Biological Activities of Chemically Synthesized Derivatives of Lipid A : Tetraacetyl-monosaccharides Linked to 2,3-Acyloxyacylglucosamine-4-phosphate

概要

論文の詳細を見る
The mitogenicity and lethal toxicity of chemically synthesized lipid A analogs, in which 2,3-acyloxyacyl-glucosamine-4-phosphate (acyl-GlcN-4P) is linked to a tetraacetyl (Ac_4)-monosaccharide, i.e., Ac_4-glucose (A-211), Ac_4-mannose (A-212), Ac_4-galactose (A-213) or Ac_4-glucosamine (A-214), were compared with those of tetraacetyl-3-deoxy-D-manno-2-octulosonic acid (Ac_4-KDO) linked to acyl-GlcN-4P (A-203). All the compounds ewre capable of increasing incorporation of ^3H-thymidine into splenocytes of C57BL/6 mice at doses of 50 and 100 μg/ml, but the mitogenic activity of A-203 at these doses seems to be stronger than those of the analogs. Intravenous injection of A-203,A-211,and A-213 did not exhibit lethal toxicity even at a high dose (50 μg/mouse) in C57BL/6 mice loaded with D-galactosamine hydrochloride. However, A-212 and A-214 showed lethality at the doses of 10 and 50 μg/mouse, respectively. The findings indicate that the biological activity of these compounds is affected by the kind of monosaccharide linked to acyl-GlcN-4P.
社団法人日本薬学会の論文
1989-09-25