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Title 

Naphthazarin derivatives(V): formation of glutathione conjugate and cytotoxic activity of 2-or 6-substituted 5,8-dimethoxy-1,4-napthoquinones in the presence of glutathinoe-S-transferase, in rat liver S-9 fraction and mouse liver perfusate

Authors 

Xiang Guo ZhengJong Seong KangHwan Mook KimGuang Zhu JinByung Zun Ahn

Publisher 

Pharmaceutical Society of Korea

Issue Date 

2000

Citation 

Archives of Pharmacal Research, vol. 23, no. 1, pp. 22-25

Keywords 

naphthazarin derivativesformation of glutathione conjugatesglutathione-S-transferaserat liver S-9 fractionmouse liver perfusion

Abstract 

Formation of glutathione (GSH) conjugates with 2- or 6-(1-hydroxymethyl)- and 2-(1-hydroxyethyl)-DMNQ derivatives (DMNQ, 5,8-dimethoxy-1,4-naphthoquone) was carried out in phosphate buffer (pH 7.4), in the presence of glutathione-S-transferase (GST), in rat liver S-9 fraction and by perfusion, and the rates of conjugates formation were compared and correlated to cytotoxicity. The GSH conjugates of 6-(1-hydroxyalky1)-DMNQ derivatives were formed faster than 2-(1-hydroxyalkyl)-DMNQ derivatives under all of the media, implying that steric hindrance was the cause of lowering the rate of conjugate formation of 2-substituted derivatives. For both isomers, addition of GST did not improve the reaction rate, compared with that in buffer, while the reaction in the S-9 fraction and the perfusate was accelerated to a great extent. The catalytic effect of the S-9 fraction and the perfusion on 2-isomers was greater than on 6-substituted ones, suggesting that S-9 fraction and the perfusate contain an effective system relaxing the steric hindrance of 2-(1-hydroxyalkyl)-DMNQ derivtives. Furthermore, a good correlation between the formation of the GSH conjugates and the cytotoxic activity of both naphthazarin isomers suggests that the steric hindrance is a cause of lowering the cytotoxicity of 2-isomers.

ISSN 

0253-6269

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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