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Compounds from wild mushrooms with antitumor potential

Ferreira, Isabel C.F.R.; Vaz, Josiana A.; Vasconcelos, M. Helena; Martins, Anabela
Fonte: Bentham Science Publicador: Bentham Science
Tipo: Artigo de Revista Científica
ENG
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36.55%
For thousands of years medicine and natural products have been closely linked through the use of traditional medicines and natural poisons. Mushrooms have an established history of use in traditional oriental medicine, where most medicinal mushroom preparations are regarded as a tonic, that is, they have beneficial health effects without known negative side-effects and can be moderately used on a regular basis without harm. Mushrooms comprise a vast and yet largely untapped source of powerful new pharmaceutical products. In particular, and most importantly for modern medicine, they represent an unlimited source of compounds which are modulators of tumour cell growth. Furthermore, they may have potential as functional foods and sources of novel molecules. We will review the compounds with antitumor potential identified so far in mushrooms, including low-molecular-weight (LMW, e.g. quinones, cerebrosides, isoflavones, catechols, amines, triacylglycerols, sesquiterpenes, steroids, organic germanium and selenium) and high-molecular-weight compounds (HMW, e.g. homo and heteroglucans, glycans, glycoproteins, glycopeptides, proteoglycans, proteins and RNA-protein complexes).

Antitumor effects of snake venom chemically modified Lys49 phospholipase A(2)-like BthTX-I and a synthetic peptide derived from its C-terminal region

GEBRIM, Luiz Carlos; MARCUSSI, Silvana; MENALDO, Danilo L.; MENEZES, Carla S. R. de; NOMIZO, Auro; HAMAGUCHI, Amelia; SILVEIRA-LACERDA, Elisangela P.; HOMSI-BRANDEBURGO, Maria Ines; SAMPAIO, Suely V.; SOARES, Andreirnar M.; RODRIGUES, Veridiana M.
Fonte: ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD Publicador: ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD
Tipo: Artigo de Revista Científica
ENG
Relevância na Pesquisa
36.67%
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-1 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 S 180 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. (C) 2009 The International Association for Biologicals. Published by Elsevier Ltd. All rights reserved.; Fundacao de Amparo a Pesquisa do Estado de Minas Gerais (FAPEMIG); Conselho Nacional de Desenvolvimento Cientffico e Tecnologico (CNPq); Instituto Nacional de Ciencia e Tecnologia de Toxinas (INCTTox); Fundacao de Amparo Pesquisa do Estado de Sao Paulo (FAPESP)

Antimycobacterial and antitumor activities of Palladium(II) complexes containing isonicotinamide (isn): X-ray structure of trans-[Pd(N(3))(2)(isn)(2)]

SOUZA, Rodrigo A. de; STEVANATO, Alessandra; TREU-FILHO, Oswaldo; NETTO, Adelino V. G.; MAURO, Antonio E.; CASTELLANO, Eduardo E.; CARLOS, Iracilda Z.; PAVAN, Fernando R.; LEITE, Clarice Q. F.
Fonte: ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER Publicador: ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Tipo: Artigo de Revista Científica
ENG
Relevância na Pesquisa
36.67%
Complexes of the type trans-[PdX(2)(isn)(2)] {X = Cl (1), N(3) (2), SCN (3), NCO (4); isn = isonicotinamide} were synthesized and evaluated for in vitro antimycobacterial and antitumor activities. The coordination mode of the isonicotinamide and the pseudohalide ligands was inferred by IR spectroscopy. Single crystal X-ray diffraction determination on 2 showed that coordination geometry around Pd(II) is nearly square planar, with the ligands in a trans configuration. All the compounds demonstrated better in vitro activity against Mycobacterium tuberculosis than isonicotinamide and pyrazinamide. Among the complexes, compound 2 was found to be the most active with MIC of 35.89 mu M. Complexes 1-4 were also screened for their in vitro antitumor activity towards LM3 and LP07 murine cancer cell lines. (C) 2010 Elsevier Masson SAS. All rights reserved.; CAPES; Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES); CNPq; Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq); Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP); FAPESP

