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1,3,4-Thiadiazole and 1,2,4-triazole-3(4 H )-thione bearing salicylate moiety: synthesis and evaluation as anti- Candida albicans BJPS
Radwan,Awwad Abdoh; Alanazi,Fares Kaed; Al-Agamy,Mohammed Hamed.
Abstract Dramatically increased occurrence of both superficial and invasive fungal infections has been observed. Candida albicans appear to be the main etiological agent of invasive fungal infections. The anti-C. albicans activity of thiosemicarbazide, 1,3,4-Thiadiazole, and 1,2,4-triazole-3(4H)-thione compounds (compounds 3-23) were investigated. The MIC values of thiadiazole and triazole derivatives 10-23 were in the range of 0.08-0.17 µmol mL-1, while that of fluconazole was 0.052 µmol mL-1. Compound 11 (5-(2-(4-chlorobenzyloxy)phenyl)-N-allyl-1,3,4-thiadiazol-2-amine) and compound 18 (5-(2-(4-chlorobenzyloxy)phenyl)-4-allyl-2H-1,2,4-triazole-3(4H)-thione) were found to be the most active compounds, with MIC values of 0.08 µmol mL-1. The newly...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Anti-Candida/docking studies; Thiadiazole; Triazole.
Ano: 2017 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000100614
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13C NMR spectral data and molecular descriptors to predict the antioxidant activity of flavonoids BJPS
Scotti,Luciana; Fernandes,Mariane Balerine; Muramatsu,Eric; Emereciano,Vicente de Paula; Tavares,Josean Fechine; Silva,Marcelo Sobral da; Scotti,Marcus Tullius.
Tissue damage due to oxidative stress is directly linked to development of many, if not all, human morbidity factors and chronic diseases. In this context, the search for dietary natural occurring molecules with antioxidant activity, such as flavonoids, has become essential. In this study, we investigated a set of 41 flavonoids (23 flavones and 18 flavonols) analyzing their structures and biological antioxidant activity. The experimental data were submitted to a QSAR (quantitative structure-activity relationships) study. NMR 13C data were used to perform a Kohonen self-organizing map study, analyzing the weight that each carbon has in the activity. Additionally, we performed MLR (multilinear regression) using GA (genetic algorithms) and molecular...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Flavonoids/antioxidant activity; 13C NMR; Kohonen self-organizing map.
Ano: 2011 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502011000200005
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2-Phenitidine derivatives as suitable inhibitors of butyrylcholinesterase BJPS
Abbasi,Muhammad Athar; Aziz-ur-Rehman,; Qureshi,Muhammad Zahid; Khan,Farhan Mehmood; Khan,Khalid Mohmmed; Ashraf,Muhammad; Afzal,Iftikhar.
This manuscript reports the synthesis of a series of N-substituted derivatives of 2-phenitidine. First, the reaction of 2-phenitidine (1) with benzene sulfonyl chloride (2) yielded N-(2-ethoxyphenyl) benzenesulfonamide (3), which further on treatment with sodium hydride and alkyl halides (4a-g) furnished into new sulfonamides (5a-g). Second, the phenitidine reacted with benzoyl chloride (6) and acetyl chloride (8) to yield the reported N-benzoyl phenitidine (7) and N-acetyl phenitidine (9), respectively. These derivatives were characterized by infrared spectroscopy, ¹H-NMR, and EI-MS, and then screened against acetylcholinesterase, butylcholinesterase, and lipoxygenase enzyme, and were found to be potent inhibitors of butyrylcholinesterase alone.
Tipo: Info:eu-repo/semantics/article Palavras-chave: 2-Phenitidine/inhibitor activity; Sulfonamides; Acetamide; Benzamide; Butyrylcholinesterase.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502013000100014
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4-Nerolidylcatechol induces autophagy in human glioblastoma cells BJPS
Massaro,Renato Ramos; Brohem,Carla Abdo; Almeida,Rebeca Leite de; Rivelli,Diogo Pineda; Miyake,Juliano Andreoli; Colquhoun,Alison; Barros,Silvia Berlanga de Moraes; Maria-Engler,Silvya Stuchi.
