Abstract
Cancer has killed millions of people worldwide. Despite the increasing knowledge about the molecular basis of tumor development, few advances have been reached in clinical therapy and diagnoses, which shows the importance of new drugs development for therapeutic and diagnosis purpose. Venomous creatures have been studied as potential sources of pharmacological agents and physiological tools. A lot of work has been done about biological activity of terrestrial animals, but comparatively less research has been undertaken on venomous marine creature, particularly fish, which means that marine toxins represent a vast and unexplored source of novel molecules with therapeutical potential. In this work, the scorpion fish Scorpaena plumieri crude venom (SPB) and a gelatinolytic protease purified from this venom (SPGP) were evaluated for their applicability for in vivo tumor detection. In vitro results showed that both. SPB and SPGP, possess a powerful antitumor effects on p53-wild-type glioblastoma cells (LD{sub 50}= 3,9 {+-} 0,98{mu}g/mL and 8,00 x 10{sup -12} {+-} 2,94 x 10{sup -12}M, respectively) and Ehrlich ascites carcinoma cells (LD{sub 50}=14,05 {+-} 2,95 {mu}g/mL and 1,22 x 10{sup -11} {+-} 6,56 x 10{sup -12}M, respectively). P53 mutant glioblastoma cells were more resistant to both, SPB and SPGP treatment (LD{sub 50} > 125
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Citation Formats
Soprani, Juliana.
Identification of anti-tumoral effect of a polypeptide isolated from Scorpionfish Scorpaena plumieri venom and assessment of its potential use for tumor diagnosis; Identificacao do efeito antitumoral de um polipeptidio isolado da peconha do peixe-escorpiao Scorpaena plumieri e avaliacao do seu potencial uso no diagnostico de tumores.
Brazil: N. p.,
2008.
Web.
Soprani, Juliana.
Identification of anti-tumoral effect of a polypeptide isolated from Scorpionfish Scorpaena plumieri venom and assessment of its potential use for tumor diagnosis; Identificacao do efeito antitumoral de um polipeptidio isolado da peconha do peixe-escorpiao Scorpaena plumieri e avaliacao do seu potencial uso no diagnostico de tumores.
Brazil.
Soprani, Juliana.
2008.
"Identification of anti-tumoral effect of a polypeptide isolated from Scorpionfish Scorpaena plumieri venom and assessment of its potential use for tumor diagnosis; Identificacao do efeito antitumoral de um polipeptidio isolado da peconha do peixe-escorpiao Scorpaena plumieri e avaliacao do seu potencial uso no diagnostico de tumores."
Brazil.
@misc{etde_21096957,
title = {Identification of anti-tumoral effect of a polypeptide isolated from Scorpionfish Scorpaena plumieri venom and assessment of its potential use for tumor diagnosis; Identificacao do efeito antitumoral de um polipeptidio isolado da peconha do peixe-escorpiao Scorpaena plumieri e avaliacao do seu potencial uso no diagnostico de tumores}
author = {Soprani, Juliana}
abstractNote = {Cancer has killed millions of people worldwide. Despite the increasing knowledge about the molecular basis of tumor development, few advances have been reached in clinical therapy and diagnoses, which shows the importance of new drugs development for therapeutic and diagnosis purpose. Venomous creatures have been studied as potential sources of pharmacological agents and physiological tools. A lot of work has been done about biological activity of terrestrial animals, but comparatively less research has been undertaken on venomous marine creature, particularly fish, which means that marine toxins represent a vast and unexplored source of novel molecules with therapeutical potential. In this work, the scorpion fish Scorpaena plumieri crude venom (SPB) and a gelatinolytic protease purified from this venom (SPGP) were evaluated for their applicability for in vivo tumor detection. In vitro results showed that both. SPB and SPGP, possess a powerful antitumor effects on p53-wild-type glioblastoma cells (LD{sub 50}= 3,9 {+-} 0,98{mu}g/mL and 8,00 x 10{sup -12} {+-} 2,94 x 10{sup -12}M, respectively) and Ehrlich ascites carcinoma cells (LD{sub 50}=14,05 {+-} 2,95 {mu}g/mL and 1,22 x 10{sup -11} {+-} 6,56 x 10{sup -12}M, respectively). P53 mutant glioblastoma cells were more resistant to both, SPB and SPGP treatment (LD{sub 50} > 125 {mu}g/mL and LD{sub 50} > 1,39 x 10{sup -9}M, respectively). The morphological changes observed in the cell lines treated with SPB and SPGP, and the data of DAPI staining, indicate that the antitumor effect of these substances occurs via apoptosis. Radioactive probes of SPB ([{sup 99m}Tc] SPB) and SPGP ([{sup 125}I] SPGP) with high specific activity and high radiochemical purity were synthesized. Data of biodistribution studies, performed by intravenous injections in Swiss mice bearing Ehrlich carcinoma cells, showed that SPB has poor uptake in tumor region. On the other hand, SPGP had a substantial uptake in tumor at ali analyzed times. Intratumoral administration of [{sup 125}I]SPGP increased its uptake by the tumoral region and substantially reduced the uptake by other organs. Biodistribution studies in animals with edema confirmed that SPGP presents longer residence time in tumoral region than into inflammation site. Hematologic and histopathologic studies showed that SPB and SPGP did not present acute toxicity, even at concentrations ten times higher than those used in biodistribution studies. These results indicate the potential of SPGP as template for the development of new drugs and radiopharmaceuticals for tumors diagnosis and therapy. (author)}
place = {Brazil}
year = {2008}
month = {Jul}
}
title = {Identification of anti-tumoral effect of a polypeptide isolated from Scorpionfish Scorpaena plumieri venom and assessment of its potential use for tumor diagnosis; Identificacao do efeito antitumoral de um polipeptidio isolado da peconha do peixe-escorpiao Scorpaena plumieri e avaliacao do seu potencial uso no diagnostico de tumores}
author = {Soprani, Juliana}
abstractNote = {Cancer has killed millions of people worldwide. Despite the increasing knowledge about the molecular basis of tumor development, few advances have been reached in clinical therapy and diagnoses, which shows the importance of new drugs development for therapeutic and diagnosis purpose. Venomous creatures have been studied as potential sources of pharmacological agents and physiological tools. A lot of work has been done about biological activity of terrestrial animals, but comparatively less research has been undertaken on venomous marine creature, particularly fish, which means that marine toxins represent a vast and unexplored source of novel molecules with therapeutical potential. In this work, the scorpion fish Scorpaena plumieri crude venom (SPB) and a gelatinolytic protease purified from this venom (SPGP) were evaluated for their applicability for in vivo tumor detection. In vitro results showed that both. SPB and SPGP, possess a powerful antitumor effects on p53-wild-type glioblastoma cells (LD{sub 50}= 3,9 {+-} 0,98{mu}g/mL and 8,00 x 10{sup -12} {+-} 2,94 x 10{sup -12}M, respectively) and Ehrlich ascites carcinoma cells (LD{sub 50}=14,05 {+-} 2,95 {mu}g/mL and 1,22 x 10{sup -11} {+-} 6,56 x 10{sup -12}M, respectively). P53 mutant glioblastoma cells were more resistant to both, SPB and SPGP treatment (LD{sub 50} > 125 {mu}g/mL and LD{sub 50} > 1,39 x 10{sup -9}M, respectively). The morphological changes observed in the cell lines treated with SPB and SPGP, and the data of DAPI staining, indicate that the antitumor effect of these substances occurs via apoptosis. Radioactive probes of SPB ([{sup 99m}Tc] SPB) and SPGP ([{sup 125}I] SPGP) with high specific activity and high radiochemical purity were synthesized. Data of biodistribution studies, performed by intravenous injections in Swiss mice bearing Ehrlich carcinoma cells, showed that SPB has poor uptake in tumor region. On the other hand, SPGP had a substantial uptake in tumor at ali analyzed times. Intratumoral administration of [{sup 125}I]SPGP increased its uptake by the tumoral region and substantially reduced the uptake by other organs. Biodistribution studies in animals with edema confirmed that SPGP presents longer residence time in tumoral region than into inflammation site. Hematologic and histopathologic studies showed that SPB and SPGP did not present acute toxicity, even at concentrations ten times higher than those used in biodistribution studies. These results indicate the potential of SPGP as template for the development of new drugs and radiopharmaceuticals for tumors diagnosis and therapy. (author)}
place = {Brazil}
year = {2008}
month = {Jul}
}