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Id: biblio-1090602
Autor: Freitas, Carla S. M. de; Soares, Aleida N.
Título: Efficacy of Leuprorelide acetate (Eligard®) in daily practice in Brazil: a retrospective study with depot formulations in patients with prostate cancer
Fonte: Int. braz. j. urol;46(3):383-389, May-June 2020. tab, graf.
Idioma: en.
Resumo: ABSTRACT Introduction: Androgen deprivation therapy (ADT) is the mainstay of therapy for advanced prostate cancer. Studies addressing the efficacy of different depot formulations of long acting luteinizing hormone releasing hormone agonists in the Brazilian population are lacking. We aimed to compare the efficacy of three schedules of leuprolide acetate in lowering PSA in a real world population. Materials and Methods: We reviewed the medical records of patients with prostate cancer seen at our institution between January 2007 and July 2018. We analyzed patients treated with long-acting leuprolide acetate and grouped these patients into three strata according to the administration of ADT every 1, 3 or 6 months. The primary outcome was the serum prostate specific antigen (PSA) levels at 6 and 12 months after treatment initiation. We used Friedman test to compare the distribution of PSA levels at baseline and at 6 and 12 months within each treatment stratum. We considered two-sided P values <0.05 as statistically significant. We analyzed toxicity descriptively. Results: We analyzed a total of 932 patients, with a median age of 72 years and a median time since diagnosis of prostate cancer of 8.5 months. ADT was administered monthly in 115 patients, quarterly in 637, and semiannually in 180. Nearly half of the patients had locally advanced disease. In comparison with baseline, median serum PSA levels were reduced at 12 months by at least 99.7% in the three strata (P <0.001 in all cases). Sexual impotence and hot flashes were the most frequently reported toxicities. Conclusion: To our knowledge, this is the largest assessment of real-world data on alternative schedules of leuprolide in a Brazilian population. Our study suggests that PSA levels can be effectively be reduced in most patients treated with monthly, quarterly, or semiannual injections of long-acting leuprolide acetate.
Descritores: Neoplasias da Próstata
Leuprolida/uso terapêutico
Antígeno Prostático Específico/metabolismo
Antineoplásicos Hormonais/uso terapêutico
-Brasil/epidemiologia
Estudos Retrospectivos
Antagonistas de Androgênios
Acetatos
Limites: Humanos
Masculino
Idoso
Responsável: BR1.1 - BIREME


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Id: biblio-950737
Autor: Lee, Won-Seok; Lim, Jin-Han; Sung, Myung-Soon; Lee, Eun-Gyeong; Oh, Yoo-Jeong; Yoo, Wan-Hee.
Título: Ethyl acetate fraction from Angelica sinensis inhibits IL-1ß-induced rheumatoid synovial fibroblast proliferation and COX-2, PGE2, and MMPs production
Fonte: Biol. Res;47:1-8, 2014. graf.
Idioma: en.
Resumo: BACKGROUND: The root of Angelica sinensis (AS), also known as "Dang-gui," was a popular herbal medicine widely used in the treatment of gynecological diseases in China, Korea, and Japan for a long time. This study aimed to determine the effects of ethyl acetate fraction from Angelica sinensis (EAAS) on the interleukin-1ß (IL-1ß)-induced proliferation of rheumatoid arthritis synovial fibroblasts (RASFs), and production of matrix metalloproteinases (MMPs), cyclooxygenase (COX) 2, and prostaglandin E2 (PGE2), involved in articular bone and cartilage destruction, by RASFs. RESULTS: RASF proliferation was evaluated with cholecystokinin octapeptide (CCK-8) reagent in the presence of IL-1ß with/without EAAS. Expression of MMPs, tissue inhibitor of metalloproteinases-1 (TIMP-1), COXs, PGE2, and intracellular mitogen-activated protein kinase (MAPK) signaling molecules, including p-ERK, p-p38, p-JNK, and NF-κB, were examined using immunoblotting or semi-quantitative reverse transcription-polymerase chain reaction and enzyme-linked immunosorbent assay. EAAS inhibited IL-1ß-induced RASF proliferation; MMP-1, MMP-3, and COX-2 mRNA and protein expressions; and PGE2 production. EAAS also inhibits the phosphorylation of ERK-1/2, p38, and JNK, and activation of NF-κB by IL-1ß. CONCLUSION: EAAS might be a new therapeutic modality for rheumatoid arthritis management.
