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1.
Acta Biol Hung ; 64(2): 249-61, 2013 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-23739892

RESUMO

A series of 2-[4-(4-substitutedbenzamido/phenylacetamido/butanamido)phenyl]-5-ethylsulphonyl-benzoxazole derivatives were synthesized and biologically evaluated as possible antimicrobial agents and inhibitors of tyrosinase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). The results demonstrated that the synthesized compounds exhibited a broad spectrum of activity with minimum inhibitory concentration (MIC) values of 128-16 µg/ml against some Gram-positive, Gram-negative bacteria as well as Candida albicans and C. krusei. The compound 10 displayed higher activity in this series against methicilline resistant Staphylococcus aureus (MRSA) with a MIC value of 16 µg/ml than the compared control drugs ampicillin and ceftriaxone. Compound 14 showed moderate tyrosinase inhibition, however, none of the compounds showed effect as inhibitor of AChE and BChE.


Assuntos
Anti-Infecciosos , Benzoxazóis , Candida albicans/crescimento & desenvolvimento , Inibidores da Colinesterase , Bactérias Gram-Negativas/crescimento & desenvolvimento , Staphylococcus aureus Resistente à Meticilina/crescimento & desenvolvimento , Acetilcolinesterase/metabolismo , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Proteínas de Bactérias/antagonistas & inibidores , Proteínas de Bactérias/metabolismo , Benzoxazóis/síntese química , Benzoxazóis/química , Benzoxazóis/farmacologia , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Relação Dose-Resposta a Droga , Proteínas Fúngicas/antagonistas & inibidores , Proteínas Fúngicas/metabolismo
2.
Clin Radiol ; 66(5): 420-5, 2011 May.
Artigo em Inglês | MEDLINE | ID: mdl-21334604

RESUMO

AIM: To evaluate the ability and the utility of diffusion-weighted (DW) magnetic resonance imaging (MRI) with high and low b values to visualize benign and malignant renal lesions, and to determine which b value (b=100, 600, or 1000s/mm(2)) was most useful in differentiating benign from malignant renal lesions. MATERIALS AND METHODS: Fifty-eight patients with 67 renal lesions and 50 normal contralateral kidneys (as control) were enrolled in the study. DW imaging was performed with b values of 100, 600, and 1000s/mm(2). Results of the histopathological evaluation were compared with the DW MRI results. Apparent diffusion coefficient (ADC) values, and the sensitivity and specificity for differentiating malignant renal lesions from benign renal lesions were calculated for each b value. RESULTS: The mean ADC values of normal renal parenchyma with b=100, 600, and 1000s/mm(2) values were (3.14±0.54)×10(-3), (2.52±0.30)×10(-3), and (2.16±0.43)×10(-3)mm(2)/s, respectively. The mean ADC values of benign renal lesions (n=35) with b=100, 600, and 1000s/mm(2) values were (2.88±0.88)×10(-3), (2.58±0.91)×10(-3), and (2.10±0.93)×10(-3)mm(2)/s, respectively. The mean ADC values of malignant renal lesions (n=32) with b=100, 600, and 1000 values were (2.74±0.58)×10(-3), (2.09±0.63)×10(-3), and (1.66±0.51)×10(-3)mm(2)/s, respectively. Using DW imaging malignant renal lesions could be differentiated from benign renal lesions, and also angiomyolipomas and oncocytomas could be differentiated from renal cell carcinoma. CONCLUSIONS: DW MRI with quantitative ADC measurements can be useful in the differentiation of benign and malignant renal lesions. High b values (b=600 and 1000s/mm(2)) had the best specificity and sensitivity.


Assuntos
Imagem de Difusão por Ressonância Magnética/métodos , Nefropatias/diagnóstico , Adolescente , Adulto , Idoso , Criança , Pré-Escolar , Diagnóstico Diferencial , Feminino , Humanos , Lactente , Nefropatias/patologia , Neoplasias Renais/diagnóstico , Neoplasias Renais/patologia , Masculino , Pessoa de Meia-Idade , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Adulto Jovem
3.
J Ethnopharmacol ; 114(1): 32-7, 2007 Oct 08.
Artigo em Inglês | MEDLINE | ID: mdl-17765419

