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Detalles de la revista
Formato
Revista
eISSN
1846-9558
Publicado por primera vez
28 Feb 2007
Periodo de publicación
4 veces al año
Idiomas
Inglés

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Volumen 64 (2014): Edición 3 (September 2014)

Detalles de la revista
Formato
Revista
eISSN
1846-9558
Publicado por primera vez
28 Feb 2007
Periodo de publicación
4 veces al año
Idiomas
Inglés

Buscar

10 Artículos
Acceso abierto

Design, Synthesis and Pharmacological Screening of β-Amino-, Thiadiazole/Thiadiazine-Phosphonate Based Triazole Motifs as Antimicrobial/Cytotoxic Agents

Publicado en línea: 08 Oct 2014
Páginas: 267 - 284

Resumen

Abstract

Three different series of phosphonate derivatives, b-aminoand fused thiadiazolo/thiadiazine-phosphonates have been synthesized using the addition and/or addition-cyclization protocol of Horner-Wadsworth-Emmons (HWE) reagents to 1,2,4-triazole-3-thiols. The design of potentially antimicrobial and anticancer phosphor esters relied on the results of computer-assisted molecular modeling. All synthesized phosphonates were evaluated for their in vitro antimicrobial activities while anticancer properties were determined for eight out of twenty new phosphonates. The tested phosphonates, except for compounds that have a nitrile moiety, exhibited moderate to significant antimicrobial activity. Nevertheless, the most active compounds were fused thiadiazole-phosphonates, which inhibited the growth of both Gram-negative and Gram-positive bacteria better than b-aminophosphonates and fused thiadiazolophosphonates. In parallel, the antitumor activity screenings of selected phosphonates from each series and substrate 1 were also done. Their antitumor properties against ten carcinoma cell lines, including breast (MCF7, MDA-MB- 231/ ATCC, MDA-MB-435, BT-549), ovarian (IGROVI, OVCAR-3, SK-OV-3), prostate (PX-3, PU-145), and liver (HEPG2), were investigated. The results showed that all synthesized compounds reflected remarkable antitumor activity against breast (especially MDA-MB-231/ATCC and BT-549), and prostate carcinoma cell lines (PC-3 and DU-145), whereas a moderate to good effect on ovarian and liver cancer cells was observed.

Palabras clave

  • β-amino/thiadiazolo/thiadiazino-phosphonates
  • 1,2,4-triazole-3-thiols
  • Horner-Wadsworth-Emmons reagents
  • in vitro antimicrobial/antineoplastic activity
Acceso abierto

Design, Synthesis and Potential Anti-Proliferative Activity of Some Novel 4-Aminoquinoline Derivatives

Publicado en línea: 08 Oct 2014
Páginas: 285 - 297

Resumen

Abstract

Novel nineteen compounds based on a 4-aminoquinoline scaffold were designed and synthesized as potential antiproliferative agents. The new compounds were N-substituted at the 4-position by aryl or heteroaryl (1-9), quinolin- 3-yl (10), 2-methylquinolin-3-yl (11), thiazol-2-yl (12), and dapsone moieties (13, 14 and 18). Bis-compounds 15, 16 and 19 were also synthesized to assess their biological activity. All the newly synthesized comounds were tested for in vitro antiproliferative activity against the MCF-7 breast cancer cell line. Seventeen of the novel compounds showed higher activity than the reference drug doxorubicin. The corresponding 7-(trifluoromethyl)-N-(3,4,5-trimethoxyphenyl)quinolin-4- amine 1, N-(7-(trifluoromethyl)quinolin-4-yl)quinolin- 3- amine (10), 2-methyl-N-(7-trifluorome-thyl)quinolin-4-yl) quinolin-3-amine (11) and N-(4-(4-aminophenylsulfonyl) phenyl)-7-chloroquinolin-4-amine (13) were almost twice to thrice as potent as doxorubicin. Biological screening of the tested compounds could offer an encouraging framework in this field that may lead to the discovery of potent anticancer agents.

Palabras clave

  • 4-aminoquinolines
  • bis-compounds
  • dapsone
  • antiproliferative activity
Acceso abierto

Development of Novel Formulations to Enhance in Vivo Transdermal Permeation of Tocopherol

Publicado en línea: 08 Oct 2014
Páginas: 299 - 309

Resumen

Palabras clave

  • tocopherol
  • topical formulation
  • chemical analysis
  • ex vivo and in vivo
  • skin barrier
Acceso abierto

Antioxidative Activity and Inhibition of Key Enzymes Linked to Type-2 Diabetes (α-Glucosidase and α-Amylase) by Khaya Senegalensis

