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de Menezes Pereira, Gabriele; Nunes, Julia H Bormio; Macedo, Vinicius Souza; Pereira, Douglas Henrique; Buglio, Kaio Eduardo; Affonso, Daniele D; Ruiz, Ana Lucia T G; de Carvalho, João Ernesto; Frajácomo, Silmara Cristina L; Lustri, Wilton R; Lima, Carmen Silvia Passos; Bergamini, Fernando R G; Cuin, Alexandre; Masciocchi, Norberto; Corbi, Pedro Paulo
Em: J Inorg Biochem, vol. 262, pp. 112752, 2024, ISSN: 1873-3344.
Resumo | Links | BibTeX | Tags: Área Pré-Clínica
@article{pmid39366100,
title = {Antibacterial profile and antiproliferative activities over human tumor cells of new silver(I) complexes containing two distinct trifluoromethyl uracil isomers},
author = {Gabriele de Menezes Pereira and Julia H Bormio Nunes and Vinicius Souza Macedo and Douglas Henrique Pereira and Kaio Eduardo Buglio and Daniele D Affonso and Ana Lucia T G Ruiz and João Ernesto de Carvalho and Silmara Cristina L Frajácomo and Wilton R Lustri and Carmen Silvia Passos Lima and Fernando R G Bergamini and Alexandre Cuin and Norberto Masciocchi and Pedro Paulo Corbi},
doi = {10.1016/j.jinorgbio.2024.112752},
issn = {1873-3344},
year = {2024},
date = {2024-10-01},
urldate = {2024-10-01},
journal = {J Inorg Biochem},
volume = {262},
pages = {112752},
abstract = {New silver(I) complexes of 5-(trifluoromethyl)uracil (5TFMU) and 6-(trifluoromethyl)uracil (6TFMU) isomers were synthesized, characterized, and evaluated as antibacterial and antiproliferative agents. Based on elemental and thermogravimetric analyses, the Ag-5TFMU and Ag-6TFMU species are formulated as AgCHFNO and AgCHFNO, respectively. Infrared and C solid-state nuclear magnetic resonance spectroscopies suggest coordination of the trifluoromethyluracil isomers to silver by both nitrogen and oxygen atoms. Confirmation of their structure and connectivity was achieved, in the absence of single crystals of suitable quality, by state-of-the-art structural powder diffraction methods. In Ag-5TFMU, the organic ligand is tridentate and two distinct metal coordination environments are found (linear AgN as well as C AgO geometries), whereas Ag-6TFMU contains a complex polymeric structure with tetradentate dianionic 6TFMU moieties and five distinct AgX (X = N, O) fragments, further stabilized by ancillary (longer) AgO contacts. These species presented modest activity over Gram-positive and Gram-negative bacterial strains, whereas Ag-6TFMU was active over a set of tumor cells, with the best activity over prostate (PC-3) and kidney cell lines and selectivity indices of 4.6 and 1.3, respectively. On the other hand, Ag-5TFMU was active over all considered tumor cells except MCF-7 (breast cancer). The best activity was found for PC-3 cells, but no selectivity was observed. The Ag-5TFMU and Ag-6TFMU species also reduced the proliferation of tongue squamous cell carcinoma cell lines SCC - 4 and SCC-15. Preliminary biophysical assays by circular dichroism suggest that the Ag-5TFMU complex interacts with DNA by intercalation, an effect not seen in Ag-6TFMU.},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Mendonça, Fernanda Ferreira; de Miranda, Alice Santos; Makino, Henrique Massao Achidate; Mendes, Lorena Marinelli; Sobral, Danielle Vieira; de Barboza, Marycel Figols; Malavolta, Luciana; Fuscaldi, Leonardo Lima
ASSESSMENT OF IN VITRO INTERACTIONS BETWEEN RADIOLABELED EGFR-TARGETING PEPTIDE INHIBITORS AND GLIOBLASTOMA CELLS Journal Article
Em: Hematology, Transfusion and Cell Therapy, vol. 46, pp. S10–S11, 2024, ISSN: 2531-1379.
