Dong Shou-jin, Zhong Yun-qing, Lu Wen-ting, Li Guan-hong, Jiang Hong-li, Mao Bing
Department of Integrated Traditional Chinese and Western Medicine, West China Hospital, West China Medical School, Sichuan University, Chengdu, 610041, China,
Inflammation. 2015 Aug;38(4):1493-501. doi: 10.1007/s10753-015-0124-2.
Baicalin, a flavonoid monomer derived from Scutellaria baicalensis called Huangqin in mandarin, is the main active ingredient contributing to S. baicalensis' efficacy. It is known in China that baicalin has potential therapeutic effects on inflammatory diseases. However, its anti-inflammatory mechanism has still not been fully interpreted. We aim to investigate the anti-inflammatory effect of baicalin on lipopolysaccharide (LPS)-induced inflammation in HBE16 airway epithelial cells and also to explore the underlying signaling mechanisms. The anti-inflammatory action of baicalin was evaluated in human airway epithelial cells HBE16 treated with LPS. Airway epithelial cells HBE16 were pretreated with a range of concentrations of baicalin for 30 min and then stimulated with 10 μg/ml LPS. The secretions of interleukin-6 (IL-6), interleukin-8 (IL-8), and tumor necrosis factor-α (TNF-α) in cell culture supernatants were quantified by enzyme-linked immunosorbent assay (ELISA). The messenger RNA (mRNA) expressions of IL-6, IL-8, and TNF-α were tested by quantitative real-time polymerase chain reaction (real-time RT-PCR). Furthermore, Western blotting was used to determine whether the signaling pathway NF-κB was involved in the anti-inflammatory action of baicalin. The inflammatory cell model was successfully built with 10 μg/ml LPS for 24 h in our in vitro experiments. Both the secretions and the mRNA expressions of IL-6, IL-8, and TNF-α were significantly inhibited by baicalin. Moreover, the expression levels of phospho-IKKα/β and phospho-NF-κB p65 were downregulated, and the phospho-IκB-α level was upregulated by baicalin. These findings suggest that the anti-inflammatory properties of baicalin may be resulted from the inhibition of IL-6, IL-8, and TNF-α expression via preventing signaling NF-κB pathway in HBE16 airway epithelial cells. In addition, this study provides evidence to understand the therapeutic effects of baicalin on inflammatory diseases in clinical practice.
黄芩苷是从黄芩（中文名为“黄岑”）中提取的一种黄酮类单体，是黄芩发挥药效的主要活性成分。在中国，人们已知黄芩苷对炎症性疾病具有潜在治疗作用。然而，其抗炎机制尚未得到充分阐释。我们旨在研究黄芩苷对脂多糖（LPS）诱导的HBE16气道上皮细胞炎症的抗炎作用，并探索其潜在的信号传导机制。在用LPS处理的人气道上皮细胞HBE16中评估黄芩苷的抗炎作用。将HBE16气道上皮细胞用一系列浓度的黄芩苷预处理30分钟，然后用10μg/ml LPS刺激。通过酶联免疫吸附测定（ELISA）对细胞培养上清液中白细胞介素-6（IL-6）、白细胞介素-8（IL-8）和肿瘤坏死因子-α（TNF-α）的分泌进行定量。通过定量实时聚合酶链反应（实时RT-PCR）检测IL-6、IL-8和TNF-α的信使核糖核酸（mRNA）表达。此外，采用蛋白质印迹法确定核因子-κB（NF-κB）信号通路是否参与黄芩苷的抗炎作用。在我们的体外实验中，用10μg/ml LPS成功构建了炎症细胞模型24小时。黄芩苷显著抑制了IL-6、IL-8和TNF-α的分泌及mRNA表达。此外，黄芩苷下调了磷酸化IKKα/β和磷酸化NF-κB p65的表达水平，并上调了磷酸化IκB-α水平。这些发现表明，黄芩苷的抗炎特性可能是通过在HBE16气道上皮细胞中阻止NF-κB信号通路来抑制IL-6、IL-8和TNF-α表达所致。此外，本研究为理解黄芩苷在临床实践中对炎症性疾病的治疗作用提供了证据。