Publicado en línea: 08 Oct 2014
Páginas: 311 - 324

Resumen

Abstract

This study evaluated the in vitro antioxidative activity of Khaya senegalensis extracts and inhibitory effects of some solvent fractions on α-glucosidase and α-amylase activities. The stem bark, root and leaf samples of the plant were sequentially extracted with ethyl acetate, ethanol and water and then tested for antioxidative activity. Our findings revealed that the ethanolic extract of the root had the highest antioxidative activity. Solvent-solvent fractionation of the root ethanolic extract yielded a butanol fraction that showed higher antioxidative activity than other fractions. Furthermore, the butanol fraction had significantly higher (p < 0.05) α-glucosidase and α-amylase inhibitory activities with IC50 values of 2.89 ± 0.46 and 97.51 ± 5.72 μg mL-1, respectively. Enzyme kinetic studies indicated that the butanol fraction is a non-competitive inhibitor for α-glucosidase with an inhibition binding constant Ki of 1.30 μg mL-1 and a competitive inhibitor of α-amylase with a Ki of 7.50 μg mL-1. GC-MS analysis revealed that the butanol fraction contained two chromones, p-anilinophenol and 3-ethyl-5-(3- ethyl-(3H)-benzothiazol-2-ylidene)-2-(p-tolylvinylamino)- 4-thiazolidinone. Data obtained in the study suggest that the butanol fraction derived from the ethanolic extract of K. senegalensis root possessed excellent antioxidative as well as α-glucosidase and a-amylase inhibitory activities while chromones and/or p-anilinophenol could be the main bioactive compounds responsible for the observed activities.

Palabras clave

  • Khaya senegalensis (Meliaceae)
  • type-2 diabetes
  • α-glucosidase
  • α-amylase
  • oxidative stress
Acceso abierto

Analysis of Active Components in Salvia Miltiorrhiza Injection Based on Vascular Endothelial Cell Protection

Publicado en línea: 08 Oct 2014
Páginas: 325 - 334

Resumen

Abstract

Correlation analysis based on chromatograms and pharmacological activities is essential for understanding the effective components in complex herbal medicines. In this report, HPLC and measurement of antioxidant properties were used to describe the active ingredients of Salvia miltiorrhiza injection (SMI). HPLC results showed that tanshinol, protocatechuic aldehyde, rosmarinic acid, salvianolic acid B, protocatechuic acid and their metabolites in rat serum may contribute to the efficacy of SMI. Assessment of antioxidant properties indicated that differences in the composition of serum powder of SMI caused differences in vascular endothelial cell protection. When bivariate correlation was carried out it was found that salvianolic acid B, tanshinol and protocatechuic aldehyde were active components of SMI because they were correlated to antioxidant properties.

Palabras clave

  • Salvia miltiorrhiza injection
  • HPLC
  • antioxidant activity
  • correlation analysis
  • salvianolic acid
Acceso abierto

Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial Agents

Publicado en línea: 08 Oct 2014
Páginas: 335 - 344

Resumen

Abstract

A series of pyrazole derivatives 9-22 were designed and synthesized. All the newly synthesized compounds were assayed for their antimicrobial activity against the Grampositive bacteria Staphyllococcus aureus and Bacillius subtilis and the Gram-negative bacteria Escherichia coli, Pseudomonas aeruginosa, in addition to the fungi organisms, Candida albicans, C. parapsilosis and C. tropicalis. Ethyl 5-(2,5-dimethylthiophen- 3-yl)-1-phenyl-1H-pyrazole-3-carboxylate (21) (MICE.coli = 0.038 μmol mL-1, MICP. aerug. = 0.067 μmol mL-1) is nearly as active as ampicillin (MIC = 0.033 and 0.067 μmol mL-1), respectively. Ethyl 5-(4-bromo-2-chlorophenyl)- 1-phenyl-1H-pyrazole-3-carboxylate (16) (MIC = 0.015 μmol mL-1) is more active than fluconazole (0.020 μmol mL-1) as a reference drug against C. parapsilosis.

Palabras clave

  • pyrazole-3-carboxylates
  • antimicrobial activity
Acceso abierto

Rosuvastatin, Sildenafil and Their Combination in Monocrotaline-Induced Pulmonary Hypertension in Rat

Publicado en línea: 08 Oct 2014
Páginas: 345 - 353

Resumen

Abstract

There is considerable interest in the pleiotropic effects of statins and their potential role in the treatment of pulmonary hypertension. Previous experimental findings indicate that a combination of lipophilic statins with phosphodiesterase type-5 inhibitor, sildenafil, can offer preventive effects on rat monocrotaline-induced pulmonary hypertension. The present study is aimed to assess whether therapeutic regimen provides any benefits. Seven days after pulmonary hypertension induction, hydrophilic rosuvastatin and sildenafil were given for 14 days to male Wistar outbred rats. Right ventricular pressure, right ventricle mass and three biomarkers were evaluated after 21 days: brain natriuretic peptide, high-density lipoprotein cholesterol and vascular endothelial growth factor. The present study demonstrates that administration of hydrophilic statin with sildenafil results in reduction of pulmonary vascular remodeling and right ventricular pressure. The results of biochemical measurements may suggest that statins play a positive role in right ventricle function or the process of angiogenesis in pulmonary hypertension development.

