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1.
Bioorg Med Chem Lett ; 29(13): 1549-1554, 2019 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-31054863

RESUMO

Chemotherapy is one of the standard methods for the treatment of malignant tumors. It aims to cause lethal damage to cellular structures, mainly DNA. Noteworthy, in recent years discoveries of novel anticancer agents from well-known antibiotics have opened up new treatment pathways for several cancer diseases. The aim of this review article is to describe new applications for the following antibiotics: doxycycline (DOX), salinomycin (SAL), monensin (MON) and ivermectin (IVR) as they are known to show anti-tumor activity, but have not yet been introduced into standard oncological therapy. To date, these agents have been used for the treatment of a broad-spectrum of bacterial and parasitic infectious diseases and are widely available, which is why they were selected. The data presented here clearly show that the antibiotics mentioned above should be recognised in the near future as novel agents able to eradicate cancer cells and cancer stem cells (CSCs) across several cancer types.


Assuntos
Antineoplásicos/uso terapêutico , Doxiciclina/uso terapêutico , Ivermectina/uso terapêutico , Monensin/uso terapêutico , Neoplasias/tratamento farmacológico , Piranos/uso terapêutico , Antineoplásicos/farmacologia , Doxiciclina/farmacologia , Humanos , Ivermectina/farmacologia , Monensin/farmacologia , Piranos/farmacologia
2.
Artigo em Chinês | WPRIM | ID: wpr-581630

RESUMO

C1027, an anticancer antibiotic, showed extremely potent cytotoxicity against cultured cancer cells, being over 10,000-fold more potent than adriamycin. C1027 acted rapidly; DNA synthesis of hepatoma cells was suppressed within 10 mintus of exposure. C1027 consists of two moieties, a new enediyne chromophore and an apoprotein; the chromophore serves as the active part of the molecule. C1027 molecule can be dissociated and reconstituted. The reconstituted C1027 was as potent as natural C1027. Through a newly developed method, enriched conjugation C1027 was conjugated to monoclonal antibodies. As determined by clonogenic assay, the conjugates displayed highly-potent, specific cytotoxicity to target cancer cells. The conjugates exerted marked therapeutic effects against hepatoma and gastric cancer xenografts in nude mice; at tolerable dose, tumor inhibition rate reached 85% (P

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