Wilson G D, d'Arcy Doherty M, Cohen G M
Br J Cancer. 1985 Jun;51(6):853-63. doi: 10.1038/bjc.1985.131.
1-Naphthol was selectively toxic to human colorectal tumours compared to corresponding normal colonic tissue removed at surgery and maintained in short-term organ culture. Nineteen of 24 tumours studied have shown a significant differential response. Three human colonic adenocarcinoma xenografts, in the short-term organ culture system, displayed the same response to 1-naphthol as primary tumours removed at surgery. 1-Naphthol, 1,2- and 1,4-naphthoquinone were also toxic to two human colonic adenocarcinoma cell lines, LoVo and COLO 206. The selective toxicity of 1-naphthol is mediated in part through an accumulation of 1-naphthol in the tumour tissue due to impaired conjugation by the tumour. The higher concentrations of 1-naphthol may then exert their toxicity either directly or by formation of naphthoquinones. Some indirect evidence was obtained for the possible involvement of 1,2- or 1,4-naphthoquinone in the cytotoxicity of 1-naphthol. Our studies suggest that further studies are warranted of the possible use of 1-naphthol or related compounds as antitumour agents.
与手术切除并在短期器官培养中维持的相应正常结肠组织相比,1-萘酚对人类结肠肿瘤具有选择性毒性。在研究的24个肿瘤中,有19个显示出显著的差异反应。在短期器官培养系统中,三种人类结肠腺癌异种移植瘤对1-萘酚的反应与手术切除的原发性肿瘤相同。1-萘酚、1,2-萘醌和1,4-萘醌对两种人类结肠腺癌细胞系LoVo和COLO 206也有毒性。1-萘酚的选择性毒性部分是由于肿瘤结合功能受损导致1-萘酚在肿瘤组织中蓄积介导的。较高浓度的1-萘酚可能直接发挥毒性作用,或通过形成萘醌发挥毒性作用。获得了一些间接证据,表明1,2-或1,4-萘醌可能参与了1-萘酚的细胞毒性作用。我们的研究表明,有必要进一步研究1-萘酚或相关化合物作为抗肿瘤药物的可能性。