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1.
Bol. latinoam. Caribe plantas med. aromát ; 19(2): 167-178, mar. 2020. ilus, tab
Artigo em Inglês | LILACS (Américas) | ID: biblio-1104197

RESUMO

The objective of this work was to evaluate the antioxidant and inhibitory activities of the ethanolic extracts of the mangosteen (Garcinia mangostana L.) grown in Montenegro, Quindío, Colombia, in three stages of maturation, including the edible (pulp) and inedible parts (pericarp and peduncle). The alcoholic samples were phytochemically characterized by Thin Layer Chromatography (TLC), High Performance Liquid Chromatography (HPLC) and by Fourier Transformation Infrared Spectroscopy (FT-IR); the antioxidant capacities were also evaluated by the diphenyl-picrylhydrazyl (DPPH•) radical method and Oxygen Radical Absorbance Capacity (ORAC), in addition to the inhibitory activity of acetylcholinesterase (AchE) and the total content of phenols and flavonoids. The tests detected phytochemical compounds such as phenols, flavonoids, alkaloids, quinones and xanthones, to which the antioxidant activity and the inhibition of AChE presented, can be attributed. In conclusion, the inedible parts of mangosteen contain higher proportions of secondary metabolites, these being the most promising sources for industrial use.


El objetivo de este trabajo fue el de evaluar las actividades antioxidantes e inhibitoria de acetilcolinesterasa de los extractos etanólicos del mangostino (Garcinia mangostana L.) de Montenegro, Quíndio, Colombia, en tres estados de maduración, incluyendo las partes comestibles (pulpa) y no comestibles (pericarpio y pedúnculo). Las muestras alcohólicas fueron caracterizadas fitoquímicamente por Cromatografía de Capa Delgada (CCD), Cromatografía Líquida de Alta Eficiencia (HPLC) y Espectroscopía Infrarroja por Transformada de Fourier (FT-IR); la capacidad antioxidante fue evaluada también por el método de captación del radical libre 2,2-difenil-1-picrilhidracilo (DPPH• dejar el radical en superíndice) y la Capacidad de Absorción de Radicales de Oxígeno (ORAC), adicionalmente la actividad inhibitoria de la acetilcolinesterasa (AchE) y el contenido total de fenoles y flavonoides. Se detectaron compuestos fitoquímicos como fenoles, flavonoides, alcaloides, quinonas y xantonas, a quienes se les puede atribuir las actividades antioxidantes y de inhibición de la acetilcolinesterasa. En conclusión, las partes no comestibles del mangostino contienen una mayor proporción de metabolitos secundarios, siendo las fuentes más promisorias para uso industrial.


Assuntos
Extratos Vegetais/farmacologia , Extratos Vegetais/química , Garcinia mangostana/química , Antioxidantes/farmacologia , Antioxidantes/química , Fenóis/análise , Flavonoides/análise , Inibidores da Colinesterase , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Delgada , Espectroscopia de Infravermelho com Transformada de Fourier , Colômbia , Clusiaceae , Etanol , Capacidade de Absorbância de Radicais de Oxigênio
2.
Bol. latinoam. Caribe plantas med. aromát ; 19(2): 161-166, mar. 2020. tab, ilus
Artigo em Inglês | LILACS (Américas) | ID: biblio-1104063

RESUMO

The methanol extract of the Balkan endemic species Jurinea tzar-ferdinandii Davidov demonstrated weak antioxidant activity against DPPH• and ABTS+• and low inhibitory potential against acetylcholinesterase (8.3% Inh.) and tyrosinase (IC50 = 208 ± 8 µg/mL) enzymes. Phytochemical investigation of the extract led to isolation and identification of apigenin, luteolin, apigenin-7-O-glucoside, apigenin-4'-O-glucoside, apigenin-7-O-gentiobioside, luteolin-4'-O-glucoside, rutin, narcissin, chlorogenic and 1,5-dicaffeoylquinic acid. With exception of apigenin and rutin, all isolated compounds are reported for the first time in the representatives of genus Jurinea. The distribution of flavonoids was discussed from chemotaxonomic point of view.


El extracto de metanol de la especie endémica de los Balcanes Jurinea tzar-ferdinandii Davidov demostró una actividad antioxidante débil contra DPPH• y ABTS+• y un bajo potencial inhibidor contra las enzimas acetilcolinesterasa (8.3% Inh.) tirosinasa (IC50 = 208 ± 8 µg/mL). La investigación fitoquímica del extracto condujo al aislamiento e identificación de apigenina, luteolina, apigenina-7-Oglucósido, apigenina-4'-O-glucósido, apigenina-7-O-gentiobiósido, luteolina-4'-O-glucósido, rutina, narcissin, clorogénico y ácido 1,5- dicafeoilquinico. Con excepción de la apigenina y la rutina, todos los compuestos aislados se informan por primera vez en el género Jurinea. La distribución de flavonoides se discute desde el punto de vista quimiotaxonómico.


Assuntos
Asteraceae/química , Antioxidantes/farmacologia , Antioxidantes/química , Fenóis/análise , Flavonoides/análise , Inibidores da Colinesterase , Monofenol Mono-Oxigenase/antagonistas & inibidores , Metanol , Península Balcânica
3.
Bol. latinoam. Caribe plantas med. aromát ; 18(6): 544-554, nov. 2019. tab, ilus
Artigo em Inglês | LILACS (Américas) | ID: biblio-1102238

RESUMO

In this work, the inhibitory activity of a wide range of polysaccharide extracts from two Iranian and French strains of Agaricus subrufescens were evaluated toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Among them, two extracts S9 and S'7 obtained from Iranian and French strains under different extraction conditions showed selective AChE inhibitory activity with IC50 values of 154.63 and 145.43 µg/mL, respectively. It should be noted that all extracts from both strains demonstrated no BChE inhibitory activity. S9 and S'7 were also tested for their effect on amyloid beta (Aß) aggregation, antioxidant activity, and neuroprotectivity. Their activity against Aß aggregation was comparable to that of donepezil as the reference drug but they induced moderate antioxidant activity by DPPH radical scavenging activity and negligible neuroprotectivity against Aß-induced damage.