ABSTRACT Gliomas account for the majority of primary malignant brain tumors and present invasive behavior into adjacent healthy tissue. While 4-NC had previously shown to induce apoptotic cell death in a melanoma model, for the glioma model described in this paper 4-NC is cytotoxic for the cells with the induction of the autophagic pathway. Trypan blue exclusion assay showed that 4-NC was cytotoxic in a dose-dependent manner for A172 and T98G cell lines. IC10 and IC50 values were at 32 µM and 41 µM for A172 and T98G respectively. Inhibition of cell proliferation was observed by total cell counts and by cell cycle analysis by flow cytometry, with cell cycle arrest of A172 and T98G cell lines respectively in the G1/G0 and S phases of the cell cycle. 4-NC...
Tipo: Info:eu-repo/semantics/article Palavras-chave: 4-Nerolidylcatechol; Glioblastoma; Cytotoxicity; Autophagy.
Ano: 2017 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000300618
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6 weeks consumption of pure fresh coconut milk caused up-regulation of eNOS and CSE protein expression in middle-aged male rats BJPS
Jansakul,Chaweewan; Naphatthalung,Jomkarn; Pradab,Sakda; Yorsin,Somruedee; Kanokwiroon,Kanyanatt.
Coconut milk (CCM) has been an important cooking ingredient in the Asia-Pacific region since ancient time. Due to its high content of saturated fatty acids, it has been considered atherogenic. We have tested if chronic consumption of fresh coconut milk by middle-aged male rat affects vascular function, plasma glucose and lipid profiles. Compared to control, CCM caused lower maximal contraction to phenylephrine of thoracic aortic rings and increased relaxation to acetylcholine that was abolished by N G-nitro-L-arginine (L-NA) or disruption of the endothelium. DL-propargylglycine caused slight increase in baseline tension of L-NA treated aortic rings of CCM-treated rats and produced higher contractile response of the aortic rings to low concentrations of...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Coconut milk; NO. H2S; Plasma glucose; Thoracic aorta.
Ano: 2018 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502018000300608
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70 years of development of Pharmaceutical Sciences: a lot to celebrate! BJPS
Aranha,Leila Rangel de Carvalho.
Tipo: Info:eu-repo/semantics/other
Ano: 2009 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502009000200001
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8-Propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one: A new coumarin with monoamine oxidase B inhibitory activity and possible anti-parkinsonian effects BJPS
Olaya,María del Pilar; Vergel,Nadezdha Esperanza; López,Jose Luis; Viña,Dolores; Guerrero,Mario Francisco.
Parkinson’s disease is a common neurodegenerative disorder. In this study, the monoamine oxidase inhibitory activity and potential anti-parkinsonian effects of 8-propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one (FCS303), a new synthetic coumarin, were evaluated. To do this, we used the reserpine model of Parkinson’s disease, an assay of levodopa/carbidopa potentiation, the catalepsy model of haloperidol, and an in vitro assay against monoamine oxidase (MAO) activity. Additionally, lipid peroxidation and protein carbonyl group quantification was performed in mice brain homogenates previously treated with haloperidol. FCS303 inhibited monoamine oxidase B (MAO-B) with an IC50 of 5.46 ± 0.36 µM; however, there was no effect on monoamine oxidase A (MAO-A). The oral...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Parkinson’s disease; Monoamine oxidase B; Coumarin; Mice; Reserpine; Levodopa; Carbidopa.
Ano: 2020 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100508
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A 2D-QSPR approach to predict blood-brain barrier penetration of drugs acting on the central nervous system BJPS
Sá,Matheus Malta de; Pasqualoto,Kerly Fernanda Mesquita; Rangel-Yagui,Carlota de Oliveira.