Descritores: Artrite Reumatoide/metabolismo
Bolsa Sinovial/citologia
Mediadores da Inflamação/metabolismo
Angelica sinensis/química
Proliferação de Células/efeitos dos fármacos
Fibroblastos/efeitos dos fármacos
-Artrite Reumatoide/patologia
Proteínas Recombinantes/farmacologia
Ensaio de Imunoadsorção Enzimática
Extratos Vegetais/farmacologia
Dinoprostona/metabolismo
Immunoblotting
NF-kappa B/efeitos dos fármacos
Raízes de Plantas/química
Metaloproteinases da Matriz/efeitos dos fármacos
Metaloproteinases da Matriz/metabolismo
Medicina Herbária
Ciclo-Oxigenase 2/efeitos dos fármacos
Ciclo-Oxigenase 2/metabolismo
Interleucina-1beta/farmacologia
Cultura Primária de Células
Reação em Cadeia da Polimerase em Tempo Real
Fibroblastos/citologia
Fibroblastos/metabolismo
Citometria de Fluxo
Articulação do Joelho/citologia
Acetatos
Limites: Humanos
Responsável: CL1.1 - Biblioteca Central


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Id: biblio-950741
Autor: Hossain, Mohammad Mobarak; Ahamed, Sayed Koushik; Dewan, Syed Masudur Rahman; Hassan, Md Mahadi; Istiaq, Arif; Islam, Mohammad Safiqul; Moghal, Md Mizanur Rahman.
Título: In vivo antipyretic, antiemetic, in vitro membrane stabilization, antimicrobial, and cytotoxic activities of different extracts from Spilanthes paniculata leaves
Fonte: Biol. Res;47:1-9, 2014. graf, tab.
Idioma: en.
Resumo: BACKGROUND: The study was conducted to evaluate the in vitro antimicrobial activity, cytotoxic, and membrane stabilization activities, and in vivo antiemetic and antipyretic potentials of ethanolic extract, n-hexane and ethyl acetate soluble fractions of Spilanthes paniculata leaves for the first time widely used in the traditional treatments in Bangladesh. RESULTS: In antipyretic activity assay, a significant reduction (P < 0.05) was observed in the temperature in the mice tested. At dose 400 mg/kg-body weight, the n-hexane soluble fraction showed the effect (36.7 ± 0.63°C ) as like as the standard (dose 150 mg/kg-body weight) after 5 h of administration. Extracts showed significant (P < 0.001) potential when tested for the antiemetic activity compared to the standard, metoclopramide. At dose 50 mg/kg-body weight, the standard showed 67.23% inhibition, whereas n-hexane and ethyl acetate soluble fractions showed 37.53% and 24.93% inhibition of emesis respectively at dose 400 mg/kg-body weight. In antimicrobial activity assay, the n-hexane soluble fraction (400 µg/disc) showed salient activity against the tested organisms. It exerts highest activity against Salmonella typhi (16.9 mm zone of inhibition); besides, crude, and ethyl acetate extracts showed resistance to Bacillus cereus and Bacillus subtilis, and Vibrio cholera respectively. All the extracts were tested for lysis of the erythrocytes. At the concentration of 1mg/ml, ethanol extract, and n-hexane and ethyl acetate soluble fractions significantly inhibited hypotonic solution induced lysis of the human red blood cell (HRBC) (27.406 ± 3.57, 46.034 ± 3.251, and 30.72 ± 5.679% respectively); where standard drug acetylsalicylic acid (concentration 0.1 mg/ml) showed 77.276 ± 0.321% inhibition. In case of heat induced HRBC hemolysis, the plant extracts also showed significant activity (34.21 ± 4.72, 21.81 ± 3.08, and 27.62 ± 8.79% inhibition respectively). In the brine shrimp lethality bioassay, the n-hexane fraction showed potent (LC50 value 48.978 µg/ml) activity, whereas ethyl acetate fraction showed mild (LC50 value 216.77 µg/ml) cytotoxic activity. CONCLUSIONS: Our results showed that the n-hexane extract has better effects than the other in all trials. In the context, it can be said that the leaves of S. paniculata possess remarkable pharmacological effects, and justify its folkloric use as antimicrobial, antipyretic, anti-inflammatory, and antiemetic agent. Therefore, further research may be suggested to find possible mode of action of the plant part.