En este trabajo, se evaluó la actividad inhibitoria de acetilcolinesterasa (AChE) y butirilcolinesterasa (BChE) para varios extractos de polisacáridos de dos cepas iraníes y francesas de Agaricus subrufescens. Los extractos más potentes mostraron valores de IC50 de 154,63 y 145 µg/ml para las cepas iraní (S9) y francesa (S'7), respectivamente, las cuales se obtuvieron de diferentes condiciones de extracción; sin embargo, todos los extractos no mostraron actividad inhibitoria de BChE. Además, S9 y S'7 se probaron para determinar su efecto sobre la agregación de beta-amiloide (Aß), así como su actividad antioxidante y neuroprotectora. Su actividad inhibitoria de la agregación de Aß fue comparable con donepezil, fármaco de referencia, pero indujeron una actividad antioxidante moderada, medida mediante la captación de radicales DPPH, y una neuroprotectora insignificante contra el daño inducido por Aß.


Assuntos
Agaricus/química , Doença de Alzheimer/tratamento farmacológico , Amiloide/efeitos dos fármacos , Antioxidantes/farmacologia , Picratos , Compostos de Bifenilo , Butirilcolinesterase , Inibidores da Colinesterase/farmacologia , Fármacos Neuroprotetores , Doença de Alzheimer/enzimologia , Polissacarídeos Fúngicos/farmacologia
4.
Bol. latinoam. Caribe plantas med. aromát ; 18(5): 527-532, sept. 2019. ilus, tab
Artigo em Inglês | LILACS (Américas) | ID: biblio-1008292

RESUMO

Chemical constituents and biological activities of the aerial parts of Piper erecticaule C.DC. have been studied for the first time. Fractionation and purification of the extracts afforded aristolactam AII (1), aristolactam BII (2), piperolactam A (3), piperolactam C (4), piperolactam D (5), together with terpenoids of ß-sitosterol, ß-sitostenone, taraxerol, and lupeol. The structures of these compounds were obtained by analysis of their spectroscopic data, as well as the comparison with that of reported data. Acetylcholinesterase inhibitory activity revealed that compounds 1 and 3 showed strong AChE inhibitory effects with the percentage inhibition of 75.8% and 74.8%, respectively.


Se estudiaron por primera vez los constituyentes químicos y actividad biológica de las partes aéreas de Piper erecticaule C.DC. El fraccionamiento y la purificación de los extractos proporcionaron aristolactama AII (1), aristolactama BII (2), piperolactama A (3), piperolactama C (4), piperolactama D (5), junto con terpenoides de ß-sitosterol, ß-sitostenona, taraxerol, y el lupeol. Las estructuras de estos compuestos se obtuvieron mediante el análisis de sus datos espectroscópicos, así como mediante la comparación con datos ya informados. La actividad inhibidora de la acetilcolinesterasa reveló que los compuestos 1 y 3 mostraron un potente efecto inhibidor de la AChE con un porcentaje de inhibición del 75.8% y 74.8%, respectivamente.


Assuntos
Aporfinas/farmacologia , Acetilcolinesterase/efeitos dos fármacos , Extratos Vegetais/química , Inibidores da Colinesterase/farmacologia , Piper/química , Alcaloides/farmacologia , Aporfinas/química , Terpenos/isolamento & purificação , Inibidores da Colinesterase/química , Alcaloides Indólicos/química , Alcaloides/química , Lactamas/química
5.
Electron. j. biotechnol ; 40: 22-29, July. 2019. tab, graf
Artigo em Inglês | LILACS (Américas) | ID: biblio-1053216

RESUMO

Background: Rosemary (Rosmarinus officinalis) contains active substances that have desirable properties for industrial and herbal medicine applications, e.g., essential oils (1.5­2.5%), tannins, flavonoids, triterpenes, saponins, resins, phytosterols, rosmarinic acid and many others. The aim of this study was to determine the influence of rosemary extract and 20% rapeseed oil substitution for animal fat on storage changes and inhibition of cholinesterases in liver pâté. Results: Preliminary research showed that rosemary extract exhibited antioxidative activity in the system of accelerated Rancimat and Oxidograph tests. Then, rosemary extract was used as an ingredient in liver pâté. During the experiment, meat samples were refrigerated and tested on days 1, 5, 8, 12 and 15 after production. The study proved that the substitution of 20% of animal fat with rapeseed oil decreased the content of saturated acids and increased the content of monoenic fatty acids by approximately 5% and polyene fatty acids by 40%. Conclusions: In addition to antioxidative activity, the rosemary extract affected the health-promoting value of the samples, which inhibited cholinesterase activity during the entire storage period. The extract inhibited AChE more than BChE.


