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KMID : 0811720210250030251
Korean Journal of Physiology & Pharmacology
2021 Volume.25 No. 3 p.251 ~ p.258
Flos magnoliae constituent fargesin has an anti-allergic effect via ORAI1 channel inhibition
Hong Phan Thi Lam

Kim Hyun-Jong
Kim Woo-Kyung
Nam Joo-Hyun
Abstract
Flos magnoliae (FM), the dry flower buds of Magnolia officinalis or its related species, is a traditional herbal medicine commonly used in Asia for symptomatic relief of and treating allergic rhinitis, headache, and sinusitis. Although several studies have reported the effects of FM on store-operated calcium entry (SOCE) via the ORAI1 channel, which is essential during intracellular calcium signaling cascade generation for T cell activation and mast cell degranulation, the effects of its isolated constituents on SOCE remain unidentified. Therefore, we investigated which of the five major constituents of 30% ethanoic FM (vanillic acid, tiliroside, eudesmin, magnolin, and fargesin) inhibit SOCE and their physiological effects on immune cells. The conventional whole-cell patch clamp results showed that fargesin, magnolin, and eudesmin significantly inhibited SOCE and thus human primary CD4+ T lymphocyte proliferation, as well as allergen-induced histamine release in mast cells. Among them, fargesin demonstrated the most potent inhibitory effects not only on ORAI1 (IC50 = 12.46 ¡¾ 1.300 ¥ìM) but also on T-cell proliferation (by 87.74% ¡¾ 1.835%) and mast cell degranulation (by 20.11% ¡¾ 5.366%) at 100 ¥ìM. Our findings suggest that fargesin can be a promising candidate for the development of therapeutic drugs to treat allergic diseases.
KEYWORD
Eudesmin, Fargesin, Mast cell, ORAI, T Lymphocyte
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