RESUMO

Calluna vulgaris L. (Ericaceae) is used for the treatment of various inflammatory ailments in traditional medicines. In order to evaluate this ethnobotanical information, its anti-inflammatory and antinociceptive activities were studied using in vivo experimental models in mice. The ethanolic extract of the plant was first fractionated into five extracts; namely, n-hexane, chloroform, ethyl acetate (EtOAc), n-butanol, and water fractions. Among them, the EtOAc Fr. was found to be the most effective and was further subjected to bioassay-guided fractionation and isolation procedures. After successive column chromatography applications, on Sephadex LH-20 and silica gel, a component, which is responsible for the above-mentioned activities of this species of Turkish origin, was isolated and its structure was elucidated as kaempferol-3-O-beta-D-galactoside, a common flavonol derivative by means of spectral techniques.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Calluna/química , Quempferóis/farmacologia , Monossacarídeos/farmacologia , Analgésicos/isolamento & purificação , Analgésicos/toxicidade , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/toxicidade , Benzoquinonas , Bioensaio , Carragenina , Edema/induzido quimicamente , Edema/tratamento farmacológico , Quempferóis/isolamento & purificação , Quempferóis/toxicidade , Masculino , Camundongos , Monossacarídeos/isolamento & purificação , Monossacarídeos/toxicidade , Dor/tratamento farmacológico , Medição da Dor , Componentes Aéreos da Planta , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Solventes/química , Testes de Toxicidade Aguda , Turquia
4.
J Ethnopharmacol ; 105(1-2): 235-40, 2006 Apr 21.
Artigo em Inglês | MEDLINE | ID: mdl-16337351

RESUMO

The ethanolic and aqueous extracts prepared from different parts of Pistacia vera L. (Anacardiaceae) as well as its oleoresin were evaluated for their in vivo anti-inflammatory and antinociceptive activities. Among the extracts screened, only the oleoresin was shown to possess a marked anti-inflammatory activity against carrageenan-induced hind paw edema model in mice without inducing any gastric damage at both 250 and 500 mg/kg doses whereas the rest of the extracts were totally inactive. While the oleoresin was found to display significant antinociceptive activity at 500 mg/kg dose, the ethanolic and aqueous extracts belonging to fruit, leaf, branch and peduncle of Pistacia vera did not exhibit any noticeable antinociception in p-benzoquinone-induced abdominal contractions in mice. Fractionation of the oleoresin indicated the n-hexane fraction to be active, which further led to recognition of some monoterpenes, mainly alpha-pinene (77.5%) by capillary gas chromatography-mass spectrometry (GC-MS) as well as the oleoresin itself. alpha-Pinene was also assessed for its antinociceptive and anti-inflammatory activities in the same manner and exerted a moderate anti-inflammatory effect at 500 mg/kg dose.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Pistacia/química , Extratos Vegetais/farmacologia , Animais , Avaliação Pré-Clínica de Medicamentos , Cromatografia Gasosa-Espectrometria de Massas , Masculino , Ratos
5.
Vet Res Commun ; 30(8): 845-50, 2006 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-17139534

RESUMO

Eight female New Zealand rabbits were used. The bulbus oculi was removed bilaterally from orbita then intraorbital muscles were revealed by dissection and their length and breadth and the distance of the muscle insertion to the corneal limbus were measured. Junction formations of the insertion tendon of intraorbital muscle to the sclera were identified.


Assuntos
Olho/anatomia & histologia , Músculo Esquelético/anatomia & histologia , Animais , Feminino , Coelhos
6.
J Laryngol Otol ; 129(2): 155-8, 2015 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-25599929

RESUMO

OBJECTIVE: This study compared the results of nasal Staphylococcus aureus carriage and nasal cytology in men with and without a moustache. METHODS: The study group comprised 118 adult men with a moustache, and the control group consisted of 123 adult men without a moustache. Samples were taken from the participants' right nasal cavity for cytology and from the left nasal cavity for microbiology. RESULTS: The results for S aureus were positive in 19.5 per cent (n = 23) of participants with a moustache and in 20.3 per cent (n = 25) of men without a moustache. This difference was not significant (p > 0.05). However, nasal cytology revealed rich eosinophil clusters in participants with a moustache. CONCLUSION: The presence or absence of a moustache had no effect on nasal S aureus colonisation. However, further research is needed to understand whether the presence of a moustache increases the risk of allergic or non-allergic rhinitis.