Links | BibTeX | Tags: Área Pré-Clínica
@article{Mendonça2024,
title = {ASSESSMENT OF IN VITRO INTERACTIONS BETWEEN RADIOLABELED EGFR-TARGETING PEPTIDE INHIBITORS AND GLIOBLASTOMA CELLS},
author = {Fernanda Ferreira Mendonça and Alice Santos de Miranda and Henrique Massao Achidate Makino and Lorena Marinelli Mendes and Danielle Vieira Sobral and Marycel Figols de Barboza and Luciana Malavolta and Leonardo Lima Fuscaldi},
doi = {10.1016/j.htct.2024.04.065},
issn = {2531-1379},
year = {2024},
date = {2024-04-00},
urldate = {2024-04-00},
journal = {Hematology, Transfusion and Cell Therapy},
volume = {46},
pages = {S10--S11},
publisher = {Elsevier BV},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Rodrigues, Fernanda Paiva Augusto; Giordano, Júlia Calviello; Sobral, Danielle Vieira; Miranda, Ana Cláudia Camargo; Fuscaldi, Leonardo Lima; de Barboza, Marycel Figols; Araújo, João Luiz Vitorino; Malavolta, Luciana
ASSESSMENT OF IN VITRO STUDIES OF [131I]I-LABELED DEDEYFELV PEPTIDE AS PROSPECTIVE BIOMARKER FOR GLIOBLASTOMA Journal Article
Em: Hematology, Transfusion and Cell Therapy, vol. 46, pp. S9–S10, 2024, ISSN: 2531-1379.
Links | BibTeX | Tags: Área Pré-Clínica
@article{Rodrigues2024,
title = {ASSESSMENT OF IN VITRO STUDIES OF [131I]I-LABELED DEDEYFELV PEPTIDE AS PROSPECTIVE BIOMARKER FOR GLIOBLASTOMA},
author = {Fernanda Paiva Augusto Rodrigues and Júlia Calviello Giordano and Danielle Vieira Sobral and Ana Cláudia Camargo Miranda and Leonardo Lima Fuscaldi and Marycel Figols de Barboza and João Luiz Vitorino Araújo and Luciana Malavolta},
doi = {10.1016/j.htct.2024.04.063},
issn = {2531-1379},
year = {2024},
date = {2024-04-00},
urldate = {2024-04-00},
journal = {Hematology, Transfusion and Cell Therapy},
volume = {46},
pages = {S9--S10},
publisher = {Elsevier BV},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Affonso, Daniele Daiane; Candido, Tuany Zambroti; de Carvalho, João Ernesto; Corbi, Pedro Paulo; Abbehausen, Camilla; Ruiz, Ana Lucia Tasca Gois; Lima, Carmen Silvia Passos
EVALUATION IN VITRO OF THE GOLD(I) COMPLEX WITH TRIPHENYLPHOSPHINE AND 4-DIMETHYLAAMINEPYRIDINE AS LIGANDS IN SKIN CANCER Journal Article
Em: Hematology, Transfusion and Cell Therapy, vol. 46, pp. S21–S22, 2024, ISSN: 2531-1379.
Links | BibTeX | Tags: Área Pré-Clínica
@article{Affonso2024,
title = {EVALUATION IN VITRO OF THE GOLD(I) COMPLEX WITH TRIPHENYLPHOSPHINE AND 4-DIMETHYLAAMINEPYRIDINE AS LIGANDS IN SKIN CANCER},
author = {Daniele Daiane Affonso and Tuany Zambroti Candido and João Ernesto de Carvalho and Pedro Paulo Corbi and Camilla Abbehausen and Ana Lucia Tasca Gois Ruiz and Carmen Silvia Passos Lima},
doi = {10.1016/j.htct.2024.04.083},
issn = {2531-1379},
year = {2024},
date = {2024-04-00},
urldate = {2024-04-00},
journal = {Hematology, Transfusion and Cell Therapy},
volume = {46},
pages = {S21--S22},
publisher = {Elsevier BV},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Mendes, Lorena Marinelli; Sobral, Danielle Vieira; dos Santos, Érica Victória; Fuscaldi, Leonardo Lima; Malavolta, Luciana
EVALUATION OF POTENTIAL PEPTIDE INHIBITORS THAT INTERACT WITH THE EGF RECEPTOR. RELEVANCE TO GLIOBLASTOMA Journal Article
Em: Hematology, Transfusion and Cell Therapy, vol. 46, 2024, ISSN: 2531-1379.
