Loureirin B (LB) is a natural product derived from Sanguis draconis, which has hypoglycaemic effects. In order to research the possible target of LB in the treatment of diabetes, molecular docking was used to simulate the interaction between LB and potential targets, and among them, glucagon‐like peptide‐1 receptor (GLP‐1R) had the optimal results. Further, spectroscopy and surface plasmon resonance (SPR) experiments were applied to detect the interaction between LB and GLP‐1R. Ultimately, after GLP‐1R siRNA interfering the expression of GLP‐1R in Ins‐1 cell, the promoting insulin secretion of LB was weaken, which directly proved that GLP‐1R plays an important role. These results show that LB promotes insulin secretion of Ins‐1 cells through GLP‐1R. Hence, the strategy of LB as a prodrug will provide a potential approach for non‐peptide GLP‐1R agonist.

中文翻译：

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Loureirin B 激活 GLP-1R 并促进 Ins-1 细胞中的胰岛素分泌

Loureirin B (LB) 是一种源自血龙血的天然产物，具有降血糖作用。为了研究LB治疗糖尿病的可能靶点，采用分子对接模拟LB与潜在靶点的相互作用，其中胰高血糖素样肽-1受体（GLP-1R）效果最佳。此外，光谱学和表面等离子共振 (SPR) 实验被用于检测 LB 和 GLP-1R 之间的相互作用。最终，GLP-1R siRNA干扰Ins-1细胞中GLP-1R的表达后，LB对胰岛素分泌的促进作用减弱，直接证明GLP-1R发挥了重要作用。这些结果表明，LB 通过 GLP-1R 促进 Ins-1 细胞的胰岛素分泌。因此，