Palabras clave

  • rosuvastatin
  • sildenafil
  • combination therapy
  • pulmonary hypertension
  • hemodynamic parameters
Acceso abierto

Influence of Process Parameters on Content Uniformity of a Low Dose Active Pharmaceutical Ingredient in a Tablet Formulation According to GMP

Publicado en línea: 08 Oct 2014
Páginas: 355 - 367

Resumen

Abstract

The article describes the development and production of tablets using direct compression of powder mixtures. The aim was to describe the impact of filler particle size and the time of lubricant addition during mixing on content uniformity according to the Good Manufacturing Practice (GMP) process validation requirements. Processes are regulated by complex directives, forcing the producers to validate, using sophisticated methods, the content uniformity of intermediates as well as final products. Cutting down of production time and material, shortening of analyses, and fast and reliable statistic evaluation of results can reduce the final price without affecting product quality. The manufacturing process of directly compressed tablets containing the low dose active pharmaceutical ingredient (API) warfarin, with content uniformity passing validation criteria, is used as a model example. Statistic methods have proved that the manufacturing process is reproducible. Methods suitable for elucidation of various properties of the final blend, e.g., measurement of electrostatic charge by Faraday pail and evaluation of mutual influences of researched variables by partial least square (PLS) regression, were used. Using these methods, it was proved that the filler with higher particle size increased the content uniformity of both blends and the ensuing tablets. Addition of the lubricant, magnesium stearate, during the blending process improved the content uniformity of blends containing the filler with larger particles. This seems to be caused by reduced sampling error due to the suppression of electrostatic charge.

Palabras clave

  • content uniformity
  • warfarin
  • validation
  • narrow therapeutic index
  • Faraday pail
  • PLS regression
Acceso abierto

Evaluation of the Antioxidant Activity of Coreopsis Tinctoria Nuff. and Optimisation of Isolation by Response Surface Methodology

Publicado en línea: 08 Oct 2014
Páginas: 369 - 378

Resumen

Abstract

The aim of the present study was to determine the antioxidant activity of Coreopsis tinctoria flowering tops (CTFT). Studies were conducted to obtain suitable extraction conditions for chlorogenic acid, quercetin, luteolin, apigenin and kaempferol, which were identified and quantified by HPLC. Response surface methodology was employed to optimise the ultrasound-assisted extraction conditions including extraction time, ethanol concentration and liquid-solid ratio. The antioxidant activity of the extracts was analysed using various antioxidant models, such as DPPH, ABTS and hydroxyl radical scavenging assay. CTFT extracted for 15.0 min with ethanol at a concentration of 60.4 % and with liquidsolid ratio 27.5:1 possessed a considerable amounts of total flavonoids and polyphenols (18.9 %). This extract showed higher scavenging activity of ABTS and hydroxyl radical activity than rutin, however not in the DPPH test. We may assume that CTFT possess antioxidant and free radical scavenging potentials.

Palabras clave

  • Coreopsis tinctoria (Asteraceae)
  • flavonoids
  • polyphenols
  • antioxidant activity
  • response surface methodology
  • HPLC
Acceso abierto

Potential of the Essential Oil from Pimenta Pseudocaryophyllus as an Antimicrobial Agent

Publicado en línea: 08 Oct 2014
Páginas: 379 - 385

Resumen

Abstract

This study evaluated the effectiveness of the essential oil of Pimenta pseudocaryophyllus in inhibiting the growth of the main bacteria responsible for bad perspiration odor (Staphylococcus epidermidis, Proteus hauseri, Micrococcus yunnanensis and Corynebacterium xerosis). The chemical profile of the essential oil was evaluated by high-resolution gas chromatography (HR-GC) and four constituents were identified, eugenol being the major component (88.6 %). The antimicrobial activity was evaluated by means of the turbidimetric method, using the microdilution assay. The minimum inhibitory concentration (MIC) values of the essential oil ranged from 500 to 1,000 μg mL-1. Scanning electron microscope (SEM) observations confirmed the physical damage and morphological alteration of the test bacteria treated with the essential oil, reference drugs and eugenol. The findings of the study demonstrated that this essential oil can be used in the formulation of personal care products.