Links | BibTeX | Tags: Área Pré-Clínica
@article{Mendes2024,
title = {EVALUATION OF POTENTIAL PEPTIDE INHIBITORS THAT INTERACT WITH THE EGF RECEPTOR. RELEVANCE TO GLIOBLASTOMA},
author = {Lorena Marinelli Mendes and Danielle Vieira Sobral and Érica Victória dos Santos and Leonardo Lima Fuscaldi and Luciana Malavolta},
doi = {10.1016/j.htct.2024.04.061},
issn = {2531-1379},
year = {2024},
date = {2024-04-00},
urldate = {2024-04-00},
journal = {Hematology, Transfusion and Cell Therapy},
volume = {46},
publisher = {Elsevier BV},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Mendonça, Fernanda Ferreira; Perez, Maria Emilia Tejeria; Decuadra, Paula; Zeni, Maia; Rey, Ana; Fuscaldi, Leonardo Lima; Malavolta, Luciana
INVESTIGATION OF THE IN VITRO ASSESSMENT OF 99MTC-LABELED LAMININ-111 PEPTIDES AS PROSPECTIVE BIOMARKERS FOR BREAST CANCER Journal Article
Em: Hematology, Transfusion and Cell Therapy, vol. 46, pp. S8–S9, 2024, ISSN: 2531-1379.
Links | BibTeX | Tags: Área Pré-Clínica
@article{Mendonça2024b,
title = {INVESTIGATION OF THE IN VITRO ASSESSMENT OF 99MTC-LABELED LAMININ-111 PEPTIDES AS PROSPECTIVE BIOMARKERS FOR BREAST CANCER},
author = {Fernanda Ferreira Mendonça and Maria Emilia Tejeria Perez and Paula Decuadra and Maia Zeni and Ana Rey and Leonardo Lima Fuscaldi and Luciana Malavolta},
doi = {10.1016/j.htct.2024.04.062},
issn = {2531-1379},
year = {2024},
date = {2024-04-00},
urldate = {2024-04-00},
journal = {Hematology, Transfusion and Cell Therapy},
volume = {46},
pages = {S8--S9},
publisher = {Elsevier BV},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Carron, Juliana; Affonso, Daniele Daiane; Souza, Suelen Aparecida Ribeiro; Ferreira, Ana Maria Castro; Carvalho, João Ernesto; Ruiz, Ana Lucia Tasca Gois; Melo, Gabriella Fraiji; Alves, Flávio Lopes; Fuscaldi, Leonardo Lima; Malavolta, Luciana; Lima, Carmen Silvia Passos
INFLUENCE OF A CONVENTIONAL CHELATOR-MODIFIED ANTI-INTEGRIN PEPTIDE ON PROLIFERATION AND MIGRATION OF HEAD AND NECK CANCER CELLS Journal Article
Em: Hematology, Transfusion and Cell Therapy, vol. 46, 2024, ISSN: 2531-1379.
