Flos magnoliae constituent fargesin has an anti-allergic effect via ORAI1 channel inhibition

• Published in: The Korean journal of physiology & pharmacology Vol. 25; no. 3; pp. 251 - 258
• Main Authors: Hong, Phan Thi Lam, Kim, Hyun Jong, Kim, Woo Kyung, Nam, Joo Hyun
• Format: Journal Article
• Language: English
• Published: Korea (South) The Korean Physiological Society and The Korean Society of Pharmacology 01.05.2021; 대한약리학회
• Subjects: Original; 약리학; Fargesin; T Lymphocyte; Mast cell; Eudesmin; ORAI
• ISSN: 1226-4512; 2093-3827; 2093-3827
• DOI: 10.4196/kjpp.2021.25.3.251

magnoliae (FM), the dry flower buds of 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) 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 (IC = 12.46 ± 1.300 µM) but also on T-cell proliferation (by 87.74% ± 1.835%) and mast cell degranulation (by 20.11% ± 5.366%) at 100 µM. Our findings suggest that fargesin can be a promising candidate for the development of therapeutic drugs to treat allergic diseases.