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1.
Genet Mol Res ; 16(1)2017 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-28301670

RESUMO

Human blood groups are a significant resource for patients, leading to a fierce international competition in the screening of rare blood groups. Some rare blood group screening programs have been implemented in western countries and Japan, but not particularly in China. Recently, the genetic background of ABO and Rh blood groups for different ethnic groups or regions in China has been focused on increasingly. However, rare blood groups such as MN, Duffy, Kidd, MNS, and Diego are largely unexplored. No systematic reports exist concerning the polymorphisms and allele frequencies of rare blood groups in China's ethnic minorities such as Uygur and Kazak populations of Xinjiang, unlike those on the Han population. Therefore, this study aimed to investigate the allele frequencies of rare blood groups, namely, MNS, Duffy, Kell, Dombrock, Diego, Kidd, Scianna, Colton, and Lutheran in the Uygur population of Xinjiang Single specific primer-polymerase chain reaction was performed for genotyping and statistical analysis of 9 rare blood groups in 158 Uygur individuals. Allele frequencies were compared with distribution among other ethnic groups. Observed and expected values of genotype frequencies were compared using the chi-square test. Genotype frequencies obeyed the Hardy-Weinberg equilibrium (P > 0.5) and allele frequencies were stable. Of all subjects detected, 4 cases carried the rare phenotype S-s- of MNS blood group (frequency of 0.0253), and 1 case carried the phenotype Jka-b- (frequency of 0.0063). Frequencies of the four groups, MNS, Duffy, Dombrock, and Diego, in the Uygur population differed from those in other ethnic groups. Gene distribution of the Kell, Kidd, and Colton was similar to that in Tibetan and Han populations, though there were some discrepancies. Gene distribution of Scianna and Lutheran groups showed monomorphism similar to that in Tibetan and Han populations. These findings could contribute to the investigation of the origin, evolution, and hematology of Uygur population of Xinjiang and assist in screening of rare blood groups in ethnic minorities, meeting of clinical blood supply demands, and building of the national rare blood group library.


Assuntos
Sistema do Grupo Sanguíneo Duffy/genética , Sistema do Grupo Sanguíneo de Kell/genética , Sistema do Grupo Sanguíneo MNSs/genética , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Povo Asiático/genética , Criança , Pré-Escolar , China , Feminino , Frequência do Gene , Genótipo , Humanos , Lactente , Masculino , Pessoa de Meia-Idade , Adulto Jovem
2.
Genet Mol Res ; 14(4): 16386-91, 2015 Dec 09.
Artigo em Inglês | MEDLINE | ID: mdl-26662434

RESUMO

The purpose of this study was to explore the radiotherapy sensitization effects and the mechanism of capecitabine (Xeloda) against the non-small-cell lung cancer cell line, A549. γ-[(60)Co] radiation was used as the intervention method. Proliferative inhibition of capecitabine on A549 cells was determined by the CCK-8 method. The effects of capecitabine on the apoptosis rate and cell cycle distribution of A549 were detected with the flow cytometric method. We found that capecitabine inhibited the proliferation of A549 in a dose-dependent manner, notably increased the cell apoptosis rate and blocked the cellular G0/G1 phase after radiotherapy by γ-[(60)Co]. Therefore, capecitabine can significantly increase the radiosensitivity of A549; its mechanism may be related to cell cycle arrest and induction of apoptosis.


Assuntos
Antimetabólitos Antineoplásicos/farmacologia , Capecitabina/farmacologia , Tolerância a Radiação/efeitos dos fármacos , Apoptose/efeitos dos fármacos , Apoptose/efeitos da radiação , Carcinoma Pulmonar de Células não Pequenas , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos da radiação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Proliferação de Células/efeitos da radiação , Humanos , Neoplasias Pulmonares , Radiação Ionizante
3.
Andrologia ; 46(8): 824-30, 2014 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-23998339

