SYNTHESIS AND BIOLOGICAL ACTIVITIES OF BISCARBOXYMETHYL LIPID A ANALOGUES

摘要

Biscarboxymethyl analogues of Escherichia coli lipid A and the biosynthetic precursor-type lipid A were synthesized in order to elucidate the role of the acidic functional groups in the biological activity.Both analogues showed respective activities similar to those of their natural counterparts,i.e.,the hexaacyl E.coli lipid A analogue showed potent immunostimulating activity,whereas the tetraacylated biosynthetic precursor-type lipid A analogue showed the antagonistic activity.The present study clearly indicates that the acidic functional groups but not phosphate groups are essential for the expression of the biological activities.