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1.
Eur Rev Med Pharmacol Sci ; 26(8): 3038-3045, 2022 04.
Artigo em Inglês | MEDLINE | ID: mdl-35503606

RESUMO

OBJECTIVE: Post-COVID-19 syndrome appears to be a multi-organ illness with a broad spectrum of manifestations, occurring after even mild acute illness. Limited data currently available has suggested that vitamin D deficiency may play a role in COVID-19 cases. However, to our knowledge, no study has examined the frequency of vitamin D deficiency in post-COVID-19 cases and its effect on the symptom severity. The aim of this study is to both screen the frequency of vitamin D deficiency in post-COVID-19 syndrome patients and to study its relation to persistent symptoms. PATIENTS AND METHODS: A cross-sectional, single-center study was conducted involving all cases attending post-COVID-19 follow-up clinic from November 2020 to May 2021. Complete history, clinical examination, and laboratory analysis [kidney functions, serum calcium, C-reactive protein, serum ferritin, Serum 25-(OH) vitamin D] was done as well as HRCT chest. RESULTS: The study included 219 post-COVID-19 cases, 84% had deficient vitamin D levels (< 20 ng/dL); 11.4% had insufficient level (20-30 ng/dL) and only 4.9 % reported normal level. There was no link between levels of vitamin D with either the acute or post-COVID-19 symptoms in the studied groups. CONCLUSIONS: Despite the prevalence of vitamin D deficiency among the study population, no association was observed between the levels of vitamin D and post-COVID-19 symptoms. It appears that post-COVID-19 syndrome pathophysiology involves a more complex interaction with the immune system. Dedicated clinical trials are advised to better study vitamin D levels and the related disease severity in COVID-19 patients.


Assuntos
COVID-19 , Deficiência de Vitamina D , COVID-19/complicações , COVID-19/epidemiologia , Estudos Transversais , Seguimentos , Humanos , Prevalência , SARS-CoV-2 , Vitamina D , Vitaminas , Síndrome de COVID-19 Pós-Aguda
2.
Radiat Environ Biophys ; 59(1): 131-144, 2020 03.
Artigo em Inglês | MEDLINE | ID: mdl-31734721

RESUMO

Biological dosimetry based on sulfhemoglobin (SHb), methemoglobin (MetHb), and carboxyhemoglobin (HbCO) levels was evaluated. SHb, MetHb and HbCO levels were estimated in erythrocytes of mice irradiated by γ rays from a 60Co source using the method of multi-component spectrophotometric analysis developed recently. In this method, absorption measurements of diluted aqueous Hb-solution were made at λ = 500, 569, 577 and 620 nm, and using the mathematical formulas based on multi-component spectrophotometric analysis and the mathematical Gaussian elimination method for matrix calculation, the concentrations of various Hb-derivatives and total Hb in mice blood were estimated. The dose range of γ rays was from 0.5 to 8 Gy and the dose rate was 0.5 Gy min-1. Among all Hb-derivatives, MetHb, SHb and HbCO demonstrated an unambiguous dose-dependent response. For SHb and MetHb, the detection limits were about 0.5 Gy and 1 Gy, respectively. After irradiation, high levels of MetHb, SHb and HbCO persisted for at least 10 days, and the maximal increase of MetHb, SHb and HbCO occurred up to 24 h following γ irradiation. The use of this "MetHb + SHb + HbCO"-derivatives-based absorbed dose relationship showed a high accuracy. It is concluded that simultaneous determination of MetHb, SHb and HbCO, by multi-component spectrophotometry provides a quick, simple, sensitive, accurate, stable and inexpensive biological indicator for the early assessment of the absorbed dose in mice.


