Purpose. The aim of this study is to investigate the plasma protein bi
nding of nicanartine and to measure its antioxidant effect on lipoprot
eins. Methods. The blood binding was studied with an erythrocyte parti
tioning method and the lipoprotein oxidation with the conjugated diene
s method. Results. Nicanartine was 24.7% LDL (low density lipoprotein)
-bound and 29.2% AAG (alphal-acid glycoprotein)-bound. Nicanartine del
ayed but did not stop the oxidation of the three density classes of li
poprotein HDL (high density lipoprotein), LDL, VLDL (very low density
lipoprotein). The addition of AAG to LDL in the conjugated dienes meth
od decreased the nicanartine fraction bound to LDL and decreased its a
ntioxidant effect. The decrease of nicanartine LDL-bound fraction and
the decrease in antioxidant effect were not parallel. Conclusions. Thi
s suggested that (a) AAG-bound nicanartine dissociated to equilibrate
the decrease in LDL-bound nicanartine consumed by oxidation, or (b) th
e oxidation conditions could involve chemical modifications of nicanar
tine and therefore modify its affinity for AAG.