Department of Endocrinology and Metabolism, Henan Provincial People's Hospital, Zhengzhou University, PR China.
Department of Endocrinology and Metabolism, Xinhua Hospital, Shanghai Jiaotong University School of Medicine, PR China.
Biochem Biophys Res Commun. 2014 Feb 21;444(4):451-4. doi: 10.1016/j.bbrc.2013.11.136. Epub 2014 Jan 31.
Glucose-stimulated insulin secretion (GSIS) is essential for the control of metabolic fuel homeostasis and its impairment is a key element in the failure of β-cells in type 2 diabetes. Trans-caryophyllene (TC), an important constituent of the essential oil of several species of plants, has been reported to activate the type 2 cannabinoid receptor (CB2R). The effects of TC on GSIS are still unknown. Our results demonstrate that administration of TC in MIN6 cells promotes GSIS in a dose dependent manner. However, inhibition of CB2R by a specific inhibitor or specific RNA interference abolished the effects of TC on GSIS, which suggests that the effects of TC on GSIS are dependent on activation of CB2R. Further study demonstrated that treatment with TC leads to the activation of small G protein Arf6 as well as Rac1 and Cdc42. Importantly, Arf6 silencing abolished the effects of TC on GSIS, which suggests that Arf6 participates in mediating the effects of TC on GSIS. We conclude from these data that TC has a novel role in regulating GSIS in pancreatic β-cells.
葡萄糖刺激的胰岛素分泌（GSIS）对于代谢燃料稳态的控制至关重要，其功能障碍是 2 型糖尿病中β细胞衰竭的关键因素。β-石竹烯（TC）是几种植物精油的重要成分，据报道它可以激活 2 型大麻素受体（CB2R）。TC 对 GSIS 的影响尚不清楚。我们的结果表明，TC 在 MIN6 细胞中的给药以剂量依赖的方式促进 GSIS。然而，通过特定抑制剂或特异性 RNA 干扰抑制 CB2R 会消除 TC 对 GSIS 的作用，这表明 TC 对 GSIS 的作用依赖于 CB2R 的激活。进一步的研究表明，TC 的处理导致小 G 蛋白 Arf6 以及 Rac1 和 Cdc42 的激活。重要的是，Arf6 沉默消除了 TC 对 GSIS 的作用，这表明 Arf6 参与介导 TC 对 GSIS 的作用。我们从这些数据中得出结论，TC 在调节胰岛β细胞中的 GSIS 方面具有新的作用。