Assuntos
Carboxihemoglobina/análise , Raios gama , Dosimetria in Vivo/métodos , Metemoglobina/análise , Sulfa-Hemoglobina/análise , Animais , Biomarcadores/análise , Eritrócitos/metabolismo , Masculino , Camundongos , Irradiação Corporal Total
3.
Int J Biol Macromol ; 118(Pt B): 1614-1626, 2018 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-29990554

RESUMO

Polymer flooding in HPHT reservoirs using modified biopolymers and their composites acquire incremental attention nowadays. Some literature reported about limitations of native starch through enhanced oil recovery applications regarding bacterial degradation, thermal and ionic stability under severe reservoir environment. In the present study, functionalization of the starch biopolymer with thiol derivative then oxidation of thiol to sulfonic acid by environmentally friendly oxidants has been prepared and confirmed, after that starch derivative copolymerized with vinyl-containing monomers by free radical/redox emulsion polymerization in presence of silica seeds. Spectroscopic characterization and structure determination carried out by different spectroscopic techniques comprising FTIR, 1H NMR, while particles size measured through DLS and TEM, and thermal analysis determined by TGA analysis. Evaluation of the prepared composite as a novel enhanced oil recovery (EOR) candidate as well as the precursors conducted at simulated reservoir condition, where the oil recovery factor and water cut percentage calculated relevant to injected pore volume. The flooding data indicate that the prepared starch functionalized sulfonic acid co-imidazolium/silica composite is favorable for enhanced oil recovery applications as it can withstand high temperature and salinity conditions and the recovery factor reaches 39% of residual oil saturation.


Assuntos
Imidazóis/química , Petróleo , Dióxido de Silício/química , Amido/química , Ácidos Sulfônicos/química , Biopolímeros , Técnicas de Química Sintética , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Oxirredução , Polimerização , Reologia , Espectroscopia de Infravermelho com Transformada de Fourier , Amido/síntese química
4.
Eur J Pain ; 21(8): 1355-1365, 2017 09.
Artigo em Inglês | MEDLINE | ID: mdl-28440034

RESUMO

BACKGROUND: Postoperative pain control is an important factor in determining recovery in total knee arthroplasty (TKA).The aim of the study was to assess the efficacy of 4 sessions of transcranial direct current stimulation (tDCS) over primary motor cortex (M1) in patients undergoing unilateral TKA. MATERIALS: Fifty patients undergoing TKA were included in the study. They were divided randomly into two groups (25 patients for each, using closed envelopes): real tDCS (2 mA, 20 min, with anodal stimulation applied over M1 postoperative for 4 consecutive days) and sham tDCS. Opioid consumption was titrated by an anaesthesiologist during the study period and was used as primary outcome. As a secondary outcome, patients were evaluated using Visual Analogue Scale (VAS) and Leeds Assessment of Neuropathic Symptoms and Signs Pain Scale (LANSS) at baseline, then the 1st, 2nd, 3rd and 4th days after operation. RESULTS: There was no significant difference between real and sham tDCS in any rating scales at baseline. The opioid consumption and LANSS scores decreased more in patients who received real tDCS over the course of the treatment than sham tDCS. Real tDCS was associated with 59% reduction in the titrated analgesia. There was no significant difference between groups (time × groups interaction) in the VAS. CONCLUSION: Since the VAS was constant, repeated sessions of anodal tDCS over M1 with an extra-cephalic cathodal electrode can achieve the same degree of analgesia with less opioid consumption over the postoperative days after TKA. Thus, tDCS is a promising tool in the field of postoperative analgesia. SIGNIFICANCE: The data of the present study suggest that four sessions of transcranial direct current brain stimulation over motor cortex could reduce morphine consumption and pain perception during the postoperative period in total knee arthroplasty.


Assuntos
Analgésicos Opioides/uso terapêutico , Artroplastia do Joelho/efeitos adversos , Artropatias/cirurgia , Dor Pós-Operatória/terapia , Estimulação Transcraniana por Corrente Contínua , Adulto , Método Duplo-Cego , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Córtex Motor , Medição da Dor , Dor Pós-Operatória/etiologia
5.
Cell Mol Biol (Noisy-le-grand) ; 62(10): 7-15, 2016 Aug 31.
Artigo em Inglês | MEDLINE | ID: mdl-27609468

