冠突散囊菌来源的2-6-H-5-B化合物的抗炎作用及机制研究

徐艳明; 黄壹敏; 石杰; 周捷玲; 周鸿艳; 蒲洪; 黄勇; 刘建新<sup>*</sup>

引用本文:	徐艳明,黄壹敏,石杰,周捷玲,周鸿艳,蒲洪,黄勇,刘建新.冠突散囊菌来源的2-6-H-5-B化合物的抗炎作用及机制研究[J].中国现代应用药学,2022,39(2):161-167.
	XU Yanming,HUANG Yimin,SHI Jie,ZHOU Jieling,ZHOU Hongyan,PU Hong,HUANG Yong,LIU Jianxin.Study on Anti-inflammatory Activity and Mechanism of Compound 2-6-H-5-B from Eurotium Cristatum[J].Chin J Mod Appl Pharm(中国现代应用药学),2022,39(2):161-167.

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冠突散囊菌来源的2-6-H-5-B化合物的抗炎作用及机制研究
徐艳明^1,2, 黄壹敏¹, 石杰³, 周捷玲¹, 周鸿艳¹, 蒲洪^1,3, 黄勇³, 刘建新¹
1.湖南医药学院药学院, 新型抗体药物及其智能运输系统湖南省重点实验室, 中药合成生物学研究湖南省重点实验室, 湖南怀化 418000;2.黑龙江中医药大学佳木斯学院, 黑龙江佳木斯 154007;3.中南大学湘雅国际转化医学联合研究院, 长沙 410013

摘要:

目的研究冠突散囊菌来源的苯甲醛衍生物(2-6-H-5-B)对脂多糖诱导的RAW264.7细胞的抗炎作用及机制。方法 RAW264.7细胞经不同浓度的苯甲醛衍生物(2-6-H-5-B)(25，50和100 μmol·L^-1)及阳性对照药地塞米松(0.5 μmol·L^-1)预处理1 h后，除对照组外，其余各组给予100 ng·mL^-1 脂多糖刺激诱导24 h。采用Griess试剂法检测NO释放水平，ELISA法分析TNF-α、IL-6和MCP-1的表达水平，以及Western blotting检测AMPK、NF-κB和MAPK信号通路的蛋白表达情况。结果化合物2-6-H-5-B可以显著抑制活化的巨噬细胞NO(P<0.01或P<0.05)、TNF-α(P<0.01)、IL-6(P<0.01)和MCP-1 (P<0.01)的产生，表现出较好的抗炎活性。研究表明，2-6-H-5-B未能明显阻断NF-κB和MAPK信号通路的活化，但可以显著增加p-AMPK的表达。结论 2-6-H-5-B是一个较有潜力的抗炎药物先导物，其抗炎活性可能与激活AMPK通路相关。

关键词: 苯甲醛衍生物(2-6-H-5-B) 茯砖茶冠突散囊菌抗炎 RAW264.7巨噬细胞

DOI：10.13748/j.cnki.issn1007-7693.2022.02.004

分类号:R965.1

基金项目:怀化市科技计划(应用基础研究类)项目(2018N2203)；国家级大学生创新创业训练计划项目(201912214019)；湖南医药学院博士科研启动资金项目

Study on Anti-inflammatory Activity and Mechanism of Compound 2-6-H-5-B from Eurotium Cristatum

XU Yanming^1,2, HUANG Yimin¹, SHI Jie³, ZHOU Jieling¹, ZHOU Hongyan¹, PU Hong^1,3, HUANG Yong³, LIU Jianxin¹

1.School of Pharmaceutical Sciences, Hunan Province Key Laboratory for Antibody-based Drug and Intelligent Delivery System, Hunan Provincial Key Laboratory for Synthetic Biology of Traditional Chinese Medicine, Hunan University of Medicine, Huaihua 418000, China;2.College of Jiamusi, Heilongjiang University of Chinese Medicine, Jiamusi 154007, China;3.Xiangya International Academy of Translational Medicine, Central South University, Changsha 410013, China

Abstract:

OBJECTIVE To study the effects and mechanisms of anti-inflammatory of benzaldehyde derivatives (2-6-H-5-B) derived from Eurotium cristatum in lipopolysaccharide stimulated RAW264.7 cells. METHODS RAW264.7 cells were pretreated with benzaldehyde derivative(compound 2-6-H-5-B)(25, 50, 100 μmol·L^-1) and postive control drug dexamethasone(0.5 μmol·L^-1) for 1 h, then cells were treated with 100 ng·mL^-1 lipopolysaccharide for 24 h except control group. The nitrite concentration in the culture medium was measured as an indicator of NO production by the Griess reagent according to the manufacturer’s protocol. The expression levels of TNF-α, IL-6 and MCP-1 in the cultured supernatant were detected by ELISA kits, and the protein expressions of AMPK, NF-κB and MAPK signaling pathways were analyzed by Western blotting. RESULTS The expression of pro-inflammatory cytokines, including TNF-α(P<0.01), IL-6(P<0.01) and MCP-1(P<0.01), as well as the production of NO(P<0.01 or P<0.05) were inhibited by compound 2-6-H-5-B. Further mechanism studies showed that 2-6-H-5-B failed to inhibit the activation of NF-κB and MAPK signaling pathways, but increased the expression of p-AMPK significantly. CONCLUSION The 2-6-H-5-B is a potential anti-inflammatory drug, and its anti-inflammatory activity may be related to the activation of AMPK pathway.

Key words: benzaldehyde derivatives(2-6-H-5-B) Fu Brick Tea Eurotium cristatum anti-inflammatory RAW264.7 macrophages