Assuntos
Extratos Vegetais/química , Inibidores da Colinesterase , Rosmarinus/química , Produtos da Carne , Antioxidantes/química , Peróxidos , Óleos Voláteis , Substitutos da Gordura , Análise de Componente Principal , Ácidos Graxos/análise , Fígado , Produtos da Carne/microbiologia
6.
Braz. J. Psychiatry (São Paulo, 1999, Impr.) ; 41(3): 218-224, May-June 2019. tab, graf
Artigo em Inglês | LILACS (Américas) | ID: biblio-1011499

RESUMO

Objective: To perform a cost-effectiveness analysis of donepezil and rivastigmine therapy for mild and moderate Alzheimer's disease (AD) from the perspective of the Brazilian Unified Health System. Method: A hypothetical cohort of 1,000 individuals of both sexes, aged >65 years, and diagnosed with AD was simulated using a Markov model. The time horizon was 10 years, with 1-year cycles. A deterministic and probabilistic sensitivity analysis was performed. Results: For mild AD, the study showed an increase in quality-adjusted life years (QALYs) of 0.61 QALY/21,907.38 Brazilian reais (BRL) for patients treated with donepezil and 0.58 QALY/BRL 24,683.33 for patients treated with rivastigmine. In the moderate AD group, QALY increases of 0.05/BRL 27,414.96 were observed for patients treated with donepezil and 0.06/BRL 34,222.96 for patients treated with rivastigmine. Conclusions: The findings of this study contradict the standard of care for mild and moderate AD in Brazil, which is based on rivastigmine. A pharmacological treatment option based on current Brazilian clinical practice guidelines for AD suggests that rivastigmine is less cost-effective (0.39 QALY/BRL 32,685.77) than donepezil. Probabilistic analysis indicates that donepezil is the most cost-effective treatment for mild and moderate AD.


Assuntos
Humanos , Masculino , Feminino , Idoso , Inibidores da Colinesterase/economia , Inibidores da Colinesterase/uso terapêutico , Doença de Alzheimer/economia , Doença de Alzheimer/tratamento farmacológico , Rivastigmina/economia , Rivastigmina/uso terapêutico , Donepezila/economia , Donepezila/uso terapêutico , Brasil , Estudos de Coortes , Resultado do Tratamento , Análise Custo-Benefício , Anos de Vida Ajustados por Qualidade de Vida , Doença de Alzheimer/diagnóstico , Programas Nacionais de Saúde
8.
Braz. J. Pharm. Sci. (Online) ; 55: e17032, 2019. tab, graf
Artigo em Inglês | LILACS (Américas) | ID: biblio-1019533

RESUMO

The aim of the present research work was to investigate the enzyme inhibitory potential of some new sulfonamides having benzodioxane and acetamide moieties. The synthesis was started by the reaction of N-2,3-dihydrobenzo[1,4]-dioxin-6-amine (1) with 4-methylbenzenesulfonyl chloride (2) in the presence of 10% aqueous Na2CO3 to yield N-(2,3-dihydrobenzo[1,4]-dioxin-6-yl)-4-methylbenzenesulfonamide (3), which was then reacted with 2-bromo-N-(un/substituted-phenyl)acetamides (6a-l) in DMF and lithium hydride as a base to afford various 2-{2,3-dihydro-1,4-benzodioxin-6-yl[(4-methylphenyl)sulfonyl]amino}-N-(un/substituted-phenyl)acetamides (7a-l). All the synthesized compounds were characterized by their IR and 1H-NMR spectral data along with CHN analysis data. The enzyme inhibitory activities of these compounds were tested against a-glucosidase and acetylcholinesterase (AChE). Most of the compounds exhibited substantial inhibitory activity against yeast a-glucosidase and weak against AChE. The in silico molecular docking results were also consistent with in vitro enzyme inhibition data.


Assuntos
Sulfonamidas/agonistas , Inibidores da Colinesterase , Inibidores de Glicosídeo Hidrolases , Análise Espectral/instrumentação , Acetamidas/análise
9.
Singapore medical journal ; : 154-160, 2019.
Artigo em Inglês | WPRIM (Pacífico Ocidental) | ID: wprim-777550

RESUMO

INTRODUCTION@#Singapore has a rapidly ageing population and an increasing prevalence of Alzheimer's disease (AD). Compliance to AD medications is associated with treatment effectiveness. We investigated compliance to acetylcholinesterase inhibitors (AChEIs) and N-methyl-D-aspartate (NMDA) receptor antagonist and treatment persistence among patients seen at the General Memory Clinic of National University Hospital, Singapore. We also identified the reasons for non-compliance.@*METHODS@#Patients seen at the General Memory Clinic between 1 January 2013 and 31 December 2014, who were prescribed AChEIs and NMDA receptor antagonist, were included in this retrospective cohort study. Non-compliance to medications was indirectly measured by failure to renew prescription within 60 days of the last day of medication supplied by the previous prescription. The reasons for non-compliance were identified.@*RESULTS@#A total of 144 patients were included. At one year, 107 patients were compliant to AD medications, while 37 patients were non-compliant. Around 60% of the non-compliant patients discontinued the use of AD medications within the first six months, and the mean persistent treatment period among this group of patients was 10.3 ± 3.5 months. The main reason for non-compliance was patients' and caregivers' perception that memory loss was of lower priority than other coexisting illnesses. Other reasons for non-compliance included side effects of medications (18.9%), perceived ineffectiveness of treatment (16.2%), inability to attend clinic (5.4%) and high cost of medications (2.7%).@*CONCLUSION@#Our findings suggest that the reasons for medication non-compliance can be identified early. Better compliance may be achieved through a multidisciplinary approach to patient education.


