Yang Guang, Yan Yao, Ma Younan, Yang Yixin
Department of Biological Sciences, Emporia State University, Emporia, Kansas.
Mol Carcinog. 2017 Aug;56(8):1965-1976. doi: 10.1002/mc.22654. Epub 2017 Apr 24.
Vitamin C has been used in complementary and alternative medicine for cancers regardless of its ineffectiveness in clinical trials and the paradoxical effects antioxidants have on cancer. Vitamin C was found to induce cytotoxicity against cancers. However, the mechanisms of action have not been fully elucidated, and the effects of vitamin C on human malignant melanoma have not been examined. This study revealed that vitamin C at millimolar concentrations significantly reduced the cell viability as well as invasiveness, and induced apoptosis in human malignant melanoma cells. Vitamin C displayed stronger cytotoxicity against the Vemurafenib-resistance cell line A2058 compared with SK-MEL-28. In contrast, vitamin C at micromolar concentrations promoted cell growth, migration and cell cycle progression, and protected against mitochondrial stress. Vemurafenib paradoxically activated the RAS-RAF-MEK-ERK signaling pathway in the Vemurafenib-resistant A2058, however, vitamin C abolished the activations. Vitamin C displayed synergistic cytotoxicity with Vemurafenib against the Vemurafenib-resistant A2058. In vivo assay suggested that lower dosage (equivalent to 0.5 g/70 kg) of vitamin C administered orally increased the melanoma growth. Therefore, vitamin C may exert pro- or anti-melanoma effect depending on concentration. The combination of vitamin C at high dosage and Vemurafenib is promising in overcoming the action of drug resistance.
尽管维生素C在临床试验中无效,且抗氧化剂对癌症有矛盾的影响,但它已被用于癌症的补充和替代医学中。维生素C被发现可诱导对癌症的细胞毒性。然而,其作用机制尚未完全阐明,且维生素C对人类恶性黑色素瘤的影响尚未得到研究。本研究表明,毫摩尔浓度的维生素C可显著降低人类恶性黑色素瘤细胞的活力和侵袭性,并诱导其凋亡。与SK-MEL-28相比,维生素C对维莫非尼耐药细胞系A2058显示出更强的细胞毒性。相反,微摩尔浓度的维生素C促进细胞生长、迁移和细胞周期进程,并保护细胞免受线粒体应激。维莫非尼反常地激活了维莫非尼耐药的A2058中的RAS-RAF-MEK-ERK信号通路,然而,维生素C消除了这种激活。维生素C与维莫非尼对维莫非尼耐药的A2058显示出协同细胞毒性。体内试验表明,口服较低剂量(相当于0.5 g/70 kg)的维生素C会增加黑色素瘤的生长。因此,维生素C可能根据浓度发挥促黑色素瘤或抗黑色素瘤作用。高剂量维生素C与维莫非尼联合使用有望克服耐药作用。