Antitumor Activity and Lethal Toxicity of Chemically Synthesized Tetraacetyl-2-keto-3-deoxyoctonic Acid-(α2→6)-D-glucosamine Analogues of Lipid A(Biological)

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The antitumor activity and lethal toxicity of three acylated derivatives of chemically synthesized 4-O-monophosphorylglucosamine-linked tetraacetyl 2-keto-3-deoxyoctonic acid (KDO) were determined. Although the antitumor activity of the compounds against ascites form of Ehrlich carcinoma in ddY mice was weaker than that of natural lipopolysaccharide, compound A-203, with di-3-tetradecanoyloxytetradecanoyl at the C-2 and C-3 positions, was effective. Compounds A-204 (di-3-dodecanoyloxytetradecanoyl) and A-205 (3-dodecanoyloxytetradecanoyl and 3-tetradecanoyloxytetradecanoyl) produced longer survival than the control group, but the differences were not significant. On the other hand, the lethal toxicity oi' A-205 in C57BL/6 mice loaded with galactosamine was most potent among the three compounds, whereas A-203 did not show lethality even at a high dose (50μg/mouse). However, the antitumor activity and lethal toxicity of the derivatives of 4-O-monophosphorylglucosamine-linked tetraacetyl-KDO did not differ from those of KDO-free 4-O-monophosphorylglucosamine derivatives.
1987-02-25