Open AccessDiscovery and analysis the anti‐pseudo‐allergic components from Perilla frutescens leaves by overexpressed MRGPRX2 cell membrane chromatography coupled with HPLC‐ESI‐IT‐TOF system
Author(s) -
Yang Liu,
Zeng Yingnan,
Wang Jue,
Zhang Yongjing,
Hou Yajing,
Qin Qiaohong,
Ma Weina,
Wang Nan
Publication year - 2020
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1111/jphp.13246
Subject(s) - perilla frutescens , degranulation , rosmarinic acid , mast cell , high performance liquid chromatography , chemistry , chromatography , receptor , pharmacology , biochemistry , biology , immunology , antioxidant
Objectives Screen and identify the anti‐pseudo‐allergic activity components of Perilla frutescens leaves that interacted with MRGPRX2 (a new reported pseudo‐allergic reaction‐related receptor). Methods An overexpressed MRGPRX2 cell membrane chromatography (CMC) coupled with HPLC‐ESI‐IT‐TOF system has been established to screen and identify the effective components from P. frutescens leaves. A frontal analysis method was performed to investigate the binding affinity between ligands and MRGPRX2. Their activity of relieving pseudo‐allergic reaction was evaluated in vitro by histamine release assay, β‐hexosaminidase release assay and intracellular Ca 2+ mobilization assay. Key findings Extract of P. frutescens leaves was proved to be effective in anti‐pseudo‐allergic reaction by inhibiting MRGPRX2. Apigenin (API) and rosmarinic acid (ROS) were confirmed to be the potential anti‐allergy compounds that could bind with MRGPRX2. The binding affinity ( K D ) of ROS and API with MRGPRX2 was (8.79 ± 0.13) × 10 −8 m and (6.54 ± 1.69) × 10 −8 m , respectively. The IC 50 of API inhibiting laboratory of allergic disease 2 cells degranulation was also determined to be (51.96 ± 0.18) μ m . Conclusions A MRGPRX2/CMC coupled with HPLC‐ESI‐IT‐TOF system was successfully established and applied to discover the effective components from P. frutescens leaves.