Descritores: Asteraceae/química
Citotoxinas/farmacologia
Membrana Eritrocítica/efeitos dos fármacos
Antipiréticos/farmacologia
Antibacterianos/farmacologia
Antieméticos/farmacologia
-Artemia/efeitos dos fármacos
Salmonella typhi/efeitos dos fármacos
Staphylococcus aureus/efeitos dos fármacos
Bacillus cereus/efeitos dos fármacos
Bacillus subtilis/efeitos dos fármacos
Vibrio cholerae/efeitos dos fármacos
Bioensaio/mortalidade
Extratos Vegetais/farmacologia
Testes de Sensibilidade Microbiana
Galinhas
Folhas de Planta/química
Asteraceae/classificação
Etanol
Membrana Eritrocítica/fisiologia
Escherichia coli/efeitos dos fármacos
Testes de Sensibilidade a Antimicrobianos por Disco-Difusão
Temperatura Alta
Hexanos
Medicina Tradicional
Acetatos
Limites: Humanos
Animais
Camundongos
Responsável: CL1.1 - Biblioteca Central


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Id: biblio-950747
Autor: Khan, Alam; Islam, Md Hedayetul; Islam, Md Ekramul; Al-Bari, Md Abdul Alim; Parvin, Mst Shahnaj; Sayeed, Mohammed Abu; Islam, Md Nurul; Haque, Md Ekramul.
Título: Pesticidal and pest repellency activities of rhizomes of Drynaria quercifolia (J. Smith) against Tribolium castaneum (Herbst)
Fonte: Biol. Res;47:1-6, 2014. ilus, graf, tab.
Idioma: en.
Resumo: BACKGROUND: Tribolium castaneum (Herbst) is a harmful pest of stored grain and flour-based products in tropical and subtropical region. In the present study, rhizome of Drynaria quercifolia (J. Smith) was evaluated for pesticidal and pest repellency activities against T. castaneum, using surface film method and filter paper disc method, respectively. In addition, activity of the isolated compound 3,4-dihydroxybenzoic acid was evaluated against the pest. RESULTS: Chloroform soluble fraction of ethanol extract of rhizome of D. quercifolia showed significant pesticidal activity at doses 0.88 to 1.77 mg/cm² and significant pest repellency activity at doses 0.94 to 0.23 mg/cm². No pesticidal and pest repellency activity was found for petroleum ether, ethyl acetate and methanol soluble fractions of ethanol extract as well as for 3,4-dihydroxybenzoic acid. CONCLUSION: Considering our findings it can be concluded that chloroform soluble fraction of rhizome of D. quercifoliais useful in controlling T. castaneum of stored grain and flour-based products.
Descritores: Praguicidas
Tribolium/efeitos dos fármacos
Controle de Pragas/métodos
Polypodiaceae/química
Rizoma/química
Hidroxibenzoatos/farmacologia
Repelentes de Insetos/farmacologia
-Extratos Vegetais/isolamento & purificação
Extratos Vegetais/química
Clorofórmio
Etanol
Metanol
Alcanos
Hidroxibenzoatos/isolamento & purificação
Dose Letal Mediana
Acetatos
Limites: Animais
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: CL1.1 - Biblioteca Central


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Id: biblio-950772
Autor: Zeb, Anwar; Sadiq, Abdul; Ullah, Farhat; Ahmad, Sajjad; Ayaz, Muhammad.
Título: Investigations of anticholinestrase and antioxidant potentials of methanolic extract, subsequent fractions, crude saponins and flavonoids isolated from Isodon rugosus
Fonte: Biol. Res;47:1-10, 2014. graf, tab.
