Abstract
Oxidized carboxymethyl-D-manno-D-glucan (MG-CM-AD)-DXR conjugates were prepared via Schiff's base formation and compared tissue distribution of the conjugates with that of DXR. The water-soluble conjugates, which had DXR contents of 11∼13% (w/w) and degrees of substitution(DS)of CM groups of 0.5∼1.0, released DXR with an increase in the DS values in 50 mM phosphate buffer(pH 7.4)at 37°C. The conjugates showed higher plasma and tumor concentration but lower heart concentration than DXR at 24 hr after the intravenous injection into Walker 256 bearingrat. The area under the concentration-time curve from 0 to 48 hr of MG-CM [0.5]-AD-DXR(DS of CM groups : 0.5) was 2 times higher on tumor, but 2 times lower on heart than that of DXR. These findings suggest that MG-CM [0.5]-AD-DXR should exhibit a higher antitumor effect and less toxicity than DXR.
