5-脂氧合酶抑制剂（3-硝基-2,4,6-三羟基苯甲酰胺衍生物）对佛波酯促进的BALB 3T3细胞转化的抗促进作用。

Antipromoting effects of 5-lipoxygenase inhibitors, 3-nitro-2,4,6- trihydroxybenzamide derivatives, on TPA-promoted transformation in BALB 3T3 cells.

作者信息

Semba M, Honda I, Shibagaki M, Nishi Y

机构信息

Quality Assurance Unit, Hatano Research Institute, Food and Drug Safety Center, Kanagawa, Japan.

出版信息

Cancer Lett. 1993 Jul 30;71(1-3):57-60. doi: 10.1016/0304-3835(93)90097-s.

DOI:10.1016/0304-3835(93)90097-s

PMID:8364900

Abstract

In order to discover the role in the promotion process of 5-lipoxygenase (5-LO), a key enzyme in the arachidonate cascade, the antipromoting effects of the 5-LO inhibiting 3-nitro-2,4,6-trihydroxybenzamide (NTB) derivatives were studied in a two-stage transformation assay system using BALB 3T3 cells. All compounds inhibited TPA-promoted transformation in a dose-dependent manner. Most of them achieved a 70-80% inhibition. Good correlations were observed between the inhibition of TPA-promoted transformation and that of 5-LO. These results indicate that 5-LO plays an important role in the promotion stage of the transformation of BALB 3T3 cells.

摘要

为了发现5-脂氧合酶（5-LO）（花生四烯酸级联反应中的关键酶）在促进过程中的作用，在使用BALB 3T3细胞的两阶段转化试验系统中研究了5-LO抑制性3-硝基-2,4,6-三羟基苯甲酰胺（NTB）衍生物的抗促进作用。所有化合物均以剂量依赖性方式抑制TPA促进的转化。其中大多数实现了70-80%的抑制率。在TPA促进的转化抑制与5-LO抑制之间观察到良好的相关性。这些结果表明，5-LO在BALB 3T3细胞转化的促进阶段起重要作用。