Idioma: en.
Resumo: BACKGROUND: Based on the ethnomedicinal uses and the effective outcomes of natural products in various diseases, this study was designed to evaluate Isodon rugosus as possible remedy in oxidative stress, alzheimer's and other neurodegenerative diseases. Acetylecholinestrase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of crude methanolic extract (Ir.Cr), resultant fractions (n-hexane (Ir.Hex), chloroform (Ir.Cf), ethyl acetate (Ir.EtAc), aqueous (Ir.Aq)), flavonoids (Ir.Flv) and crude saponins (Ir.Sp) of I. rugosus were investigated using Ellman's spectrophotometric method. Antioxidant potential of I. rugosus was determined using DPPH, H2O2 and ABTS free radicals scavenging assays. Total phenolic and flavonoids contents of plant extracts were determined and expressed in mg GAE/g dry weight and mg RTE/g of dry sample respectively. RESULTS: Among different fractions Ir.Flv and Ir.Cf exhibited highest inhibitory activity against AChE (87.44 ± 0.51, 83.73 ± 0.64%) and BChE (82.53 ± 0.71, 88.55 ± 0.77%) enzymes at 1 mg/ml with IC50 values of 45, 50 for AChE and 40, 70 µg/ml for BChE respectively. Activity of these fractions were comparable to galanthamine causing 96.00 ± 0.30 and 88.61 ± 0.43% inhibition of AChE and BChE at 1 mg/ml concentration with IC50 values of 20 and 47 µg/ml respectively. In antioxidant assays, Ir.Flv, Ir.Cf, and Ir.EtAc demonstrated highest radicals scavenging activities in DPPH and H2O2 assays which were comparable to ascorbic acid. Ir.Flv was found most potent with IC50 of 19 and 24 µg/ml against DPPH and H2O2 radicals respectively. Whereas antioxidant activates of plant samples against ABTS free radicals was moderate. Ir.Cf, Ir.EtAc and Ir.Cr showed high phenolic and flavonoid contents and concentrations of these compounds in different fractions correlated well to their antioxidant and anticholinestrase activities. CONCLUSION: It may be inferred from the current investigations that the Ir.Sp, Ir.Flv and various fractions of I. rugosus are good sources of anticholinesterase and antioxidant compounds. Different fractions can be subjected to activity guided isolation of bioactive compounds effective in neurological disorders.
Descritores: Saponinas/análise
Flavonoides/análise
Extratos Vegetais/química
Inibidores da Colinesterase/análise
Isodon/química
Antioxidantes/análise
-Picratos/metabolismo
Acetilcolinesterase/efeitos dos fármacos
Saponinas/isolamento & purificação
Espectrofotometria/métodos
Ácidos Sulfônicos/metabolismo
Flavonoides/isolamento & purificação
Compostos de Bifenilo/metabolismo
Butirilcolinesterase/efeitos dos fármacos
Clorofórmio
Sequestradores de Radicais Livres/metabolismo
Estresse Oxidativo/efeitos dos fármacos
Concentração Inibidora 50
Isodon/classificação
Isodon/enzimologia
Componentes Aéreos da Planta/química
Misturas Complexas
Metanol
Benzotiazóis/metabolismo
Radicais Livres/análise
Hexanos
Peróxido de Hidrogênio/metabolismo
Medicina Tradicional
Acetatos
Responsável: CL1.1 - Biblioteca Central


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Id: biblio-1089372
Autor: Shen, Congxiang; Chen, Fang; Wang, Huigang; Zhang, Xinyu; Li, Guanxue; Wen, Zhong.
Título: Individualized treatment for allergic rhinitis based on key nasal clinical manifestations combined with histamine and leukotriene D4 levels / Tratamento individualizado para a rinite alérgica baseado nas principais manifestações clínicas nasais e dos níveis de histamina e leucotrieno D4
Fonte: Braz. j. otorhinolaryngol. (Impr.);86(1):63-73, Jan.-Feb. 2020. tab, graf.
Idioma: en.
Projeto: Science and Technology Program Project of Guangdong Province.
