意大利牛舌草化学成分及其抗炎活性研究  

Chemical constituents of Anchusa italica Retz.and their anti-inflammatory activity

作　　者：郭文辉 徐晓琴 孙宇 马国需 石磊岭[3] 陈良 GUO Wen-hui;XU Xiao-qin;SUN Yu;MA Guo-xu;SHI Lei-ling;CHEN Liang(The Fourth College of Clinical Medicine,Xinjiang Medical University;State Key Laboratory of Pathogenesis,Prevention and Treatment of High Incidence Diseases in Central Asia,Department of Pharmacy,Traditional Chinese Medicine Hospital Affiliated to Xinjiang Medical University,Urumqi 830000,China;Xinjiang Institute of Chinese and Ethnic Medicine,Urumqi 830002,China;Institute of Medicinal Plant Development,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100193,China)

机构地区：[1]新疆医科大学第四临床医学院 [2]新疆医科大学附属中医医院药学部,省部共建中亚高发病成因与防治国家重点实验室,乌鲁木齐830000 [3]新疆维吾尔自治区中药民族药研究所,乌鲁木齐830002 [4]中国医学科学院北京协和医学院药用植物研究所,北京100193

出　　处：《天然产物研究与开发》2025年第3期465-471,共7页Natural Product Research and Development

基　　金：新疆维吾尔自治区自然科学基金(2021D01C222);新疆地产中药民族药新药研发培育项目(2017-02-08);国家重点研发计划项目(2017YFC1703901);中央本级重大增减支项目(2060302)。

摘　　要：为阐明意大利牛舌草药效物质基础,本研究采用硅胶柱色谱、半制备型高效液相色谱技术等对意大利牛舌草70%乙醇提取物的乙酸乙酯部位进行分离纯化,通过NMR、MS等现代波谱学方法鉴定所得化合物的结构,从中共分离鉴定了19个化合物,分别为:羟基酪醇(1)、咖啡酸乙酯(2)、3,4-二羟基苄胺(3)、对羟基苯甲酸(4)、香草醛(5)、1,2,4-苯三酚(6)、原儿茶醛(7)、(E)-4-(2-hydroxyvinyl)-2-methoxyphenol(8)、原儿茶酸(9)、异鼠李素(10)、丙三醇(11)、对羟基苯甲醛(12)、咖啡因(13)、caffeic acid ethylene ester(14)、原儿茶酸乙酯(15)、phenylethylβ-D-glcoside(16)、benzylβ-D-glucopyranoside(17)、3,4-dihydroxyphenyl caffeate(18)、山柰酚-3-O-芸香糖苷(19)。化合物1~3、6~8、12~18为首次从该植物中分离得到,其中10个化合物(1、3、6~8、13~17)为首次从牛舌草属中分离得到。同时采用脂多糖诱导的RAW 264.7细胞炎症模型,以吲哚美辛作为阳性对照,测定各化合物的体外抗炎活性。结果显示,化合物1、2、10、13抗炎活性相对较好,IC_(50)值分别为19.6、14.9、11.3、10.2μmol/L。To elucidate the material basis of the pharmacological effects of Anchusa italica Retz.,the study was carried out to isolate and purify the chemical components from the ethyl acetate site of 70%ethanol extract of the plant by silica gel and semi-preparative high-performance liquid chromatography and identify the structures of the compounds by modern spectroscopic methods such as NMR,MS,and so on.Nineteen compounds were isolated and identified as:hydroxytyrosol(1),ethyl caffeate(2),3,4-dihydroxybenzylamine(3),4-hydroxybenzoic acid(4),vanillin(5),1,2,4-benzenetriol(6),3,4-dihydroxyphenylacetaldehyde(7),(E)-4-(2-hydroxyvinyl)-2-methoxyphenol(8),protocatechuic acid(9),isorhamnetin(10),glycerol(11),4-hydroxybenzaldehyde(12),caffeine(13),caffeic acid ethylene ester(14),ethyl 3,4-dihydroxybenzoate(15),phenylethylβ-D-glcoside(16),benzylβ-D-glucopyranoside(17),3,4-dihydroxyphenyl caffeate(18),kaempferol-3-O-rutinoside(19).Compounds 1-3,6-8,12-18 were isolated from this plant for the first time,among which 10 compounds(1,3,6-8,13-17)were isolated for the first time from the genus Anchusa L..Meanwhile,the in vitro activities of the compounds were determined by using the lipopolysaccharide-induced RAW 264.7 cell inflammation model,with indomethacin as the positive control.The bioactivity results showed that compounds 1,2,10,and 13 had relatively high anti-inflammatory activities with IC_(50) values of 19.6,14.9,11.3,and 10.2μmol/L.

关 键 词：意大利牛舌草 化学成分 抗炎活性 羟基酪醇 咖啡酸乙酯 异鼠李素 

分 类 号：R284.1[医药卫生—中药学]