RESUMO

Antimicrobial resistance of methicillin-resistant Staphylococcus aureus (MRSA) poses a serious problem for clinicians worldwide. The present study attempted to evaluate the susceptibility patterns of MRSA to various antimicrobials and the prevalence of inducible clindamycin resistance as well as the relevant antibiotic and antiseptic resistance genes among these isolates. Totally, 40 MRSA isolates were recovered from examined milk and meat product samples (18.60%). Multi-drug resistance (MDR) was remarkably observed among 85% of these isolates. There was a good correlation between phenotypic determination of methicillin, amoxicillin/clavulinic acid and tetracycline resistances and PCR detections of mecA, blaZ and tet(K) genes, respectively, but norA gene was not detected in the four ciprofloxacin resistant isolates. Although, 55% of MRSA expressed resistance to benzalkonium chloride (BC), neither qacA/B nor smr gene was detected. Of 20 isolates exhibiting erythromycin- clindamycin discordant resistance pattern, 8 displayed positive double disk diffusion (D-zone) test denoting inducible macrolide-lincosamide-streptogramin B (MLSB) resistance phenotype with the inducibly expressed erm(A) and erm(C) genes in 87.5% of these isolates. Besides, the remaining 12 isolates showed MS phenotype (resistant to macrolides and type B streptogramins only) with a variety of erm(A), mph(C), msr(A) or a combination of these genes including erm(C). Finally, the constitutive MLSB phenotype with the constitutive expression of erm(A), erm(B) and erm(C) genes was comprised in 2 isolates with higher minimum inhibitory concentration (MIC) values for erythromycin (512 and 1024 µg/ml) and clindamycin (16 and 32 µg/ml). These findings suggested the importance of monitoring the evolution of MRSA resistance.


Assuntos
Farmacorresistência Bacteriana Múltipla , Produtos da Carne/microbiologia , Staphylococcus aureus Resistente à Meticilina/genética , Staphylococcus aureus Resistente à Meticilina/isolamento & purificação , Leite/microbiologia , Animais , Clindamicina/farmacologia , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Egito , Eritromicina/farmacologia , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Fenótipo
6.
J Postgrad Med ; 60(1): 69-71, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24625943

RESUMO

Xanthoma disseminatum (XD) is a rare, benign, non-Langerhans cell histiocytic disorder. The pathogenesis is not clear. It manifests with multiple, grouped, red-brown to yellow papules and nodules involving the skin, mucous membranes, and internal organs. We present a case of progressive XD in a 10-year-old male child. The patient presented with progressive, bilateral and symmetrical, reddish-brown, coalescent papules on the neck, around both eyes and all over his trunk and extremities. Skin lesions were accompanied by blurred vision and hoarseness of voice. Examination revealed xanthomatous infiltration of cornea, oral, pharyngeal, and laryngeal mucosae. The patient had diabetes insipidus that was diagnosed 2 years before the appearance of skin lesions. Medical treatment with corticosteroids (20 mg/day) and azathioprine (2 mg/kg/day) did not stop the disease progression.


Assuntos
Diabetes Insípido/complicações , Histiocitose de Células não Langerhans/patologia , Neoplasias Laríngeas/patologia , Dermatopatias/patologia , Antineoplásicos/uso terapêutico , Azatioprina/uso terapêutico , Biópsia , Criança , Diabetes Insípido/diagnóstico , Glucocorticoides/uso terapêutico , Histiocitose de Células não Langerhans/complicações , Histiocitose de Células não Langerhans/tratamento farmacológico , Humanos , Neoplasias Laríngeas/cirurgia , Laringoscopia , Masculino , Prednisolona/uso terapêutico , Pele/patologia , Dermatopatias/complicações , Dermatopatias/tratamento farmacológico , Resultado do Tratamento
7.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-672064

RESUMO

A rapid,sensitive and simple spectrofluorimetric method was developed for the estimation of atorvastatin.In this method,the native fluorescence characteristics of atorvastatin have been studied in both acidic and basic media.High sensitivity was obtained with 5% acetic acid at 389 nm using 276 nm for excitation.Regression analysis showed a good correlation coefficient (r=0.9995) between fluorescence intensity and concentration over the range of 1.5-4 μg/mL with detection limit of 0.012 μg/mL.The proposed method was successfully applied to the analysis of atorvastatin in pure and pharmaceutical dosage forms with average recovery of 100.29±0.47%.The results were compared favorably with those of the reported method.