Assuntos
Cabelo/microbiologia , Cavidade Nasal/microbiologia , Mucosa Nasal/microbiologia , Infecções Estafilocócicas/microbiologia , Staphylococcus aureus/crescimento & desenvolvimento , Adulto , Portador Sadio/imunologia , Portador Sadio/microbiologia , Eosinofilia/diagnóstico , Eosinofilia/imunologia , Eosinofilia/microbiologia , Face , Humanos , Masculino , Cavidade Nasal/patologia , Mucosa Nasal/patologia , Rinite/imunologia , Rinite/microbiologia , Rinite/patologia , Infecções Estafilocócicas/imunologia , Infecções Estafilocócicas/patologia , Infecções Estafilocócicas/prevenção & controle
7.
Curr Med Chem ; 22(8): 1004-15, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25515512

RESUMO

Dementia is a strongly age-related syndrome due to cognitive decline that can be considered a typical example of the combination of physiological and pathological aging-associated changes occurring in old people; it ranges from intact cognition to mild cognitive impairment, which is an intermediate stage of cognitive deterioration, and dementia. The spread of this syndrome has induced to study and try to reduce dementia modifiable risk factors. They include insulin resistance and hyperinsulinaemia, high blood pressure, obesity, smoking, depression, cognitive inactivity or low educational attainment as well as physical inactivity and incorrect diet, which can be considered one of the most important factors. One emerging strategy to decrease the prevalence of mild cognitive impairment and dementia may be the use of nutritional interventions. In the last decade, prospective data have suggested that high fruit and vegetable intakes are related to improved cognitive functions and reduced risks of developing a neurodegenerative process. The protective effects against neurodegeneration could be in part due to the intake of flavonoids that have been associated with several health benefits such as antioxidant and anti-inflammatory activities, increased neuronal signaling, and improved metabolic functions. The present article is aimed at reviewing scientific studies that show the protective effects of flavonoid intake against mild cognitive impairment and dementia.


Assuntos
Anti-Inflamatórios/uso terapêutico , Antioxidantes/uso terapêutico , Demência/prevenção & controle , Flavonoides/uso terapêutico , Fármacos Neuroprotetores/uso terapêutico , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Disfunção Cognitiva/prevenção & controle , Flavonoides/farmacologia , Humanos , Fármacos Neuroprotetores/farmacologia
8.
Fertil Steril ; 76(1): 138-42, 2001 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-11438332

RESUMO

OBJECTIVE: To describe the pathology-specific response to transurethral resection of ejaculatory ducts (TURED) in patients with complete or partial ejaculatory duct obstruction and to evaluate the role of TURED in light of powerful assisted reproductive technologies. DESIGN: Retrospective clinical study. SETTING: University hospital. PATIENT(S): Thirty-eight infertile men with obstruction of the ejaculatory ducts. INTERVENTION(S): Diagnosis by transrectal ultrasonography or magnetic resonance imaging, and treatment with TURED. MAIN OUTCOME MEASURE(S): Changes in semen variables, pregnancy outcomes, and complication rates were analyzed before and after surgery. RESULT(S): Improvement in semen variables was significantly better in patients with partial obstruction (94%) of ducts than in those with complete obstruction (59%) (P=.04). Cystic obstruction, especially midline and eccentric cysts, responded best to TURED. Before surgery, all patients were candidates for IVF/ICSI; after surgery, 32% of azoospermic men and 81% of oligospermic men conceived spontaneously or were referred for IUI instead of IVF/ICSI. CONCLUSION(S): Ejaculatory duct obstruction due to cysts appears to respond best to TURED. In addition, TURED may decrease the need for IVF/ICSI as primary treatment in many cases. Finally, TURED may allow IVF/ICSI to be performed with ejaculated rather than surgically retrieved sperm.


Assuntos
Ductos Ejaculatórios/cirurgia , Infertilidade Masculina/cirurgia , Adulto , Constrição Patológica/diagnóstico , Constrição Patológica/etiologia , Constrição Patológica/cirurgia , Cistos/complicações , Cistos/cirurgia , Ductos Ejaculatórios/diagnóstico por imagem , Ductos Ejaculatórios/patologia , Feminino , Fertilização in vitro , Doenças dos Genitais Masculinos/complicações , Doenças dos Genitais Masculinos/cirurgia , Humanos , Infertilidade Masculina/diagnóstico , Infertilidade Masculina/etiologia , Imageamento por Ressonância Magnética , Masculino , Pessoa de Meia-Idade , Complicações Pós-Operatórias , Gravidez , Taxa de Gravidez , Estudos Retrospectivos , Injeções de Esperma Intracitoplásmicas , Ultrassonografia , Uretra/cirurgia
9.
J Hosp Infect ; 57(3): 241-4, 2004 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-15236854

