The flavonoid baicalin exhibits anti-inflammatory activity by binding to chemokines
The flavonoid baicalin exhibits anti-inflammatory activity by binding to chemokines
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DOI：
10.1016/s0162-3109(00)00244-7
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发表时间：
2000-09-01
期刊：
影响因子：
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通讯作者：
Wang, JM
中科院分区：
文献类型：
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作者：
Li, BQ;Fu, T;Wang, JM
黄芩苷(BA)是从药用植物黄芩中分离得到的一种黄酮类化合物，具有抗炎、抗病毒等活性。为了阐明BA的作用机制(S)，我们测试了BA对炎症和感染的关键介质趋化因子或趋化因子受体的干扰作用。我们观察到BA抑制了一些趋化因子与人白细胞或表达特定趋化因子受体的细胞的结合。这与趋化因子诱导细胞迁移的能力降低有关。大鼠皮下注射BA和CXC趋化因子IL-8可显著抑制IL-8诱导的中性粒细胞浸润。BA并不直接与趋化因子竞争与受体的结合，而是通过与趋化因子配体的选择性结合发挥作用。BA与CXC(基质细胞衍生因子-1α，IL-8)、CC(巨噬细胞炎性蛋白(MIP)-1β，单核细胞趋化蛋白(MCP)-2)和C(淋巴动蛋白(LTN))亚家族的肟树脂结合的趋化因子相互作用的事实支持了这一结论，BA不与CX3C趋化因子/神经触动因子或其他细胞因子，如肿瘤坏死因子-α和干扰素-γ相互作用，表明其作用具有选择性。这些结果提示BA的抗炎机制之一可能是结合多种趋化因子，限制其生物学功能。(C)2000 Elsevier Science B.V.保留所有权利。
Baicalin (BA) is a flavonoid compound purified from the medicinal plant Scutellaria baicalensis Georgi acid has been reported to possess anti-inflammatory and anti-viral activities. In order to elucidate the mechanism(s) of action of BA, we tested whether BA could interfere with chemokines or chemokine receptors, which are critical mediators of inflammation and infection. We observed that BA inhibited the binding of a number of chemokines to human leukocytes or cells transfected to express specific chemokine receptors. This was associated with a reduced capacity of the chemokines to induce cell migration. Go-injection of BA with CXC chemokine interleukin-8 (IL-8) into rat skin significantly inhibited IL-8 elicited neutrophil infiltration. BA did not directly compete with chemokines for binding to receptors, but rather acted through its selective binding to chemokine ligands. This conclusion was supported by the fact that BA cross-linked to oxime resin bound chemokines of the CXC (stromal cell-derived factor (SDF)-1 alpha, IL-8), CC (macrophage inflammatory protein (MIP)-1 beta, monocyte chemotactic protein (MCP)-2), and C (lymphotactin (Ltn)) subfamilies, BA did not interact with CX3C chemokine fractalkine/neurotactin or other cytokines, such as TNF-alpha and IFN-gamma, indicating that its action is selective. These results suggest that one possible anti-inflammatory mechanism of BA is to bind a variety of chemokines and limit their biological function. (C) 2000 Elsevier Science B.V. All rights reserved.