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.

Rosa odorata Sweet var. gigantea (Coll. et Hemsl.) Rehd. et Wils.  /  gastritis-cancer transformation  /  gugongguoic acid A  /  5-galloylquinic acid  /  gallocatechin gallate  /  quercitrin  /  luteolin