目的 研究皱叶香薷Elsholtzia rugulosa的化学成分及其抗炎抗病毒活性。方法 采用溶剂提取法对皱叶香薷进行分级萃取，运用多种色谱方法分离纯化，通过核磁共振和质谱等波谱方法鉴定分离物的结构，并通过RT-qPCR法进一步测定化合物对H1N1流感病毒诱导的炎症因子白细胞介素-6（interleukin-6，IL-6）、白细胞介素-1β（interleukin-1beta，IL-1β）、肿瘤坏死因子-α（tumor necrosis factor-α，TNF-α）及γ干扰素诱导蛋白-10（interferon-γ-inducible protein 10，IP-10）mRNA表达水平的影响，以评价其抗炎活性。结果 从皱叶香薷的95%乙醇提取物中共分离出14种化合物，分别鉴定为5-hydroxy-4-methyl-5-(3-methylbut-2-enoyl) furan-2(5H)-one（1）、rugulolide A（2）、rugulolide B（3）、rugulolide D（4）、迷迭香酸（5）、迷迭香酸甲酯（6）、迷迭香酸丁酯（7）、3'''-deoxyshimobashiraside A（8）、木犀草素（9）、木犀草苷（10）、大波斯菊苷（11）、植物醇（12）、齐墩果酸（13）、咖啡酸（14）。RT-qPCR法从14个化合物中筛选得出5个抗炎活性较好的化合物（化合物1～4、10），能显著下调细胞中H1N1流感病毒诱导的炎症因子（IL-6、IL-1β、TNF-α及IP-10）mRNA表达水平，可显著抑制流感引起的炎症反应。结论 化合物1为1个新的单帖内酯类化合物，命名为皱叶香薷内酯E；化合物2～4为首次从香薷属植物中分离得到。化合物1能剂量相关性地抑制流感病毒诱导的炎症因子（IL-6、IL-1β、TNF-α及IP-10）mRNA表达水平，从而发挥显著的抗炎抗病毒效果。

Objective To study the chemical composition of Elsholtzia rugulosa and its anti-inflammatory and antiviral activities.Methods E. rugulosa was subjected to graded extraction by solvent extraction method, separated and purified by various chromatographic methods, and the structures of the isolates were identified by spectroscopic methods such as nuclear magnetic resonance (NMR) and mass spectrometry (MS), and the compounds’ anti-inflammatory and anti-viral activities against H1N1 influenza virus-induced inflammatory factors, interleukin-6 (IL-6), interleukin-1beta (IL-1β), tumor necrosis factor-alpha (TNF-α), and Interferon-gamma-inducible protein 10 (IP-10) mRNA expression levels were evaluated to determine their anti-inflammatory activities.Results A total of 14 compounds were isolated from the 95% ethanol extract of E. rugulosa. The compounds were identified as rugulolide E (1), rugulolide B (2), rugulolide D (3), rugulolide A (4), rosmarinic acid (5), methyl rosmarinate (6), butyl rosmarinate (7), 3'''-deoxyshimobashiraside A (8), luteolin (9), luteolin 7-O-glucoside (10), cosmosiin (11), phytol (12), oleanolic acid (13), Caffeic acid (14). RT-qPCR screening of five compounds from 14 compounds resulted in five compounds with better anti-inflammatory activity (compounds 1—4, and 10), and the compounds significantly down-regulated the expression of mRNAs of H1N1 influenza virus-induced inflammatory factors in the cells (IL-6, IL-1β, TNF-α, and IP-10) mRNA expression levels, which could significantly inhibit influenza-induced inflammatory responses.Conclusion Compound 1 is a new monoterpene lactone compound named rugulolide E; Compounds 2—4 were isolated for the first time from E. rugulosa. Compound 1 significantly inhibited the mRNA expression levels of influenza virus-induced inflammatory factors (IL-6, IL-1β, TNF-α, and IP-10) in a dose-dependent manner, thus exerting anti-inflammatory and antiviral effects.

R284.1

广东省自然科学基金面上项目（2021A1515011512）