Fast Screening of Biomembrane-Permeable Compounds in Herbal Medicines Using Bubble-Generating Magnetic Liposomes Coupled with LC–MS

Xiaoting Gu,Dongwu Wang,Youping Liu,Xin Di,Xin Wang

doi:10.3390/molecules26061742

Abstract

A novel strategy based on the use of bionic membrane camouflaged magnetic particles and LC–MS was developed to quickly screen the biomembrane-permeable compounds in herbal medicines. The bionic membrane was constructed by bubble-generating magnetic liposomes loaded with NH4HCO3 (BMLs). The lipid bilayer structure of the liposomes enabled BMLs to capture biomembrane-permeable compounds from a herbal extract. The BMLs carrying the compounds were then separated from the extract by a magnetic field. Upon heat treatment, NH4HCO3 rapidly decomposed to form CO2 bubbles within the liposomal bilayer, and the captured compounds were released from BMLs and analyzed by LC–MS. Jinlingzi San (JLZS), which contains various natural ingredients, was chosen to assess the feasibility of the proposed method. As a result, nine potential permeable compounds captured by BMLs were identified for the first time. Moreover, an in vivo animal study found that most of the compounds screened out by the proposed method were absorbed into the blood. The study provides a powerful tool for rapid and simultaneous prediction of multiple biomembrane-permeable components.

Highlights

Chinese herbal medicines have been deemed as a momentous combinatorial chemical library of therapeutic agents [1]
This study presents a novel screening strategy based on bubble-generating magnetic liposomes (BMLs) to screen the potential biomembranepermeable components from herbal medicines
Inspired by the above research, we developed a strategy based on BMLs that integrated features of capturing fat-soluble compounds into the lipid layer, magnetic separation from impurities by a magnetic field, and thermo-responsive controlled release of captured compounds to quickly screen the biomembrane-permeable compounds in herbal medicines

Summary

Introduction

Chinese herbal medicines have been deemed as a momentous combinatorial chemical library of therapeutic agents [1]. The routine procedure of screening bioactive compounds from herbal medicines is to extract and isolate complex mixtures and to evaluate the pharmacological activities of the individual compounds in vivo or in vitro [2]. This screening method is expensive and time consuming, with no consideration of the synergistic action of the multiple components in herbal medicines. Developing a more suitable method for rapid screening of active ingredients is helpful for the application of herbal medicines and the discovery of lead compounds. This study presents a novel screening strategy based on bubble-generating magnetic liposomes (BMLs) to screen the potential biomembranepermeable components from herbal medicines

Methods

Results

Conclusion