Inhibition of the uptake of oxidized low‐density lipoprotein in macrophage J774 by the antibiotic ikarugamycin

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Abstract
The antiprotozoal antibiotic ikarugamycin was found to significantly inhibit oxidized low‐density lipoprotein(LDL)‐induced accumulation of cholesteryl ester in macrophage J774 at a concentration over 1–4 μM. Cholesteryl ester synthesis from [14C]oleate in the macrophages was similarly inhibited by the antibiotic, while the synthesis of triacylglycerol and polar lipids was not affected. The internalization of oxidized [125I]LDL in macrophages was reduced to 50% by 2 μM ikarugamycin, while cell‐surface binding of oxidized [125I]LDL, lysosomal hydrolysis of the internalized oxidized [125I]LDL and microsomal acyl‐coenzyme A: cholesterol acyltransferase was not detectably inhibited by 5 μM ikarugamycin. The results demonstrated that ikarugamycin inhibited cholesteryl ester accumulation in macrophage J774 by specifically inhibiting the uptake of oxidized LDL.