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首页> 外文期刊>Biophysical Chemistry: An International Journal Devoted to the Physical Chemistry of Biological Phenomena >New antineoplastic agent based on a dibenzoylmethane derivative: Cytotoxic effect and direct interaction with DNA
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New antineoplastic agent based on a dibenzoylmethane derivative: Cytotoxic effect and direct interaction with DNA

机译：基于二苯甲酰甲烷衍生物的新抗肿瘤剂：细胞毒性效应和与DNA的直接相互作用

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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.
机译：黑色素瘤仅占所有皮肤癌症的4％，而且是最致命的皮肤肿瘤。达卡尔尿是通过公共卫生系统在巴西治疗巴西的首选药物，主要是由于其成本低。然而，它是低特异性的烷基化剂，并且仅在20％的病例中引发治疗反应。可用于治疗黑素瘤的其他药物是昂贵的，肿瘤细胞通常对这些药物产生抗性。对抗黑色素瘤的斗争要求新颖，更具体的药物，这些药物有效地杀死耐药性肿瘤细胞。二苯甲酰甲烷（1,3-二苯基丙烷-1,3-二酮）衍生物是有前途的抗肿瘤剂。在这项研究中，我们研究了使用光学镊子与DNA分子的1,3-二苯基-2-苄基-1,3-丙二酮（DPBP）的细胞毒性作用及其与DNA分子的直接相互作用。 DPBP表现出对肿瘤细胞的有希望的结果，并具有41.94的选择性指数。此外，我们证明了DPBP直接与DNA分子相互作用的能力。 DPBP可以在体外与DNA相互作用的事实使我们能够假设这种相互作用也可能在体内发生，因此，DPBP可能是治疗耐药黑色素患者的替代方案。这些调查结果可以指导新的更有效的药物的发展。

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