RESUMO

The aim of the present study was to determine the incidence of bacteraemia after urodynamic study (UDS) in patients with lower urinary tract symptoms, and to evaluate the role of bacteraemia as a morbidity factor related to UDS. A total of 57 patients (mean age: 52.8 years, range: 8-76 years) were evaluated by UDS. Prophylactic antibiotics were not administered to any of the patients before the procedure. Before UDS, urine cultures were examined for the presence of infection of the urinary tract (UTI). Venous blood was taken before and just after performing UDS. There was no bacterial growth in blood cultures of any patients before the UDS. Of the 57 patients, two had bacteriuria before study. After UDS, bacteraemia was determined in four (7%) out of 55 patients. The two patients with a bacteriuria before the procedure also had positive blood cultures. Infectious complications are the most important morbidity factors related to the UDS. Despite the use of strict aseptic techniques, bacteraemia may occur in patients undergoing UDS. The results of the present study may help when counselling patients who are to undergo UDS.


Assuntos
Bacteriemia/etiologia , Infecção Hospitalar/etiologia , Cateterismo Urinário/efeitos adversos , Urodinâmica , Adolescente , Adulto , Idoso , Assepsia/métodos , Bacteriemia/diagnóstico , Bacteriemia/epidemiologia , Bacteriemia/metabolismo , Criança , Infecção Hospitalar/diagnóstico , Infecção Hospitalar/epidemiologia , Infecção Hospitalar/metabolismo , Contaminação de Equipamentos , Reutilização de Equipamento , Infecções por Escherichia coli/etiologia , Feminino , Humanos , Incidência , Masculino , Pessoa de Meia-Idade , Morbidade , Seleção de Pacientes , Estudos Prospectivos , Infecções por Pseudomonas/etiologia , Fatores de Risco , Segurança , Infecções Estafilocócicas/etiologia , Cateterismo Urinário/instrumentação , Transtornos Urinários/diagnóstico
10.
Asian J Androl ; 5(2): 95-9, 2003 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-12778317

RESUMO

AIM: To investigate the level of malondialdehyde (MDA), a direct indicator of lipid peroxidation-induced injury by reactive oxygen species (ROS), in testicular biopsy specimens from infertile patients. METHODS: Levels of MDA were measured in testicular biopsy specimens from 29 consequent-randomized infertile men, aged 29.58+/-4.76 (21 to approximately 45) years. All patients were evaluated by a complete medical and reproductive history, physical examination, semen analysis (at least two), serum follicle-stimulating hormone and free testosterone levels, testicular biopsy and contact imprint. Scrotal colour Doppler ultrasonography was used to confirm suspected varicocele. The testicular MDA level was measured using the thiobarbituric acid test and the results were expressed per unit tissue weight. RESULTS: As a causal factor in infertility, varicocele was identified in 17 (58.6 %) patients, and idiopathic infertility, testicular failure and obstruction in 4 (13.8 %) patients each. The testicular MDA level was 13.56 (6.01), 49.56 (24.04), 58.53 (48.07), and 32.64 (21.51), 32.72 (13.61), 23.07 (7.82), 42,12 (34.76) pmol/mg tissue in the normal spermatogenesis (control), late maturation arrest, Sertoli cell only (SCO) and hypospermatogenesis (mild, moderate, severe) groups, respectively. The elevation of MDA levels was significant in the testicular tissue from SCO and maturation arrest groups compared with the controls (P<0.05). In addition, the elevation in testicular MDA levels between the SCO and the moderate hypospermatogenesis, and the moderate hypospermatogenesis and the maturation arrest groups was significant (P<0.05). CONCLUSION: Severe pathologic changes in the testicular tissue are associated with a high level of lipid peroxidation. These findings suggest that overproduction of ROS may play a role in the mechanism of testicular degeneration associated with infertility.


Assuntos
Infertilidade Masculina/etiologia , Espécies Reativas de Oxigênio/metabolismo , Doenças Testiculares/complicações , Doenças Testiculares/etiologia , Adulto , Senescência Celular , Humanos , Masculino , Malondialdeído/metabolismo , Células de Sertoli/patologia , Espermatogênese , Espermatozoides , Doenças Testiculares/patologia , Doenças Testiculares/fisiopatologia , Testículo/metabolismo , Testículo/fisiopatologia
11.
J Ethnopharmacol ; 91(1): 57-60, 2004 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-15036468