RESUMO

Cystic fibrosis transmembrane conductance regulator (CFTR) has been demonstrated to be expressed in mature spermatozoa and correlated with sperm quality. Sperm CFTR expression in fertile men is higher than that in infertile men suffering from teratospermia, asthenoteratospermia, asthenospermia and oligospermia, but it is unknown whether CFTR is correlated with sperm parameters when sperm parameters are normal. In this study, 282 healthy and fertile men with normal semen parameters were classified into three age groups, group (I): age group of 20-29 years (98 cases, 27.1 ± 6.2), group (II): age group of 30-39 years (142 cases, 33.7 ± 2.6) and group (III): age group of more than or equal to 40 years (42 cases, 44.1 ± 4.6). Sperm concentration, total count and progressive motility were analysed by computer-assisted sperm analysis. Sperm morphology was analysed by modified Papanicolaou staining. Sperm CFTR expression was conducted by indirect immunofluorescence staining. There was a significant positive correlation (P < 0.001) between CFTR expression and sperm progressive motility (r = 0.221) and normal morphology (r = 0.202), but there were no correlations between sperm CFTR expression and semen volume, sperm concentration, sperm total count as well as male age (P > 0.05). Our findings show that CFTR expression is associated with sperm progressive motility and normal morphology in healthy and fertile men with normal sperm parameters, but not associated with the number of spermatozoa and male age.


Assuntos
Regulador de Condutância Transmembrana em Fibrose Cística/metabolismo , Motilidade dos Espermatozoides , Espermatozoides/metabolismo , Adulto , Envelhecimento/metabolismo , Biomarcadores/metabolismo , Fertilidade , Voluntários Saudáveis , Humanos , Masculino , Pessoa de Meia-Idade , Espermatozoides/citologia , Adulto Jovem
4.
Phytother Res ; 24(11): 1734-8, 2010 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-20564501

RESUMO

OBJECTIVES: The aim of the present study was to investigate the effect of an antidiabetic polysaccharide (IJP) from Inula japonica on gastrointestinal transit in normal mice and on constipation in two models of constipated mice. METHODS: Two models of constipation in mice were respectively induced by fasted water for 4 days or induced by diphenoxylate. The normal and constipated mice were administered IJP once at doses of 100 and 400 mg/kg (p.o.), the gastrointestinal vermicular motion, start time of defecation, number and weight of stool were investigated. RESULTS: After administration of IJP, the gastrointestinal propulsive rate was increased by 9.79% and 10.42%, the start time of defecation was shortened by 37.27% and 44.06%, the number of feces increased by 115.4% and 130.8% in normal mice. In fasting-water constipated mice, the start time of defecation was shortened by 9.69% and 30.52% by IJP, defecation granules raised by 22.09% and 39.53%, wet feces weights were increased by 23.50% and 39.14% compared with the untreated constipated mice. In diphenoxylate-induced mice, the start time of defecation was shortened by 25.48% and 28.13%, defecation granules raised by 100.0% and 118.0%. CONCLUSIONS: Consumption of IJP effectively improved bowel movement, stool output observed in this study. IJP may be practical in relieving constipation in the elderly diabetic population.


Assuntos
Constipação Intestinal/tratamento farmacológico , Trânsito Gastrointestinal/efeitos dos fármacos , Hipoglicemiantes/farmacologia , Inula/química , Polissacarídeos/farmacologia , Animais , Defecação/efeitos dos fármacos , Modelos Animais de Doenças , Feminino , Flores/química , Hipoglicemiantes/isolamento & purificação , Masculino , Camundongos , Polissacarídeos/isolamento & purificação
5.
Am J Hypertens ; 12(12 Pt 1-2): 1260-3, 1999 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-10619591

RESUMO

Cells dissociated from spontaneously hypertensive rat (SHR) parathyroid glands were grown in culture. Media harvested from the cell cultures were analyzed for parathyroid hypertensive factor (PHF) using the blood pressure bioassay. Cells raised in DMEM containing normal (1.8 mmol/L) CaCl2 secreted a negligible amount of PHF, while cells cultured in Ham's F-12 medium containing low (0.3 mmol/L) CaCl2 secreted higher amounts of PHF. The PHF secretion in Ham's F-12 medium was highest in early passage cells, and was maintained for approximately 12 to 15 passages. PHF purified from the cell culture medium exhibited chromatographic properties identical to those previously described for PHF isolated from SHR plasma or SHR parathyroid gland organ culture medium. These results support the parathyroid gland as the organ of origin of PHF.


