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Id: biblio-950716
Autor: Hung, Tran Manh; Dang, Nguyen Hai; Dat, Nguyen Tien.
Título: Methanol extract from Vietnamese Caesalpinia sappan induces apoptosis in HeLa cells
Fonte: Biol. Res;47:1-5, 2014. ilus, graf, tab.
Idioma: en.
Projeto: Vietnam National Foundation for Science and Technology Development.
Resumo: BACKGROUND: This study evaluated the cytotoxic activity of extracts from Caesalpinia sappan heartwood against multiple cancer cell lines using an MTT cell viability assay. The cell death though induction of apoptosis was as indicated by DNA fragmentation and caspase-3 enzyme activation. RESULTS: A methanol extract from C. sappan (MECS) showed cytotoxic activity against several of the cancer cell lines. The most potent activity exhibited by the MECS was against HeLa cells with an IC50 value of 26.5 ± 3.2 µg/mL. Treatment of HeLa cells with various MECS concentrations resulted in growth inhibition and induction of apoptosis, as indicated by DNA fragmentation and caspase-3 enzyme activation. CONCLUSION: This study is the first report of the anticancer properties of the heartwood of C. sappan native to Vietnam. Our findings demonstrate that C. sappan heartwood may have beneficial applications in the field of anticancer drug discovery.
Descritores: Extratos Vegetais/farmacologia
Apoptose
Caesalpinia/química
Feixe Vascular de Plantas/metabolismo
Antineoplásicos Fitogênicos/farmacologia
-Sais de Tetrazólio
Vietnã
Ensaios de Seleção de Medicamentos Antitumorais/métodos
Células HeLa
Sobrevivência Celular
Concentração Inibidora 50
Citotoxinas/farmacologia
Linhagem Celular Tumoral
Proliferação de Células/efeitos dos fármacos
Metanol
Ativação Enzimática/efeitos dos fármacos
Caspase 3/metabolismo
Fragmentação do DNA
Formazans
Inibidores do Crescimento/farmacologia
Indicadores e Reagentes
Camundongos Endogâmicos C57BL
Antineoplásicos Fitogênicos/isolamento & purificação
Limites: Humanos
Animais
Feminino
Camundongos
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: CL1.1 - Biblioteca Central


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Id: biblio-950723
Autor: Rosas, Carlos; Sinning, Mariana; Ferreira, Arturo; Fuenzalida, Marcela; Lemus, David.
Título: Celecoxib decreases growth and angiogenesis and promotes apoptosis in a tumor cell line resistant to chemotherapy
Fonte: Biol. Res;47:1-9, 2014. ilus, graf.
Idioma: en.
Projeto: Fondo Nacional de Desarrollo Científico y Tecnológico, Chile.
Resumo: BACKGROUND: During the last few years it has been shown in several laboratories that Celecoxib (Cx), a non-steroidal anti-inflammatory agent (NSAID) normally used for pain and arthritis, mediates antitumor and antiangiogenic effects. However, the effects of this drug on a tumor cell line resistant to chemotherapeutical drugs used in cancer have not been described. Herein we evaluate the angiogenic and antitumor effects of Cx in the development of a drug-resistant mammary adenocarcinoma tumor (TA3-MTXR). RESULTS: Cx reduces angiogenesis in the chick embryonic chorioallantoic membrane assay (CAM), inhibits the growth and microvascular density of the murine TA3-MTXR tumor, reduces microvascular density of tumor metastases, promotes apoptosis and reduces vascular endothelial growth factor (VEGF) production and cell proliferation in the tumor. CONCLUSION: The antiangiogenic and antitumor Cx effects correlate with its activity on other tumor cell lines, suggesting that Prostaglandins (PGs) and VEGF production are involved. These results open the possibility of using Celecoxib combined with other experimental therapies, ideally aiming to get synergic effects.
Descritores: Pirazóis/farmacologia
Sulfonamidas/farmacologia
Neoplasias da Mama/tratamento farmacológico
Anti-Inflamatórios não Esteroides/farmacologia
Apoptose/efeitos dos fármacos
Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos
Neoplasias Pulmonares/secundário
Neovascularização Patológica/tratamento farmacológico
-Pirazóis/administração & dosagem
Sulfonamidas/administração & dosagem
Neoplasias da Mama/patologia
Ensaios de Seleção de Medicamentos Antitumorais
Galinhas
Marcação In Situ das Extremidades Cortadas
Inibidores da Angiogênese/farmacologia
Linhagem Celular Tumoral
Fator A de Crescimento do Endotélio Vascular/antagonistas & inibidores
Membrana Corioalantoide
Proliferação de Células/efeitos dos fármacos
Celecoxib
Limites: Animais
Feminino
Embrião de Galinha
Camundongos
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: CL1.1 - Biblioteca Central