RESUMO

The chloroform:medianol (1:1) extracts of a number of the plant species belonging to eight families, namely Corydalis solida (L.) Swartz subsp. solida and Glaucium corniculatum (L.) J. H. Rudolph (Papaveraceae), Rhododendron ponticum L. subsp. ponticum and Rhododendron luteum Sweet. (Ericaceae), Buxus sempervirens L. (Buxaceae), Vicia faba L. (Fabaceae), Robinia pseudoacacia L. (Caeselpiniaceae), Tribulus terrestris L. and Zygophyllum fabago L. (Zygophyllaceae), Lycopodium clavatum L. (Lycopodiaceae), Fumaria vaillantii Lois., Fumaria capreolata L., Fumaria kralikii Jordan, Fumaria asepala Boiss., Fumaria densiflora DC., Fumaria flabellata L., Fumaria petteri Reichb. subsp. thuretii (Boiss.) Pugsley, Fumaria macrocarpa Boiss. ex Hausskn., Fumaria cilicica Hauskkn., Fumaria parviflora Lam. and Fumaria judaica Boiss. (Fumariaceae) were screened for their anticholinesterase activity on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes by in vitro Ellman method at 10 microg/ml and 1 mg/ml concentrations. The extracts did not show any noticeable inhibitory activity against both of the enzymes at 10 microg/ml. The extracts of Rhododendron ponticum subsp. ponticum, Rhododendron luteum, Corydalis solida subsp. solida, Glaucium corniculatum, and Buxus sempervirens showed remarkable inhibitory activity above 50% inhibition rate on AChE at 1 mg/ml. Among them, Rhododendron ponticum subsp. ponticum, Corydalis solida subsp. solida and Buxus sempervirens were the most active extracts against BChE having 95.46 +/- 1.03%, 93.08 +/- 0.97%, and 93.45 +/- 0.88% inhibition rates, respectively. Among the extracts screened, all of the Fumaria extracts displayed highly potent inhibition against both of the enzymes at 1 mg/ml concentration compared to the standard.


Assuntos
Butirilcolinesterase , Inibidores da Colinesterase/farmacologia , Extratos Vegetais/farmacologia , Inibidores da Colinesterase/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Turquia
12.
Andrology ; 2(2): 219-24, 2014 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-24357639

RESUMO

The objective of this study was to determine the prevalence of male pelvic dysfunction (MPD) and its correlation in men ≥40 years of age in a population-based study. This study was designed as a non-interventional, observational, cross-sectional field survey. Participating males of ≥40 years were randomly selected from 19 provinces of Turkey. All participants were asked to complete a survey including data regarding demographics, socio-economic status, socio-cultural factors, medical and sexual history, current medications, comorbidities and three validated questionnaires assessing lower urinary tract symptoms (International Prostate Symptom Score), erectile dysfunction (International Index of Erectile Function) and ejaculatory behaviour (Male Sexual Health Questionnaire-4). MPD was defined by combining abnormal scores calculated from all three questionnaires. All data were analysed statistically and p < 0.05 was accepted as significant. A total of 2730 males of ≥40 years (mean, 54.2 ± 10.6 years) were enrolled in this study. The prevalence of MPD was calculated as 24.4% among all participants. The prevalence of MPD was lowest at age between 40 and 49 years (9.1%) and highest at ≥70 years (76.6%), exhibiting correlation with age. Each decade of increase in age was associated with a 3.4-fold increase in presence of MPD. At logistic regression analyses; age, diabetes, hypertension, dyslipidemia, cardiovascular disease, obesity and lower income were found to be independent predictors for increased prevalence of MPD. This study reports prevalence of MPD as 24.4% in males of ≥40 years. Furthermore, age was found to be the main independent predictor of having MPD.


Assuntos
Disfunção Erétil/epidemiologia , Sintomas do Trato Urinário Inferior/epidemiologia , Pelve/patologia , Ejaculação Precoce/epidemiologia , Fatores Etários , Idoso , Doenças Cardiovasculares , Causalidade , Estudos Transversais , Diabetes Mellitus , Dislipidemias , Ejaculação/fisiologia , Humanos , Hipertensão , Masculino , Pessoa de Meia-Idade , Obesidade , Pobreza , Saúde Reprodutiva , Comportamento Sexual , Inquéritos e Questionários , Turquia
13.
Curr Med Chem ; 19(14): 2252-61, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22414107