Assuntos
Fatores Biológicos/metabolismo , Hipertensão/metabolismo , Glândulas Paratireoides/metabolismo , Animais , Biomarcadores , Pressão Sanguínea , Cálcio/sangue , Células Cultivadas , Hipertensão/fisiopatologia , Masculino , Glândulas Paratireoides/citologia , Glândulas Paratireoides/crescimento & desenvolvimento , Ratos , Ratos Endogâmicos SHR
6.
Steroids ; 61(11): 657-63, 1996 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-8916361

RESUMO

Pharmacological doses of 24R,25-dihydroxyvitamin D3 (24,25D3) inhibited both phasic and tonic contraction of Sprague-Dawley (SD) rat tail artery helical strips induced by KCl, norepinephrine (NE), and arginine vasopressin (AVP) in organ-bath studies. 24,25D3 also decreased the tension dependent on external calcium influx induced by KCl, AVP, and NE and the tension dependent on internal calcium release from intracellular calcium stores induced by NE. In vascular smooth muscle cells isolated from SD rat tail artery, 24,25D3 reduced membrane L-type calcium channel current and the increment of intracellular calcium concentration induced by KCl. It is suggested that 24,25D3 directly relaxed precontracted SD rat-tail artery by its inhibitory effect on plasma membrane and intracellular organelle calcium channels.


Assuntos
24,25-Di-Hidroxivitamina D 3/farmacologia , Bloqueadores dos Canais de Cálcio/farmacologia , Canais de Cálcio/efeitos dos fármacos , Músculo Liso Vascular/efeitos dos fármacos , Animais , Cálcio/metabolismo , Canais de Cálcio/metabolismo , Membrana Celular/efeitos dos fármacos , Membrana Celular/metabolismo , Masculino , Músculo Liso Vascular/metabolismo , Norepinefrina/farmacologia , Ratos , Ratos Sprague-Dawley
7.
J Pharm Pharmacol ; 52(4): 451-9, 2000 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-10813558

RESUMO

The effects of Ginkgo biloba leaf extract on rat brain or livermonoamine oxidase (MAO)-A and -B activity, biogenic amine concentration in nervous tissue, N-methyl-D-aspartate (NMDA)- and N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine (DSP-4)-induced neurotoxicity and antioxidant activity was investigated to determine the effects of the extract on monoamine catabolism and neuroprotection. Ginkgo biloba leaf extract was shown to produce in-vitro inhibition of rat brain MAO-A and -B. The Ginkgo biloba extract was chromatographed on a reverse-phase HPLC system and two of the components isolated were shown to be MAO inhibitors (MAOIs). These MAOIs were identified by high-resolution mass spectrometry as kaempferol and isorhamnetin. Pure kaempferol and a number of related flavonoids were examined as MAOIs in-vitro. Kaempferol, apigenin and chrysin proved to be potent MAOIs, but produced more pronounced inhibition of MAO-A than MAO-B. IC50 (50% inhibition concentration) values for the ability of these three flavones to inhibit MAO-A were 7 x 10(-7), 1 x 10(-6) and 2 x 10(-6) M, respectively. Ginkgo biloba leaf extract and kaempferol were found to have no effect ex-vivo on rat or mouse brain MAO or on concentrations of dopamine, noradrenaline, 5-hydroxytryptamine and 5-hydroxyindoleacetic acid. Kaempferol was shown to protect against NMDA-induced neuronal toxicity in-vitro in rat cortical cultures, but did not prevent DSP-4-induced noradrenergic neurotoxicity in an in-vivo model. Both Ginkgo biloba extract and kaempferol were demonstrated to be antioxidants in a lipid-peroxidation assay. This data indicates that the MAO-inhibiting activity of Ginkgo biloba extract is primarily due to the presence of kaempferol. Ginkgo biloba extract has properties indicative of potential neuroprotective ability.