Links | BibTeX | Tags: Área Pré-Clínica
@article{Carron2024,
title = {INFLUENCE OF A CONVENTIONAL CHELATOR-MODIFIED ANTI-INTEGRIN PEPTIDE ON PROLIFERATION AND MIGRATION OF HEAD AND NECK CANCER CELLS},
author = {Juliana Carron and Daniele Daiane Affonso and Suelen Aparecida Ribeiro Souza and Ana Maria Castro Ferreira and João Ernesto Carvalho and Ana Lucia Tasca Gois Ruiz and Gabriella Fraiji Melo and Flávio Lopes Alves and Leonardo Lima Fuscaldi and Luciana Malavolta and Carmen Silvia Passos Lima},
doi = {10.1016/j.htct.2024.04.081},
issn = {2531-1379},
year = {2024},
date = {2024-04-00},
urldate = {2024-04-00},
journal = {Hematology, Transfusion and Cell Therapy},
volume = {46},
publisher = {Elsevier BV},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Lima, Carmen Silvia Passos; Candido, Tuany Zambroti; de Carvalho, João Ernesto; Ruiz, Ana Lucia Tasca Gois; Corbi, Pedro Paulo
PRELIMINARY ANTI-PROLIFERATIVE ACTIVITIES OF A PALLADIUM(II) COMPLEX OVER SQUAMOUS CELL CARCINOMA OF TONGUE Journal Article
Em: Hematology, Transfusion and Cell Therapy, vol. 46, pp. S16–S17, 2024, ISSN: 2531-1379.
Links | BibTeX | Tags: Área Pré-Clínica
@article{Lima2024,
title = {PRELIMINARY ANTI-PROLIFERATIVE ACTIVITIES OF A PALLADIUM(II) COMPLEX OVER SQUAMOUS CELL CARCINOMA OF TONGUE},
author = {Carmen Silvia Passos Lima and Tuany Zambroti Candido and João Ernesto de Carvalho and Ana Lucia Tasca Gois Ruiz and Pedro Paulo Corbi},
doi = {10.1016/j.htct.2024.04.075},
issn = {2531-1379},
year = {2024},
date = {2024-04-00},
urldate = {2024-04-00},
journal = {Hematology, Transfusion and Cell Therapy},
volume = {46},
pages = {S16--S17},
publisher = {Elsevier BV},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Mendonça, Fernanda Ferreira; Vieira, Júlia Torquato; Sobral, Danielle Vieira; dos Santos, Érica Victória; Fuscaldi, Leonardo Lima; Malavolta, Luciana
SYNTHESIS AND EVALUATION OF BIOACTIVE PEPTIDES FROM LAMININ-111 IN TRIPLE-NEGATIVE BREAST CANCER CELLS Journal Article
Em: Hematology, Transfusion and Cell Therapy, vol. 46, 2024, ISSN: 2531-1379.
Links | BibTeX | Tags: Área Pré-Clínica
@article{Mendonça2024c,
title = {SYNTHESIS AND EVALUATION OF BIOACTIVE PEPTIDES FROM LAMININ-111 IN TRIPLE-NEGATIVE BREAST CANCER CELLS},
author = {Fernanda Ferreira Mendonça and Júlia Torquato Vieira and Danielle Vieira Sobral and Érica Victória dos Santos and Leonardo Lima Fuscaldi and Luciana Malavolta},
doi = {10.1016/j.htct.2024.04.064},
issn = {2531-1379},
year = {2024},
date = {2024-04-00},
urldate = {2024-04-00},
journal = {Hematology, Transfusion and Cell Therapy},
volume = {46},
publisher = {Elsevier BV},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Fuscaldi, Leonardo Lima; Sobral, Danielle Vieira; Durante, Ana Claudia Ranucci; Mendonça, Fernanda Ferreira; Miranda, Ana Cláudia Camargo; Salgueiro, Carla; de Castiglia, Silvia Gomez; Yamaga, Lilian Yuri Itaya; da Cunha, Marcelo Livorsi; Malavolta, Luciana; de Barboza, Marycel Figols; Mejia, Jorge
Em: Front. Chem., vol. 11, 2023, ISSN: 2296-2646.
