determines higher binding energy towards PTGS2, with lower IC50 values (12.27, 9.08, and 41.68 μM, respectively). The high-throughput and high-sensitivity analysis by 2DµCFs-QTOF-HRMS, combined with a high-accuracy screening of MCMSE, provides strong technical support for the discovery of trace transdermal bioactive components of herbal patches. The integration of the two technologies could accelerate the study of action mechanisms, quality control, and product improvement of herbal patches.
期刊介绍:
This journal is an international medium directed towards the needs of academic, clinical, government and industrial analysis by publishing original research reports and critical reviews on pharmaceutical and biomedical analysis. It covers the interdisciplinary aspects of analysis in the pharmaceutical, biomedical and clinical sciences, including developments in analytical methodology, instrumentation, computation and interpretation. Submissions on novel applications focusing on drug purity and stability studies, pharmacokinetics, therapeutic monitoring, metabolic profiling; drug-related aspects of analytical biochemistry and forensic toxicology; quality assurance in the pharmaceutical industry are also welcome.
Studies from areas of well established and poorly selective methods, such as UV-VIS spectrophotometry (including derivative and multi-wavelength measurements), basic electroanalytical (potentiometric, polarographic and voltammetric) methods, fluorimetry, flow-injection analysis, etc. are accepted for publication in exceptional cases only, if a unique and substantial advantage over presently known systems is demonstrated. The same applies to the assay of simple drug formulations by any kind of methods and the determination of drugs in biological samples based merely on spiked samples. Drug purity/stability studies should contain information on the structure elucidation of the impurities/degradants.