对大叶蔷薇（Rosa macrophylla Lindl.）不同部位（花、枝、叶、果）乙醇提取物的总酚和类黄酮含量进行测定，并对其体外的抗氧化能力、抗肿瘤活性和抗炎活性进行评价；利用UPLC-MS/MS技术分析大叶蔷薇叶和果的次生代谢产物组成差异，并对次生代谢产物与生物活性之间的相关性进行分析。结果显示：大叶蔷薇各部位乙醇提取物的总酚和类黄酮含量均较高，分别为123.96~277.93和80.20~714.73 mg·g^-1。叶乙醇提取物的总酚含量最高，DPPH·清除能力、ABTS⁺·清除能力和总抗氧化能力最强，对人宫颈癌HeLa细胞、人胃癌MGC-803细胞和人肺癌A549细胞的半数抑制率均最小；在0~60 μg·mL^-1范围内，果乙醇提取物对小鼠RAW 264.7巨噬细胞表现出较小的细胞毒性，且随着乙醇提取物质量浓度增加，小鼠RAW 264.7巨噬细胞的NO释放量逐渐下降，并具有一定的剂量依赖性。比较代谢组学分析结果显示：叶和果的次生代谢产物组成存在明显差异，共得到175种差异代谢产物。Pearson相关性分析结果显示：叶和果乙醇提取物的生物活性与差异代谢产物存在一定的相关性。综上所述，大叶蔷薇叶乙醇提取物的抗氧化能力最强，抗肿瘤活性最好；而果乙醇提取物具有最佳的抗炎活性；松萝酸和金合欢素等可能是叶抗肿瘤活性的物质基础，表儿茶素没食子酸酯、矢车菊素-3-O-葡萄糖苷、吲哚-3-甲醛、葫芦巴碱和根皮苷等可能是果抗炎活性的物质基础。

The total phenol and flavonoid contents in the ethanol extracts from different parts (flowers, branches, leaves, and fruits) of Rosa macrophylla Lindl. were assayed, and their anti-oxidant ability, anti-tumor activity, and anti-inflammatory activity were evaluated in vitro; the differences in composition of secondary metabolites between the leaves and fruits of R. macrophylla were investigated by using UPLC-MS/MS technology, and the correlations between the secondary metabolites and their bioactivities were analyzed. The results show that the total phenol and flavonoid contents in the ethanol extracts from different parts of R. macrophylla are all relatively high, which are 123.96-277.93 and 80.20-714.73 mg·g^-1 respectively. The ethanol extract from the leaves has the highest total phenol content, the strongest DPPH· scavenging ability, ABTS⁺· scavenging ability, and total anti-oxidant ability, and the half inhibitory rate against human cervical cancer HeLa cells, human gastric cancer MGC-803 cells, and human lung cancer A549 cells; within the range of 0-60 μg·mL^-1, the ethanol extract from the fruits exhibits relatively low cytotoxicity towards mouse RAW 264.7 macrophages, and with the increase of the ethanol extract mass concentration, the NO release amount from mouse RAW 264.7 macrophages gradually decreases in a dose-dependent manner to some degree. The comparative metabolomics analysis result shows that there are obvious differences in composition of secondary metabolites between leaves and fruits, and a total of 175 differential metabolites are identified. The Pearson correlation analysis result shows that there is a certain correlation between the bioactivities of the ethanol extracts from leaves and fruits and their differential metabolites. In conclusion, the ethanol extract from the leaves of R. macrophylla exhibits the strongest anti-oxidant ability and the best anti-tumor activity; while the ethanol extract from the fruits has the best anti-inflammatory activity; usnic acid and acacetin, etc. may be the material basis for the anti-tumor activity of the leaves, while epicatechin gallate, cyanidin-3-O-glucoside, indole-3-carboxaldehyde, trigonelline, and phlorizin, etc. may be the material basis for the anti-inflammatory activity of the fruits.