Assuntos
Flavonoides , Ginkgo biloba/química , Quempferóis , Inibidores da Monoaminoxidase/análise , Fármacos Neuroprotetores/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plantas Medicinais , Quercetina/análogos & derivados , Ácido 3,4-Di-Hidroxifenilacético/metabolismo , Administração Oral , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/enzimologia , Encéfalo/metabolismo , Células Cultivadas , Cromatografia Líquida de Alta Pressão , Dopamina/metabolismo , Relação Dose-Resposta a Droga , Ácido Hidroxi-Indolacético/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/enzimologia , Masculino , Camundongos , Monoaminoxidase/efeitos dos fármacos , Monoaminoxidase/metabolismo , Inibidores da Monoaminoxidase/farmacologia , N-Metilaspartato/farmacologia , Neurônios/citologia , Neurônios/efeitos dos fármacos , Norepinefrina/metabolismo , Extratos Vegetais/química , Quercetina/análise , Quercetina/farmacologia , Ratos , Ratos Sprague-Dawley , Serotonina/metabolismo , Células Tumorais Cultivadas/efeitos dos fármacos , Células Tumorais Cultivadas/metabolismo
8.
J Pharm Pharmacol ; 53(11): 1515-23, 2001 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-11732754

RESUMO

The activity of CVT-E002, an aqueous extract containing mainly oligosaccharides and polysaccharides from North American ginseng (Panax quinquefolium), as an immunobooster on murine spleen cells and peritoneal macrophages, was studied in-vitro. CVT-E002 stimulated the proliferation of normal mouse spleen cells, of which the major responding subpopulation was identified as B lymphocytes. CVT-E002 also activated peritoneal exudate macrophages leading to enhanced interleukin-1 (IL-1), interleukin-6 (IL-6), tumour necrosis factor-alpha (TNF-alpha) and nitric oxide (NO) production. In addition, CVT-E002 stimulated in-vivo immunoglobulin G (IgG) production in treated mice. These results identify some of the immunomodulating activities of CVT-E002 and suggest its use clinically for the modulation of immune responses.


Assuntos
Adjuvantes Imunológicos/farmacologia , Panax/química , Extratos Vegetais/farmacologia , Animais , Divisão Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Imunidade Inata/efeitos dos fármacos , Imunoglobulina G/sangue , Imunoglobulina G/efeitos dos fármacos , Interleucina-1/metabolismo , Interleucina-6/metabolismo , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos C57BL , Óxido Nítrico/metabolismo , Baço/citologia , Baço/efeitos dos fármacos , Fator de Necrose Tumoral alfa/metabolismo
9.
J Pharm Pharmacol ; 53(6): 849-57, 2001 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-11428661

RESUMO

Alcoholic extracts of the roots and leaves of three Echinacea species (E. purpurea, E. angustifolia and E. pallida) were analysed for the presence of characteristic chemicals by HPLC directly coupled to ultraviolet absorbance and electrospray mass spectrometric detectors. The method permitted rapid characterization and tentative identification of a large number of caffeoyl conjugates and alkamides in all the samples investigated. The roots of the three species differed markedly in their contents of characteristic compounds. Cichoric acid and verbascoside predominated in extracts of E. purpurea root whereas cynarine and dodeca-2E,4E,8Z,10Z/E-tetraenoic acid isobutylamide were the major chemicals characteristic of E. angustifolia root extracts. Echinacoside and 6-O-caffeoylechinacoside predominated in extracts of E. pallida roots. Characteristic alkamides were also examined by electrospray tandem mass spectrometry (MS/MS) and these compounds provided characteristic fragmentation patterns. Extracts of the roots and leaves of all three species were found to have antioxidant properties in a free radical scavenging assay and in a lipid peroxidation assay.


Assuntos
Antioxidantes/farmacologia , Echinacea/química , Extratos Vegetais/farmacologia , Plantas Medicinais , Cromatografia Líquida de Alta Pressão , Sequestradores de Radicais Livres , Humanos , Peroxidação de Lipídeos , Espectrometria de Massas , Neuroblastoma/patologia , Extratos Vegetais/química , Folhas de Planta/química , Raízes de Plantas/química , Espectrofotometria Ultravioleta , Células Tumorais Cultivadas
11.
Planta Med ; 62(5): 431-5, 1996 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-8923809

RESUMO

Tetramethylpyrazine (TMP) is a compound purified from a medicinal plant Ligusticum wallichii Franch. Its effects on in vivo blood pressure, in vitro vascular contractility, and intracellular calcium regulation in rats were examined in the present study to see if it was a possible calcium antagonist in the vascular tissue. Data showed that TMP was hypotensive and had a direct vascular effect. It not only blocked the entry of extracellular calcium through calcium channels but also inhibited the release of intracellular stored calcium in the vascular smooth muscle cell. It was a true calcium antagonist.


