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Mast cells are immune effector cells mediating allergic inflammation by the secretion of inflammatory mediators such as histamine and pro-inflammatory cytokines. Orientin is a naturally occurring bioactive flavonoid that possesses diverse biological properties, including anti-inflammation, anti-oxidative, anti-tumor, and cardio protection. The objective of this study was to rule out the effectiveness of orientin in mast cell-mediated allergic inflammation. In this study, in vitro effects of orientin were evaluated in RBL-2H3, mouse bone marrow-derived mast cells, rat peritoneal mast cells, and in vivo effects were evaluated by inducing passive cutaneous anaphylaxis (PCA) in Imprinting Control Region (ICR) mice. Findings show that orientin suppressed the immunoglobulin E (IgE)-mediated mast cell degranulation by reducing intracellular calcium level in a concentration-dependent manner. Orientin suppressed the secretion of pro-inflammatory cytokines in mast cells. This inhibitory effects of orientin was through inhibition of FcεRI-mediated signaling proteins. In addition, oral administration of orientin suppressed the IgE-mediated PCA reactions in a dose-dependent manner, which was evidenced by reduced Evan's blue pigmentation and ear swelling. Based on these findings, we suggest that orientin might have potential to alleviate allergic reaction and mast cell-mediated allergic disease.


Hima Dhakal, Soyoung Lee, Jin Kyeong Choi, Taeg Kyu Kwon, Dongwoo Khang, Sang-Hyun Kim. Inhibitory effects of orientin in mast cell-mediated allergic inflammation. Pharmacological reports : PR. 2020 Aug;72(4):1002-1010

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PMID: 32048267

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