Avaliação da interferência do diabetes na biodistribuição e na atividade antitumoral da cisplatina em camundongos; Evaluation of the interference of diabetes in the biodistribution and antitumor activity

Faria, Márcia Cristina da Silva
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Dissertação de Mestrado Formato: application/pdf
Publicado em 23/09/2011 PT
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A cisplatina (Cis-diamino-dicloro-platina II) é um dos mais efetivos quimioterápicos, porém seu uso clínico é altamente limitado devido à sua nefrotoxicidade. Estudos sugerem que o diabetes atua como fator protetor contra a nefrotoxicidade da cisplatina, entretanto, os mecanismos envolvidos ainda não foram elucidados. Esta nefroproteção tem sido associada ao menor acúmulo de cisplatina nos rins, o que poderia ser atribuído a problemas no transporte ativo das células do túbulo proximal ou ainda a alterações farmacocinéticas provocadas pelo diabetes. Entretanto, não se sabe ainda se os mecanismos envolvidos na nefroproteção do diabetes interferem na atividade antitumoral da cisplatina. No presente estudo foram avaliados os efeitos do diabetes na nefrotoxicidade e na atividade antitumoral da cisplatina em camundongos portadores de sarcoma 180, divididos em 4 grupos (n=8): (i) C, grupo controle (sem tratamento); (ii) CIS, grupo tratado com cisplatina; (iii) DB, grupo diabético (estreptozotocina) e (iv) DB+CIS grupo diabético tratado com cisplatina. Os parâmetros avaliados foram: marcadores de função renal e de estresse oxidativo, histopatologia do tecido renal, desenvolvimento do tumor, sobrevida dos animais, genotoxicidade da cisplatina...

Isolamento e caracterização funcional de uma fosfolipase A2 de Bothrops jararaca: avaliação do potencial antitumoral e inflamatório; Isolation and functional characterization of a phospholipase A2 from Bothrops jararaca snake venom: evaluation of its antitumor and inflammatory potential

Araújo, Rafhaella Carolina Cedro
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Dissertação de Mestrado Formato: application/pdf
Publicado em 02/12/2014 PT
Relevância na Pesquisa
36.67%
As fosfolipases A2 (PLA2s) catalisam a hidrólise de ácidos graxos na posição sn-2 das membranas fosfolipídicas e liberam, como subprodutos, ácidos graxos livres. As PLA2s do grupo IIA são encontradas em peçonhas de serpentes da família Viperidae e desempenham diversas atividades apresentando potencial miotóxico, neurotóxico, hemolítico, edematogênico, citotóxico, hipotensivo, anticoagulante, inibição/ativação da agregação plaquetária, bactericida e pró-inflamatório. Esse trabalho teve como objetivo o isolamento e a caracterização funcional de uma PLA2 isolada da peçonha de Bothrops jararaca. Para a purificação dessa proteína, denominada BJ-PLA2-I, foram necessários três passos cromatográficos consecutivos: cromatografia de exclusão molecular em Sephacryl S-200, cromatografia de troca iônica em Source TM 15Q/50mL e cromatografia de troca iônica em MonoQ TM 5/50 GL. A BJ-PLA2-I apresentou elevado grau de pureza por SDS-PAGE e por cromatografia de fase reversa C18, em HPLC. Apresentou ainda, características ácidas, com pI em torno de 4,4 e teve a sua massa molecular determinada por dois métodos, obtendo-se valores bem próximos de 14,8 kDa (SDS-PAGE) e 14,2 kDa (MALDI-TOF). Esse fato é comum considerando que a espectrometria de massas é um método mais preciso e determina de maneira mais exata a massa molecular. O sequenciamento N-terminal da BJ-PLA2-I resultou em 60 resíduos de aminoácidos. O alinhamento múltiplo com outras fosfolipases A2 de serpentes do mesmo gênero mostrou similaridade entre elas...

