College of Pharmaceutical Science, Zhejiang Chinese Medical University, Hangzhou 310053, China.
Academy of Chinese Medical Sciences, Zhejiang Chinese Medical University, Hangzhou 310053, China.
Mediators Inflamm. 2021 Mar 13;2021:6684120. doi: 10.1155/2021/6684120. eCollection 2021.
is a well-known traditional Chinese herb with anti-inflammatory properties that is widely used in the treatment of lung conditions such as silicosis, tuberculosis, and pneumogastric hemorrhage. However, little information on the anti-inflammatory ingredients and their activities is available. In this study, an effect fraction of (EFBS) was enriched, and its anti-inflammatory activities and underlying mechanisms were investigated. EFBS was enriched by polyamide column chromatography and characterized by HPLC; an LPS-induced acute lung injury model was used to evaluate the anti-inflammatory activities of EFBS. Meanwhile, the main anti-inflammation-contributing ingredients and possible molecular mechanism of anti-inflammatory activity in EFBS were verified by component-knockout method combined with LPS-induced RAW264.7 cell model. The EFBS mainly consisted of coelonin (15.88%), batatasin III (32.49%), 3'--methylbatatasin III (6.96%), and 3-hydroxy-5-methoxy bibenzyl (2.51%). Pretreatment with the EFBS (20 mg/kg and 60 mg/kg) for five days prior to the administration of LPS resulted in decreases in wet-to-dry lung weight ratio, neutrophil number, MPO activity, total protein concentration, NO level, and MDA level, as well as IL-1, IL-6, MCP-1, and TNF- concentrations in the bronchoalveolar lavage fluid. Western blot analysis demonstrated the increased expressions of iNOS, COX-2, and NF-B p65 in the LPS treatment group, all of which were ameliorated by EFBS pretreatment. Histological examination confirmed the protective effect of the EFBS. Additionally, component-knockout assay confirmed that these four quantitative components contributed significantly to the anti-inflammatory effect of EFBS. Coelonin, batatasin III, 3'--methylbatatasin III and 3-hydroxy-5-methoxy bibenzyl were the main anti-inflammatory components of EFBS and could regulate the expression of downstream inflammatory cytokines by inhibiting p65 nuclear translocation. These findings uncover, in part, the molecular basis underlying the anti-inflammatory activity of .
是一种具有抗炎特性的著名中药,广泛用于治疗矽肺、肺结核和胃出血等肺部疾病。然而,关于其抗炎成分及其活性的信息很少。在这项研究中,我们富集了 (EFBS)有效部位,并研究了其抗炎活性及其作用机制。EFBS 通过聚酰胺柱色谱法进行富集,并通过 HPLC 进行表征;采用 LPS 诱导的急性肺损伤模型评价 EFBS 的抗炎活性。同时,通过成分敲除法结合 LPS 诱导的 RAW264.7 细胞模型,验证了 EFBS 的主要抗炎成分及其抗炎活性的可能分子机制。EFBS 主要由 coelonin(15.88%)、batatasin III(32.49%)、3'--methylbatatasin III(6.96%)和 3-羟基-5-甲氧基二苯并基(2.51%)组成。在 LPS 给药前用 EFBS(20mg/kg 和 60mg/kg)预处理 5 天,可降低湿重/干重肺重比、中性粒细胞数、MPO 活性、总蛋白浓度、NO 水平和 MDA 水平,以及支气管肺泡灌洗液中的 IL-1、IL-6、MCP-1 和 TNF-浓度。Western blot 分析表明,LPS 处理组 iNOS、COX-2 和 NF-B p65 的表达增加,EFBS 预处理可改善这些表达。组织学检查证实了 EFBS 的保护作用。此外,成分敲除试验证实这四个定量成分对 EFBS 的抗炎作用有显著贡献。coelonin、batatasin III、3'--methylbatatasin III 和 3-羟基-5-甲氧基二苯并基是 EFBS 的主要抗炎成分,可通过抑制 p65 核易位来调节下游炎症细胞因子的表达。这些发现部分揭示了 的抗炎活性的分子基础。