Abstract Context Rubus species (Rosaceae) have been used in folk medicine to treat diabetes due to their hypoglycaemic activity. Objective To screen the active components that act as hypoglycaemic agents in Rubus amabilis Focke and the underlying mechanisms. Materials and methods Aqueous stem extract of R. amabilis was incubated with MIN6 β-cells, PBS was used as the blank control. Then the cells were washed, cell membrane-bound components were dissociated and identified by UPLC/MS. Total procyanidins (PCs) in R. amabilis was enriched and the cytotoxicity and anti-proliferation on β-cell were evaluated by MTT assay. PCs at 25, 50, and 75 μg/mL was applied for 24 h to determine its effects on palmitate (PA)-induced apoptosis and GSIS. Western blotting was employed to detect the protein expression of PI3K/Akt/FoxO1 signalling. The antioxidant indices were also measured. Results β-Cell membrane-bound components were identified as three procyanidin B dimers and a C trimer. PCs showed no significant cytotoxicity up to a concentrations of 100 μg/mL. PCs treatment reversed the elevated apoptosis rate and impaired GSIS induced by PA. PCs markedly decreased the intracellular ROS and MDA production and increased the SOD activity. Moreover, PCs promoted the phosphorylation of Akt and FoxO1, and regulated Pdx-1 and Bax expression in MIN6 cells. Discussion and conclusion: The active components that act as hypoglycaemic agents in R. amabilis are procyanidins, which protected MIN6 cells against PA-induced apoptosis by activating PI3K/Akt/FoxO1 signalling. These results indicate that β-cell extraction, combined with UPLC/MS, is a valid method for screening antidiabetic components from herbal medicines.

中文翻译：

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筛选来自红豆杉的活性成分以保护胰腺 β 细胞

摘要背景 悬钩子属（蔷薇科）因其降血糖活性已被用于民间医学治疗糖尿病。目的筛选红豆杉中具有降血糖作用的活性成分及其作用机制。材料和方法 天竺葵的含水茎提取物与MIN6 β-细胞一起孵育，PBS 用作空白对照。然后洗涤细胞，解离细胞膜结合组分并通过UPLC/MS鉴定。富集了红豆杉中的总原花青素（PCs），并通过MTT法评估了对β细胞的细胞毒性和抗增殖作用。应用 25、50 和 75 μg/mL 的 PC 24 小时，以确定其对棕榈酸酯 (PA) 诱导的细胞凋亡和 GSIS 的影响。采用蛋白质印迹法检测 PI3K/Akt/FoxO1 信号转导的蛋白表达。还测量了抗氧化指数。结果 β-细胞膜结合成分被鉴定为三个原花青素 B 二聚体和一个 C 三聚体。PCs 在浓度高达 100 μg/mL 时没有表现出明显的细胞毒性。PCs 治疗逆转了由 PA 诱导的细胞凋亡率升高和 GSIS 受损。PC 显着降低细胞内 ROS 和 MDA 的产生并增加 SOD 活性。此外，PC 促进 Akt 和 FoxO1 的磷酸化，并调节 MIN6 细胞中 Pdx-1 和 Bax 的表达。讨论和结论：在 R. amabilis 中作为降糖药的活性成分是原花青素，它通过激活 PI3K/Akt/FoxO1 信号保护 MIN6 细胞免受 PA 诱导的细胞凋亡。这些结果表明 β 细胞提取结合 UPLC/MS，