[Inhibition of sodium artesunate on rat erythrocyte membrane Na(+)-K(+)-exchanging ATPase in vitro].
OBJECTIVE
To study the effects of sodium artesunate (SA) on Na(+)-K(+)-exchanging ATPase activity of rat erythrocyte membrane in vitro.


METHODS
SA of different concentrations (0, 0.5, 1, 5 and 10 mumol . L-1) were added respectively in the reaction system. The Na(+)-K(+)-exchanging ATPase activity was calculated by measuring the amount of inorganic phosphate released in the reaction system.


RESULTS
Along with the increase of SA concentration (0, 0.5, 1, 5 and 10 mumol . L-1), the Na(+)-K(+) -exchanging ATPase activity decreased, the inhibitory rates were 15%, 29%, 46%, and 75%, respectively. Increasing the concentration of substrate ATP to 125, 250, 375 and 500 mumol . L-1 and determining the kinetics of enzyme. Making the Eadie-Hofstee kinetic curve by linear-regression analysis. The result revealed that the inhibitory effect of SA on the enzyme was competitive.


CONCLUSIONS
SA affected the ion transfer of host erythrocyte membrane and membrane function.
Wang
J Y
JY
Institute of Microbiology and Epidemiology, Academy of Military Medical Sciences, Beijing, China.
Yuan
L Z
LZ
Wang
M D
MD
D000818:Animals; D037621:Artemisinins; D000077332:Artesunate; D004910:Erythrocyte Membrane / Q000187:drug effects / Q000201:enzymology*; D005260:Female; D066298:In Vitro Techniques; D051381:Rats; D017208:Rats, Wistar; D012717:Sesquiterpenes / Q000494:pharmacology*; D000254:Sodium-Potassium-Exchanging ATPase / Q000378:metabolism*
D037621:Artemisinins; D012717:Sesquiterpenes; D000077332:Artesunate; D000254:Sodium-Potassium-Exchanging ATPase