An antiprotozoan antibiotic
Ikarugamycin is a macrocyclic antibiotic first isolated from Streptomyces sp. that demonstrates potent antiprotozoal activity.[1] It exhibits cytotoxic effects in cancer cell lines, inhibiting cell proliferation (IC50 = 221.3 nM in HL-60 cells) through genotoxicity and by inducing apoptosis and activation of caspases.[2] It also was shown to significantly inhibit oxidized low-density lipoprotein-induced accumulation of cholesteryl esters in macrophages at 1-4 μM.[3] Additionally, ikarugamycin is used to inhibit clathrin-coated pit-mediated endocytosis.[4]
Reference:
[1]. Jomon, K., Kuroda, Y., Ajisaka, M., et al. A new antibiotic, ikarugamycin. J.Antibiot.(Tokyo) 25(5), 271-280 (1972).
[2]. Popescu, R., Heiss, E.H., Ferk, F., et al. Ikarugamycin induces DNA damage, intracellular calcium increase, p38 MAP kinase activation and apoptosis in HL-60 human promyelocytic leukemia cells. Mutation Research 709-710, 60-66 (2011).
[3]. Hasumi, K., Shinohara, C., Naganuma, S., et al. Inhibition of the uptake of oxidized low-density lipoprotein in macrophage J774 by the antibiotic ikarugamycin. European Journal of Biochemistry 205(2), 841-846 (1992).
[4]. Luo, T., Fredericksen, B.L., Hasumi, K., et al. Human immunodeficiency virus type 1 Nef-induced CD4 cell surface downregulation is inhibited by ikarugamycin. Journal of Virology 75(5), 2488-2492 (2001).
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