摘要
蜘蛛香(Valeriana jatamansi Jones)作为我国多个民族常用的传统草药具有广泛的药用价值,从蜘蛛香中筛选有效化合物并研究其作用机制,对蜘蛛香的综合开发和利用具有重要的意义。本研究采用脂多糖(LPS)处理RAW264.7细胞作为炎症细胞模型,对从蜘蛛香干燥根及根茎中分离得到的14个环烯醚萜类化合物进行抗炎活性研究。结果显示,化合物1、2、3、5、8、9均可以明显抑制NO的产生,其中化合物1和2的抑制效果最为显著,IC_(50)值分别为0.88和0.62μmol/L。进一步实验研究结果显示,化合物1和2可抑制LPS诱导的RAW264.7细胞中TNF-α、IL-1β、IL-6的分泌,下调iNOS、COX-2、NLRP3蛋白表达及IκBα、STAT3和mTOR的磷酸化水平,但是对MAPKs蛋白家族无明显影响。综上说明化合物1和2可能通过下调NF-κB及mTOR/STAT3信号通路,减少炎症相关蛋白的表达以及炎症因子的分泌,从而降低LPS诱导的巨噬细胞的炎性反应。
Valeriana jatamansi Jones,a traditional herbal medicine used by many ethnic groups in China,has a wide range of medicinal value.Studying the active ingredients of V.jatamansi and its mechanism of action is of great significance to the comprehensive development and utilization of V.jatamansi.In this study,RAW264.7 cells treated with lipopolysaccharide(LPS)were used as an inflammatory cell model to investigate the anti-inflammatory activities of 14 iridoids isolated from the dried roots and rhizomes of V.jatamansi.The results showed that compounds 1,2,3,5,8 and 9 could significantly inhibit the production of NO,among which compounds 1 and 2 Chad the most significant inhibitory effect,with IC_(50) values of 0.88 and 0.62μmol/L,respectively.Further experiments showed that compounds 1 and 2 could inhibit the secretion of TNF-α,IL-1β and IL-6,down-regulate the expression of iNOS,COX-2,NLRP3 and the phosphorylation levels of IκBα,STAT3 and mTOR in LPS-induced RAW264.7 cells,but had no significant effect on the MAPKs protein family.In summary,compounds 1 and 2 may reduce the expression of inflammation-related proteins and the secretion of inflammatory factors by down-regulating NF-κB and mTOR/STAT3 signaling pathways,thereby reducing the LPS-induced inflammatory response of macrophages.
作者
姜明言
饶凯瑞
廖彩岑
刘欢
李洪梅
李蓉涛
刘丹
JIANG Ming-yan;RAO Kai-rui;LIAO Cai-cen;LIU Huan;LI Hong-mei;LI Rong-tao;LIU Dan(Faculty of Life Science and Technology,Kunming University of Science and Technology,Kunming 650500,China)
出处
《天然产物研究与开发》
CAS
CSCD
2021年第6期913-920,共8页
Natural Product Research and Development
基金
国家自然科学基金(81860618,32060106)
云南省应用基础研究计划面上项目(2018FB031)。