Antimycobacterial and antitumor activities of Palladium(II) complexes containing isonicotinamide (isn): X-ray structure of trans-[Pd(N-3)(2)(isn)(2)]

de Souza, Rodrigo A.; Stevanato, Alessandra; Treu-Filho, Oswaldo; Netto, Adelino V. G.; Mauro, Antonio E.; Castellano, Eduardo E.; Carlos, Iracilda Z.; Pavan, Fernando R.; Leite, Clarice Q. F.
Fonte: Elsevier France-editions Scientifiques Medicales Elsevier Publicador: Elsevier France-editions Scientifiques Medicales Elsevier
Tipo: Conferência ou Objeto de Conferência Formato: 4863-4868
ENG
Relevância na Pesquisa
36.67%
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES); Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq); Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP); Complexes of the type trans-[PdX2(isn)(2)] {X = Cl (1), N-3 (2), SCN (3), NCO (4); isn = isonicotinamide} were synthesized and evaluated for in vitro antimycobacterial and antitumor activities. The coordination mode of the isonicotinamide and the pseudohalide ligands was inferred by IR spectroscopy. Single crystal X-ray diffraction determination on 2 showed that coordination geometry around Pd(II) is nearly square planar, with the ligands in a trans configuration. All the compounds demonstrated better in vitro activity against Mycobacterium tuberculosis than isonicotinamide and pyrazinamide. Among the complexes, compound 2 was found to be the most active with MIC of 35.89 mu M. Complexes 1-4 were also screened for their in vitro antitumor activity towards LM3 and LP07 murine cancer cell lines. (C) 2010 Elsevier Masson SAS. All rights reserved.

Antitumor effect of Bothrops jararaca venom

da Silva, R. J.; da Silva, M. G.; Vilela, L. C.; Fecchio, D.
Fonte: Carfax Publishing Publicador: Carfax Publishing
Tipo: Artigo de Revista Científica Formato: 99-104
ENG
Relevância na Pesquisa
36.67%
MANY experimental studies have been carried out using snake venoms for the treatment of animal tumors, with controversial results. While some authors have reported an antitumor effect of treatment with specific snake venom fractions, others have reported no effects after this treatment. The aim of this study was to evaluate the effect of Bothrops jararaca venom (BjV) on Ehrlich ascites tumor (EAT) cells in vivo and in vitro. In the in vivo study, Swiss mice were inoculated with EAT cells by the intraperitoneal (i.p.) route and treated with BjV venom (0.4 mg/kg, i.p.), on the 1st, 4th, 7th, 10th, and 13th days. Mice were evaluated for total and differential cells number on the 2nd, 5th, 8th, 11th and 14th days. The survival time was also evaluated after 60 days of tumor growth. In the in vitro study, EAT and normal peritoneal cells were cultivated in the presence of different BjV concentrations (2.5, 5.0, 10.0, 20.0, 40.0, and 80 mug) and viability was verified after 3, 6, 12 and 24 h of cultivation. Results were analyzed statistically by the Kruskal-Wallis and Tukey tests at the 5% level of significance. It was observed that in vivo treatment with BjV induced tumor growth inhibition, increased animal survival time, decreased mortality...

Antitumor and cytotoxic activity of Kielmeyera coriacea mart. Zucc. and Pyrostegia venusta (ker-gawl.) Miers extracts

Silva, Regildo Márcio Gonçalves da; Rodrigues, Débora Thaís Miranda; Valadares, Fillipi; Oliva Neto, Pedro de; Santos, Lucinéia dos; Silva, Luciana Pereira
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 4142-4148
ENG
Relevância na Pesquisa
36.75%
This study aimed to investigate the antitumor and cytotoxicity activities of Kielmeyera coriacea and Pyrostegia venusta extracts. Therefore, the hydroalcoholic extracts of P. venusta flowers and K. coriacea leaves were prepared. The extracts were evaporated and the dry extracts were diluted at concentrations of 1.0, 0.1, 0.01 and 0.001 mg/ml for carrying out the bioassays. Artemia salina eggs were incubated in saline solution at 28°C for 24 h. The larvae were treated with different extracts concentrations and the mortality was evaluated after 24 and 48 h. Five discs of potato were placed in Petri dishes and 50 μl of inoculum of Agrobacterium tumefaciens were added to it at 28°C for 24 h incubation. So, 50 μl of the extracts in different concentrations were added. Positive and negative controls were made. The P. venusta and K. coriacea extracts did not show statistically significant acute toxicity. K. coriacea extract showed (mean% of tumor ± standard deviation) 15.30 ± 3.24, 6.34 ± 3.82, 7.57 ± 2.92 and 5.77 ± 2.85 and P. venusta showed 25.82 ± 5.15, 38.40 ± 8.28, 15.75 ± 4.44 and 13.38 ± 7.92, with their concentrations for the antitumor bioassay, and the positive control showed 25.80 ± 6.14. According to the obtained results it was established that the K. coriacea and P. venusta extracts showed antitumor activity but did not show significant cytotoxic activity in A. salina test.

