Synthesis and carbohydrate-binding activity of poly(ethyl-eneglycol)-Ricinus communis agglutinin I conjugates

The synthesis of poly(ethyleneglycol) (PEG)-lectin conjugates was investigated to provide new reagents for evaluation as biological response modifiers. PEG was activated with 1,1′-carbonyldiimidazole (CDI), followed by conjugation with Ricinus communis I (RCAI) lectin. The resulting conjugates were heterodisperse with respect to molecular weight. Carbohydrate-binding activity was retained. The conjugates were separated by affinity chromatography into fractions differing in apparent carbohydrate-binding affinity. Conjugation of RCAI with PEG4 (mol.wt. 3350) or PEG 6 (mol.wt.8000) appeared to provide less hindrance of the lectin binding site compared to conjugates prepared with PEG 20 (mol.wt. 20 000). Results of free amine assays indicated that higher ratios of PEG to RCAI in conjugates correlated with loss of low-affinity binding and retention of high-affinity binding. The data showed the feasibility of preparing PEG-lectin conjugates for in vivo use.