Resumo: Abstract Introduction The types of allergic rhinitis are roughly classified based on the causative antigens, disease types, predilection time, and symptom severity. Objective To examine the clinical typing and individualized treatment approach for allergic rhinitis and to determine the optimal treatment method for this disease using various drug combination therapies. Methods A total of 108 participants with allergic rhinitis were divided into three groups based on symptoms. Subsequently, each group was further categorized into four subgroups based on the medications received. The efficacy of the treatments was evaluated using the visual analog scale VAS scores of the total and individual nasal symptoms, decline index of the symptom score, histamine and leukotriene levels, and mRNA and protein expression levels of histamine 1 and cysteinyl leukotriene 1 receptors. Results Loratadine + mometasone furoate and loratadine + mometasone furoate + montelukast significantly improved the sneezing symptom and reduced the histamine levels compared with the other combination therapies (p < 0.05). Meanwhile, montelukast + mometasone furoate and montelukast + mometasone furoate + loratadine considerably improved the nasal obstruction symptom and decreased the leukotriene D4 levels compared with the other combination therapies (p < 0.05). Conclusion Clinical symptom evaluation combined with experimental detection of histamine and leukotriene levels can be an objective and accurate method to clinically classify the allergic rhinitis types. Furthermore, individualized treatment based on allergic rhinitis classification can result in a good treatment efficacy.

Resumo Introdução A rinite alérgica é basicamente classificada de acordo com os antígenos causadores, tipos de doença, peridiocidade e gravidade dos sintomas. Objetivo Avaliar os tipos clínicos e a abordagem terapêutica individualizada para cada tipo de rinite alérgica e determinar o método de tratamento ideal utilizando várias terapias de combinação de fármacos. Método Um total de 108 participantes com rinite alérgica foram divididos em três grupos com base nos sintomas. Posteriormente, cada grupo foi subsequentemente categorizado em quatro subgrupos com base nos medicamentos recebidos. A eficácia dos tratamentos foi avaliada utilizando os escores da escala visual analógica EVA dos sintomas nasais totais e individualmente, índice de declínio do escore de sintomas, níveis de histamina e leucotrienos e níveis de expressão de mRNA e proteína dos receptores de histamina 1 e cisteinil-leucotrieno 1. Resultados As associações entre loratadina + furoato de mometasona, assim como a de loratadina + furoato de mometasona + montelucaste melhoraram significativamente o sintoma de espirros e reduziram os níveis de histamina em comparação às outras terapias combinadas (p < 0,05). Por outro lado, a associação montelucaste + furoato de mometasona, assim como a associação montelucaste + furoato de mometasone + loratadina melhoraram consideravelmente o sintoma de obstrução nasal e diminuíram os níveis de leucotrieno D4 em comparação com as outras combinações (p < 0,05). Conclusão A avaliação clínica dos sintomas combinada com a detecção experimental dos níveis de histamina e leucotrieno pode ser um método objetivo e preciso para classificar clinicamente os tipos de rinite alérgica. Além disso, o tratamento individualizado baseado na classificação da rinite alérgica pode resultar no aumento da eficácia do tratamento.
Descritores: Histamina/sangue
Leucotrieno D4/sangue
Quimioterapia Combinada/métodos
Medicina de Precisão/métodos
Rinite Alérgica/sangue
-Quinolinas/uso terapêutico
Espirro
RNA Mensageiro/genética
Receptores Histamínicos H1/genética
Obstrução Nasal/tratamento farmacológico
Resultado do Tratamento
Loratadina/uso terapêutico
Receptores de Leucotrienos/genética
Antialérgicos/uso terapêutico
Rinite Alérgica/diagnóstico
Rinite Alérgica/tratamento farmacológico
Furoato de Mometasona/uso terapêutico
Acetatos/uso terapêutico
Mucosa Nasal
Limites: Humanos
Masculino
Feminino
Adolescente
Adulto
Pessoa de Meia-Idade
Idoso
Adulto Jovem
Tipo de Publ: Ensaio Clínico Controlado
Responsável: BR1.1 - BIREME


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Id: biblio-1053475
Autor: Lin, Chenqiang; Jia, Xianbo; Fang, Yu; Chen, Longjun; Zhang, Hui; Lin, Rongbin; Chen, Jichen.