Assuntos
Idoso , Idoso de 80 Anos ou mais , Doença de Alzheimer , Tratamento Farmacológico , Epidemiologia , Psicologia , Cuidadores , Inibidores da Colinesterase , Custos de Medicamentos , Feminino , Humanos , Comunicação Interdisciplinar , Masculino , Adesão à Medicação , Pessoa de Meia-Idade , Cooperação do Paciente , Qualidade de Vida , Receptores de N-Metil-D-Aspartato , Estudos Retrospectivos , Singapura , Epidemiologia , Resultado do Tratamento
10.
Artigo em Inglês | WPRIM (Pacífico Ocidental) | ID: wprim-765974

RESUMO

Pediatric chronic intestinal pseudo-obstruction is a rare disorder characterized by a severe impairment of gastrointestinal motility leading to intestinal obstruction symptoms in the absence of mechanical causes. The diagnosis is usually clinical and diagnostic work is usually aimed to rule out mechanical obstruction and to identify any underlying diseases. Treatment is challenging and requires a multidisciplinary effort. In this manuscript we describe the youngest child successfully treated with the orally administrable, long-acting, reversible anti-cholinesterase drug, pyridostigmine. Like other drugs belonging to cholinesterase inhibitors, pyridostigmine enhances gut motility by increasing acetylcholine availability in the enteric nervous system and neuro-muscular junctions. Based on the direct evidence from the reported case, we reviewed the current literature on the use of pyridostigmine in severe pediatric dysmotility focusing on intestinal pseudo-obstruction. The overall data emerged from the few published studies suggest that pyridostigmine is an effective and usually well tolerated therapeutic options for patients with intestinal pseudo-obstruction. More specifically, the main results obtained by pyridostigmine included marked reduction of abdominal distension, reduced need of parenteral nutrition, and improvement of oral feeding. The present case and review on pyridostigmine pave the way for eagerly awaited future randomized controlled studies testing the efficacy of cholinesterase inhibitors in pediatric severe gut dysmotility.


Assuntos
Acetilcolina , Criança , Inibidores da Colinesterase , Diagnóstico , Sistema Nervoso Entérico , Feminino , Motilidade Gastrointestinal , Humanos , Obstrução Intestinal , Pseudo-Obstrução Intestinal , Nutrição Parenteral , Brometo de Piridostigmina
11.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wprim-773731

RESUMO

A total of 27 endophytic fungal strains were isolated from Huperzia serrata,which were richly distributed in the stems and leaves while less distributed in roots. The 27 strains were identified by Internal Transcribed Spacer( ITS) r DNA molecular method and one of the strains belongs to Basidiomycota phylum,and other 26 stains belong to 26 species,9 general,6 families,5 orders,3 classes of Ascomycota Phylum. The dominant strains were Colletotrichum genus,belonging to Glomerellaceae family,Glomerellales order,Sordariomycetes class,Ascomycota Phylum,with the percentage of 48. 15%. The inhibitory activities of the crude extracts of 27 endophytic fungal strains against acetylcholinesterase( ACh E) and nitric oxide( NO) production were evaluated by Ellman's method and Griess method,respectively. Crude extracts of four fungi exhibited inhibitory activities against ACh E with an IC50 value of 42. 5-62. 4 mg·L~(-1),and some fungi's crude extracts were found to inhibit nitric oxide( NO) production in lipopolysaccharide( LPS)-activated RAW264. 7 macrophage cells with an IC50 value of 2. 2-51. 3 mg·L~(-1),which indicated that these fungi had potential anti-inflammatory activities.The chemical composition of the Et OAc extract of endophytic fungus HS21 was also analyzed by LCMS-IT-TOF. Seventeen compounds including six polyketides,four diphenyl ether derivatives and seven meroterpenoids were putatively identified.


Assuntos
Acetilcolinesterase , Animais , Anti-Inflamatórios , Farmacologia , Ascomicetos , Química , Classificação , Inibidores da Colinesterase , Metabolismo , Endófitos , Classificação , Huperzia , Microbiologia , Camundongos
12.
Acta toxicol. argent ; 26(3): 104-112, Dec. 2018. ilus, tab
Artigo em Português | LILACS (Américas) | ID: biblio-1001122

RESUMO

Anualmente milhões de agricultores são intoxicados no mundo, e destes, mais de 20 mil morrem em consequência da exposição a agrotóxicos. Intoxicações por organofosforados (OF) e carbamatos (CAR) representam as maiores ameaças à saúde dos trabalhadores rurais. Os OF e CAR atuam na inibição da enzima colinesterase, sendo assim a inibição desta mostra-se um excelente indicador da severidade da intoxicação. O objetivo deste estudo foi analisar o impacto do uso de OF e CAR em trabalhadores rurais na cidade de Mato Queimado/RS. Foi realizado um estudo transversal, prospectivo e experimental. Investigaramse 27 trabalhadores rurais expostos. Foram realizadas coletas sanguíneas e dados epidemiográficos nos meses de fevereiro e março de 2014. A atividade da colinesterase foi determinada através do método bioquímico cinético colorimétrico. A faixa etária média dos participantes foi 34,6 anos (± 8,5). A forma de contato mais prevalente foi a aplicação do produto (88,9%). O tempo médio de exposição foi de 10,7 anos. 70,4% relataram usar equipamentos de proteção individual (EPI), sendo mais frequente o uso de máscara (55,5%). A média dos valores de colinesterase para foi de 3244,45 U/I (± 345,8), níveis estes abaixo dos de referência. Através dos resultados obtidos nesta pesquisa torna-se imprescindível a utilização de meios de monitoramento biológico dos trabalhadores rurais na finalidade de prevenção e promoção da saúde.


Annually millions of rural workers are intoxicated in the world, and of these, more than 20,000 die as a result of exposure to pesticides. Intoxication by insecticides organophosphate (OF) and carbamates (CAR) represent the greatest threats to the health of rural workers. OF CAR and act on the inhibition of cholinesterase enzyme, thus inhibition of this proves to be an excellent indicator of the severity of the intoxication. The objective of this study was to analyze the impact of using OF CAR and in rural workers in the city of Mato Queimado/RS. A cross-sectional, prospective and experimental study was conducted. Twenty-three rural workers exposed were investigated. Sample collection and data demographic were conducted in February and March 2014. The cholinesterase activity was determined by biochemical kinetic colorimetric method. The average age of participants was 34.6 years (± 8.5). The most prevalent form of contact is via the application of the product (88.9%). The mean duration of exposure was 10.7 years. Still, 70.4% reported using personal protective equipment (PPE), more frequent use of mask (55.5%). The average values for cholinesterase was 3244.45 U/l (± 345.8) levels below those of the reference. The results obtained in this study are essential to use biological monitoring means of rural workers in purpose of prevention and health promotion.


