苦参
阿司咪唑
药理学
化学
刮伤
氧化苦参碱
组胺
医学
色谱法
声学
物理
苦参碱
作者
Zhe Zhang,Jianhao Pan,Tao Zhu,Nathalie M. Malewicz,Kaihe Ye,Jianhui Rong,Yong Ming Luo,Yongli Situ,Alexei Verkhratsky,Yong Wang,Jianhao Zhao,Dan Tang,Hong Nie
摘要
Abstract Objectives This study aimed to discover the active compounds of Sophora flavescens Ait. (SF), the anti-itch effects and underlying mechanisms of oxymatrine (OMT), one of the bioactive compounds from SF. Methods Dorsal root ganglion cell membrane immobilized chromatography was used to screen potential anti-pruritic active compounds from SF. The scratching behaviour was analysed to systematically study the anti-pruritic effects of OMT in chloroquine- (CQ), peptide Ser–Leu–Ile–Gly–Arg–Leu- (SLIGRL), histamine- (HIS) and allyl-isothiocyanate-(AITC)-induced itch mice models. Real-time quantitative PCR, in-vivo study and molecular docking were employed to explore the underlying mechanisms. Key findings All in all, 21 compounds of SF were identified and 5 potential bioactive compounds were discovered. OMT significantly reduced scratching bouts in two HIS-independent itch models induced by CQ and SLIGRL but was not effective in the HIS-induced itch model. OMT reduced scratching bouts in a dose-dependent manner and decreased the messenger RNA (mRNA) expression of transient receptor potential ankyrin 1 (TRPA1) channel in two HIS-independent itch models; in addition, OMT reduced the wipes and scratching bouts induced by AITC. Conclusions This study discovered five potential anti-pruritic compounds including OMT in the SF extract, and OMT has strong anti-pruritic effects in HIS-independent itch via TRPA1 channel.
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