8.
Andrologia ; 43(6): 387-91, 2011 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-21848911

RESUMO

This study aimed to assess seminal plasma fibronectin in fertile and infertile males. Ninety infertile males were investigated; asthenozoospermia (n = 27), asthenoteratozoospermia (n = 30), oligoasthenoteratozoospermia (n = 33) compared with 20 healthy fertile controls. They were subjected to semen analysis, seminal plasma fibronectin estimation by radial immune diffusion, serum testosterone (T) and follicle stimulating hormone (FSH) estimation by ELISA. There was significant increase of seminal plasma fibronectin among different infertile groups compared with the controls. Significant negative correlation was elicited between seminal fibronectin and sperm count, sperm motility grades A, B, A + B, sperm velocity, linear velocity, linearity index, sperm normal forms and serum T. Seminal fibronectin showed significant positive correlation with grade D sperm motility and serum FSH. ROC curve analysis discriminating controls and other infertile groups demonstrated criteria value of < 674 mg l(-1) (sensitivity 100% and specificity 96.4%). It is concluded that increased seminal fibronectin is associated with decreased sperm count and sperm motility.


Assuntos
Fertilidade , Fibronectinas/metabolismo , Infertilidade Masculina/metabolismo , Sêmen/metabolismo , Adulto , Estudos de Casos e Controles , Ensaio de Imunoadsorção Enzimática , Hormônio Foliculoestimulante/sangue , Humanos , Masculino , Curva ROC , Contagem de Espermatozoides , Testosterona/sangue
9.
Drug Discov Ther ; 4(2): 100-8, 2010 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22491167

RESUMO

The study aimed to combine two antidiabetic agents with different mechanisms of action, namely, metformin HCl and rosiglitazone maleate, in a tablet to improve glycemic control in patients with type II diabetes. The preformulation study started with development and validation of an HPLC method for the determination of both drugs in the mixture. The results of visual inspection, TLC, DSC, and FT-IR verified the absence of any physical or chemical interaction between both compounds. Four compatible excipients were selected for the formulation of the tablets by wet granulation according to a 2(2) factorial design. The prepared tablet blends were acceptable in terms of the modal size of particle distribution, bulk density, Hausner's ratio, Carr's index, and flowability. All formulations fulfilled the pharmacopoeial specifications for weight variation, content uniformity, friability, and hardness. They released 100% of the drug during the first 45 min, displaying higher dissolution efficiency than commercially available Rosiplus tablets. The tablet formulation that passed the physical and chemical stability study for 24 months at ambient conditions was tested in vivo on healthy volunteers in a cross-over design. Statistical analysis proved that the prepared tablets were bioequivalent to the commercial ones in terms of both the rate and the extent of absorption.


Assuntos
Diabetes Mellitus Tipo 2 , Espectroscopia de Infravermelho com Transformada de Fourier , Química Farmacêutica , Excipientes/química , Dureza , Humanos , Metformina , Solubilidade , Comprimidos
10.
Cochrane Database Syst Rev ; (4): CD005071, 2007 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-17943837

RESUMO

BACKGROUND: Male factor infertility accounts for 50% of all infertility. The treatment of idiopathic male infertility is empirical. Urinary, purified, and recombinant gonadotrophins have been used to improve sperm parameters in idiopathic male infertility with the goal of increasing pregnancy rates. Research addressing pregnancy rates in partners of men treated with gonadotrophins has had conflicting results and needs to be analysed. OBJECTIVES: To determine the effectiveness of gonadotrophin administration in men with idiopathic subfertility in improving spontaneous pregnancy rate and in assisted reproductive technique cycles. SEARCH STRATEGY: We searched the Cochrane Menstrual Disorders and Subfertility Group trials register (31 May 2007), the Cochrane Central Register of Controlled Trials (The Cochrane Library, issue 2, 2007), MEDLINE (1966 to May 2007), EMBASE and Biological Abstracts (1980 to Week 21 2007). Searches were not limited by language. The bibliographies of included, excluded trials and abstracts of major meetings were searched for additional trials. Authors and pharmaceutical companies were contacted for missing and unpublished data. SELECTION CRITERIA: Truly randomised controlled trials where gonadotrophins were administered for the treatment of idiopathic male subfertility with reporting of pregnancy rates were included in the review. DATA COLLECTION AND ANALYSIS: Two reviewers independently assessed trial quality and extracted data. Study authors were contacted for additional information. Adverse effects information was collected from the trials. We analysed data regarding pregnancy occurring within three months after gonadotrophin therapy. MAIN RESULTS: Four RCTs with 278 participants were included in the analysis. None of the studies had an adequate sample size and they had variable follow-up periods. None of the studies reported live birth or miscarriage rates. Compared to placebo or no treatment, gonadotrophins showed a significantly higher pregnancy rate per couple randomized within three months of completing therapy ( OR 4.17, 95% CI 1.30 to 7.09). AUTHORS' CONCLUSIONS: The number of trials and participants is insufficient to draw final conclusions. A large multicenter study with adequate power is needed.