Resumo | Links | BibTeX | Tags: Área Pré-Clínica
@article{Fuscaldi2023,
title = {Radiochemical and biological assessments of a PSMA-I&S cold kit for fast and inexpensive 99mTc-labeling for SPECT imaging and radioguided surgery in prostate cancer},
author = {Leonardo Lima Fuscaldi and Danielle Vieira Sobral and Ana Claudia Ranucci Durante and Fernanda Ferreira Mendonça and Ana Cláudia Camargo Miranda and Carla Salgueiro and Silvia Gomez de Castiglia and Lilian Yuri Itaya Yamaga and Marcelo Livorsi da Cunha and Luciana Malavolta and Marycel Figols de Barboza and Jorge Mejia},
doi = {10.3389/fchem.2023.1271176},
issn = {2296-2646},
year = {2023},
date = {2023-10-12},
urldate = {2023-10-12},
journal = {Front. Chem.},
volume = {11},
publisher = {Frontiers Media SA},
abstract = {<jats:p>The expression of prostate-specific membrane antigen (PSMA) is upregulated in prostate cancer (PCa) cells and PSMA-ligands have been radiolabeled and used as radiopharmaceuticals for targeted radionuclide therapy (TRT), single photon emission computed tomography (SPECT) or positron emission tomography (PET) molecular imaging, and radioguided surgery in PCa patients. Herein, we aimed at radiolabeling the PSMA-I&S cold kit with <jats:sup>99m</jats:sup>Tc, resulting in a radiopharmaceutical with high radiochemical yield (RCY) and stability for SPECT imaging and radioguided surgery in PCa malignancies. Various pre-clinical assays were conducted to evaluate the [<jats:sup>99m</jats:sup>Tc]Tc-PSMA-I&S obtained by the cold kit. These assays included assessments of RCY, radiochemical stability in saline, lipophilicity, serum protein binding (SPB), affinity for LNCaP-PCa cells (binding and internalization studies), and <jats:italic>ex vivo</jats:italic> biodistribution profile in naive and LNCaP-PCa-bearing mice. The radiopharmaceutical was obtained with good RCY (92.05% ± 2.20%) and remained stable for 6 h. The lipophilicity was determined to be −2.41 ± 0.06, while the SPB was ∼97%. The binding percentages to LNCaP cells were 9.41% ± 0.57% (1 h) and 10.45% ± 0.45% (4 h), with 63.12 ± 0.93 (1 h) and 65.72% ± 1.28% (4 h) of the bound material being internalized. Blocking assays, employing an excess of unlabeled PSMA-I&S, resulted in a reduction in the binding percentage by 2.6 times. The <jats:italic>ex vivo</jats:italic> biodistribution profile confirmed high accumulation of [<jats:sup>99m</jats:sup>Tc]Tc-PSMA-I&S in the tumor and the tumor-to-contralateral muscle ratio was ∼6.5. In conclusion, [<jats:sup>99m</jats:sup>Tc]Tc-PSMA-I&S was successfully obtained by radiolabeling the cold kit using freshly eluted [<jats:sup>99m</jats:sup>Tc]NaTcO<jats:sub>4</jats:sub>, exhibiting good RCY and radiochemical stability. The preclinical assays demonstrated that the radiopharmaceutical shows favorable characteristics for SPECT imaging and radioguided surgery in PCa patients.</jats:p>},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Bergamini, Fernando R. G.; Nunes, Julia H. B.; Manzano, Carlos Marrote; de Carvalho, Marcos Alberto; Ribeiro, Marcos Antônio; Ruiz, Ana Lucia Tasca Gois; de Carvalho, João Ernesto; Lustri, Wilton Rogério; de Paiva, Raphael Enoque Ferraz; Portes, Marcelo Cecconi; da Costa Ferreira, Ana Maria; Corbi, Pedro Paulo
Investigating the antiproliferative activities of new CuII complexes with pyridine hydrazone derivatives of nalidixic acid Journal Article
Em: Journal of Inorganic Biochemistry, vol. 234, 2022, ISSN: 0162-0134.