RESUMO

Alzheimer's disease (AD) has become one of the deadliest diseases for human beings with special incidence in elderly population. It is a progressive neurodegenerative disease and the most prevalent cause of dementia. The neuropathology of AD has not been fully elucidated yet, however, cholinergic hypothesis is the most accepted theory nowadays, resulting from the cholinergic deficit emerging in the brains of AD patients. Shortage of the neurotransmitters, acetylcholine and butyrylcholine has been demonstrated, and therefore, inhibition of the enzymes; acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) that break down acetylcholine and butyrylcholine has become a standard approach for AD treatment. However, cholinesterase inhibitors are only effective in symptomatic treatment and have no ability to impede the disease. The pathogenesis of AD is highly complex and another hypothesis is the formation of amyloid plaques containing beta-amyloid peptide, which causes neurolesions in the brains of AD patients. Beta-amyloid peptide is generated after the sequential cleavage of amyloid precursor protein, especially by the beta- and gamma-secretase in the amyloidogenic pathway. The secretases involved in the processing of amyloid precursor protein are of particular interest and, consequently, the inhibition of secretase enzyme family of protease type has become another desired treatment strategy for AD. On the other hand, medicinal plants are attractive sources for drug research and development as they produce chemically-varying molecules with preferred biological activities. The aim of this article is to review the available data on selected inhibitors from plant secondary metabolites with emphasis on cholinesterase, prolyl endopeptidase, and secretase enzyme families as being the current treatments of AD.


Assuntos
Acetilcolinesterase/metabolismo , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/enzimologia , Produtos Biológicos/farmacologia , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/farmacologia , Extratos Vegetais/farmacologia , Animais , Produtos Biológicos/química , Produtos Biológicos/metabolismo , Inibidores da Colinesterase/química , Inibidores da Colinesterase/metabolismo , Humanos , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Plantas Medicinais/química , Plantas Medicinais/metabolismo
14.
Mini Rev Med Chem ; 11(10): 836-42, 2011 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-21762104

RESUMO

Cholinesterase enzyme family consisting of acetylcholinesterase (AChE) and butrylcholinesterase (BChE) is important in pathogenesis of Alzheimer's disease (AD), explained by "cholinergic hypothesis". Accordingly, deficiency of the neuromediator called "acetylcholine" excessive amount of BChE has been well-described in the brains of AD patients. Consequently, cholinesterase inhibition has become one of the most-prescribed treatment strategies for AD. In fact, cholinesterase inhibitors have been also reported for their effectiveness in some other diseases including glaucoma, myasthenia gravies, as well as Down syndrome, lately. They play a role in the action of mechanism of insecticidal drugs such as carbamate derivatives as well as nerve gases such as malathion and parathion. All these utilizations can make them a multi-targeted drug class putting a special emphasis on AD therapy in the first place. Several inhibitors of cholinesterases with synthetic and natural origins are available in drug market; however, the reasons including side effects, relatively low bioavailability, etc. limit their uses in medicine and there is still a great demand to discover new cholinesterase inhibitors. Galanthamine, an alkaloid derivative isolated from snowdrop (Galanthus nivalis L.), is the latest anticholinesterase drug used against AD. Huperzine A, isolated from Huperzia serrata (Thunb.) Trev. is the most-promising drug candidate with potent anticholinesterase effect and it is a licensed anti-AD drug in China. In this review, a short introduction will be given on known cholinesterase inhibitors and, then, galanthamine and huperzine A will be covered in regard with their cholinesterase inhibitory potentials and mass productions by organic synthesis and in vitro culture techniques.


Assuntos
Inibidores da Colinesterase/química , Alcaloides/biossíntese , Alcaloides/química , Alcaloides/farmacologia , Doença de Alzheimer/tratamento farmacológico , Inibidores da Colinesterase/uso terapêutico , Galantamina/biossíntese , Galantamina/química , Galantamina/farmacologia , Humanos , Huperzia/química , Huperzia/citologia , Liliaceae/química , Liliaceae/citologia , Sesquiterpenos/química , Sesquiterpenos/farmacologia
15.
Ir J Med Sci ; 179(3): 443-5, 2010 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-18850240

RESUMO

BACKGROUND: Although screw breakage or loosening are rarely encountered, they were reported to occur after instability of the internal fixation. METHODS: A man with a history of traumatic pelvic fracture 6 months ago presented to our clinic with inability to void. An anterior urethral meatotomy was made and a calcified but intact screw was removed from the urethra. CONCLUSIONS: Screw migration with urological manifestations are extremely rare and usually include bladder migration with a subsequent voiding of the screw. We present a case in which internal urethrotomy for posterior urethral stricture caused erosion of a bone screw into the urethra which was subsequently removed by anterior meatotomy.


