Development of Endogenous Cannabinoid Receptor Modulating Compounds As Anti-inflammatory Cosmeceutical Agents
분야
의약학 > 해부학
저자
( Bong Woo Kim ) , ( Bu Mahn Park ) , ( Jeong Eun Jeon ) , ( Hyun Jung Kim ) , ( Sung Ku Ahn ) , ( Seung Phil Hong ) , ( Se Kyoo Jeong )
발행기관
한국피부장벽학회
간행물정보
한국피부장벽학회지 2012년, 제14권 제2호, 72~79쪽(총8쪽)
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1j700326.pdf [무료 PDF 뷰어 다운로드]
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    영문초록
    Many inflammatory mediators, including histamine, inflammatory proteases, arachidonic acid metabolites and cytokines are released by mast cell activation. However, little is known about the endogenous modulators for mast cell activation and their mechanism. Endogenous cannabinoids found in peripheral tissues, such as palmitoylethanolamide (PEA), have been proposed as having autacoid activity, which can down-regulate mast cell activation and local inflammation. Based on the chemical structure of agonists and antagonists, 30 compounds were synthesized and their modulating activity on human cannabinoid receptor 1 (CB1R) and 2 (CB2R) were tested using CB1R or CB2R transfected CHO cell line, respectively. Among the tested compounds, a few potential CB1R agonists were screened and further investigated on mast cell activation model. Using a cultured rat mast cell line, effect of selected compounds on Fcε RI-induced histamine and β-hexosaminidase release were measured. As a result, newly synthesized CB1R agonists down-regulated the release of histamine by IgE activation in mast cells, Furthermore, inhibitory effect on histamine release was also observed in mast cells activated by protease-activated receptor (PAR)-2 agonists. Taken together, CB1R agonists can down-regulate the mast cell activation, and might be a used for relieving inflammatory symptoms mediated by mast cell activation, such as atopic dermatitis, psoriasis, contact dermatitis or chronic urticarial.
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