Assuntos
Hormônio Foliculoestimulante/uso terapêutico , Infertilidade Masculina/tratamento farmacológico , Gonadotropinas/uso terapêutico , Humanos , Masculino , Oligospermia/tratamento farmacológico , Ensaios Clínicos Controlados Aleatórios como Assunto
11.
Cochrane Database Syst Rev ; (1): CD005071, 2006 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-16437514

RESUMO

BACKGROUND: Male factor infertility accounts for 50% of infertility. The treatment of idiopathic male infertility is empirical. Urinary, purified, and recombinant gonadotrophins have been used to improve sperm parameters in idiopathic male infertility with the goal of increasing pregnancy rates. Research addressing pregnancy rates in partners of men treated with gonadotrophins has had conflicting results and needs to be analysed. OBJECTIVES: To determine the effectiveness of gonadotrophin administration to men with idiopathic subfertility on spontaneous pregnancy rate and in assisted reproductive techniques (ARTs). SEARCH STRATEGY: We searched the Cochrane Menstrual Disorders and Subfertility Group trials register (19 November 2004), the Cochrane Central Register of Controlled Trials (The Cochrane Library, issue 4, 2004), MEDLINE (1966 to April 2005), EMBASE and Biological Abstracts (1980 to November 2004). Searches were not limited by language. The bibliographies of included, excluded trials and abstracts of major meetings were searched for additional trials. Authors and pharmaceutical companies were contacted for missing and unpublished data. SELECTION CRITERIA: Truly randomised controlled trials where gonadotrophins were administered for the treatment of idiopathic male subfertility with reporting of pregnancy rates were included in the review. DATA COLLECTION AND ANALYSIS: Two reviewers independently assessed trial quality and extracted data. Study authors were contacted for additional information. Adverse effects information was collected from the trials. We analysed data regarding pregnancy occurring within 3 months after gonadotrophin therapy. MAIN RESULTS: Four RCTs with 278 participant were included in the analysis. None of the studies had an adequate sample size and they had variable follow-up periods. None of the studies reported live birth or miscarriage rates. Compared to placebo or no treatment, gonadotrophins showed a significantly higher pregnancy rate per couple randomized within 3 months of completing therapy (OR 3.03, 95% CI 1.30 to 7.09). Pregnancy rate was 13.4% (19/142) in the gonadotrophin group and 4.4% (6/136) in the control group. AUTHORS' CONCLUSIONS: The number of trials and participants is insufficient to draw final conclusions. A large multicenter study with adequate power is needed.


Assuntos
Hormônio Foliculoestimulante/uso terapêutico , Infertilidade Masculina/tratamento farmacológico , Gonadotropinas/uso terapêutico , Humanos , Masculino , Oligospermia/tratamento farmacológico , Ensaios Clínicos Controlados Aleatórios como Assunto
12.
Nucleosides Nucleotides Nucleic Acids ; 19(4): 723-33, 2000 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-10960031

RESUMO

A novel synthesis of condensed bicyclic thiopyrimidine glycosides utilising 1H-cyclopentapyrimidine-2(3H)-thiones and alpha-bromoglucose or alpha-bromogalactose tetraacetate as starting components is described.


