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成分法尔吉辛具有抗组胺作用,可抑制ORAI1通道。

constituent fargesin has an anti-allergic effect ORAI1 channel inhibition.

作者信息

Hong Phan Thi Lam, Kim Hyun Jong, Kim Woo Kyung, Nam Joo Hyun

机构信息

Department of Physiology, Dongguk University College of Medicine, Gyeongju 38066, Korea.

Channelopathy Research Center (CRC), Dongguk University College of Medicine, Goyang 10326, Korea.

出版信息

Korean J Physiol Pharmacol. 2021 May 1;25(3):251-258. doi: 10.4196/kjpp.2021.25.3.251.

Abstract

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.

摘要

辛夷(FM),即玉兰或其近缘种的干燥花蕾,是一种传统草药,在亚洲常用于缓解症状以及治疗过敏性鼻炎、头痛和鼻窦炎。尽管多项研究报道了FM对储存性钙内流(SOCE)及ORAI1通道的影响,而ORAI1通道在T细胞活化和肥大细胞脱颗粒的细胞内钙信号级联产生过程中至关重要,但其分离成分对SOCE的影响仍不明确。因此,我们研究了30%乙醇提取物FM的五种主要成分(香草酸、椴树苷、桉油素、木兰脂素和辛夷脂素)中哪些会抑制SOCE及其对免疫细胞的生理作用。传统的全细胞膜片钳结果显示,辛夷脂素、木兰脂素和桉油素显著抑制SOCE,从而抑制人原代CD4 T淋巴细胞增殖以及肥大细胞中过敏原诱导的组胺释放。其中,辛夷脂素在100 μM时不仅对ORAI1表现出最有效的抑制作用(IC = 12.46 ± 1.300 μM),而且对T细胞增殖(抑制87.74% ± 1.835%)和肥大细胞脱颗粒(抑制20.11% ± 5.3,66%)也有显著抑制作用。我们的研究结果表明,辛夷脂素有望成为开发治疗过敏性疾病药物的候选药物。

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