Assuntos
Humanos , Masculino , Adulto , Pessoa de Meia-Idade , Trabalhadores Rurais , Carbamatos/envenenamento , Carbamatos/sangue , Exposição Ocupacional/estatística & dados numéricos , Intoxicação por Organofosfatos/sangue , Brasil/epidemiologia , Inibidores da Colinesterase/sangue , Colinesterases/sangue , Agroquímicos/envenenamento
13.
Braz. j. microbiol ; 49(1): 169-176, Jan.-Mar. 2018. tab, graf
Artigo em Inglês | LILACS (Américas) | ID: biblio-889211

RESUMO

ABSTRACT Major health challenges as the increasing number of cases of infections by antibiotic multiresistant microorganisms and cases of Alzheimer's disease have led to searching new control drugs. The present study aims to verify a new way of obtaining bioactive extracts from filamentous fungi with potential antimicrobial and acetylcholinesterase inhibitory activities, using epigenetic modulation to promote the expression of genes commonly silenced. For such finality, five filamentous fungal species (Talaromyces funiculosus, Talaromyces islandicus, Talaromyces minioluteus, Talaromyces pinophilus, Penicillium janthinellum) were grown or not with DNA methyltransferases inhibitors (procainamide or hydralazine) and/or a histone deacetylase inhibitor (suberohydroxamic acid). Extracts from T. islandicus cultured or not with hydralazine inhibited Listeria monocytogenes growth in 57.66 ± 5.98% and 15.38 ± 1.99%, respectively. Increment in inhibition of acetylcholinesterase activity was observed for the extract from P. janthinellum grown with procainamide (100%), when compared to the control extract (39.62 ± 3.76%). Similarly, inhibition of acetylcholinesterase activity increased from 20.91 ± 3.90% (control) to 92.20 ± 3.72% when the tested extract was obtained from T. pinophilus under a combination of suberohydroxamic acid and procainamide. Concluding, increases in antimicrobial activity and acetylcholinesterase inhibition were observed when fungal extracts in the presence of DNA methyltransferases and/or histone deacetylase modulators were tested.


Assuntos
Antibacterianos/farmacologia , Inibidores da Colinesterase/farmacologia , Penicillium/química , Talaromyces/química , Acetilcolinesterase/química , Acetilcolinesterase/metabolismo , Antibacterianos/química , Antibacterianos/metabolismo , Proteínas de Bactérias/química , Proteínas de Bactérias/metabolismo , Inibidores da Colinesterase/química , Inibidores da Colinesterase/metabolismo , Cromatina/metabolismo , Listeria monocytogenes/efeitos dos fármacos , Listeria monocytogenes/enzimologia , Listeria monocytogenes/crescimento & desenvolvimento , Penicillium/metabolismo , Talaromyces/metabolismo
14.
Artigo em Coreano | WPRIM (Pacífico Ocidental) | ID: wprim-766468

RESUMO

Dementia is a clinical syndrome characterized by a cluster of symptoms and signs that manifest as difficulties in cognitive functions such as memory, psychological and psychiatric changes, and impairments in activities of daily living. As a result of worldwide trends of population aging, dementia has had a huge impact on public health in almost all countries. Disease modification therapies for dementia have not yet been developed. However, pharmacotherapy is essential in patients with dementia to combat delays in their cognitive and functional decline. In this article, we review the current pharmacotherapy for dementia. Three acetylcholinesterase inhibitors—donepezil, rivastigmine, galantamine—and memantine are the only medications that have been approved for the treatment of dementia. We present the indications, dose recommendations, side effects, and criteria for National Health Insurance coverage in Korea of these medications for dementia treatment. Although the Ministry of Food and Drug Safety in Korea has not approved any medications for managing the behavioral and psychological symptoms of dementia, some antipsychotics and antidepressants have been studied and used clinically for those purposes. Clinicians may consider vitamin E, Ginkgo biloba extract, choline alfoscerate, or omega-3 fatty acids as additional treatment options. Non-steroid anti-inflammatory drugs, estrogen hormone therapy, and statins are not generally recommended for dementia treatment. We believe that our findings will aid clinicians in the treatment of patients with cognitive decline.


Assuntos
Acetilcolinesterase , Atividades Cotidianas , Envelhecimento , Antidepressivos , Antipsicóticos , Inibidores da Colinesterase , Cognição , Demência , Tratamento Farmacológico , Estrogênios , Ácidos Graxos Ômega-3 , Ginkgo biloba , Glicerilfosforilcolina , Humanos , Inibidores de Hidroximetilglutaril-CoA Redutases , Coreia (Geográfico) , Memantina , Memória , Programas Nacionais de Saúde , Saúde Pública , Rivastigmina , Vitamina E , Vitaminas
15.
Artigo em Inglês | WPRIM (Pacífico Ocidental) | ID: wprim-775172

