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 compounds1 , 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 Compound1 is a novel compound, designated as gugongguoic acid A. Compound2 was isolated from the genus Rosa for the first time. Compounds5 ,9 ,11 ,13 ,15 , and17 were isolated from this plant species for the first time. All 18 compounds exhibited inhibitory activity against MC cell proliferation. Among them, compounds1 , 9 ,14 —18 showed inhibition rates greater than 50%, which represent potential bioactive constituents for intervening in the gastritis–cancer transformation process.

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天津市科技计划项目（24ZXZSSS00260）；天津市科技计划项目（25ZYCGCG00390）