Título: Enhanced production of prodigiosin by Serratia marcescens FZSF02 in the form of pigment pellets
Fonte: Electron. j. biotechnol;40:58-64, July. 2019. graf, tab, ilus.
Idioma: en.
Projeto: Scientific Research in the Public Interest of Fujian Province; . Science and Technology Innovation Team Program of Fujian Academy of Agricultural Sciences; . Finance Support of Fujian China.
Resumo: Background: Prodigiosin has been demonstrated to be an important candidate in investigating anticancer drugs and in many other applications in recent years. However, industrial production of prodigiosin has not been achieved. In this study, we found a prodigiosin-producing strain, Serratia marcescens FZSF02, and its fermentation strategies were studied to achieve the maximum yield of prodigiosin. Results: When the culture medium consisted of 16.97 g/L of peanut powder, 16.02 g/L of beef extract, and 11.29 mL/L of olive oil, prodigiosin reached a yield of 13.622 ± 236 mg/L after culturing at 26 °C for 72 h. Furthermore, when 10 mL/L olive oil was added to the fermentation broth at the 24th hour of fermentation, the maximum prodigiosin production of 15,420.9 mg/L was obtained, which was 9.3-fold higher than the initial level before medium optimization. More than 60% of the prodigiosin produced with this optimized fermentation strategy was in the form of pigment pellets. To the best of our knowledge, this is the first report on this phenomenon of pigment pellet formation, which made it much easier to extract prodigiosin at low cost. Prodigiosin was then purified and identified by absorption spectroscopy, HPLC, and LCMS. Purified prodigiosin obtained in this study showed anticancer activity in separate experiments on several human cell cultures: A549, K562, HL60, HepG2, and HCT116. Conclusions: This is a promising strain for producing prodigiosin. The prodigiosin has potential in anticancer medicine studies.
Descritores: Prodigiosina/biossíntese
Prodigiosina/farmacologia
Serratia marcescens/metabolismo
Antineoplásicos/farmacologia
-Arachis/química
Pós
Prodigiosina/isolamento & purificação
Espectrometria de Massas
Células Tumorais Cultivadas/efeitos dos fármacos
Cromatografia Líquida de Alta Pressão
Cromatografia Líquida
Técnicas de Cultura de Células
Fermentação
Azeite de Oliva/química
Acetatos
Nitrogênio
Responsável: CL1.1 - Biblioteca Central


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Id: biblio-886682
Autor: TIETBOHL, LUIS A C; OLIVEIRA, ADRIANA P; ESTEVES, RICARDO S; ALBUQUERQUE, RICARDO D D G; FOLLY, DIOGO; MACHADO, FRANCISCO P; CORRÊA, ARTHUR L; SANTOS, MARCELO G; RUIZ, ANA L G; ROCHA, LEANDRO.
Título: Antiproliferative activity in tumor cell lines, antioxidant capacity and total phenolic, flavonoid and tannin contents of Myrciaria floribunda
Fonte: An. acad. bras. ciênc;89(2):1111-1120, Apr.-June 2017. tab, graf.
Idioma: en.
Resumo: ABSTRACT Myrciaria floribunda (H. West ex Willd.) O. Berg, Myrtaceae, is a native plant species of the Atlantic Rain Forest, from north to south of Brazil. The lyophilized ethyl acetate extract from the leaves of M. floribunda was investigated for its antiproliferative activity in tumor cell lines, antioxidant capacity and its total phenolic, flavonoid and tannin contents. Antiproliferative activity was tested in vitro against seven human cancer cells and against immortalized human skin keratinocytes line (HaCat, no cancer cell). Antioxidant activity was determined using 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and oxygen radical absorbing capacity (ORAC) assays and total phenolic, flavonoid and tannin contents were determined by spectrophotometric techniques. Ethyl acetate extract of M. floribunda exhibited antiproliferative activity against cancer cell lines with total growth inhibition (TGI) between 69.70 and 172.10 µg/mL. For HaCat cell, TGI value was 213.60 µg/mL. M. floribunda showed a strong antioxidant potential: EC50 of 45.89±0.42 µg/mL and 0.55±0.05 mmol TE/g for DPPH and ORAC, respectively. Total phenolic content was 0.23±0.013g gallic acid equivalents (GAE)/g extract and exhibited 13.10±1.60% of tannins content. The content of flavonoid was 24.08±0.44% expressed as rutin equivalents. These results provide a direction for further researches about the antitumoral potential of M. floribunda.