RESUMO

BACKGROUND@#Acetylcholinesterase inhibitor insecticides (AChEIIs) were used extensively in the agrarian region of Anuradhapura for the past few decades. As a result, the region faced a heightened risk of toxicity. Carbaryl, carbofuran, chlorpyrifos, dimethoate, and fenthion were the five hazardous AChEIIs banned from Anuradhapura in 2014. Assessment of post-ban trends in acute poisoning will reveal the impact of the ban. Data on availability and sales of remaining AChEIIs will guide towards preventive measures against related toxicities.@*METHODS@#Cross-sectional surveys were conducted at Anuradhapura district of Sri Lanka. Details related to acute AChEII poisoning were sorted from the Teaching Hospital Anuradhapura. Main insecticide vendors in Anuradhapura were surveyed to find information on availability and sales of AChEIIs. Chi-square for goodness of fit was performed for trends in acute poisoning and sales.@*RESULTS@#Hospital admissions related to acute AChEII poisoning have declined from 554 in 2013 to 272 in 2017. Deaths related to acute AChEII poisoning have declined from 27 in 2013 to 13 in 2017. Sales of all five banned AChEIIs had reduced by 100%. Sales of the remaining AChEIIs were declining, except for acephate, phenthoate, and profenofos. However, one of the top selling, most frequently abused carbosulfan, had the highest risk of toxicity. Chi-square for goodness of fit showed a significance (P < 0.001) between the trends of hospital admissions for acute AChEII poisoning and the sales related to AChEIIs.@*CONCLUSIONS@#Hospital admissions related to acute poisoning was declining along with the overall sales of remaining AChEIIs, during the post-AChEII ban period. Nevertheless, future vigilance is needed on the remaining AChEIIs to predict and prevent related toxicities.


Assuntos
Agricultura , Inibidores da Colinesterase , Classificação , Envenenamento , Comércio , Estudos Transversais , Países em Desenvolvimento , Feminino , Regulamentação Governamental , Política de Saúde , Hospitalização , Humanos , Incidência , Inseticidas , Classificação , Envenenamento , Masculino , Envenenamento , Epidemiologia , Mortalidade , Fatores de Risco , Sri Lanka , Epidemiologia
16.
Artigo em Inglês | WPRIM (Pacífico Ocidental) | ID: wprim-741612

RESUMO

The present study was undertaken to investigate the isolated compounds from the stem bark of Garcinia atroviridis as potential cholinesterase inhibitors and the ligand-enzyme interactions of selected bioactive compounds in silico. The in vitro cholinesterase results showed that quercetin (3) was the most active AChE inhibitor (12.65 ± 1.57 µg/ml) while garcinexanthone G (6) was the most active BChE inhibitor (18.86 ± 2.41 µg/ml). It is noteworthy to note that compound 6 was a selective inhibitor with the selectivity index of 11.82. Molecular insight from docking interaction further substantiate that orientation of compound 6 in the catalytic site which enhanced its binding affinity as compared to other xanthones. The nature of protein-ligand interactions of compound 6 is mainly hydrogen bonding, and the hydroxyl group of compound 6 at C-10 is vital in BChE inhibition activity. Therefore, compound 6 is a notable lead for further drug design and development of BChE selective inhibitor.


Assuntos
Butirilcolinesterase , Domínio Catalítico , Inibidores da Colinesterase , Colinesterases , Simulação por Computador , Desenho de Fármacos , Garcinia , Ligação de Hidrogênio , Técnicas In Vitro , Quercetina , Xantonas
17.
Brasília; CONITEC; out. 2017. graf, tab.
Não convencional em Português | LILACS (Américas), BRISA | ID: biblio-908680