In vitro and in vivo antitumor activity of crude extracts obtained from Brazilian Chromobacterium sp isolates

Menezes,C.B.A.; Silva,B.P.; Sousa,I.M.O.; Ruiz,A.L.T.G.; Spindola,H.M.; Cabral,E.; Eberlin,M.N.; Tinti,S.V.; Carvalho,J.E.; Foglio,M.A.; Fantinatti-Garboggini,F.
Fonte: Associação Brasileira de Divulgação Científica Publicador: Associação Brasileira de Divulgação Científica
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/01/2013 EN
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Natural products produced by microorganisms have been an important source of new substances and lead compounds for the pharmaceutical industry. Chromobacterium violaceum is a Gram-negative β-proteobacterium, abundant in water and soil in tropical and subtropical regions and it produces violacein, a pigment that has shown great pharmaceutical potential. Crude extracts of five Brazilian isolates of Chromobacterium sp (0.25, 2.5, 25, and 250 µg/mL) were evaluated in an in vitro antitumor activity assay with nine human tumor cells. Secondary metabolic profiles were analyzed by liquid chromatography and electrospray ionization mass spectrometry resulting in the identification of violacein in all extracts, whereas FK228 was detected only in EtCE 308 and EtCE 592 extracts. AcCE and EtCE 310 extracts showed selectivity for NCI/ADR-RES cells in the in vitro assay and were evaluated in vivo in the solid Ehrlich tumor model, resulting in 50.3 and 54.6% growth inhibition, respectively. The crude extracts of Chromobacterium sp isolates showed potential and selective antitumor activities for certain human tumor cells, making them a potential source of lead compounds. Furthermore...

Cytotoxic, antitumor and leukocyte migration activities of resveratrol and sitosterol present in the hidroalcoholic extract of Cissus sicyoides L., Vitaceae, leaves

Lucena,Flávia R. S.; Almeida,Edvaldo R.; Aguiar,Jaciana S.; Silva,Teresinha G.; Souza,Valdênia M. O.; Nascimento,Silene C.
Fonte: Sociedade Brasileira de Farmacognosia Publicador: Sociedade Brasileira de Farmacognosia
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/11/2010 EN
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Cissus sicyoides L. pertains to the Vitaceae family. It is popularly known as "insulina, cipo-pucá, bejuco caro, puci, anil trepador". A vasoconstrictor effect and an antibacterial activity have also been allocated to it. In Brazil, C. sicyoides was evaluated for its anticonvulsant and anti-diabetc properties. Phytochemistry studies identified and isolated sitosterol and resveratrol compounds from its aerial parts which are pointed out as having antitumor activities. The goal of this study was to investigate the cytotoxic and antitumor activities of Cissus sicyoides hydroalcoholic extract as well as its ability to repair leukocytes cells to injured tissue. Cissus sicyoides did not demonstrate cytotoxic activity but showed an inhibition of tumor growth in face of the tumors tested. The extract had a strong chemotactic effect on the twenty four hours period after treatment. The hidroalchoolic extract of Cissus sicyoides presented antitumor activity which was prompted by T lymphocytes recruitment to the local lesion and suggests a new pathway to antitumor activity by activation of lymphoid lineage.