Drugs acting on the central nervous system (CNS) have to cross the blood-brain barrier (BBB) in order to perform their pharmacological actions. Passive BBB diffusion can be partially expressed by the blood/brain partition coefficient (logBB). As the experimental evaluation of logBB is time and cost consuming, theoretical methods such as quantitative structure-property relationships (QSPR) can be useful to predict logBB values. In this study, a 2D-QSPR approach was applied to a set of 28 drugs acting on the CNS, using the logBB property as biological data. The best QSPR model [n = 21, r = 0.94 (r² = 0.88), s = 0.28, and Q² = 0.82] presented three molecular descriptors: calculated n-octanol/water partition coefficient (ClogP), polar surface area (PSA), and...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Two-dimensional quantitative structure-property relationships (2D-QSPR); Calculated n-octanol/water partition coefficient (ClogP); Blood-brain barrier; Benzodiazepines.
Ano: 2010 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502010000400016
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A colleague, a friend, a fellow in the journeys: in honor of Professor Durval Mazzei Nogueira BJPS
Barbério,José Carlos.
Tipo: Info:eu-repo/semantics/other
Ano: 2011 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502011000100001
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A comparative study of two separate analytical techniques for the simultaneous determination of diclofenac sodium and diacerein from combined dosage form BJPS
Mallick,Sanhita Basu; Chattopadhyay,Helen; De,Amit Kumar; Datta,Sriparna.
ABSTRACT Diclofenac sodium (DS) and diacerein (DC) have emerged as a potential combination therapy for the treatment of knee osteoarthritis. Therefore a validated analytical method is essential for the simultaneous estimation of both from combined dosage form. A ratio derivative spectrophotometric and a chromatographic technique have been developed for the simultaneous determination of DS and DC. The quantification was done at 263.00 nm for DC and 304.50 nm for DS in the first method, whereas 257 nm for DC and at 274 nm for DS for LC-DAD analysis in chromatographic method using acetate buffer and methanol as the mobile phase at a flow-rate 0.50 mL/min. Both of these methods are found to be linear in the concentration range under study with r2 value 0.999...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Diacerein/comparative study; Diclofenac sodium/comparative study; High Pressure Liquid Chromatography; LC-DAD; Ratio derivative spectroscopy/validation.
Ano: 2017 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000200601
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A critical analysis of the hepatotoxicity cases described in the literature related to Herbalife (r) products BJPS
Zambrone,Flávio Ailton Duque; Corrêa,Cristiana Leslie; Amaral,Ligia Mesquita Sampaio do.
Abstract The aim of this study was to assess the hepatotoxicity cases described in the literature, attributed to the consumption of Herbalife(r) products, and to determine whether a causal relationship exists between the reported cases of liver injury and the use of these products. A literature search was performed on the PubMed, LILACS and PAHO databases. Seven publications reporting a total of 53 cases of hepatotoxicity linked to the use of Herbalife(r) products were retrieved. All of the studies lacked sufficient information to some degree, whether related to patients' history, concomitant use of medication and/or other compounds (including alcohol), observations on interrupted use (dechallenge), results found with markers, viral serology and...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Hepatotoxicity; Herbalife(r); Herbalife products(r)/consumption/hepatotoxicity; Dietary supplements; Causality assessment.
Ano: 2015 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502015000400785
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A fully validated microbiological assay for daptomycin injection and comparison to HPLC method BJPS
Christ,Ana Paula; Machado,Mariana Souto; Ribas,Karla Giacomelli; Schwarzbold,Alexandre Vargas; Silva,Cristiane de Bona da; Adams,Andréa Inês Horn.
abstract Daptomycin (DPT) was the first lipopeptide antibiotic available for commercialization. It is active against gram-positive bacteria, including resistant strains. This work aimed to develop and validate a turbidimetric microbiologic assay to determine daptomycin in an injectable form. A 3x3 design was employed, at concentrations of 1, 2 and 4.0 µg/mL. The microorganism test used was Staphylococcus aureus ATCC 6538p, and Antibiotic Medium 3 was used as the culture medium. Method validation demonstrated that the bioassay was linear (r=0.9995), precise (RSD=2.58%), accurate (recovery 100.48± 2.11%), and robust. Degradation kinetics was also performed in an alkaline medium, indicating that daptomycin degradation follows first order kinetics under these...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Daptomycin/determination; Daptomycin injection/quality control; Turbidimetric microbiological assay/quantitative analysis..
