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1 mg
5 mg
10 mg
1 mM
1.3316 mL
6.6578 mL
13.3156 mL
5 mM
0.2663 mL
1.3316 mL
2.6631 mL
10 mM
0.1332 mL
0.6658 mL
1.3316 mL
50 mM
0.0266 mL
0.1332 mL
0.2663 mL
Description
Salinomycin (Coxistac, Bio-cox, Procoxacin), traditionally used as an anti-coccidial drug, has recently been shown to possess anti-cancer and anti-cancer stem cell (CSC) effects.
Salinomycin, a polyether ionophore antibiotic isolated from Streptomyces albus, has been shown to kill CSCs in different types of human cancers, most likely by interfering with ABC(ATP-binding cassette) drug transporters, the Wnt/β-catenin signaling pathway, and other CSC pathways. Salinomycin exhibits antimicrobial activity against Gram-positive bacteria including Bacillus subtilis, Staphylococcus aureus, Micrococcus flavus, Sarcina lutea, Mycobacterium spp., some filamentous fungi, Plasmodium falciparum, and Eimeria spp., protozoan parasites responsible for the poultry disease coccidiosis. In addition, salinomycin has early been shown to act in different biological membranes, including cytoplasmic and mitochondrial membranes, as a monovalent cation ionophore with strict selectivity for alkali ions and a strong preference for K+, thereby promoting mitochondrial and cytoplasmic K+ efflux and inhibiting oxidative phosphorylation. Salinomycin can induce massive apoptosis in human cancer cells of different origin that display multiple mechanisms of drug and apoptosis resistance.
In vivo
Salinomycin is able to effectively eliminate CSCs and to induce partial clinical regression of heavily pretreated and therapy-resistant cancers. It has also been demonstrated as a positive ionotropic and chronotropic agent that increased cardiac output, left ventricular systolic pressure, heart rate, mean arterial pressure, coronary artery vasodilatation and blood flow, and plasma catecholamine concentration. These results have been obtained in experiments with mongrel dogs that has received a single intravenous injection of 150 μg/kg salinomycin. However, It has been reported with a considerable toxicity of salinomycin in mammals, such as horses, pigs, cats, and alpacas after accidental oral or inhalative intake. Risk assessment data recently published by the European Food Safety Authority declare an acceptable daily intake (ADI) of 5 μg/kg salinomycin for humans, because daily intake of more than 500 μg/kg salinomycin by dogs leads to neurotoxic effects, such as myelin loss and axonal degeneration. Intravenous administration of 200-250 μg/kg salinomycin every second day for three weeks results in partial regression of tumor metastasis and shows only minor acute and long-term side effects, but no severe acute and long-term side effects observed with conventional chemotherapeutic drugs.
Stereoisomer of α-ethyl-6-[5-[2-(5-ethyltetrahydro-5-hydroxy-6-methyl-2H-pyran-2-yl)-15-hydroxy-2,10,12-trimethyl-1,6,8-trioxadispiro[4.1.5.3]pentadec-13-en-9-yl]-2-hydroxy-1,3-dimethyl-4-oxoheptyl]tetrahydro-5-methyl-2H-pyran-2-acetic acid
Antibiotic 61477
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