Descritores: Fenóis/análise
Flavonoides/análise
Myrtaceae/química
Proliferação de Células/efeitos dos fármacos
Antioxidantes/farmacologia
-Picratos
Compostos de Bifenilo
Brasil
Linhagem Celular Tumoral
Capacidade de Absorbância de Radicais de Oxigênio
Indicadores e Reagentes
Acetatos/farmacologia
Acetatos/química
Limites: Humanos
Tipo de Publ: Estudo de Avaliação
Responsável: BR1.1 - BIREME


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Id: biblio-886716
Autor: BASTOS, ISLA V G A; OLIVEIRA, TATIANE B DE; RODRIGUES, MARIA D; MILITÃO, GARDÊNIA C G; SILVA, TERESINHA G DA; TURATTI, IZABEL C C; LOPES, NORBERTO P; MELO, SEBASTIÃO J DE.
Título: Use of GC/MS to identify chemical constituents and cytotoxic activity of the leaves of Phoradendron mucronatum and Phoradendron microphyllum (Viscaceae)
Fonte: An. acad. bras. ciênc;89(2):991-1001, Apr.-June 2017. tab.
Idioma: en.
Resumo: ABSTRACT Phoradendron mucronatum and P. microphyllum are plants that found in tropical and subtropical areas, used in traditional medicine and popularly known as mistle-thrush. The aim of this study was to identify the chemical constituents of different leaf extracts from P. mucronatum and P. microphyllum and assess cytotoxic activity against strains from a human tumour cells. Extracts obtained with hexane, dichloromethane, chloroform and ethyl acetate from the leaves were analysed by gas chromatography coupled with mass spectrometry (GC-MS) and the cytotoxicity was assessed by the MTT method (bromide (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide)). The tested human tumour cells were NCI-H292 (human pulmonar mucoepidermoid carcinoma), MCF-7 (human breast adenocarcinoma) and HEp-2 (epidermoid carcinoma of the larynx). Analysis by GC/MS of the extracts from leaves of P. microphyllum and P. mucronatum detected 51 different compounds, such as alkaloids, diterpenes, triterpenes, sterols, alcohols, aldehydes, fatty acids and hydrocarbons. In the cytotoxic evaluation, hexane and ethyl acetate extracts from the leaves P. microphyllum inhibited cell growth of NCI-H292 strains (72.97%) and HEp-2 (87.53%), respectively. The extracts of P. mucronatum species showed an inhibitory effect towards NCI-H292 (83.19%/hexane), MCF-7 (88.69%/dichloromethane) and HEp-2 (93.40%/hexane). The extracts showed cytotoxic activity against the tested strains, especially the P. mucronatum, which presented the highest percentages of inhibition of cell growth.
Descritores: Extratos Vegetais/química
Folhas de Planta/química
Viscaceae/química
Phoradendron/química
-Sais de Tetrazólio
Tiazóis
Extratos Vegetais/farmacologia
Clorofórmio/química
Reprodutibilidade dos Testes
Testes de Toxicidade
Linhagem Celular Tumoral
Proliferação de Células/efeitos dos fármacos
Células MCF-7
Hexanos/química
Cromatografia Gasosa-Espectrometria de Massas
Cloreto de Metileno/química
Acetatos/química
Limites: Humanos
Tipo de Publ: Estudo de Avaliação
Responsável: BR1.1 - BIREME


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Id: biblio-899288
Autor: André, Weibson Paz Pinheiro; Cavalcante, Géssica Soares; Ribeiro, Wesley Lyeverton Correia; Santos, Jessica Maria Leite dos; Macedo, Iara Tersia Freitas; Paula, Haroldo César Beserra de; Morais, Selene Maia de; Melo, Janaina Viana de; Bevilaqua, Claudia Maria Leal.
