Abstract
The present work evaluates both in vitro and in vivo antitumor activity of BPB-modified BthTX-I and its cationic synthetic peptide derived from the 115-129 C-terminal region. BPB-BthTX-I presented cytotoxicity of 10-40% on different tumor cell lines, which were also susceptible to the lytic action of the synthetic peptide. Injection of the modified protein or the peptide in mice, 5 days after transplantation of S180 tumor cells, reduced 30 and 36% of the tumor size on day 14th and 76 and 79% on day 60th, respectively, when compared to the untreated control group. Thus, these antitumor properties might be of interest in the development of therapeutic strategies against cancer.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / therapeutic use
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Crotalid Venoms / chemistry*
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Crotalid Venoms / pharmacology
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Crotalid Venoms / therapeutic use
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Drug Evaluation, Preclinical
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Humans
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Jurkat Cells
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Lysine / chemistry
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Male
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Melanoma, Experimental / pathology
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Mice
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Mice, Inbred BALB C
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Peptide Fragments / chemical synthesis
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Peptide Fragments / pharmacology*
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Peptide Fragments / therapeutic use
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Phospholipases A2 / chemistry
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Protein Engineering
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Protein Structure, Tertiary / physiology
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Snake Venoms / chemistry
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Snake Venoms / pharmacology*
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Crotalid Venoms
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Peptide Fragments
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Snake Venoms
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bothropstoxin
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Phospholipases A2
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Lysine