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Id: biblio-886755
Autor: VICTOR, MAURICIO M; DAVID, JORGE M; SAKUKUMA, MARIA C K; COSTA-LOTUFO, LETÍCIA V; MOURA, ANDREA F; ARAÚJO, ANA J.
Título: Terpene Esters from Natural Products: Synthesis and Evaluation of Cytotoxic Activity
Fonte: An. acad. bras. ciênc;89(3):1369-1379, July-Sept. 2017. tab, graf.
Idioma: en.
Resumo: ABSTRACT Natural steroids and triterpenes such as b-sitosterol, stigmasterol, lupeol, ursolic and betulinic acids were transformed into its hexanoic and oleic esters, to evaluate the influence of chemical modification towards the cytotoxic activities against tumor cells. The derivatives were evaluated against five tumor cell lines [OVCAR-8 (ovarian carcinoma); SF-295 (glioblastoma); HCT-116 (colon adenocarcinoma); HL-60 (leukemia); and PC-3 (prostate carcinoma)] and the results showed only betulinic acid hexyl ester exhibits cytotoxic potential activity.
Descritores: Triterpenos/farmacologia
Lamiaceae/química
Triterpenos Pentacíclicos/farmacologia
Fabaceae/química
Antineoplásicos/farmacologia
-Triterpenos/isolamento & purificação
Triterpenos/química
Ensaios de Seleção de Medicamentos Antitumorais
Lamiaceae/classificação
Concentração Inibidora 50
Linhagem Celular Tumoral
Ésteres
Triterpenos Pentacíclicos/isolamento & purificação
Triterpenos Pentacíclicos/química
Fabaceae/classificação
Antineoplásicos/isolamento & purificação
Antineoplásicos/química
Limites: Humanos
Responsável: BR1.1 - BIREME


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Id: biblio-1049323
Autor: Payolla, Filipe Boccato; Aleixo, Nadia Andrade; Nogueira, Flávia Aparecida Resende; Massabni, Antonio Carlos.
Título: In vitro Studies of Antitumor Activity of Vanadium Complexes with Orotic and Glutamic Acids / Estudos in vitro da Atividade Antitumoral de Complexos de Vanádio com Ácidos Órotico e Glutâmico / Estudios in vitro de la Actividad Antitumoral de Complejos de Vanadio con Ácidos Orótico y Glutámico
Fonte: Rev. bras. cancerol;66(1), 20200129.
Idioma: en.
Resumo: Introduction: Three vanadium complexes with orotic and glutamic acids, in their anion forms, were prepared and their in vitro cytotoxicity toward human lung fibroblasts (MRC-5), human hepatocellular carcinoma (HepG2) and human colorectal adenocarcinoma (Caco-2) are reported. Objective: Describe the synthesis and characterization of new vanadium complexes with orotic and glutamic acids, and test its antitumor activity against HepG2 and Caco-2. Method: The complexes were formulated as VO (oro), VO (α-glu) and VO (γ-glu) based on chemical, thermogravimetric analyses and infrared spectra. Results: Resazurin assay demonstrates its cytotoxicity against the HepG2 and Caco-2 cell lines with the IC50 ranging from 7.90 to 44.56 µmol.L-1. The cytotoxicity profiles indicate that the tumoral lines show more activity than the cells MRC-5, with selectivity indexes ranging from 1.58 to 8.96. Conclusion: The three complexes had better in vitro activity than cisplatin for both normal and cancer cell lines. The IC50 values are two to six times better for the cancer cell ines and five to seven times better for the normal cell lines. This study indicates that the complexes obtained are promising candidates for antitumor drugs.

Introdução: Foram preparados três complexos de vanádio com ácidos orótico e glutâmico, em suas formas aniônicas, e foi testada sua citotoxicidade in vitro para fibroblastos pulmonares humanos (MRC-5), carcinoma hepatocelular humano (HepG2) e adenocarcinoma colorretal humano (Caco-2). Objetivo: Descrever a síntese e caracterização de novos complexos de vanádio com ácidos orótico e glutâmico e testar sua atividade antitumoral contra HepG2 e Caco-2. Método: Os complexos foram formulados como VO (oro), VO (α-glu) e VO (γ-glu) com base em análises químicas, termogravimétricas e espectros no infravermelho. Resultados: O ensaio de resazurina demonstrou sua citotoxicidade contra as linhagens celulares HepG2 e Caco-2 com o IC50 variando de 7,90 a 44,56 µmol.L-1. Os perfis de citotoxicidade indicam que as linhas tumorais apresentam maior atividade que as células MRC-5, com índices de seletividade variando de 1,58 a 8,96. Conclusão: Os três complexos tiveram melhor atividade in vitro do que a cisplatina, tanto para linhagens celulares normais como cancerosas. Os valores de IC50 são de duas a seis vezes melhores para as linhagens celulares cancerosas e de cinco a sete vezes melhores para as linhagens celulares normais. Este estudo indica que os complexos obtidos são promissores candidatos a fármacos antitumorais.