In Vitro Antitumor Activity of Sesquiterpene Lactones from Lychnophora trichocarpha

Saúde-Guimarães,D.A.; Raslan,D.S.; Oliveira,A.B.
Fonte: Sociedade Brasileira de Plantas Medicinais Publicador: Sociedade Brasileira de Plantas Medicinais
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/06/2014 EN
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The sesquiterpene lactones lychnopholide and eremantholide C were isolated from Lychnophora trichocarpha Spreng. (Asteraceae), which is a plant species native to the Brazilian Savannah or Cerrado and popularly known as arnica. Sesquiterpene lactones are known to present a variety of biological activities including antitumor activity. The present paper reports on the evaluation of the in vitro antitumor activity of lychnopholide and eremantholide C, in the National Cancer Institute, USA (NCI, USA), against a panel of 52 human tumor cell lines of major human tumors derived from nine cancer types. Lychnopholide disclosed significant activity against 30 cell lines of seven cancer types with IC100 (total growth concentration inhibition) values between 0.41 µM and 2.82 µM. Eremantholide C showed significant activity against 30 cell lines of eight cancer types with IC100 values between 21.40 µM and 53.70 µM. Lychnopholide showed values of lethal concentration 50% (LC50) for 30 human tumor cell lines between 0.72 and 10.00 µM, whereas eremantholide C presented values of LC50 for 21 human tumor cell lines between 52.50 and 91.20 µM. Lychnopholide showed an interesting profile of antitumor activity. The α-methylene-γ-lactone present in the structure of lychnopholide...

Antitumor activity of C-phycocyanin from Arthronema africanum (Cyanophyceae)

Gardeva,Elena; Toshkova,Reneta; Yossifova,Liliya; Minkova,Kaledona; Ivanova,Natalia; Gigova,Liliana
Fonte: Instituto de Tecnologia do Paraná - Tecpar Publicador: Instituto de Tecnologia do Paraná - Tecpar
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/10/2014 EN
Relevância na Pesquisa
36.67%
Pure C-phycocyanin (C-PC) was isolated from Arthronema africanum to evaluate its potential antitumor effects in vivo and in vitro. Experimental myeloid Graffi tumor in hamsters was used as a model. The cell proliferation assay showed that C-PC treatment, at concentration of 100 µg mL-1 for 24 h, significantly inhibited the growth of Graffi tumor cells (51.4% viability). Agarose gel electrophoresis of the genomic DNA of treated cells displayed time-and concentration-dependent fragmentation pattern, typical for apoptosis. Apoptotic process was related to the increase in cellular manganese and copper/zinc superoxide dismutases and glutathione reductase activities, coupled with a low catalase activity. In vivo C-PC administration (5.0 mg kg-1 body weight) suppressed the tumor transplantability and growth, while the mean survival time of the tumor-bearing hamsters was increased. The results revealed promising antitumor activities of A. africanum C-PC and suggested the potential of this natural biliprotein pigment for future pharmacological and medical applications. The study provided new data on the mechanism of the C-PC induced apoptosis in which the imbalance of antioxidant enzymes that favoured hydrogen peroxide accumulation might play a leading role.

Avaliação do Potencial Citotóxico, Genotóxico e Antitumoral do Ditionato de cis-Tetraamino(oxalato)rutênio(III) em Diferentes Linhagens Celulares; Assessment of the Potential genotoxic and the Antitumor Ditionato Tetraamino cis-(oxalate) ruthenium (III) in Different Cell lines

PEREIRA, Flávia de Castro
Fonte: Universidade Federal de Goiás; BR; UFG; Mestrado em Biologia; Ciências Biolóicas Publicador: Universidade Federal de Goiás; BR; UFG; Mestrado em Biologia; Ciências Biolóicas
Tipo: Dissertação Formato: application/pdf
POR
Relevância na Pesquisa
36.85%
Despite the resounding success of cisplatin and closely related platinum antitumor agents, the movement of other transition-metal antitumor agents toward the clinic has been exceptionally slow. Non-Platinum chemotherapeutic metallopharmaceuticals hold much promise for the future, and needs to be actively explored in a large variety of tumor types in combination therapies. The preparations of metallocomplexes with potential antitumor activity has been one of the main targets of transition metal chemistry since Rosenberg s discovery of cisplatin cisdiamminedichloridoplatinum (II), cis-[Pt(NH3)2Cl2]} cytotoxic activity in the 1960s. In 1978, cisplatin was approved as the first platinumbased drug for the oncology treatment, although several negative side-effects (nephrotoxicity, neurotoxicity, nausea, etc.) had been induced on treated patients. Nevertheless, cisplatin was followed by carboplatin {cis-diammine-1,1´ - yclobutanedicarboxylateplatinum(II), [Pt(NH3)2(cbdc)], approved in 1985} and oxaliplatin 1R,2Rdiamminocyclohexaneoxalatoplatinum(II), [Pt(dach)(ox)], approved in 1996}, which met requirements of improving antitumor activity and reducing disadvantages of cisplatin, carboplatin and oxaliplatin represent the second, and third platinum-based drug generations...

