School of Pharmaceutical Science, Zhejiang Chinese Medical University, Hangzhou 310053, Zhejiang, China.
Zhejiang Research Institute of Chinese Medicine Co., Ltd, Hangzhou 310053, Zhejiang, China.
Fitoterapia. 2020 Jul;144:104496. doi: 10.1016/j.fitote.2020.104496. Epub 2020 Feb 10.
Farfarae Flos is the dried flower buds of Tussilago farfara L. which is widely used to treat allergic and inflammatory diseases in Chinese folk. Tussilagone (TSL), a sesquiterpene compound purified from Farfarae Flos, has been confirmed the main active component in the plant. However, its anti-allergic activity hasn't been reported yet. The purpose of this study is to investigate the anti-allergic effect of TSL in ovalbumin (OVA)-induced allergic rhinitis (AR) guinea pigs and immunoglobulin E (IgE)-stimulated RBL-2H3 cells. The AR symptoms such as nasal scratching, sneezing and runny nose were scored and the histological changes of nasal mucosa were observed by H&E staining. The levels of histamine, OVA-specific IgE, IL-6 and TNF-α in the serum were measured by ELISA. In IgE-stimulated RBL-2H3 cells, the phosphoryration of Lyn, Syk, Akt, NF-κB p65, ERK and p38 MAPK were investigated by western blot analysis. The results showed that intraperitoneal injection of TSL at doses of 25 and 50 mg/kg significantly alleviated the allergic symptoms and the histological changes of nasal mucosa in OVA-induced allergic rhinitis guinea pigs. Moreover, the levels of histamine, IgE and IL-6 in the serum decreased significantly (p < .05). In vitro, TSL suppressed the phosphorylation of Lyn, Syk, Akt, NF-κB p65, ERK and p38 MAPK in IgE-stimulated RBL-2H3 cells. These results indicate TSL has therapeutic effect on allergic rhinitis in guinea pigs. The anti-allergic mechanism may be through the inhibition of allergic and inflammatory related pathways in mast cells.
款冬花为菊科植物款冬 Tussilago farfara L. 的干燥花蕾，在民间广泛用于治疗过敏性和炎症性疾病。款冬酮（TSL），一种从款冬花中分离得到的倍半萜化合物，已被确认为该植物的主要活性成分。然而，其抗过敏性活性尚未见报道。本研究旨在探讨 TSL 对卵清蛋白（OVA）诱导的变应性鼻炎（AR）豚鼠和免疫球蛋白 E（IgE）刺激的 RBL-2H3 细胞的抗过敏作用。通过 H&E 染色观察鼻黏膜组织学变化，对豚鼠的鼻挠、打喷嚏和流鼻涕等 AR 症状进行评分。通过 ELISA 法测定血清中组胺、OVA 特异性 IgE、IL-6 和 TNF-α的水平。在 IgE 刺激的 RBL-2H3 细胞中，通过 Western blot 分析研究 Lyn、Syk、Akt、NF-κB p65、ERK 和 p38 MAPK 的磷酸化。结果表明，腹腔注射 TSL 剂量为 25 和 50mg/kg 可显著缓解 OVA 诱导的过敏性鼻炎豚鼠的过敏症状和鼻黏膜组织学变化。此外，血清中组胺、IgE 和 IL-6 水平显著降低（p<.05）。体外，TSL 抑制 IgE 刺激的 RBL-2H3 细胞中 Lyn、Syk、Akt、NF-κB p65、ERK 和 p38 MAPK 的磷酸化。这些结果表明 TSL 对豚鼠变应性鼻炎具有治疗作用。其抗过敏机制可能是通过抑制肥大细胞中过敏和炎症相关途径。