Assuntos
Parafusos Ósseos/efeitos adversos , Migração de Corpo Estranho/complicações , Fixação Interna de Fraturas/efeitos adversos , Fraturas Ósseas/cirurgia , Ossos Pélvicos/lesões , Adulto , Dilatação Patológica , Migração de Corpo Estranho/diagnóstico por imagem , Humanos , Masculino , Complicações Pós-Operatórias/diagnóstico por imagem , Radiografia , Uretra/patologia , Bexiga Urinária/lesões
16.
Food Chem Toxicol ; 48(3): 781-8, 2010 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-20026160

RESUMO

The members of Scutellaria L. (Lamiaceae) is known to be rich particularly in flavonoids and among them, S. baicalensis has been recorded to be used for memory-enhancing purpose. Therefore, we initiated a study to screen the methanol extracts prepared from the aerial parts of 33 Turkish Scutellaria species for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, which are the key enzymes taking place in pathogenesis of Alzheimer's disease. Besides, the methanol extracts were tested in vitro against another enzyme, tyrosinase, which is associated with melanin hyperpigmentation. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenger effect, ferrous ion-chelating ability, and ferric-reducing antioxidant power (FRAP) of the ethyl acetate and methanol extracts were also determined. AChE, BChE, and tyrosinase inhibition of the extracts were performed on ELISA microplate reader by spectrophotometric method. The extracts showed weak inhibition against AChE and BChE, while the best tyrosinase inhibition was caused by the methanol extract of S. brevibracteata subsp. subvelutina. The extracts had a very high DDPH radical scavenging effect and moderate antioxidant activity in ferrous ion-chelating and FRAP tests.


Assuntos
Acetilcolinesterase/metabolismo , Antioxidantes/farmacologia , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Scutellaria/química , Algoritmos , Compostos de Bifenilo , Ensaio de Imunoadsorção Enzimática , Flavonoides/farmacologia , Sequestradores de Radicais Livres/farmacologia , Quelantes de Ferro/farmacologia , Oxidantes , Fenóis/farmacologia , Picratos , Extratos Vegetais/farmacologia , Turquia
17.
Food Chem Toxicol ; 47(8): 1747-51, 2009 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-19394400

RESUMO

We have investigated anticholinesterase potential of the methanol extracts from the leaf, wood, flower, twig, and stem bark of the female and male individuals and rhizodermis and fruit from the female tree of Maclura pomifera (Rafin.) Schneider (Moraceae) along with its major isoflavonoids; osajin and pomiferin as well as their semi-synthetic derivatives; iso-osajin and iso-pomiferin. Anticholinesterase activity was determined by Ellman method using ELISA microplate reader. Osajin and pomiferin had a noticeable inhibition of AChE with IC(50) values of 2.239 and 0.096 mM, respectively, while their iso-derivatives were found to display less inhibition towards AChE. The extracts and compounds did not inhibit BChE. The extracts were analyzed for osajin and pomiferin contents by LC-DAD-MS and only the fruits and female flowers contained osajin (fruit: 8.87%, female flowers: 0.19%, w/w) and pomiferin (fruit: 13.6%, female flowers: 0.36%, w/w).


Assuntos
Maclura/química , Animais , Benzopiranos/química , Benzopiranos/isolamento & purificação , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/farmacologia , Cromatografia Líquida de Alta Pressão , Electrophorus , Ensaio de Imunoadsorção Enzimática , Galantamina/farmacologia , Isoflavonas/química , Isoflavonas/isolamento & purificação , Espectrometria de Massas , Extratos Vegetais/farmacologia
18.
Food Chem Toxicol ; 47(6): 1304-10, 2009 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-19285534

RESUMO

The dichloromethane, ethyl acetate, ethanol, and aqueous extracts of Cyclotrichium niveum (CN) and Thymus praecox subsp. caucasicus var. caucasicus (TP), Echinacea purpurea (EPU), and E. pallida (EPA) along with the essential oils of CN and TP were assessed for their anti-acetylcholinesterase (AChE) and antioxidant activities. AChE inhibition was estimated using spectrophotometric method of Ellman. Antioxidant activity was evaluated by 2,2-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and ferrous ion-chelating power tests. Ferric-reducing antioxidant power (FRAP) of CN and TP were also tested. CN essential oil was found to contain isomenthone (56.21%) and pulegone (19.76%). The ethyl acetate (83.11-87.98%) and dichloromethane (73.45-84.02%) extracts of CN showed the highest AChE inhibition. The ethyl acetate and ethanol extracts of TP exerted significant DPPH scavenger effect. The water extracts of CN and TP and the chloroform extract of the aerial parts of EPU displayed the highest ferrous ion-chelating effect. The leaf and flower essential oils of TP had the best FRAP.


