Research and Development Division, Korean Promotion Institute for Traditional Medicine Industry, Gyeongsan 710-210, Republic of Korea.
Am J Chin Med. 2014;42(4):935-47. doi: 10.1142/S0192415X14500591.
Mast cells are central players in immediate-type hypersensitvity and inflammatory responses. In the present study, the effects of britanin on the passive cutaneous anaphylaxis (PCA) reaction in mice and on the phorbol 12-myristate 13-acetate and calcium ionophore A23187 (PMACI)-induced production of pro-inflammatory cytokines in human mast cell line (HMC-1) were evaluated. The oral administration of britanin (10-20 mg/kg) decreased the mast cell-mediated PCA reaction in IgE-sensitized mice. In the activity and mechanism of britanin in vitro assay, britanin suppressed the gene expression and secretion of pro-inflammatory cytokines in a dose-dependent manner in HMC-1. In addition, britanin attenuated PMACI-induced activation of NF-κB as indicated by the inhibition of the degradation of IκBα, nuclear translocation of NF-κB, NF-κB/DNA binding activity assay, and blocked the phosphorylation of p38 MAP kinase, in a dose-dependent manner. We conclude that britanin may have potential as a treatment for allergic-inflammatory diseases.
肥大细胞是速发型超敏反应和炎症反应的核心参与者。在本研究中，评估了布列他尼对小鼠被动皮肤过敏反应（PCA）和佛波醇 12-肉豆蔻酸 13-乙酸酯和钙离子载体 A23187（PMACI）诱导的人肥大细胞系（HMC-1）中促炎细胞因子产生的影响。布列他尼（10-20mg/kg）经口给予可降低 IgE 致敏小鼠的肥大细胞介导的 PCA 反应。在布列他尼的体外活性和机制研究中，布列他尼以剂量依赖性方式抑制 HMC-1 中促炎细胞因子的基因表达和分泌。此外，布列他尼还抑制了 IκBα 的降解、NF-κB 的核易位、NF-κB/DNA 结合活性测定以及 p38 MAP 激酶的磷酸化，从而减弱了 PMACI 诱导的 NF-κB 激活，同样呈剂量依赖性。我们得出结论，布列他尼可能具有治疗过敏性炎症性疾病的潜力。