Título: Anthelmintic effect of thymol and thymol acetate on sheep gastrointestinal nematodes and their toxicity in mice / Efeito anti-helmíntico do timol e acetato de timila sobre nematoides gastrintestinais de ovinos e toxicidade em camundongos
Fonte: Rev. bras. parasitol. vet;26(3):323-330, July-Sept. 2017. tab, graf.
Idioma: en.
Projeto: CNPq; . CAPES; . AUXPE - PROEX.
Resumo: Abstract Thymol is a monoterpene and acetylation form of this compound can reduce the toxicity and enhance its biological effects. The objective of this study was to evaluate the effect of thymol and thymol acetate (TA) on egg, larva and adult Haemonchus contortus and the cuticular changes, acute toxicity in mice and the efficacy on sheep gastrointestinal nematodes. In vitro tests results were analyzed by analysis of variance (ANOVA) and followed by comparison with Tukey test or Bonferroni. The efficacy of in vivo test was calculated by the BootStreet program. In the egg hatch test (EHT), thymol (0.5 mg/mL) and TA (4 mg/mL) inhibited larval hatching by 98% and 67.1%, respectively. Thymol and TA (8 mg/mL) inhibited 100% of larval development. Thymol and TA (800 µg/mL) reduced the motility of adult worms, by 100% and 83.4%, respectively. Thymol caused cuticular changes in adult worm teguments. In the acute toxicity test, the LD50 of thymol and TA were 1,350.9 mg/kg and 4,144.4 mg/kg, respectively. Thymol and TA reduced sheep egg count per gram of faeces (epg) by 59.8% and 76.2%, respectively. In in vitro tests thymol presented better anthelmintic activity than TA. However TA was less toxic and in in vivo test efficacy was similar.

Resumo Timol é um monoterpeno e a acetilação deste composto pode reduzir a toxicidade e potencializar os seus efeitos biológicos. O objetivo deste trabalho foi avaliar o efeito do timol e acetato de timolila (AT) sobre ovos, larvas e adultos de Haemonchus contortus e suas alterações cuticulares, toxicidade aguda em camundongos e a eficácia sobre nematoides gastrintestinais de ovinos. Os resultados dos testes in vitro foram analisados por análise de variância (ANOVA) e comparados pelo testes de Tukey ou Bonferroni. A eficácia do teste de redução da contagem de ovos nas fezes (RCOF) foi calculada pelo programa BootStreet. No teste de inibição da eclosão de ovos (TEO), timol (0,5 mg/mL) e AT (4 mg/mL) inibiram a eclosão das larvas em 98% e 67,1%, respectivamente. Timol e AT (8 mg/mL) inibiram 100% do desenvolvimento larval. Timol e AT (800 μg/mL) reduziram a motilidade dos nematoides adultos, em 100% e 83,4%, respectivamente. O timol provocou alterações cuticulares nos nematoides adultos. No teste de toxicidade aguda, a DL50 do timol e AT foi de 1.350,9 mg/kg e 4.144,4 mg/kg, respectivamente. Timol e AT reduziram a contagem de ovos por gramas de fezes (OPG) dos ovinos em 59,8% e 76,2%, respectivamente. Nos testes in vitro timol apresentou atividade melhor anti-helmíntica do que AT. Entretanto, AT foi menos tóxico do que o timol e no teste in vivo apresentaram eficácia semelhante.
Descritores: Doenças dos Ovinos/parasitologia
Doenças dos Ovinos/tratamento farmacológico
Timol/toxicidade
Timol/uso terapêutico
Nematoides/efeitos dos fármacos
Infecções por Nematoides/veterinária
-Acetilação
Timol/farmacologia
Ovinos
Haemonchus/efeitos dos fármacos
Anti-Helmínticos/uso terapêutico
Anti-Helmínticos/farmacologia
Acetatos/uso terapêutico
Acetatos/farmacologia
Infecções por Nematoides/tratamento farmacológico
Limites: Animais
Feminino
Camundongos
Responsável: BR1.1 - BIREME



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