Title : In vitro influences of alcohols on mouse synaptosomes, and structure-activity relationships - Tanii_1995_Arch.Toxicol_69_617 |
Author(s) : Tanii H , Zhang XP , Ohyashiki T |
Ref : Archives of Toxicology , 69 :617 , 1995 |
Abstract :
Little information is available on the structure-central nervous system membrane toxicity relationship of alcohols. The purpose of the present study was to study in vitro influence of alcohols (n = 20) on the activity of the toxic indicator Na+/K(+)-adenosine triphosphatase (Na+/K(+)-ATPase) and acetylcholinesterase (AchE), and membrane fluidity in mouse brain synaptosomes, in terms of the structure-activity relationship. The potency of inhibition for the enzymes (IC50) and the potency of increasing membrane fluidity (IC12.5) were determined experimentally, and n-octanol/water partition coefficient (P) and the steric constant Taft Es are cited from the literature. Regression analysis revealed that log 1/IC50 for Na+/K(+)-ATPase is a function of log P and Taft Es. The situation was true for AchE activity. The results indicate that the hydrophobicity expressed as log P and the steric effect of the alcohols play an important role in inhibiting both enzyme activities. A linear relationship between log 1/IC12.5 for membrane fluidity and log P is shown, indicating a significant effect of the alcohols on membrane fluidity. Based on these results, it is suggested that the alcohols inhibit the Na+/K(+)-ATPase and AchE activity through a direct action on the enzymes and/or through changing the membrane fluidity. |
PubMedSearch : Tanii_1995_Arch.Toxicol_69_617 |
PubMedID: 8660139 |
Tanii H, Zhang XP, Ohyashiki T (1995)
In vitro influences of alcohols on mouse synaptosomes, and structure-activity relationships
Archives of Toxicology
69 :617
Tanii H, Zhang XP, Ohyashiki T (1995)
Archives of Toxicology
69 :617