Assuntos
Ciclopentanos/síntese química , Nucleosídeos de Pirimidina/síntese química , Cromatografia em Camada Fina , Glicosídeos/síntese química , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Tionas/síntese química
13.
Toxicology ; 142(2): 79-86, 2000 Jan 03.
Artigo em Inglês | MEDLINE | ID: mdl-10685507

RESUMO

The purpose of the present study was to examine the effects of administration of sublethal doses of O,O-diethyl-O-p-nitrophenyl phosphorothioate (parathion) on serum epinephrine (EPI) and norepinephrine (NE), as well as on night-time rat pineal melatonin synthesis, both in the presence and absence of propranolol, a beta-adrenergic receptor antagonist. In the first experiment, two groups of adult albino rats were administered parathion orally (1.08 and 2.17 mg/kg/day; the total received by each animal was 6.5 and 13.0 mg/kg body weight over 6 days); another two groups received corn oil only. Animals were killed at 23:00 and 01:00 h by decapitation. Serum EPI was augmented at 01:00 h, but NE was increased at 01:00 and 23:00 h due to administration of the high dose of parathion (13 mg/kg). In the second experiment, two groups of adult male albino rats were administered parathion orally (13 mg/kg); another two groups received an intraperitoneal injection of propranolol (20 mg/kg body weight, 1 h before the lights were turned off). In addition, two groups were given a saline injection. Four hours after darkness onset, pineal N-acetyltransferase (NAT) activity as well as pineal and serum melatonin levels were measured. Parathion by itself significantly augmented nocturnal pineal NAT activity and serum melatonin levels in otherwise untreated rats; the insecticide was ineffective in reference to this enzyme when it was given in conjunction with the beta-adrenergic receptor antagonist propranolol. The augmentation of NAT activity by parathion also caused significant reduction in pineal serotonin (5-HT); again, this response was blocked by propranolol treatment. The results are consistent with the idea that parathion influences pineal 5-HT metabolism either at the level of the beta-adrenergic receptor or via the sympathetic innervation to the pineal gland.


Assuntos
Arilamina N-Acetiltransferase/metabolismo , Inseticidas/toxicidade , Paration/toxicidade , Glândula Pineal/efeitos dos fármacos , Receptores Adrenérgicos beta/fisiologia , Animais , Ritmo Circadiano , Masculino , Melatonina/biossíntese , Norepinefrina/sangue , Glândula Pineal/enzimologia , Ratos , Serotonina/metabolismo
15.
Nucleosides Nucleotides ; 18(10): 2307-15, 1999 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-10616732

RESUMO

N3-beta-D-glucopyranosyl, galactopyranosyl and xylopyranosyl 6-methyl-2-methylthiouracil and their 5-bromo derivatives have been synthesized by coupling an alpha-acetobromosugar with the corresponding thiouracil. The new modified thiouridine analogues were evaluated for their inhibitory activity against Human Immunodeficiency Virus (HIV) replication in MT-4 cells as well as for their cytotoxicity.


Assuntos
Fármacos Anti-HIV/síntese química , Antineoplásicos/síntese química , Metiltiouracila/síntese química , Nucleosídeos/síntese química , Animais , Fármacos Anti-HIV/química , Fármacos Anti-HIV/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular , HIV-1/efeitos dos fármacos , Metiltiouracila/análogos & derivados , Metiltiouracila/química , Metiltiouracila/farmacologia , Camundongos , Camundongos Nus , Transplante de Neoplasias , Nucleosídeos/química , Nucleosídeos/farmacologia , Replicação Viral/efeitos dos fármacos
16.
Nucleosides Nucleotides ; 17(5): 855-68, 1998 May.
Artigo em Inglês | MEDLINE | ID: mdl-9708328

RESUMO

Condensation of cyanothioacetamide or cyanoacetamide with sodium salts of 2-formyl-1-cycloalkanones afforded the corresponding cycloalkane ring fused pyridine-2(1H)-thiones and -2-pyridones. The latter compounds served as a key intermediates for the synthesis of a new class of cycloalkane ring fused pyridine glycosides.