Links | BibTeX | Tags: Área Pré-Clínica
@article{Bergamini2022,
title = {Investigating the antiproliferative activities of new CuII complexes with pyridine hydrazone derivatives of nalidixic acid},
author = {Fernando R.G. Bergamini and Julia H.B. Nunes and Carlos Marrote Manzano and Marcos Alberto de Carvalho and Marcos Antônio Ribeiro and Ana Lucia Tasca Gois Ruiz and João Ernesto de Carvalho and Wilton Rogério Lustri and Raphael Enoque Ferraz de Paiva and Marcelo Cecconi Portes and Ana Maria da Costa Ferreira and Pedro Paulo Corbi},
doi = {10.1016/j.jinorgbio.2022.111881},
issn = {0162-0134},
year = {2022},
date = {2022-09-00},
urldate = {2022-09-00},
journal = {Journal of Inorganic Biochemistry},
volume = {234},
publisher = {Elsevier BV},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Candido, Tuany Zambroti; de Paiva, Raphael Enoque Ferraz; Figueiredo, Mariana Cecchetto; de Oliveira Coser, Lilian; Frajácomo, Silmara Cristina Lazarini; Abbehausen, Camilla; Cardinalli, Izilda Aparecida; Lustri, Wilton Rogerio; Carvalho, João Ernesto; Ruiz, Ana Lucia Tasca Gois; Corbi, Pedro Paulo; Lima, Carmen Silvia Passos
Em: Pharmaceutics, vol. 14, não 2, 2022, ISSN: 1999-4923.
Resumo | Links | BibTeX | Tags: Área Pré-Clínica
@article{Candido2022,
title = {Silver Nimesulide Complex in Bacterial Cellulose Membranes as an Innovative Therapeutic Method for Topical Treatment of Skin Squamous Cell Carcinoma},
author = {Tuany Zambroti Candido and Raphael Enoque Ferraz de Paiva and Mariana Cecchetto Figueiredo and Lilian de Oliveira Coser and Silmara Cristina Lazarini Frajácomo and Camilla Abbehausen and Izilda Aparecida Cardinalli and Wilton Rogerio Lustri and João Ernesto Carvalho and Ana Lucia Tasca Gois Ruiz and Pedro Paulo Corbi and Carmen Silvia Passos Lima},
doi = {10.3390/pharmaceutics14020462},
issn = {1999-4923},
year = {2022},
date = {2022-02-00},
urldate = {2022-02-00},
journal = {Pharmaceutics},
volume = {14},
number = {2},
publisher = {MDPI AG},
abstract = {<jats:p>Oxidative stress and inflammation act on skin squamous cell carcinoma (SSCC) development and progression. Curative therapy for SSCC patients is mainly based on surgical resection, which can cause various sequelae. Silver ions have in vitro activities over tumor cells, while nimesulide has antioxidant and anti-inflammatory activities. This study aimed to evaluate the effects of a silver(I) complex with nimesulide (AgNMS) incorporated in a sustained release device based on bacterial cellulose membrane, named AgNMS@BCM, on topic SSCC treatment. The antiproliferative effect of AgNMS complex was evaluated in the SCC4, SCC15 and FaDu SCC lines. AgNMS complex activity on exposure of phosphatidylserine (PS) residues and multicaspase activation were evaluated on FaDu cells by flow cytometry. The AgNMS@BCM effects were evaluated in a SSCC model induced by 7,12-dimethylbenzanthracene/12-o-tetradecanoyl-phorbol-13-acetate (DMBA/TPA) in mice. Toxicity and tumor size were evaluated throughout the study. AgNMS complex showed antiproliferative activity in SCC15 and FaDu lines in low to moderate concentrations (67.3 µM and 107.3 µM, respectively), and induced multicaspase activation on FaDu cells. The AgNMS@BCM did not induce toxicity and reduced tumor size up to 100%. Thus, the application of AgNMS@BCM was effective and safe in SSCC treatment in mice, and can be seen as a potential and safe agent for topic treatment of SSCC in humans.</jats:p>},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Sobral, Danielle V.; Fuscaldi, Leonardo L.; Durante, Ana Claudia R.; Mendonça, Fernanda F.; de Oliveira, Larissa R.; Miranda, Ana Cláudia C.; Mejia, Jorge; Montor, Wagner R.; de Barboza, Marycel F.; Malavolta, Luciana
Em: Pharmaceuticals, vol. 15, não 2, 2022, ISSN: 1424-8247.