RESUMO

CONTEXTO: A doença de Alzheimer (DA) é uma afecção crônica e progressiva que leva à neurodegeneração gradual e demência e se caracteriza por perda cognitiva progressiva, sintomas neuropsiquiátricos (comportamentais) e prejuízo das atividades da vida diária (funcionais) dos doentes. Por meio do Protocolo Clínico e Diretrizes Terapêuticas (PCDT) da DA o Ministério da Saúde preconiza tratamento com inibidores das colinesterases ­ donepezila, galantamina e rivastigmina - para melhorar a função cognitiva e o estado clínico geral de pacientes com doença de gravidade leve a moderada. O presente relatório foi elaborado como parte da conduta de revisão do PCDT da DA e tem por objetivo avaliar as evidências de segurança e eficácia de memantina como tratamento da DA leve, moderada e grave. TECNOLOGIA: Cloridrato de memantina. INDICAÇÃO: Doença de Alzheimer (CID-10 G30). PERGUNTA: Memantina é eficaz e segura no tratamento de pacientes com doença de Alzheimer leve, moderada e grave quando comparada a inibidores da colinesterase ou placebo na evolução de sintomas cognitivos, sintomas comportamentais ou neuropsiquiátricos, atividades da vida diária, impressão clínica global e efeitos adversos? EVIDÊNCIAS CIENTÍFICAS: Foram realizadas buscas nas bases de dados Medline/PubMed, Embase e Cochrane Library por meio de estratégias elaboradas com termos específicos para cada base. Foram avaliadas 10 metanálises e 1 revisão sistemática da Cochrane. Dentre os 11 estudos incluídos, sete se referiam ao uso de memantina em monoterapia versus placebo e em 4 se avaliou a combinação de memantina com inibidores da acetilcolinesterase versus inibidores em monoterapia. Entre os estudos nos quais se avaliou a monoterapia com memantina, há um deles no qual se incluem somente participantes com DA leve à moderada, não havendo evidência de eficácia na DA leve, mas pequeno benefício na DA moderada nos desfechos de cognição e impressão clínica global. Em dois destes estudos se avaliou apenas o desfecho de sintomas comportamentais, com benefício em um deles. Dos 4 estudos restantes houve evidência de benefício em todos os desfechos da pergunta PICO, com exceção de 1 estudo em que não houve evidência de benefício em desfechos comportamentais e na impressão clínica global. A avaliação da combinação de memantina com inibidores da acetilcolinesterase versus monoterapia com inibidores da acetilcolinesterase, nos 4 estudos incluídos, mostra evidência de benefício em todos os desfechos (cognição, comportamento, funcional e impressão clínica global); benefício apenas para sintomas comportamentais em 1 e sem benefício para sintomas funcionais em 2 estudos. Sugere-se, dessa forma, a incorporação de memantina combinada a inibidores da acetilcolinesterase nos casos moderados e de memantina em monoterapia nos casos graves de DA. ANÁLISE DE IMPACTO ORÇAMENTÁRIO: O impacto orçamentário estimou quais seriam os gastos decorrentes de uma possível incorporação da memantina no SUS. Foram contemplados os pacientes com a forma moderada da doença além de um aumento da população elegível referente aos pacientes com a forma grave da doença. No primeiro ano, a estimativa foi de aproximadamente R$ 10 milhões, enquanto a estimativa para os 5 primeiros anos após a incorporação foi de aproximadamente R$ 73 milhões. A análise de sensibilidade apontou que os gastos para os 5 primeiros anos podem variar entre aproximadamente, R$ 50 milhões e R$ 131 milhões. RECOMENDAÇÃO DA CONITEC: Apesar do tamanho do efeito ser pequeno, ele é significativo e influencia favoravelmente a qualidade de vida dos doentes e cuidadores. Assim a CONITEC, em sua 57ª reunião ordinária realizada nos dias 05 e 06 de julho de 2017, recomendou preliminarmente a incorporação no SUS da memantina combinada aos inibidores da acetilcolinesterase nos casos moderados e da memantina em monoterapia nos casos graves de Doença de Alzheimer conforme Protocolo Clínico e Diretrizes Terapêuticas. A matéria será disponibilizada em Consulta Pública com recomendação preliminar favorável à incorporação. CONSULTA PÚBLICA: A consulta pública nº 34, de 02 de agosto de 2017 referente à recomendação inicial da CONITEC favorável à incorporação de memantina para doença de Alzheimer apresentada pela Secretaria de Ciência, Tecnologia e Insumos Estratégicos (SCTIE/MS) nos autos do processo MS/SIPAR nº 25000.063591/2017-11 ficou disponível para contribuições entre os dias 04/08 e 23/08/2017. Ao todo, foram recebidas 22 contribuições, sendo 4 do formulário "experiência ou opinião" e 18 do formulário "técnico-científico". Entre as contribuições recebidas 2 do formulário técnico-científico foram excluídas (9%); 4 apresentavam posicionamento contra ou parcialmente contra a recomendação (18% - 3 técnicas e 1 opinião) e 16 a favor ou parcialmente a favor da recomendação (73% - 13 técnicas e 3 opiniões). Em posicionamentos contrários reforçou-se o baixo efeito do medicamento nos desfechos apresentados nos estudos, mas não foram apresentadas novas evidências que pudessem modificar o parecer inicial, no qual se considerou como relevante o efeito na qualidade de vida dos pacientes e cuidadores como observados nos estudos selecionados para análise. DELIBERAÇÃO FINAL: Os membros da CONITEC presentes na reunião do plenário do dia 31/08/2017 deliberaram, por unanimidade, recomendar a incorporação de memantina para doença de Alzheimer, conforme Protocolo Clínico e Diretrizes Terapêuticas do Ministério da Saúde. Foi assinado o Registro de Deliberação nº 292/2017. DECISÃO: publicou-se a Portaria nº 49, de 8 de novembro de 2017 por meio da qual se tornou pública a decisão de aprovar a incorporação da memantina para doença de Alzheimer, conforme Protocolo Clínico e Diretrizes Terapêuticas, no âmbito do Sistema Único de Saúde - SUS.(AU)


Assuntos
Humanos , Doença de Alzheimer/tratamento farmacológico , Inibidores da Colinesterase/uso terapêutico , Memantina/uso terapêutico , Brasil , Análise Custo-Benefício , Avaliação da Tecnologia Biomédica , Sistema Único de Saúde
18.
Rev. Hosp. Ital. B. Aires (2004) ; 37(3): 105-111, Sept. 2017. tab.
Artigo em Espanhol | LILACS (Américas) | ID: biblio-1087981

RESUMO

La enfermedad con cuerpos de Lewy incluye 2 entidades que podrían ser consideradas variantes clínicas de una misma patología: la demencia con cuerpos de Lewy y la demencia en enfermedad de Parkinson. Con la finalidad de describir correctamente lo que sucede en la evolución de la enfermedad se divide el cuadro en etapa prodrómica y de demencia propiamente dicha. La primera está clínicamente representada por aquel período en el cual, si bien el paciente exhibe algunos signos y síntomas propios de la enfermedad, no reúne criterios de demencia. A pesar de ser difícil de definir y por carecerse todavía de contundentes datos clínicos y biomarcadores, se caracteriza principalmente por deterioro leve selectivo en función atencional ­ visuoespacial, trastorno del sueño REM y disautonomía‒. La segunda etapa está claramente caracterizada en los criterios de consenso del año 2005. Recientemente hemos publicado la validación de un instrumento llamado ALBA Screening Instrument, que permite diagnosticar con alta sensibilidad y especificidad la enfermedad aun en etapas tempranas y diferenciarla de otras patologías semejantes. La tomografía por emisión de positrones (PET) para transportador de dopamina es el procedimiento de referencia (gold standard) del diagnóstico. El tratamiento sintomático con anticolinesterásicos y neurolépticos atípicos favorece una buena evolución de la enfermedad y es fundamental tener en cuenta evitar medicamentos que pueden dañar gravemente a los pacientes como los anticolinérgicos y antipsicóticos típicos. Los avances en el diagnóstico y la difusión del impacto de esta enfermedad en la población contribuirán a generar mayores esfuerzos de investigación para hallar un tratamiento eficaz, preventivo o curativo o de ambas características. (AU)