Ano: 2015 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502015000400775
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A fully validated microbiological assay to evaluate the potency of ceftriaxone sodium BJPS
Manfio,Maria Luisa; Agarrayua,Danielle Araújo; Machado,Jaison Carlosso; Schmidt,Cleber Alberto.
Ceftriaxone (CFTX) sodium is a third-generation, broad-spectrum cephalosporin that is resistant to beta-lactamases. An alternative bioassay for the assessment of the potency of this drug in pharmaceutical formulations has not been previously reported. Thus, this paper reports the development and full validation of a 3 x 3 agar diffusion bioassay using a cylinder-plate method to quantify CFTX sodium in pharmaceutical samples. The strain Staphylococcus aureus ATCC 6538P was used as the test microorganism, and the results of the proposed bioassay displayed high linearity, precision, accuracy, specificity and robustness. All potency results were statistically analyzed using an analysis of variance (ANOVA) and were found to be linear (r=0.99999) in the range of...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Ceftriaxone/agar diffusion assay; Ceftriaxone/quality control; Ceftriaxone/microbiological assay; Drugs/quality control.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502013000400015
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A green approach for the quantification of daptomycin in pharmaceutical formulation by UV spectrophotometry BJPS
Tótoli,Eliane Gandolpho; Salgado,Hérida Regina Nunes.
abstract Daptomycin is the first approved drug from a new class of antimicrobials, the cyclic lipopeptides, and is a very important antimicrobial agent in current clinical practice. Currently, there are no "green" analytical methods described in the literature to analyze the typical pharmaceutical dosage form of daptomycin. Thus, the aim of this work was to validate an environment-friendly spectrophotometric method in the UV region, for the analysis of daptomycin as a lyophilized powder. Water was used as diluent and the analyses were carried out on a spectrophotometer at 221 nm. The method met all validation requirements of the ICH guidelines, over a concentration range of 6-21 µg mL-1. A Student's t-test demonstrated that the proposed method was...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Antimicrobials/quality control; Daptomycin/determination; Spectrophotometry/UV region/quantitative analysis; Spectrophotometry/green analytical method.
Ano: 2015 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502015000400811
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A model for drug dispensing service based on the care process in the Brazilian health system BJPS
Soares,Luciano; Diehl,Eliana Elisabeth; Leite,Silvana Nair; Farias,Mareni Rocha.
Access to medication emphasizes the availability of the product at the expense of providing a service. The goal of this paper is to propose a theoretical model for a drug dispensing service, beginning with a reflection on the current realities of the Unified Health System and drug dispensation in Brazil. A conceptual analytical research made by a methodological course called disciplined imagination was mainly the approach applied to develop the model. The drug dispensing service is part of the care process, which considers access as an attribute; reception, connection and accountability, management, and clinical pharmaceutical aspects as components; and the rational use of drugs as the purpose. The proposed model addresses access to the dispensing service...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Drugs/dispensing practice; Pharmaceutical service; Unified health system; Health services/access.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502013000100012
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A new methodology for polyvalent intravenous immunoglobulin solution production with a two-stage process of viral inactivation BJPS
Lucena,Antônio Edson de Souza; Sampaio,Divaldo de Almeida; Silva,Ednaldo Rosas da; Paiva,Virgínia Florêncio de; Santiago,Ana Cláudia; Leite,Ana Cristina Lima.
Highly purified intravenous immunoglobulin G concentrate (IV IgG) was produced with the use of polyethylene glycol associated to a single-stage precipitation by ethanol, instead of the classic Cohn-Oncley process, which employs cold alcohol as the precipitating agent, in a three-stage process. Precipitation of crude fraction containing more than 95% of immunoglobulin G was performed by liquid chromatography with a cation exchanger, CM-Sepharose, as a stationary phase. During the process, the product was subjected to two-stage viral inactivation. The first stage was performed by the action of sodium caprylate, 30 mM at pH 5.1+/- 0.1, and the second stage was performed by the action of a solvent-detergent mixture. The finished product was formulated at 5%...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Blood derivatives; Immunoglobulins; Polyethylene glycol; Ultrafiltration; Ion exchange chromatography.