Introducción: Tres complejos de vanadio con ácidos orótico y glutámico, en sus formas aniónicas, fueram preparados. Su citotoxicidad in vitro hacia los fibroblastos pulmonares humanos (MRC-5), el carcinoma hepatocelular humano (HepG2) y el adenocarcinoma colorrectal humano (Caco-2) son reportados. Objetivo: Los principales objetivos de este trabajo son describir la síntesis y caracterización de nuevos complejos de vanadio con ácidos orótico y glutámico y probar su actividad antitumoral contra el HepG2 y el Caco-2. Método: Los complejos fueron formulados como VO (oro), VO (α-glu) y VO (γ-glu) basados en análisis químicos, termogravimétricos y espectros infrarrojos. El ensayo de resazurina demuestra su citotoxicidad contra las líneas celulares HepG2 y Caco-2 con el IC50 que van de 7,90 a 44,56 µmol.L-1. Los perfiles de citotoxicidad indican que las líneas tumorales presentan mayor actividad que los MRC-5, con índices de selectividad que van de 1,58 a 8,96. Conclusión: Los tres complejos tuvieron mejor actividad in vitro que el cisplatino, tanto para líneas celulares normales como para líneas celulares cancerosas. Los valores del IC50 son de dos a seis veces mejores para las líneas celulares de cáncer y de cinco a siete veces mejores para las líneas celulares normales. Este estudio indica que los complejos obtenidos son candidatos prometedores para fármacos antitumorales.
Descritores: Ácido Orótico/farmacologia
Compostos de Vanádio/farmacologia
Ácido Glutâmico/farmacologia
Linhagem Celular Tumoral/efeitos dos fármacos
-Técnicas In Vitro
Ensaios de Seleção de Medicamentos Antitumorais
Neoplasias Colorretais/tratamento farmacológico
Adenocarcinoma/tratamento farmacológico
Carcinoma Hepatocelular/tratamento farmacológico
Fibroblastos Associados a Câncer/efeitos dos fármacos
Neoplasias Pulmonares/tratamento farmacológico
Antineoplásicos/farmacologia
Limites: Humanos
Responsável: BR440.1 - Biblioteca Geraldo Matos de Sá . Hospital do Câncer I


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Id: biblio-1039079
Autor: He, Suna; Wang, Bowen; Zhang, Runfang; Zhou, Huanhuan; Yang, Qian.
Título: Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes
Fonte: Braz. J. Pharm. Sci. (Online);55:e18204, 2019. tab, graf.
Idioma: en.
Resumo: The development and clinical application of 2-methoxyestradiol (2-ME) as a new type of antitumor drug are limited due to its poor solubility, rapid metabolism in vivo, and large oral dosage. 2-ME-loaded pH-sensitive liposomes (2-ME-PSLs) was prepared containing the lipids, Lipoid E-80 (E-80), cholesteryl hemisuccinate (CHEMS), and cholesterol (CHOL) via thin-film ultrasonic dispersion. First, preparation conditions of 2-ME-PSLs were optimized by orthogonal test. Then 2-ME-PSL was characterized, and the release behavior and stability of 2-ME-PSL in vitro were evaluated. The optimal preparation conditions for 2-ME-PSLs were as follows: 2-ME : E-80+CHEMS 1:15; CHOL : E-80+CHEMS 1:5; ultrasonication time 20 minutes. The mean particle size, PDI, zeta potential, and entrapment efficiency (EE) of 2-ME-PSLs were 116 ± 9 nm, 0.161 ± 0.025, −22.4 ± 1.7 mV, and 98.6 ± 0.5%, respectively. As viewed under a transmission electron microscope, 2-ME-PSLs were well dispersed and almost spherical. They exhibited significant pH-sensitive properties and were fairly stable when diluted with a physiological solution. In conclusion, 2-ME-PSLs were successfully prepared and possessed a favorable pH sensitivity and good dissolution stability with a normal solution
Descritores: Técnicas In Vitro/instrumentação
/farmacocinética
AMERICAN HOSPITAL ASSOCIATION9TEMEFOS/farmacocinética
Lipossomos/análise
-Ensaios de Seleção de Medicamentos Antitumorais/classificação
Concentração de Íons de Hidrogênio/efeitos dos fármacos
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas


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Id: lil-623942
Autor: Oliveira, Marilda Meirelles de.
Título: Antitumor activity of chemical modified natural compounds
Fonte: Mem. Inst. Oswaldo Cruz;86(supl.2):61-65, 1991. ilus, graf.
Idioma: en.
Conferência: Apresentado em: Brazilian-Sino Symposium on Chemistry and Pharmacology of Natural Products, Rio de Janeiro, Dec. 10-14, 1989.
Resumo: Search of new activity substances starting from chemotherapeutic agents, continously appears in international literature. Perhaps this search has been done more frequently in the field of anti-tumor chemotherapy on account of the unsuccess in saving advanced stage patients. The new point in this matter during the last decade was computer aid in planning more rational drugs. In near future "the accessibility of supercomputers and emergence of computer net systems, willopen new avenues to rational drug design" (Portoghese, P. S. J. Med. Chem. 1989, 32, 1). Unknown pharmacological active compounds synthetized by plants can be found even without this eletronic devices, as tradicional medicine has pointed out in many contries, and give rise to a new drug. These compounds used as found in nature or after chemical modifications have produced successful experimental medicaments as FAA, "flavone acetic acid" with good results as inibitors of slow growing animal tumors currently in preclinical evaluation for human treatment. In this lecture some international contributions in the field of chemical modified compounds as antineoplasic drugs will be examined, particularly those done by Brazilian researches.
Descritores: Antineoplásicos Fitogênicos/isolamento & purificação
Antineoplásicos Fitogênicos/síntese química
Antineoplásicos Fitogênicos/química
-Brasil
Ensaios de Seleção de Medicamentos Antitumorais
Desenho de Fármacos
Avaliação de Medicamentos
Antineoplásicos
Limites: Humanos
Animais
Responsável: BR1.1 - BIREME


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Id: lil-623939
Autor: Camargo, J. L. V. de.
Título: Medium-term protocols for in vivo evaluation of chemical modifiers of carcinogenesis
Fonte: Mem. Inst. Oswaldo Cruz;86(supl.2):47-50, 1991. ilus, tab.
Idioma: en.
Conferência: Apresentado em: Brazilian-Sino Symposium on Chemistry and Pharmacology of Natural Products, Rio de Janeiro, Dec. 10-14, 1989.
Resumo: Cancer development is a long-term multistep process which allows interventional measure before the clincial disease emerges. the detection of natural substances which can block the process of carcinogenesis is a important as the identification of anti-tumoral drugs since they might be used in chemoprevention of cancer in high-risk groups. In vivo rodent models of chemical caecinogenesis have been used to study plant-derived inhibitors of carcinofenesis such as indols, coumarins, isothiocyanates, flavones, phenols and allyl-sulfides. Since the standard in vivo rodent bioassay is prolonged and expensive, shorter reliable protocols are needed. Two in vivo medium-term protocols for evaluation of modifiers of carcinogenesis are presented, one related to liver and the other to bladder cancer. Both protocols use rats, last 8 and 36 weeks and are based on the two-step concept of carcinogenesis: initiation and promotion. The protocols use respectively the development of altered foci of hepatocytes expressing immunochistochemically the placental form of gluthation S-transferase and the appearence of pre-neoplastic urothelium and papillomas as the "end-points". the use of these protocols for detection of plantpderived inhibitors of carcinogenesis appear warranted.
Descritores: Anticarcinógenos/isolamento & purificação
Anticarcinógenos/uso terapêutico
Anticorpos Antineoplásicos
-Plantas Medicinais/química
Ensaios de Seleção de Medicamentos Antitumorais
Limites: Animais
Responsável: BR1.1 - BIREME


