New antineoplastic agent based on a dibenzoylmethane derivative: Cytotoxic effect and direct interaction with DNA
| Autor: | T.A. Moura, Bruno C. Publio, Andressa Antunes Prado de França, Pollyanna de Moraes França Ferreira, Fernanda R. Nascimento, Marcio S. Rocha, Anésia A. Santos, Gaspar Diaz-Muñoz, Jefferson Viktor De Paula Barros Baeta, Marisa Alves Nogueira Diaz |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Drug Optical Tweezers Dibenzoylmethane Dacarbazine media_common.quotation_subject Biophysics Antineoplastic Agents Optical tweezers 01 natural sciences Biochemistry Mice Structure-Activity Relationship Dibenzoylmethane derivative 03 medical and health sciences chemistry.chemical_compound Chalcones In vivo 0103 physical sciences Tumor Cells Cultured medicine Animals Cytotoxic T cell 010306 general physics Melanoma Cell Proliferation media_common Dose-Response Relationship Drug Molecular Structure Chemistry Organic Chemistry DNA Neoplasm DNA medicine.disease In vitro 030104 developmental biology Cancer research Drug Screening Assays Antitumor medicine.drug |
| Zdroj: | LOCUS Repositório Institucional da UFV Universidade Federal de Viçosa (UFV) instacron:UFV |
| ISSN: | 0301-4622 |
| DOI: | 10.1016/j.bpc.2018.04.009 |
| Popis: | Melanoma accounts for only 4% of all skin cancers but is among the most lethal cutaneous neoplasms. Dacarbazine is the drug of choice for the treatment of melanoma in Brazil through the public health system mainly because of its low cost. However, it is an alkylating agent of low specificity and elicits a therapeutic response in only 20% of cases. Other drugs available for the treatment of melanoma are expensive, and tumor cells commonly develop resistance to these drugs. The fight against melanoma demands novel, more specific drugs that are effective in killing drug-resistant tumor cells. Dibenzoylmethane (1,3-diphenylpropane-1,3-dione) derivatives are promising antitumor agents. In this study, we investigated the cytotoxic effect of 1,3-diphenyl-2-benzyl-1,3-propanedione (DPBP) on B16F10 melanoma cells as well as its direct interaction with the DNA molecule using optical tweezers. DPBP showed promising results against tumor cells and had a selectivity index of 41.94. Also, we demonstrated the ability of DPBP to interact directly with the DNA molecule. The fact that DPBP can interact with DNA in vitro allows us to hypothesize that such an interaction may also occur in vivo and, therefore, that DPBP may be an alternative to treat patients with drug-resistant melanomas. These findings can guide the development of new and more effective drugs. |
| Databáze: | OpenAIRE |
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