Estudo do potencial genotóxico, citotóxico e antitumoral do composto Cloreto de cis-tetraaminodiclororutênio(III) sobre diferentes células tumorais; To study the potential genotoxic, cytotoxic and antitumor compound Chloride, cis-tetraaminodiclororutênio (III) on various tumor cells

LIMA, Aliny Pereira de
Fonte: Universidade Federal de Goiás; BR; UFG; Mestrado em Biologia; Ciências Biolóicas Publicador: Universidade Federal de Goiás; BR; UFG; Mestrado em Biologia; Ciências Biolóicas
Tipo: Dissertação Formato: application/pdf
POR
Relevância na Pesquisa
36.67%
Current inorganic drugs such cisplatin and related compounds widely used in the treatment cancer, however its application is limited by its severe toxicity and drug resistence. These limitations have prompted a search for news metal-based antitumor agents. Ruthenium (III) complexes represent a new family of promising metal-based anticancer drugs. In the present study, was investigated in vitro the effects of the compound on cell viability, cintetics cell cycle phases, mechanisms of apoptosis and DNA damage on tumors cells. Results of the viability using MTT reduction test and the trypan blue exclusion assay on K-562 cells revealed that this compound significantly reduced the viability of the K-562 tumors cells (IC50 approximately 10.74 and 73.45 μM), respectively, moreover viability assays on A549 lung tumor cells showed that cis-(dichloro)tetrammineruthenium(III) induced effect moderate this cell lines (IC50 > 383 μM). Additionally was observed that this compound exhibits little cytotoxicity towards MRC-5 normal human fibroblast cells (IC50 > 383 μM) when compared to K562 tumor cell line (IC50 10.74 μM). Clonogenic Assay was performed on A549 cells, and observed that lower concentrations (0.38 and 3.8 μM) cis-(dichloro)tetrammineruthenium(III) diminished colony forming ability and highest concentrations (95 and 383 μM) no colony was observed. In cell cycle analysis on K-562 and S180 tumor cells cistetrammineruthenium( III) induced change in the distribution the cell cycle phase since that % of cells entering G1...

Estudo da atividade citotóxica, antitumoral e determinação do perfil tóxico de complexos de rutênio(II)/aminoácidos em células do tumor de Ehrlich in vitro e in vivo; Study of cytotoxic, antitumor activity and toxicity prolife determination the ruthenium(II)/amino acids complexes in Ehrlich tumor cells in vitro and in vivo

Mello, Francyelli Mariana dos Santos
Fonte: Universidade Federal de Goiás; Brasil; UFG; Programa de Pós-graduação em Ciências Farmacêuticas (FF); Faculdade Farmácia - FF (RG) Publicador: Universidade Federal de Goiás; Brasil; UFG; Programa de Pós-graduação em Ciências Farmacêuticas (FF); Faculdade Farmácia - FF (RG)
Tipo: Dissertação Formato: application/pdf
POR
Relevância na Pesquisa
36.75%
Ruthenium complexes represent a new alternative anticancer chemotherapeutics, with activity against several types of cancer, including those resistant to cisplatin, low toxicity and selectivity for tumor cells. The new amino acids/ruthenium(II) complexes (RuAA) w ere tested against Ehrlich ascitic tumor (TAE) cells, murino mammary carcinoma, in vitro and in vivo . The concentration that inhibits 50% of cell viability (IC 50 ) was determined by MTT assay to TAE and L929 cells. Based on the values of IC50 value was determined selective potential of RuAA and selected two complexes most promising, estimated the LD50 (median lethal dose). The toxicological profile of RuMet and RuTrp was determined by acute oral toxicity following the class method, hippocratic screening, and determination of the genotoxic potential evaluated by the comet assay. The effectiveness of the antitumor potential of RuMet and RuTrp was established by the percentage of inhibition of tumor growth and increased survival in vivo after 24 hours of inoculation of TAE. Swiss mice were treated at doses of 2 and 6 mg/kg/day v.ip for 7 days. Hippocratic screening, assessment the viability of TAE cells after treatment...

