固公果果实干预胃炎-癌转化的活性成分研究OA
Active components of Rosa odorata var.gigantea fruits in intervening gastritis-cancer transformation
目的 研究固公果Rosa odorata var.gigantea果实干预胃炎癌转化的活性成分.方法 利用N-甲基-N'-硝基-N-亚硝基胍(N-methyl-N'-nitro-N-nitrosoguanidine,MNNG)诱导人胃黏膜上皮细胞(GES-1 细胞)转化获得人胃黏膜上皮炎-癌转化模型细胞(MC细胞),对固公果果实 60%乙醇提取物的不同极性组分进行活性筛选,采用硅胶柱、ODS柱色谱、Sephadex LH-20 柱色谱及制备型高效液相等多种色谱方法对活性组分进行分离、纯化,通过理化数据结合波谱技术鉴定化合物结构,采用CCK-8 法对分离得到的单体成分进行活性测试,评价其对MC细胞的抑制作用.结果 从固公果果实的活性组分中分离鉴定 18 个化合物,分别为(2R,3R)-3-[(1'S,2'R,6'S)-2',6'-二羟基-1'-(没食子酰基)环己基]-2,3-二羟基丙酸(1)、microphyllose A(2)、咖啡酸(3)、3,5-二咖啡酰基奎宁酸(4)、5-没食子酰奎宁酸(5)、香草酸乙酯(6)、原花青素 B2(7)、3-O-没食子酰奎宁酸(8)、没食子儿茶素没食子酸酯(9)、6-O-没食子酰基-β-D-葡萄糖(10)、没食子酸甲酯(11)、3,4,5-三-O-没食子酰奎宁酸(12)、没食子酸乙酯(13)、3,5,4'-三羟基二苯乙烯(14)、槲皮苷(15)、槲皮素(16)、木犀草素(17)、白桦脂酸(18).活性测试结果显示,抑制率大于 50%的化合物为 1、9、14～18,其半数抑制浓度(median inhibition concentration,IC50)值分别为 93.47、81.7、37.44、81.58、86.01、44.02、66.12 μmol/L.结论 化合物 1 为新化合物,命名为固公果酸A,化合物 2 为首次从蔷薇属植物中分离得到,化合物 5、9、11、13、15、17 为首次从该植物中分离得到.18 个化合物对MC细胞均具有增殖抑制活性,其中化合物1、9、14、15、16、17、18抑制率大于50%,是潜在的干预胃炎-癌转化的活性成分.
Objective This study aimed to explore the bioactive constituents of Rosa odorata Sweet var.gigantea(Coll.et Hemsl.)Rehd.et Wils.fruits that intervene in the gastritis-cancer transformation process.Methods The transformation of human gastric mucosal epithelial cells(GES-1 cells)was induced by N-methyl-N'-nitro-N-nitrosoguanidine(MNNG)to obtain human gastric mucosal epithelial dermatitis-cancer transformation model cells(MC cells).,The activity screening was conducted on the different polar fractions from the 60%ethanol extract of R.odorata var.gigantea fruits.Active fractions were isolated and purified using multiple chromatographic techniques,including silica gel column chromatography,ODS column chromatography,Sephadex LH-20 column chromatography,and preparative high-performance liquid chromatography(preparative HPLC).The chemical structures of the isolated compounds were elucidated based on physico-chemical properties and spectroscopic data.The CCK-8 assay was utilized to evaluate the anti-proliferative activity of the isolated monomeric compounds against MC cells.Results A total of 18 compounds were isolated and identified from the active fractions of R.odorata var.gigantea fruits,namely:(2R,3R)-3-[(1'S,2'R,6'S)-2',6'-dihydroxy-1'-(galloyl)cyclohexyl]-2,3-dihydroxypropanoic acid(1),microphyllose A(2),caffeic acid(3),3,5-dicaffeoylquinic acid(4),5-galloylquinic acid(5),ethyl vanillate(6),procyanidin B2(7),3-O-galloylquinic acid(8),gallocatechin gallate(9),6-O-galloyl-β-D-glucose(10),methyl gallate(11),3,4,5-tri-O-galloylquinic acid(12),ethyl gallate(13),3,5,4'-trihydroxystilbene(14),quercitrin(15),quercetin(16),luteolin(17),and betulinic acid(18).The results of the activity assay indicated that compounds 1,9,14-18 with an inhibition rate exceeding 50%exhibited the following IC50 values:93.47,81.79,37.44,81.58,86.01,44.02,and 66.12 μmol/L.Conclusion Compound 1 is a novel compound,designated as gugongguoic acid A.Compound 2 was isolated from the genus Rosa for the first time.Compounds 5,9,11,13,15,and 17 were isolated from this plant species for the first time.All 18 compounds exhibited inhibitory activity against MC cell proliferation.Among them,compounds 1,9,14-18 showed inhibition rates greater than 50%,which represent potential bioactive constituents for intervening in the gastritis-cancer transformation process.
陈宇航;姚彬;尹孝荣;原震;张静泽;刘岱琳
天津中医药大学,天津 301617天津现代创新中药科技有限公司,天津 300384天津中医药大学,天津 301617天津现代创新中药科技有限公司,天津 300384天津现代创新中药科技有限公司,天津 300384天津现代创新中药科技有限公司,天津 300384
医药卫生
固公果胃炎-癌转化固公果酸A5-没食子酰奎宁酸没食子儿茶素没食子酸酯槲皮苷木犀草素
Rosa odorata Sweet var.gigantea(Coll.et Hemsl.)Rehd.et Wils.gastritis-cancer transformationgugongguoic acid A5-galloylquinic acidgallocatechin gallatequercitrinluteolin
《中草药》 2026 (3)
806-816,11
天津市科技计划项目(24ZXZSSS00260)天津市科技计划项目(25ZYCGCG00390)
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