Assuntos
Pressão Sanguínea/efeitos dos fármacos , Bloqueadores dos Canais de Cálcio/farmacologia , Cálcio/metabolismo , Músculo Liso Vascular/fisiologia , Plantas Medicinais , Pirazinas/farmacologia , Animais , Artérias/efeitos dos fármacos , Artérias/fisiologia , Técnicas In Vitro , Masculino , Potenciais da Membrana/efeitos dos fármacos , Contração Muscular/efeitos dos fármacos , Músculo Liso Vascular/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley
12.
J Psychiatry Neurosci ; 26(3): 221-8, 2001 May.
Artigo em Inglês | MEDLINE | ID: mdl-11394191

RESUMO

OBJECTIVE: A combination herbal product containing American ginseng extract, Panax quinquefolium, (200 mg) and Ginkgo biloba extract (50 mg) (AD-FX; CV Technologies, Edmonton, Alta.) was tested for its ability to improve the symptoms of attention-deficit hyperactivity disorder (ADHD). DESIGN: Open study. PATIENTS: 36 children ranging in age from 3 to 17 years who fit the diagnostic criteria for ADHD. INTERVENTIONS: AD-FX capsules were taken twice a day on an empty stomach for 4 weeks. Patients were instructed not to change any other medications during the study. OUTCOME MEASURES: At the beginning of the study, after 2 weeks, and then at the end of the 4-week trial, parents completed the Conners' Parent Rating Scale--revised, long version, a questionnaire that assesses a broad range of problem behaviours (and was used as an indication of ADHD symptom severity). RESULTS: After 2 weeks of treatment, the proportion of the subjects exhibiting improvement (i.e., decrease in T-score of at least 5 points) ranged from 31% for the anxious-shy attribute to 67% for the psychosomatic attribute. After 4 weeks of treatment, the proportion of subjects exhibiting improvement ranged from 44% for the social problems attribute to 74% for the Conners' ADHD index and the DSM-IV hyperactive-impulsive attribute. Five (14%) of 36 subjects reported adverse events, only 2 of which were considered related to the study medication. CONCLUSIONS: These preliminary results suggest AD-FX treatment may improve symptoms of ADHD and should encourage further research on the use of ginseng and Ginkgo biloba extracts to treat ADHD symptoms.


Assuntos
Transtorno do Deficit de Atenção com Hiperatividade/tratamento farmacológico , Ginkgo biloba , Panax , Extratos Vegetais/uso terapêutico , Plantas Medicinais , Adolescente , Transtorno do Deficit de Atenção com Hiperatividade/diagnóstico , Transtorno do Deficit de Atenção com Hiperatividade/psicologia , Criança , Pré-Escolar , Combinação de Medicamentos , Feminino , Humanos , Masculino , Projetos Piloto , Resultado do Tratamento
13.
Acta Pharmacol Sin ; 21(12): 1145-52, 2000 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-11603291