Ano: 2010 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502010000400020
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A novel 96-microwell-based high-throughput spectrophotometric assay for pharmaceutical quality control of crizotinib, a novel potent drug for the treatment of non-small cell lung cancer BJPS
Wani,Tanveer Ahmed; Darwish,Ibrahim Ali.
Tipo: Info:eu-repo/semantics/article Palavras-chave: Crizotinib/capsules/quality control 1; 2-Naphthoquinone-4-sulphonate Spectrophotometry/quality control of medicines.
Ano: 2015 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502015000200439
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A novel approach in mucoadhesive drug delivery system to improve zidovudine intestinal permeability BJPS
Pedreiro,Liliane Neves; Cury,Beatriz Stringhetti Ferreira; Chaud,Marco Vinícius; Gremião,Maria Palmira Daflon.
ABSTRACT Zidovudine (AZT) mucoadhesive solid dispersions (SD) were prepared using a sodium starch glycolate (SSG) and hypromellose phthalate (HPMCP) mixtures as carrier to enhance the intestinal permeability and bioavailability of zidovudine. SDs were prepared using the co-precipitation method followed by solvent evaporation and characterized according to their physicochemical properties such as particle size, crystallinity, thermal behavior, and liquid uptake ability. In vitro drug dissolution, mucoadhesiveness and AZT intestinal permeability were also determined. Thermal behavior and X-ray diffraction patterns demonstrated the amorphous state of AZT in SD systems. The HPMCP polymer restricted the liquid uptake ability in the acid medium; however, this...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Zidovudine; Solid dispersion; Mucoadhesion; P-glycoprotein; Intestinal permeability..
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000400715
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A novel dosage form for buccal administration of bupropion BJPS
Almeida,Nilsa Maria Galvão; Lima,Renata; Alves,Thaís Francine Ribeiro; Rebelo,Márcia de Araújo; Severino,Patrícia; Chaud,Marco Vinícius.
Bupropion is an antidepressant used in the treatment of smoking. The purpose of this study was to prepare controlled-release hydrogel films for buccal administration of bupropion and investigate its physicochemical and cytotoxic properties. The films were prepared from ultrapure sodium carboxymethylcellulose, hydroxypropylmethylcellulose K4M, and medium-viscosity chitosan. Evaluation of film physicochemical characteristics was based on scanning electron microscopy, bupropion content, mechanical strength (burst strength, relaxation, resilience, and traction), and cytotoxicity. Bupropion content in bilayer films was 121 mg per 9 cm2. The presence of bupropion modified film mechanical strength, but did not compromise the use of this pharmaceutical form. As...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Bupropion/buccal administration; Bilayer films/drugs rellease; Drugs/controlled-release; Tobacco/control.
Ano: 2015 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502015000100091
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A novel effect of geraniin on OPG/RANKL signaling in osteoblasts BJPS
Zhang,Xiaochao; Yang,Renhua; Long,Jiang; He,Bo; Zhang,Yue; Fu,Ting; Shen,Zhiqiang; Chen,Peng.
In this study, the effects of geraniin on osteoprotegerin/receptor activator of nuclear factor-κB ligand(OPG/RANKL) in regulating the proliferation of osteoblasts and suppression of osteoclast-like cells (OLC) in OLC-osteoblast co-cultured system in vitro were investigated. Osteoblasts were cultured and identified with alkaline phosphatase (ALP), gomori stain, and mineralized nodule stain. OLCs were isolated from long bones of Sprague-Dawley (SD) rats and identified with tartrate-resistant acid phosphatase(TRAP) stain. Methyl thiazolyl tetrazolium assay was used to examine the proliferation of osteoblasts, and immunocytochemistry and in situ hybridization to analyze the expression OPG/RANKL in osteoblasts co-cultured with osteoclasts under the action of...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Geraniin/effect; Osteoblasts; Osteoprotegerin; Receptor activator of nuclear factor -κ B ligand..
Ano: 2018 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502018000300618
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