Department of Pharmacology, School of Pharmaceutical Sciences, Jilin University, Changchun 130021, China.
Molecules. 2018 Nov 21;23(11):3039. doi: 10.3390/molecules23113039.
Coptisine is one of the main components of isoquinoline alkaloids in the coptidis rhizome. The effect of coptisine on allergic rhinitis has not been investigated. In this study, we report the effects and mechanisms of coptisine using monoclonal anti-2,4,6-dinitrophenyl-immunoglobulin (Ig) E/human serum albumin (DNP-IgE/HSA)-stimulated rat basophilic leukemia cells (RBL-2H3 cells) in vitro and an ovalbumin (OVA)-induced allergic rhinitis (AR) in mice. The results showed that coptisine markedly decreased the levels of β-hexosaminidase, histamine, interleukin (IL)-4, and tumor necrosis factor (TNF)-α. Coptisine also prevented morphological changes, such as restoring an elongated shape, inhibiting granule release on toluidine blue staining, and reorganizing inhibited filamentous actins (F-actin). Additionally, coptisine blocked the phosphorylation of phosphoinositide3-kinase (PI3K)/Akt (as known as protein kinase B(PKB)) in RBL-2H3 cell. Furthermore, the results showed that coptisine suppressed OVA-induced allergic rhinitis symptoms, such as nasal rubbing and OVA-specific IgE, and histamine, IL-4 and TNF- levels in the serum of AR mice. These data suggested that coptisine should have inhibitory effects on the inflammatory responses of mast cells, and may be beneficial for the development of coptisine as a potential anti-allergic drug.
小檗碱是黄连根茎中异喹啉生物碱的主要成分之一。小檗碱对过敏性鼻炎的作用尚未得到研究。在这项研究中,我们报告了小檗碱使用单克隆抗 2,4,6-二硝基苯基-免疫球蛋白(Ig)E/人血清白蛋白(DNP-IgE/HSA)刺激的大鼠嗜碱性白血病细胞(RBL-2H3 细胞)体外和卵清蛋白(OVA)诱导的过敏性鼻炎(AR)在小鼠中的作用和机制。结果表明,小檗碱可显著降低β-己糖胺酶、组胺、白细胞介素(IL)-4 和肿瘤坏死因子(TNF)-α的水平。小檗碱还可预防形态学变化,如恢复长形、抑制甲苯胺蓝染色的颗粒释放,并重新组织抑制丝状肌动蛋白(F-actin)。此外,小檗碱可阻断 RBL-2H3 细胞中磷酸肌醇 3-激酶(PI3K)/Akt(也称为蛋白激酶 B(PKB))的磷酸化。此外,结果表明,小檗碱可抑制 OVA 诱导的过敏性鼻炎症状,如鼻擦和 AR 小鼠血清中的 OVA 特异性 IgE、组胺、IL-4 和 TNF-α水平。这些数据表明,小檗碱对肥大细胞的炎症反应具有抑制作用,可能有助于开发小檗碱作为一种潜在的抗过敏药物。