Antitumor effects of snake venom chemically modified Lys49 phospholipase A2-like BthTX-I and a synthetic peptide derived from its C-terminal region

• Published in: Biologicals 2009-08, Vol.37 (4), p.222-229
• Main Authors: Gebrim, Luiz Carlos, Marcussi, Silvana, Menaldo, Danilo L, de Menezes, Carla S R, Nomizo, Auro, Hamaguchi, Amélia, Silveira-Lacerda, Elisângela P, Homsi-Brandeburgo, Maria Inês, Sampaio, Suely V, Soares, Andreimar M, Rodrigues, Veridiana M
• Format: Article
• Language: English
• Subjects: Animals; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antineoplastic Agents - therapeutic use; Crotalid Venoms - chemistry; Crotalid Venoms - pharmacology; Crotalid Venoms - therapeutic use; Drug Evaluation, Preclinical; Humans; Jurkat Cells; Lysine - chemistry; Male; Melanoma, Experimental - pathology; Mice; Mice, Inbred BALB C; Peptide Fragments - chemical synthesis; Peptide Fragments - pharmacology; Peptide Fragments - therapeutic use; Phospholipases A2 - chemistry; Protein Engineering; Protein Structure, Tertiary - physiology; Snake Venoms - chemistry; Snake Venoms - pharmacology; Tumor Cells, Cultured
• ISSN: 1045-1056; 1095-8320
• DOI: 10.1016/j.biologicals.2009.01.010

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.