Trigonelline, one of the alkaloids contained in coffee, is important not only as one of the constituents of aroma and flavor in coffee but also as a useful source of nutrition. Its anti-microbial, anti-carcinogenic, and anti-hyperglycemic effects have been investigated in previous studies. However, there have not been any studies examining the anti-degranulation effect of trigonelline. In this study, the anti-degranulation effect of trigonelline was evaluated in in vitro and in vivo models using a rat basophilic leukemia cell line, RBL-2H3 cells, and a passive cutaneous anaphylaxis (PCA) reaction in mice, respectively. In the β-hexosaminidase release assay, trigonelline effectively suppressed antigen-induced degranulation of RBL-2H3 cells in a dose-dependent manner without cytotoxicity. Trigonelline also inhibited FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3 K, and Akt, in antigen-stimulated RBL-2H3 cells and suppressed the PCA response in mice. Moreover, trigonelline also inhibited the microtubule formation in RBL-2H3 cells, indicating that trigonelline could inhibit IgE-sensitized mast cell degranulation by attenuating both the intracellular calcium-dependent and independent pathways. These results revealed that trigonelline possesses the anti-degranulation effect against the development of allergic diseases.

中文翻译：

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Trigonelline：具有抗脱粒特性的生物碱。

Trigonelline是咖啡中所含的一种生物碱，不仅作为咖啡香气和风味的组成成分之一，而且作为营养的有用来源也很重要。在先前的研究中已经研究了其抗微生物，抗癌和抗高血糖的作用。但是，尚未有任何研究检查trigonelline的抗脱粒作用。在这项研究中，分别使用大鼠嗜碱性粒细胞白血病细胞系，RBL-2H3细胞和小鼠被动皮肤过敏反应（PCA）在体外和体内模型中评估了Trigonelline的抗脱颗粒作用。在β-己糖胺酶释放试验中，曲古萘林以剂量依赖性方式有效抑制抗原诱导的RBL-2H3细胞脱粒，而无细胞毒性。Trigonelline还抑制了抗原刺激的RBL-2H3细胞中FcεRI介导的细胞内信号通路，例如PLCγ1，PI3 K和Akt的磷酸化，并抑制了小鼠的PCA反应。此外，曲安奈林还抑制RBL-2H3细胞中的微管形成，表明曲安奈林可通过减弱细胞内钙依赖性和独立途径来抑制IgE敏感的肥大细胞脱粒。这些结果表明，三氯萘林对变应性疾病的发展具有抗脱粒作用。提示trigonelline可通过减弱细胞内钙依赖性和非依赖性途径来抑制IgE敏感的肥大细胞脱粒。这些结果表明，三氯萘林对变应性疾病的发展具有抗脱粒作用。提示trigonelline可通过减弱细胞内钙依赖性和非依赖性途径来抑制IgE敏感的肥大细胞脱粒。这些结果表明，三氯萘林对变应性疾病的发展具有抗脱粒作用。