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Almeida, F. R. C
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Id: lil-623938
Autor: Rao, V. S. N; Almeida, F. R. C; Moraes, A. P; Silva, J. V; Nascimento, S. C; Moraes, M. O.
Título: Evaluation of the purified fraction of Wilbrandia (c. f. ) verticillata for antitumour activity
Fonte: Mem. Inst. Oswaldo Cruz;86(supl.2):43-45, 1991. tab.
Idioma: en.
Conferência: Apresentado em: Brazilian-Sino Symposium on Chemistry and Pharmacology of Natural Products, Rio de Janeiro, Dec. 10-14, 1989.
Resumo: Cucurbatacins are known to produce cytotoxic and anticancer activities. Two novel norcucurbitacin glucosides (Wvl and Wv2) have recently been isolated from a purified fraction obtained from the rhizome of Wilbrandia verticillata. The present study evaluates the cytotoxic and anti-tumour activities of the norcucurbitacins. We have found a regular cytotoxicity in KB cells (Cy50 = 12µg/ml) as well as a significant inhibition in the Walker 256 carcinosarcoma growth (approximately 75%).
Descritores: Triterpenos/isolamento & purificação
Triterpenos/uso terapêutico
Antineoplásicos Fitogênicos/isolamento & purificação
Antineoplásicos Fitogênicos/uso terapêutico
-Brasil
Ensaios de Seleção de Medicamentos Antitumorais
Células KB
Carcinoma 256 de Walker
Fitoterapia
Limites: Humanos
Animais
Ratos
Responsável: BR1.1 - BIREME


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Id: biblio-839471
Autor: Karri, Veera Venkata Satyanarayana Reddy; Dhandapani, Nagasamy Venkatesh; Mannemala, Sai Sandeep; Radhakrishna, Kollipara; Mulukutla, Shashank; Sudunagunta, Dedeepya.
Título: Ameliorating the antitumor activity of lenalidomide using PLGA nanoparticles for the treatment of multiple myeloma
Fonte: Braz. J. Pharm. Sci. (Online);53(2):e15185, 2017. tab, graf.
Idioma: en.
Resumo: Abstract Lenalidomide (LND) is an anti-cancer drug and an effective derivative of thalidomide used for multiple myeloma therapy. Because of its poor solubility in water, LND is known to cause low oral bioavailability (below 33%), and as a direct consequence of this, the dosing frequency is extended thus increasing risk of toxicity. To improve its bioavailability and sustained release, the present study aims to formulate polymeric nanoparticles (NPs) for LND using [Poly (lactic-co-glycolic acid)] (PLGA) as a polymer. The polymeric NPs were evaluated for particle size, SEM, XRD, drug content, entrapment efficiency (EE), in vitro release studies and in vivo bioavailability studies in rats. The formulated NPs possessed a size of 179±0.9 nm and a zeta potential of -24.4 ± 0.2 mV. The drug loading and EE of the optimized formulation was 32 ± 0.37 % and 78 ± 0.92% respectively. After oral administration of LND PLGA-NPs, the relative bioavailability was enhanced about 3.67-fold compared to LND. This study demonstrates the novel drug delivery for LND with PLGA-NPs as effective drug delivery system for sustained delivery of LND.
Descritores: Ensaios de Seleção de Medicamentos Antitumorais/estatística & dados numéricos
Nanopartículas/estatística & dados numéricos
Mieloma Múltiplo/prevenção & controle
-Polímeros/análise
Solubilidade/efeitos dos fármacos
Limites: Animais
Masculino
Feminino
Ratos
Tipo de Publ: Técnicas In Vitro
Responsável: BR1.1 - BIREME


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Alves, Ricardo José
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Id: biblio-839451
Autor: Freire, Rachel Lima Marcelino; Marques, Maria Betânia de Freitas; Souza-Fagundes, Elaine Maria de; Oliveira, Renata Barbosa de; Alves, Ricardo José.
Título: Synthesis and evaluation of platinum complexes with potential antitumor activity
Fonte: Braz. J. Pharm. Sci. (Online);53(1):e15235, 2017. tab, graf.
Idioma: en.
Resumo: Abstract A novel series of platinum (II) complexes was synthesized and the complexes were evaluated for their in vitro cytotoxicity against four human cancer cells lines. Five platinum complexes showed activity against at least one tumor cell line. Complexes 3 and 6 were promising, being active, at micromolar concentrations, against all the assayed tumor cell lines. Compound 3 was selected for further studies in mice with Ehrlich solid tumors and it was able to reduce the rate of tumor growth significantly during the first seven days. However, at the end of the experiments, there was no significant difference between the group of animals treated with 3 and the control group. The low solubility of the compound in the assay conditions can explain, at least in part, these results.
Descritores: Platina/análise
Ensaios de Seleção de Medicamentos Antitumorais/instrumentação
-Testes Imunológicos de Citotoxicidade/classificação
Carcinoma de Ehrlich/classificação
Citotoxinas/efeitos adversos
Limites: Animais
Masculino
Feminino
Ratos
Responsável: BR1.1 - BIREME



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