RESUMO

AIM: To determine the concentrations of chemical characteristic to extracts of leaves and flowers of Hypericum perforatum (St John's wort) in a number of selected samples and, following chemical characterization, to investigate the effects of these extracts on several pharmacological properties including effects of the extracts on inhibition of 5-hydroxytryptamine (5-HT) uptake and on antioxidant properties. METHODS: The samples were analyzed for the presence of characteristic chemicals by high performance liquid chromatography (HPLC) directly coupled to ultraviolet wavelength absorbance and positive or negative mode electrospray mass spectrometric detection. The effects of extracts on 5-HT uptake were determined by quantifying 3H-5-HT incorporation into rat hippocampal prisms. Estimates of effects of extracts on free radical scavenging capacity were made using a dynamic assay based on the ability of compounds to prevent the initiation of a colored reaction produced by the horseradish peroxidase catalyzed formation of hydroxyl free radicals from hydrogen peroxide using 2',2'-azinobis (3-ethylbenzthiazoline-6-sulfonic acid) as the color indicator. RESULTS: The chemical profile of a number of extracts were determined and found to differ substantially from each other. Inhibition of 5-HT uptake was found to correlate with hyperforin content and free radical scavenging capacity was found to correlate with the content of several flavonoids including quercetin and hyperoside. CONCLUSION: Standardized extracts of H perforatum varied substantially in the concentration of several characteristic chemicals. The correlation between pharmacological activity and certain characteristic chemicals found in these extracts indicates that the medicinal benefit derived from selected extracts will vary considerably depending on their chemical composition.


Assuntos
Hypericum/química , Perileno/análogos & derivados , Quercetina/análogos & derivados , Quercetina/farmacologia , Terpenos/farmacologia , Animais , Antracenos , Antioxidantes/farmacologia , Compostos Bicíclicos com Pontes , Sequestradores de Radicais Livres/farmacologia , Hipocampo/metabolismo , Masculino , Perileno/isolamento & purificação , Perileno/farmacologia , Floroglucinol/análogos & derivados , Quercetina/isolamento & purificação , Ratos , Ratos Sprague-Dawley , Inibidores Seletivos de Recaptação de Serotonina/farmacologia , Terpenos/isolamento & purificação
14.
J Psychiatry Neurosci ; 24(5): 442-52, 1999 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-10586535

RESUMO

OBJECTIVE: To determine if HT-1001, an extract of American ginseng, affects scopolamine-induced memory and performance deficits in a spatial learning task, alters brain concentrations of aminergic neurotransmitters, and alters choline uptake in synaptosome preparations. DESIGN: Animal study. ANIMALS: 48 Sprague Dawley rats. INTERVENTIONS: Long-term oral administration of a test material or control solution. Intraperitoneal administration of scopolamine (2 mg/kg) 30 minutes before testing. OUTCOME MEASURES: Performance on Morris water maze task, choline uptake, aminergic neurotransmitter analysis, in vitro monoamine oxidase analysis (of compounds). RESULTS: HT-1001 protected against scopolamine-induced amnesia and increased choline uptake in synaptosomal preparations. HT-1001 did not alter brain concentrations of norepinephrine, dopamine, 5-HT (serotonin), 3,4-dihydroxyphenylacetic acid or 5-hydroxyindoleactic acid. HT-1001 had a very weak ability to inhibit monoamine oxidase activity in vitro. CONCLUSIONS: HT-1001 demonstrates a capacity to protect against scopolamine-induced memory deficits.


Assuntos
Fármacos do Sistema Nervoso Central/farmacologia , Aprendizagem em Labirinto/efeitos dos fármacos , Rememoração Mental/efeitos dos fármacos , Orientação/efeitos dos fármacos , Panax , Plantas Medicinais , Saponinas/farmacologia , Escopolamina/toxicidade , Animais , Ginsenosídeos , Masculino , Ratos , Ratos Sprague-Dawley
15.
Bioorg Med Chem Lett ; 11(20): 2715-7, 2001 Oct 22.
Artigo em Inglês | MEDLINE | ID: mdl-11591508

RESUMO

A series of N(1)- and N(2)-propargylphenelzine derivatives and analogues (1-7) was synthesized. In addition to their activity as monoamine oxidase inhibitors, two of the compounds, N(1)- and N(2)-propargylphenelzines (3 and 6), were found to be potent at preventing DSP-4-induced noradrenaline (NA) depletion in mouse hippocampus, suggesting that they have neuroprotective properties.


Assuntos
Fármacos Neuroprotetores/síntese química , Fenelzina/síntese química , Animais , Hipocampo/efeitos dos fármacos , Hipocampo/metabolismo , Camundongos , Inibidores da Monoaminoxidase/síntese química , Inibidores da Monoaminoxidase/química , Fármacos Neuroprotetores/química , Norepinefrina/metabolismo , Fenelzina/análogos & derivados , Fenelzina/química , Fenelzina/farmacologia
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