组织工程与重建外科杂志 ›› 2025, Vol. 21 ›› Issue (2): 172-.

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托伐普坦抑制B16F10细胞黑色素合成的机制研究

  

  • 出版日期:2025-04-01 发布日期:2025-05-13

Study on the mechanism of tolvaptan inhibiting melanogenesis in B16F10 cells

  • Online:2025-04-01 Published:2025-05-13

摘要: 目的 研究托伐普坦在黑色素合成中的作用和机制。方法 本研究以B16F10细胞为模型,通过细胞活性检 测及黑色素含量测定,观察托伐普坦对细胞活力及黑色素含量的影响。通过酪氨酸酶活性检测,观察托伐普坦对细胞 酪氨酸酶(TYR)活性的影响;通过蛋白免疫印迹实验,检测托伐普坦对TYR家族和其他参与黑色素合成的蛋白质表达 水平的影响。结果 细胞活性检测和黑色素含量测定显示,托伐普坦在不影响细胞活力的情况下,能显著降低细胞内 黑色素含量。酪氨酸酶活性检测显示,托伐普坦不影响TYR的催化活性。蛋白免疫印迹实验显示,托伐普坦下调TYR 家族蛋白、小眼相关转录因子(MITF)、环腺苷酸反应元件结合蛋白(CREB)和黑素皮质素 1受体(MC1R)的表达水平。 结论 托伐普坦具有抑制黑色素合成的作用,其作用机制可能是通过MC1R/cAMP信号通路实现的。

关键词: 托伐普坦,  B16F10细胞,  黑色素,  环磷酸腺苷,  黑素皮质素1受体

Abstract: Objective  To investigate the effects and mechanism of tolvaptan on melanogenesis. Methods  This study used B16F10 cells as a model. The effects of tolvaptan on cell viability and melanin content were evaluated through cell viability assays and melanin content quantification. The effect of tolvaptan on tyrosinase (TYR) activity was observed by tyrosinase activity detection. Western blot analysis was employed to investigate the impact of tolvaptan on the expression levels of TYR family proteins and other key proteins involved in melanogenesis. Results Cell viability assays and melanin content quantification demonstrated that tolvaptan significantly reduced intracellular melanin levels without compromising cellular viability. Tyrosinase activity assays revealed no inhibitory effect of tolvaptan on TYR catalytic function. Western blot analysis indicated that tolvaptan downregulated the protein expression of TYR family members, microphthalmia-associated transcription factor (MITF), cAMP-responsive element-binding protein (CREB), and melanocortin 1 receptor (MC1R). Conclusion Tolvaptan can inhibit melanogenesis, and the molecular mechanism may be achieved through the MC1R/cAMP signaling pathway.

Key words: Tolvaptan,  B16F10 cells,  Melanin,  cAMP,  MC1R