Resumo | Links | BibTeX | Tags: Área Pré-Clínica
@article{Sobral2022,
title = {Comparative Evaluation of Radiochemical and Biological Properties of 131I- and [99mTc]Tc(CO)3-Labeled RGD Analogues Planned to Interact with the αvβ3 Integrin Expressed in Glioblastoma},
author = {Danielle V. Sobral and Leonardo L. Fuscaldi and Ana Claudia R. Durante and Fernanda F. Mendonça and Larissa R. de Oliveira and Ana Cláudia C. Miranda and Jorge Mejia and Wagner R. Montor and Marycel F. de Barboza and Luciana Malavolta},
doi = {10.3390/ph15020116},
issn = {1424-8247},
year = {2022},
date = {2022-02-00},
urldate = {2022-02-00},
journal = {Pharmaceuticals},
volume = {15},
number = {2},
publisher = {MDPI AG},
abstract = {<jats:p>Radiolabeled peptides with high specificity for overexpressed receptors in tumor cells hold great promise for diagnostic and therapeutic applications. In this work, we aimed at comparing the radiolabeling efficiency and biological properties of two different RGD analogs: GRGDYV and GRGDHV, labeled with iodine-131 (131I) and technetium-99m-tricarbonyl complex [99mTc][Tc(CO)3]+. Additionally, we evaluated their interaction with the αvβ3 integrin molecule, overexpressed in a wide variety of tumors, including glioblastoma. Both peptides were chemically synthesized, purified and radiolabeled with 131I and [99mTc][Tc(CO)3]+ using the chloramine-T and tricarbonyl methodologies, respectively. The stability, binding to serum proteins and partition coefficient were evaluated for both radioconjugates. In addition, the binding and internalization of radiopeptides to rat C6 glioblastoma cells and rat brain homogenates from normal animals and a glioblastoma-induced model were assessed. Finally, ex vivo biodistribution studies were carried out. Radiochemical yields between 95–98% were reached for both peptides under optimized radiolabeling conditions. Both peptides were stable for up to 24 h in saline solution and in human serum. In addition, the radiopeptides have hydrophilic characteristics and a percentage of binding to serum proteins around 35% and 50% for the [131I]I-GRGDYV and [99mTc]Tc(CO)3-GRGDHV fragments, respectively. Radiopeptides showed the capacity of binding and internalization both in cell culture (C6) and rat brain homogenates. Biodistribution studies corroborated the results obtained with brain homogenates and confirmed the different binding characteristics due to the exchange of radionuclides and the presence of the tricarbonyl complex. Thereby, the results showed that both radiopeptides might be considered for future clinical applications.</jats:p>},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Fuscaldi, Leonardo L.; Sobral, Danielle V.; Durante, Ana Claudia R.; Mendonça, Fernanda F.; Miranda, Ana Cláudia C.; da Cunha, Marcelo L.; Malavolta, Luciana; Mejia, Jorge; de Barboza, Marycel F.
Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer Journal Article
Em: Pharmaceuticals, vol. 14, não 5, 2021, ISSN: 1424-8247.