Lewy body disease includes 2 entities that could be considered clinical variants of the same pathology: Dementia with Lewy bodies and Parkinson's disease Dementia. Two stages of the disease are described in this review, a prodromal stage and one of explicit dementia. The first one is clinically represented by that period in which, the patient exhibits some typical features of the disease, but not dementia criteria. Despite being difficult to define the prodromal stage and that strong clinical data and biomarkers are still lacking, there is evidence to characterize it mainly by mild selective impairment in attention and visuo-spatial function, REM sleep disorder and dysautonomia. The second stage is clearly characterized in the known consensus criteria of 2005. We have recently published the validation of an instrument called ALBA Screening Instrument which showed a high sensitivity and specificity for diagnosis of the disease even in the early stages. It´s useful to differentiate the disease from other similar pathologies. Positron Emission Tomography for dopamine transporter is the gold standard of diagnosis in life. Symptomatic treatment with anticholinesterases and atypical neuroleptics help patients in their evolution of the disease. Anticholinergics and typical antipsychotics are agents to avoid in the treatmen of the disease because can severely damage patients. Future advances in the diagnosis and dissemination of the knowledge of the disease will contribute to generate greater research efforts to find an effective preventive and / or curative treatment. (AU)


Assuntos
Humanos , Doença por Corpos de Lewy/tratamento farmacológico , Doença por Corpos de Lewy/diagnóstico por imagem , Doença de Parkinson/patologia , Atenção , Sinais e Sintomas , Antipsicóticos/efeitos adversos , Antipsicóticos/uso terapêutico , Benzotropina/efeitos adversos , Biperideno/efeitos adversos , Carbidopa/administração & dosagem , Carbidopa/uso terapêutico , Levodopa/administração & dosagem , Levodopa/uso terapêutico , Triexifenidil/efeitos adversos , Inibidores da Colinesterase/uso terapêutico , Clozapina/administração & dosagem , Clozapina/uso terapêutico , Antagonistas Muscarínicos/efeitos adversos , Antagonistas de Dopamina/efeitos adversos , Agonistas de Dopamina/efeitos adversos , Antagonistas Colinérgicos/efeitos adversos , Risperidona/efeitos adversos , Doença por Corpos de Lewy/diagnóstico , Doença por Corpos de Lewy/etiologia , Doença por Corpos de Lewy/genética , Doença por Corpos de Lewy/patologia , Transtorno do Comportamento do Sono REM/complicações , Demência , Disautonomias Primárias/complicações , Sintomas Prodrômicos , Rivastigmina/administração & dosagem , Rivastigmina/uso terapêutico , Fumarato de Quetiapina/administração & dosagem , Fumarato de Quetiapina/uso terapêutico , Olanzapina/efeitos adversos , Donepezila/administração & dosagem , Donepezila/uso terapêutico , Haloperidol/efeitos adversos , Antagonistas dos Receptores Histamínicos/efeitos adversos , Hipnóticos e Sedativos/efeitos adversos , Antidepressivos Tricíclicos/efeitos adversos
19.
Pulmäo RJ ; 26(1): 19-22, 2017.
Artigo em Português | LILACS (Américas) | ID: biblio-883594

RESUMO

Neste artigo de atualização discutiremos, à luz dos mais recentes e relevantes trabalhos, a terapia dupla com broncodilatadores de longa ação para os pacientes com Doença Pulmonar Obstrutiva Crônica (DPOC) no período estável, destacando sua proteção quanto a exacerbações, dispneia, qualidade de vida, utilizando como orientador de sua oportunidade de uso a recomendação mais recente do Iniciativa Global para Doenças Pulmonares (GOLD) da sigla em língua inglesa.


In this update article we will discuss the light of the most recent and relevant studies on dual therapy with long acting bronchodilators for patients with chronic obstructive pulmonary disease (COPD) in the stable period, highlighting their protection against exacerbations, dyspnea, quality of life, Using the most recent recommendation of the Global Initiative for Lung Disease (GOLD) as the guideline of their opportunity to use the English acronym.


Assuntos
Humanos , Masculino , Feminino , Broncodilatadores , Inibidores da Colinesterase , Agonistas Adrenérgicos beta , Doença Pulmonar Obstrutiva Crônica/tratamento farmacológico , Doença Pulmonar Obstrutiva Crônica/terapia
20.
Artigo em Inglês | WPRIM (Pacífico Ocidental) | ID: wprim-152983

RESUMO

OBJECTIVE: Donepezil is used to improve cognitive impairment of dementia with Lewy bodies (DLB). Visuo-spatial dysfunction is a well-known symptom of DLB. Non-verbal Raven’s Colored Progressive Matrices (RCPM) were used to assess both visual perception and reasoning ability in DLB subjects treated with donepezil. METHODS: Twenty-one DLB patients (mean age, 78.7±4.5 years) were enrolled. RCPM assessment was performed at the time of starting donepezil and within one year after starting donepezil. RESULTS: There were significant improvements of RCPM in the total scores between one year donepezil treatment (p=0.013), in both Set A score (p=0.002) and Set AB score (p=0.015), but trend in the Set B score (p=0.083). CONCLUSION: Donepezil is useful for improving visuo-spatial impairment in DLB, but not for problem-solving impairment.


Assuntos
Inibidores da Colinesterase , Transtornos Cognitivos , Demência , Humanos , Corpos de Lewy , Doença por Corpos de Lewy , Processamento Espacial , Percepção Visual
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