In vitro evaluation of the growth inhibitory activities of 15 drugs against Babesia gibsoni (Aomori strain)

Apicoplast-Targeting Antibacterials Inhibit the Growth of Babesia Parasites

“…Ciprofloxacin and thiostrepton were more effective than rifampin in the cultures with a high initial parasitemia. The IC 50 s of the three apicoplast inhibitors for Babesia parasites were lower than those of other drugs used in previous studies, including ketoconazole (13), gossypol (15), heparin (14), EGTA (52), clindamycin phosphate, and chloroquine diphosphate (45). The IC 50 s for Babesia parasites were in a similar range to those for other drugs tested as babesicidal drugs, including triclosan (11), clotrimazole (12,13), tetracyclines (45,51), staurosporine (18), purvalanol A (49), N-acetyl-leucinyl-leucinyl-norleucinal (ALLN) (53), (Ϫ)-epigallocatechin-3-gallate (EGCG) (2), and nerolidol (3).…”

“…The IC 50 s of the three apicoplast inhibitors for Babesia parasites were lower than those of other drugs used in previous studies, including ketoconazole (13), gossypol (15), heparin (14), EGTA (52), clindamycin phosphate, and chloroquine diphosphate (45). The IC 50 s for Babesia parasites were in a similar range to those for other drugs tested as babesicidal drugs, including triclosan (11), clotrimazole (12,13), tetracyclines (45,51), staurosporine (18), purvalanol A (49), N-acetyl-leucinyl-leucinyl-norleucinal (ALLN) (53), (Ϫ)-epigallocatechin-3-gallate (EGCG) (2), and nerolidol (3). The IC 50 s of the three inhibitors were higher than the IC 50 s of other babesicidal drugs, including quinuronium sulfate (21), imidocarb dipropionate (19,59), clindamycin phosphate (19), atovaquone (45,55), and epoxomicin (1).…”

“…The IC 50 s for Babesia parasites were in a similar range to those for other drugs tested as babesicidal drugs, including triclosan (11), clotrimazole (12,13), tetracyclines (45,51), staurosporine (18), purvalanol A (49), N-acetyl-leucinyl-leucinyl-norleucinal (ALLN) (53), (Ϫ)-epigallocatechin-3-gallate (EGCG) (2), and nerolidol (3). The IC 50 s of the three inhibitors were higher than the IC 50 s of other babesicidal drugs, including quinuronium sulfate (21), imidocarb dipropionate (19,59), clindamycin phosphate (19), atovaquone (45,55), and epoxomicin (1). The IC 50 s of clindamycin phosphate reported in the present study were in a similar range to those for B. gibsoni (44).…”

“…Clindamycin phosphate was used as a control, at concentrations of 0.5, 5, 100, and 500 M (28,47). Diminazene aceturate was compared with antibacterials at concentrations of 1, 5, 10, 50, 100, 1,000, and 2,000 nM (45). To evaluate inhibitory effects in the presence of high parasitemia (to resemble acute cases of infection), other parasite cultures were adjusted to 10% initial parasitemia for B. bovis and to 7% initial parasitemia for B. bigemina (10).…”

Artemisone Uptake in Plasmodium falciparum -Infected Erythrocytes

“…(7,8). Interestingly, while chloroquine (an accepted inhibitor of hemozoin formation) is only a fewfold less potent than DHA against sensitive P. falciparum strains in vitro, it is nearly 200 times less potent than DHA against Babesia gibsoni (16). Furthermore, artemisone itself is not readily decomposed in model studies involving heme-Fe(II) under aqueous conditions (10).…”