Assuntos
Antioxidantes/farmacologia , Inibidores da Colinesterase/farmacologia , Echinacea/química , Lamiaceae/química , Animais , Compostos de Bifenilo/química , Electrophorus , Sequestradores de Radicais Livres/química , Cromatografia Gasosa-Espectrometria de Massas , Quelantes de Ferro/química , Quelantes de Ferro/farmacologia , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Oxirredução , Fenóis/química , Fenóis/farmacologia , Picratos/química , Extratos Vegetais/farmacologia , Solventes
19.
Chem Biol Interact ; 181(3): 383-9, 2009 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-19596285

RESUMO

Flavonoids are one of the largest classes of plant secondary metabolites and are known to possess a number of significant biological activities for human health. In this study, we examined in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of four flavonoid derivatives--quercetin, rutin, kaempferol 3-O-beta-D-galactoside and macluraxanthone. The in vitro results showed that quercetin and macluraxanthone displayed a concentration-dependant inhibition of AChE and BChE. Macluraxanthone showed to be the most potent and specific inhibitor of both the enzymes having the IC(50) values of 8.47 and 29.8 microM, respectively. The enzyme kinetic studies revealed that quercetin inhibited both the enzymes in competitive manner, whereas the mode of inhibition of macluraxanthone was non-competitive against AChE and competitive against BChE. The inhibitory profiles of the compounds have been compared with standard AChE inhibitor galanthamine. To get insight of the intermolecular interactions, the molecular docking studies of these two compounds were performed at the active site 3D space of both the enzymes, using ICM-Dock module. Docking studies exhibited that macluraxanthone binds much more tightly with both the enzymes than quercetin. The calculated docking and binding energies also supported the in vitro inhibitory profiles (IC(50) values). Both the compounds showed several strong hydrogen bonds to several important amino acid residues of both the enzymes. A number of hydrophobic interactions could also explain the potency of the compounds to inhibit AChE and BChE.


Assuntos
Inibidores da Colinesterase/farmacologia , Flavonoides/farmacologia , Xantonas/farmacologia , Acetilcolinesterase/efeitos dos fármacos , Butirilcolinesterase/efeitos dos fármacos , Inibidores da Colinesterase/farmacocinética , Flavonoides/farmacocinética , Humanos , Modelos Moleculares , Xantonas/farmacocinética
20.
Phytomedicine ; 15(12): 1087-92, 2008 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-18606529

RESUMO

In the current study, vasorelaxant effect produced by the aqueous extract of Melissa officinalis L. ssp. officinalis (MOO) (Lamiaceae) and its possible mechanism in isolated rat aortic rings precontracted with phenylephrine were examined. In the first series of experiments, effect of MOO on the baseline and phenylephrine (10(-5)M) precontracted arteries was investigated, while in the second group of experiments, endothelium intact or endothelium denuded effect was determined. The agents used were N(omega)-nitro-L-arginine (L-NAME), an irreversible inhibitor of nitric oxide (NO) synthase, indomethacin (10 microM), a cyclooxygenase (COX) inhibitor, and glibenclamide (10 microM), an ATP-sensitive potassium channel blocker. The extract was found to exert a vasorelaxant effect and rosmarinic acid quantity, the characteristic compound of the plant, was analyzed by reversed-phase high-performance liquid chromatography (18.75%), and was further confirmed by LC-MS analysis giving a prominent [M(+1)] molecular ion peak at m/z 365. Total phenol amount in the extract was determined using Folin-Ciocalteau reagent (0.284 mg/mg extract). Vasorelaxant effect of the extract was entirely dependent on the presence of endothelium and was abolished by pretreatment with L-NAME, whereas pretreatment with indomethacin and glibenclamide reduced the relaxation to a minor extent. Rosmarinic acid was also tested in the same manner as the extract and was found to exert vasorelaxant effect. These results suggest that the aqueous extract of MOO vasodilates via nitric oxide pathway with the possible involvement of prostacycline and endothelium-derived hyperpolarizing factor (EDHF) pathways as well.


Assuntos
Aorta Torácica/efeitos dos fármacos , Endotélio Vascular/efeitos dos fármacos , Melissa/química , Extratos Vegetais/farmacologia , Vasodilatadores/farmacologia , Animais , Cromatografia Líquida de Alta Pressão , Cinamatos/análise , Depsídeos/análise , Técnicas In Vitro , Masculino , Espectrometria de Massas , Molibdênio/química , Fenóis/análise , Ratos , Ratos Wistar , Compostos de Tungstênio/química , Ácido Rosmarínico
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