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1.
Future Med Chem ; 11(7): 677-691, 2019 04.
Article in English | MEDLINE | ID: mdl-30947530

ABSTRACT

Aim: To determine the computer-predicted anticancer activity of mupirocin and to compare its activities with those determined for another polyene antibiotic, batumin. Materials & methods: Molecular docking, cytotoxicity assays, cell microscopy and cell cycle progression were studied in cancer and nontumorigenic cell lines. Results & conclusion: Cytotoxicity of mupirocin against several cancerous cell lines was detected with the highest one (IC50 = 5.4 µg/ml) against melanoma cell line. The profile of cytotoxicity of mupirocin was similar to that reported for batumin. Nevertheless, the morphology of cells treated with these antibiotics and alterations in cell cycle progression suggested possible dissimilarity in their mechanisms of action. Selective cytotoxicity of mupirocin against melanoma cells potentiates further studies to discover nontoxic drugs for melanoma prevention.


Subject(s)
Anti-Bacterial Agents/chemistry , Antineoplastic Agents/chemistry , Melanoma/drug therapy , Mupirocin/chemistry , Anti-Bacterial Agents/pharmacology , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Cell Survival , Drug Design , Humans , Molecular Docking Simulation , Mupirocin/pharmacology , Organic Chemicals/chemistry , Organic Chemicals/pharmacology , Polyenes/chemistry , Polyenes/pharmacology
2.
Future Med Chem ; 10(18): 2187-2199, 2018 Sep 01.
Article in English | MEDLINE | ID: mdl-30081676

ABSTRACT

AIM: To determine the computer-predicted anticancer activity of antibiotic batumin. MATERIALS & METHODS: Cytotoxicity assays, cell morphology microscopy and cell cycle progression were studied in cancer and nontumorigenic cell lines. An in vivo experiment on Lewis lung carcinoma (3LL)-transplanted mice was conducted to evaluate potential antimetastatic. RESULTS & CONCLUSION: Cytotoxicity against melanoma and lung carcinoma cells (IC50 ≈ 5 µg/ml) was detected. Hypercondensed chromatin and apoptotic body formation in batumin-treated cells suggested the induction of apoptosis supported also by an observed increase in the quantity of cells occupying the sub-G1 cell cycle phase. Twofold reduction in the number and volume of lung metastases in Lewis lung carcinoma (3LL)-bearing batumin-treated mice was demonstrated. Highly specific cytotoxicity of batumin against cancer cell lines potentiates further studies.


Subject(s)
Anti-Bacterial Agents/pharmacology , Apoptosis/drug effects , Polyenes/pharmacology , Pseudomonas/chemistry , Animals , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/therapeutic use , Binding Sites , Cell Line, Tumor , Female , G1 Phase Cell Cycle Checkpoints/drug effects , Humans , Lung Neoplasms/drug therapy , Lung Neoplasms/pathology , Mice , Mice, Inbred C57BL , Molecular Docking Simulation , Organic Chemicals/chemistry , Organic Chemicals/pharmacology , Organic Chemicals/therapeutic use , Polyenes/chemistry , Proto-Oncogene Proteins c-mdm2/chemistry , Proto-Oncogene Proteins c-mdm2/metabolism , Pseudomonas/metabolism , Transplantation, Heterologous
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