Wick M M
J Invest Dermatol. 1978 Aug;71(2):163-4. doi: 10.1111/1523-1747.ep12546959.1.
L-dopa methyl ester has been shown to be an effective antitumor agent against the B-16 melanoma in vivo. We have now examined the analog, dopamine, a major catabolite of L-dopa. Dopamine administration at a daily dose of 600 mg/kg resulted in a 48% (p less than .001) increase in survival of treated mice as compared to non-treated controls. In vitro, an effect similar to that observed with L-dopa methyl ester was noted, specifically, a rapid and profound inhibition of thymidine incorporation with little effect on uridine or leucine incorporation. We have postulated that the inhibition of a DNA polymerase might be the site of action of these novel antitumor agents.
L-多巴甲酯已被证明是一种在体内对B-16黑色素瘤有效的抗肿瘤剂。我们现在研究了其类似物多巴胺,L-多巴的一种主要分解代谢产物。与未治疗的对照组相比,每天以600mg/kg的剂量给予多巴胺,使治疗小鼠的存活率提高了48%(p<0.001)。在体外,观察到了与L-多巴甲酯类似的效果,具体而言,对胸苷掺入有快速而显著的抑制作用,而对尿苷或亮氨酸掺入的影响很小。我们推测,抑制DNA聚合酶可能是这些新型抗肿瘤剂的作用位点。