Infusions and decoctions of Castanea sativa flowers as effective antitumor and antimicrobial matrices

Carocho, Márcio; Calhelha, Ricardo C.; Queiroz, Maria João R.P.; Bento, Albino; Morales, Patricia; Soković, Marina; Ferreira, Isabel C.F.R.
Fonte: Instituto Politécnico de Bragança Publicador: Instituto Politécnico de Bragança
Tipo: Artigo de Revista Científica
ENG
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36.67%
Chestnut trees are one of the most important crops in the North-eastern part of Portugal, representing millions of euros of yearly income. There are many ancestral claims of the health benefits of the consumption of chestnut flowers in infusions that remain unproven. In this manuscript, the antitumor and antimicrobial potential of chestnut flowers from two cultivars, Judia and Longal, extracted through infusions and decoctions are reported. In terms of antitumor activity, the most sensitive cell lines were HepG2 and HCT15 with the cultivar Judia showing higher activity for HCT15 and Longal for HepG2, regardless of the extraction methods. Regarding the antibacterial activity of the extracts, decoctions proved to be more effective with lower minimum inhibition concentrations, while infusions were better in terms of antifungal activity. The good overall antimicrobial activity could justify the inclusion of the flowers in food chain processing to act as a natural antimicrobial. Furthermore, the results corroborate some of the ancestral claims of the consumption of these flowers.; The authors are grateful to PRODER Project No 46577 – PlantLact and to the Foundation for Science and Technology (FCT, Portugal) for financial support to the research center CIMO (Pest-OE/AGR/UI0690/2011) and Ricardo Calhelha’s grant (SFRH/BPD/68344/2010)...

Oil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate

Rolfsen Ferreira da Silva, Gisela Bevilacqua; Scarpa, Maria Virginia; Carlos, Iracilda Zepone; Quilles, Marcela Bassi; Comeli Lia, Raphael Carlos; Tabosa do Egito, Eryvaldo Socrates; Oliveira, Anselmo Gomes de
Fonte: Dove Medical Press Ltd Publicador: Dove Medical Press Ltd
Tipo: Artigo de Revista Científica Formato: 585-594
ENG
Relevância na Pesquisa
36.75%
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES); Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq); Methyl dihydrojasmonate (MJ) has been studied because of its application as an antitumor drug compound. However, as MJ is a poorly water-soluble compound, a suitable oil-in-water microemulsion (ME) has been studied in order to provide its solubilization in an aqueous media and to allow its administration by the parenteral route. The ME used in this work was characterized on the pseudo-ternary phase diagram by dynamic light scattering and rheological measurements. Regardless of the drug presence, the droplet size was directly dependent on the oil/surfactant (O/S) ratio. Furthermore, the drug incorporation into the ME significantly increased the ME diameter, mainly at low O/S ratios. The rheological evaluation of the systems showed that in the absence of drug a Newtonian behavior was observed. On the other hand, in the presence of MJ the ME systems revealed pseudoplastic behavior, independently of the O/S ratio. The in vivo studies demonstrated that not only was the effect on the tumor inhibition inversely dependent on the MJ-loaded ME administered dose, but also it was slightly higher than the doxorubicin alone...