Assuntos
Fármacos Anti-HIV/síntese química , Cicloparafinas/síntese química , Desenho de Fármacos , Piridinas/síntese química , Espectroscopia de Ressonância Magnética , Modelos Químicos
17.
Nucleosides Nucleotides ; 17(8): 1355-63, 1998 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-9672701

RESUMO

The synthesis of new 4- and 5-substituted-3-cyanopyridine nucleosides has been performed by reacting the silylated pyridines and penta-omicron-acetyl-alpha -D-glycopyranose in dichloroethane in the presence of SnCl4. The free nucleosides were tested for their potential activity against HIV and different types of tumor.


Assuntos
Piridinas/química , Pirimidinas/química , Pirimidinas/síntese química
19.
Biomed Environ Sci ; 8(1): 45-53, 1995 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-7605599

RESUMO

The purpose of the present study was to examine the effects of administration of sublethal doses of carbaryl on nighttime rat pineal melatonin synthesis in the presence and absence of propranolol, a beta-adrenergic receptor antagonist. Two groups of adult male albino rats were administered orally N-methyl-l-naphthylcarbamate (carbaryl) (8.33 mg/kg BW daily in corn oil) for six successive days; another two groups received corn oil only. On the last day of carbaryl treatment, half of the animals received an intraperitoneal injection of propranolol (20 mg/kg body weight, one hour before lights off). The other two groups were given a saline injection. Four hours after darkness onset, pineal N-acetyltransferase (NAT) and hydroxyindole-O-methyltransferase (HIOMT) activities as well as pineal concentrations of 5-hydroxytryptophan (5HTP), serotonin (5HT), 5-hydroxyindole acetic acid (5HIAA) and pineal and serum melatonin levels were measured. Nocturnal NAT activity was increased due to carbaryl administration but the pesticide was ineffective in stimulating NAT activity in rats treated with propranolol. Pineal 5HT was decreased due to carbaryl administration but 5HTP and 5HIAA levels were unaffected. Pineal and serum melatonin levels were decreased due to propranolol treatment. The results indicate that carbaryl may influence pineal NAT activity by a mechanism that involves beta-adrenergic neural transmission.


Assuntos
Arilamina N-Acetiltransferase/efeitos dos fármacos , Carbaril/antagonistas & inibidores , Ritmo Circadiano/efeitos dos fármacos , Glândula Pineal/enzimologia , Propranolol/farmacologia , Animais , Escuridão , Masculino , Ratos , Estimulação Química
20.
Toxicology ; 97(1-3): 183-9, 1995 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-7716784

RESUMO

Parathion, an organophosphorous insecticide, was previously shown to enhance the nighttime rise in pineal N-acetyltransferase (NAT) activity and serum melatonin levels. The purpose of the present study was to test whether parathion acts on the pineal gland by means of a beta-adrenergic receptor mechanism. Whereas parathion (total dose 6.5 mg/kg body wt over 6 days) by itself significantly augmented nocturnal pineal NAT activity and serum melatonin levels in otherwise untreated rats, the insecticide was ineffective in reference to this enzyme when it was given in conjunction with the beta-adrenergic receptor antagonist propranolol (20 mg/kg body wt, 1 h before lights off). The augmentation of NAT activity by parathion also caused significant reductions in pineal serotonin (5-HT); again, this response was blocked by propranolol treatment. Neither pineal hydroxyindole-O-methyltransferase (HIOMT) activity nor pineal levels of 5-hydroxytryptophan or hydroxyindole acetic acid (5-HIAA) were significantly changed as a result of either parathion or propranolol treatment. The results are consistent with the idea that parathion influences pineal 5-HT metabolism either at the level of the beta-adrenergic receptor or via the sympathetic innervation to the pineal gland.


Assuntos
Paration/toxicidade , Glândula Pineal/efeitos dos fármacos , Propranolol/farmacologia , Receptores Adrenérgicos beta/efeitos dos fármacos , Serotonina/metabolismo , Animais , Arilamina N-Acetiltransferase/metabolismo , Ritmo Circadiano , Masculino , Melatonina/sangue , Glândula Pineal/metabolismo , Ratos
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