Cytotoxic effect of radiolabeled C5a on U937 cells in vitro

We studied whether the receptor (R) for C5a could be exploited to deliver the radiolabeled ligand into U937 cells. A doseresponse for uptake of 125I-C5a was demonstrated. Incorporation of [3H]leucine by unstimulated or γ-INF-stimulated U937 cells treated with 125I-C5a, was significantly lower compared with cells treated with 125I alone. Trypan blue exclusion experiments indicated that γ-INF stimulated cells incubated with 125I-C5a were less viable than cells exposed to 125I or C5a alone. The results suggest that 125I-C5a is internalized into myeloid cells via C5a-R and is more cytotoxic in vitro than the radiolabel alone, but only at/above a specific activity of 4 μCi/μg.