Antitumor activity of leaves of Himatanthus drasticus (Mart.) Plumel-Apocynaceae (janaguba) in the treatment of Sarcoma 180 tumor

Sousa,Eliane Leite de; Grangeiro,Ana Ruth Sampaio; Bastos,Isla Vanessa Gomes Alves; Rodrigues,Guilherme Carvalho Ribeiro; Silva,Maria Joselice e; Anjos,Falba Bernadete Ramos dos; Souza,Ivone Antonia de; Sousa,Cicero Ernandes Leite de
Fonte: Universidade de São Paulo, Faculdade de Ciências Farmacêuticas Publicador: Universidade de São Paulo, Faculdade de Ciências Farmacêuticas
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/06/2010 EN
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Himatanthus drasticus, also known as janaguba, is used popularly in Brazil's Northeastern region in the treatment of cancer. However, no scientific reports are available. The present study is the first investigation on the antitumor activity of crude methanolic extract from Himatanthus drasticus leaves against Sarcoma 180 tumor and on its side effects including acute oral toxicity. The OECD 423 methodology was used to study acute oral toxicity, and the STOCK methodology to assess antitumor activity. The crude extract showed low toxicity at the tested doses (50, 300 and 2000 mg/kg) administered orally. The histopathological analyses demonstrated alterations in liver lung, spleen and kidney. It also showed activity against Sarcoma 180 tumor in male Swiss albino mice, evidencing tumor growth inhibition of 67.7% and 68% at 300 mg/kg and 400 mg/kg doses, respectively.

Synthesis, antitumor and antimicrobial activity of novel 1-substituted phenyl-3-[3-alkylamino(methyl)-2-thioxo-1,3,4-oxadiazol-5-yl] β-carboline derivatives

Savariz,Franciele C.; Formagio,Anelise S. N.; Barbosa,Valéria A.; Foglio,Mary Ann; Carvalho,João E. de; Duarte,Marta C. T.; Dias Filho,Benedito P.; Sarragiotto,Maria Helena
Fonte: Sociedade Brasileira de Química Publicador: Sociedade Brasileira de Química
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/01/2010 EN
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36.67%
With the purpose of activity enhancement of 1-substituted phenyl-3-(2-thioxo-1,3,4-oxadiazol-5-yl) β-carbolines 1a-c, reported as potential antitumor agents in our previous study, herein we report the synthesis and antitumor activity evaluation of several novel Mannich bases 2-7(a-c), by the introduction of different alkylamino(methyl) groups in the 1,3,4-oxadiazole unity of 1a-c. The antimicrobial activities of 1a-c and of 2-7(a-c) were also evaluated. Additionally, an in silico study of the ADME properties of novel synthesized β-carboline derivatives 2-7(a-c) was performed by evaluation of their Lipinski's parameters and topological polar surface area (TPSA) and percentage of absorption (% ABS) data.

Evaluation of molecular descriptors for antitumor drugs with respect to noncovalent binding to DNA and antiproliferative activity

Portugal, José
Fonte: BioMed Central Publicador: BioMed Central
Tipo: Artículo Formato: 259768 bytes; application/pdf
ENG
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34 pages, 6 additional files, 5 tables, 4 figures.; [Background ] Small molecules that bind reversibly to DNA are among the antitumor drugs currently used in chemotherapy. In the pursuit of a more rational approach to cancer chemotherapy based upon these molecules, it is necessary to exploit the interdependency between DNA-binding affinity, sequence selectivity and cytotoxicity. For drugs binding noncovalently to DNA, it is worth exploring whether molecular descriptors, such as their molecular weight or the number of potential hydrogen acceptors/donors, can account for their DNA-binding affinity and cytotoxicity.; [Results] Fifteen antitumor agents, which are in clinical use or being evaluated as part of the National Cancer Institute’s drug screening effort, were analyzed in silico to assess the contribution of various molecular descriptors to their DNA-binding affinity, and the capacity of the descriptors and DNA-binding constants for predicting cell cytotoxicity. Equations to predict drug-DNA binding constants and growth-inhibitory concentrations were obtained by multiple regression following rigorous statistical procedures.; [Conclusions] For drugs binding reversibly to DNA, both their strength of binding and their cytoxicity are fairly predicted from molecular descriptors by using multiple regression methods. The equations derived may be useful for rational drug design. The results obtained agree with that compounds more active across the National Cancer Institute’s 60-cell line data set tend to have common structural features.; Supported by a grant from the former Spanish Ministry of Education and Science (BFU2007-60998) and the FEDER program of the European Community.; Peer reviewed