Antitumor effects of snake venom chemically modified Lys49 phospholipase A2-like BthTX-I and a synthetic peptide derived from its C-terminal region.
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.
Gebrim
Luiz Carlos
LC
Instituto de Genética e Bioquímica, Universidade Federal de Uberlândia, Uberlândia, MG, Brazil.
Marcussi
Silvana
S
Menaldo
Danilo L
DL
de Menezes
Carla S R
CS
Nomizo
Auro
A
Hamaguchi
Amélia
A
Silveira-Lacerda
Elisângela P
EP
Homsi-Brandeburgo
Maria Inês
MI
Sampaio
Suely V
SV
Soares
Andreimar M
AM
Rodrigues
Veridiana M
VM
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D003435:Crotalid Venoms / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical; D006801:Humans; D019169:Jurkat Cells; D008239:Lysine / Q000737:chemistry; D008297:Male; D008546:Melanoma, Experimental / Q000473:pathology; D051379:Mice; D008807:Mice, Inbred BALB C; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D054467:Phospholipases A2 / Q000737:chemistry; D015202:Protein Engineering; D017434:Protein Structure, Tertiary / Q000502:physiology; D012910:Snake Venoms / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D003435:Crotalid Venoms; D010446:Peptide Fragments; D012910:Snake Venoms; C078097:bothropstoxin; D054467:Phospholipases A2; D008239:Lysine