Resumo | Links | BibTeX | Tags: Área Pré-Clínica
@article{Fuscaldi2021,
title = {Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer},
author = {Leonardo L. Fuscaldi and Danielle V. Sobral and Ana Claudia R. Durante and Fernanda F. Mendonça and Ana Cláudia C. Miranda and Marcelo L. da Cunha and Luciana Malavolta and Jorge Mejia and Marycel F. de Barboza},
doi = {10.3390/ph14050385},
issn = {1424-8247},
year = {2021},
date = {2021-05-00},
urldate = {2021-05-00},
journal = {Pharmaceuticals},
volume = {14},
number = {5},
publisher = {MDPI AG},
abstract = {<jats:p>Prostate-specific membrane antigen (PSMA) is a glycoprotein present in the prostate, that is overexpressed in prostate cancer (PCa). Recently, PSMA-directed radiopharmaceuticals have been developed, allowing the pinpointing of tumors with the Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging techniques. The aim of the present work was to standardize and validate an automatic synthesis module-based radiolabeling protocol for [68Ga]Ga-PSMA-11, as well as to produce a radiopharmaceutical for PET imaging of PCa malignancies. [68Ga]Ga-PSMA-11 was evaluated to determine the radiochemical purity (RCP), stability in saline solution and serum, lipophilicity, affinity to serum proteins, binding and internalization to lymph node carcinoma of the prostate (LNCaP) cells, and ex vivo biodistribution in mice. The radiopharmaceutical was produced with an RCP of 99.06 ± 0.10%, which was assessed with reversed-phase high-performance liquid chromatography (RP-HPLC). The product was stable in saline solution for up to 4 h (RCP > 98%) and in serum for up to 1 h (RCP > 95%). The lipophilicity was determined as −3.80 ± 0.15, while the serum protein binding (SPB) was <17%. The percentages of binding to LNCaP cells were 4.07 ± 0.51% (30 min) and 4.56 ± 0.46% (60 min), while 19.22 ± 2.73% (30 min) and 16.85 ± 1.34% (60 min) of bound material was internalized. High accumulation of [68Ga]Ga-PSMA-11 was observed in the kidneys, spleen, and tumor, with a tumor-to-contralateral-muscle ratio of >8.5 and a tumor-to-blood ratio of >3.5. In conclusion, an automatic synthesis module-based radiolabeling protocol for [68Ga]Ga-PSMA-11 was standardized and the product was evaluated, thus verifying its characteristics for PET imaging of PCa tumors in a clinical environment.</jats:p>},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Sobral, Danielle V.; Fuscaldi, Leonardo L.; Durante, Ana Claudia R.; Rangel, Mayara G.; Oliveira, Larissa R.; Mendonça, Fernanda F.; Miranda, Ana Cláudia C.; Cabeza, Jorge M.; Montor, Wagner R.; Cabral, Francisco R.; Barboza, Marycel F. F.; Malavolta, Luciana
Radiochemical and biological properties of peptides designed to interact with EGF receptor: Relevance for glioblastoma Journal Article
Em: Nuclear Medicine and Biology, vol. 88-89, pp. 14–23, 2020, ISSN: 0969-8051.
Links | BibTeX | Tags: Área Pré-Clínica
@article{Sobral2020,
title = {Radiochemical and biological properties of peptides designed to interact with EGF receptor: Relevance for glioblastoma},
author = {Danielle V. Sobral and Leonardo L. Fuscaldi and Ana Claudia R. Durante and Mayara G. Rangel and Larissa R. Oliveira and Fernanda F. Mendonça and Ana Cláudia C. Miranda and Jorge M. Cabeza and Wagner R. Montor and Francisco R. Cabral and Marycel F.F. Barboza and Luciana Malavolta},
doi = {10.1016/j.nucmedbio.2020.07.001},
issn = {0969-8051},
year = {2020},
date = {2020-09-00},
urldate = {2020-09-00},
journal = {Nuclear Medicine and Biology},
volume = {88-89},
pages = {14--23},
publisher = {Elsevier BV},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}
Nunes, Julia H. Bormio; de Paiva, Paula P.; Ruiz, Ana Lúcia T. G.; de Carvalho, João Ernesto; Corbi, Pedro P.
Em: Toxicology in Vitro, vol. 60, pp. 359–368, 2019, ISSN: 0887-2333.
Links | BibTeX | Tags: Área Pré-Clínica
@article{BormioNunes2019,
title = {New findings on the antiproliferative activity of the silver(I) complex with 5-fluorouracil against human multi-resistant NCI/ADR-RES ovarian tumor cells},
author = {Julia H. Bormio Nunes and Paula P. de Paiva and Ana Lúcia T.G. Ruiz and João Ernesto de Carvalho and Pedro P. Corbi},
doi = {10.1016/j.tiv.2019.06.018},
issn = {0887-2333},
year = {2019},
date = {2019-10-00},
urldate = {2019-10-00},
journal = {Toxicology in Vitro},
volume = {60},
pages = {359--368},
publisher = {Elsevier BV},
keywords = {Área Pré-Clínica},
pubstate = {published},
tppubtype = {article}
}