Palabras clave

  • Pimenta pseudocaryophyllus (Myrtaceae)
  • essential oil
  • eugenol
  • antimicrobial activity
  • scanning electron microscopy
10 Artículos
Acceso abierto

Design, Synthesis and Pharmacological Screening of β-Amino-, Thiadiazole/Thiadiazine-Phosphonate Based Triazole Motifs as Antimicrobial/Cytotoxic Agents

Publicado en línea: 08 Oct 2014
Páginas: 267 - 284

Resumen

Abstract

Three different series of phosphonate derivatives, b-aminoand fused thiadiazolo/thiadiazine-phosphonates have been synthesized using the addition and/or addition-cyclization protocol of Horner-Wadsworth-Emmons (HWE) reagents to 1,2,4-triazole-3-thiols. The design of potentially antimicrobial and anticancer phosphor esters relied on the results of computer-assisted molecular modeling. All synthesized phosphonates were evaluated for their in vitro antimicrobial activities while anticancer properties were determined for eight out of twenty new phosphonates. The tested phosphonates, except for compounds that have a nitrile moiety, exhibited moderate to significant antimicrobial activity. Nevertheless, the most active compounds were fused thiadiazole-phosphonates, which inhibited the growth of both Gram-negative and Gram-positive bacteria better than b-aminophosphonates and fused thiadiazolophosphonates. In parallel, the antitumor activity screenings of selected phosphonates from each series and substrate 1 were also done. Their antitumor properties against ten carcinoma cell lines, including breast (MCF7, MDA-MB- 231/ ATCC, MDA-MB-435, BT-549), ovarian (IGROVI, OVCAR-3, SK-OV-3), prostate (PX-3, PU-145), and liver (HEPG2), were investigated. The results showed that all synthesized compounds reflected remarkable antitumor activity against breast (especially MDA-MB-231/ATCC and BT-549), and prostate carcinoma cell lines (PC-3 and DU-145), whereas a moderate to good effect on ovarian and liver cancer cells was observed.

Palabras clave

  • β-amino/thiadiazolo/thiadiazino-phosphonates
  • 1,2,4-triazole-3-thiols
  • Horner-Wadsworth-Emmons reagents
  • in vitro antimicrobial/antineoplastic activity
Acceso abierto

Design, Synthesis and Potential Anti-Proliferative Activity of Some Novel 4-Aminoquinoline Derivatives

Publicado en línea: 08 Oct 2014
Páginas: 285 - 297

Resumen

Abstract

Novel nineteen compounds based on a 4-aminoquinoline scaffold were designed and synthesized as potential antiproliferative agents. The new compounds were N-substituted at the 4-position by aryl or heteroaryl (1-9), quinolin- 3-yl (10), 2-methylquinolin-3-yl (11), thiazol-2-yl (12), and dapsone moieties (13, 14 and 18). Bis-compounds 15, 16 and 19 were also synthesized to assess their biological activity. All the newly synthesized comounds were tested for in vitro antiproliferative activity against the MCF-7 breast cancer cell line. Seventeen of the novel compounds showed higher activity than the reference drug doxorubicin. The corresponding 7-(trifluoromethyl)-N-(3,4,5-trimethoxyphenyl)quinolin-4- amine 1, N-(7-(trifluoromethyl)quinolin-4-yl)quinolin- 3- amine (10), 2-methyl-N-(7-trifluorome-thyl)quinolin-4-yl) quinolin-3-amine (11) and N-(4-(4-aminophenylsulfonyl) phenyl)-7-chloroquinolin-4-amine (13) were almost twice to thrice as potent as doxorubicin. Biological screening of the tested compounds could offer an encouraging framework in this field that may lead to the discovery of potent anticancer agents.

Palabras clave

  • 4-aminoquinolines
  • bis-compounds
  • dapsone
  • antiproliferative activity
Acceso abierto

Development of Novel Formulations to Enhance in Vivo Transdermal Permeation of Tocopherol

Publicado en línea: 08 Oct 2014
Páginas: 299 - 309

Resumen

Palabras clave

  • tocopherol
  • topical formulation
  • chemical analysis
  • ex vivo and in vivo
  • skin barrier
Acceso abierto

Antioxidative Activity and Inhibition of Key Enzymes Linked to Type-2 Diabetes (α-Glucosidase and α-Amylase) by Khaya Senegalensis

Publicado en línea: 08 Oct 2014
Páginas: 311 - 324

Resumen

Abstract

This study evaluated the in vitro antioxidative activity of Khaya senegalensis extracts and inhibitory effects of some solvent fractions on α-glucosidase and α-amylase activities. The stem bark, root and leaf samples of the plant were sequentially extracted with ethyl acetate, ethanol and water and then tested for antioxidative activity. Our findings revealed that the ethanolic extract of the root had the highest antioxidative activity. Solvent-solvent fractionation of the root ethanolic extract yielded a butanol fraction that showed higher antioxidative activity than other fractions. Furthermore, the butanol fraction had significantly higher (p < 0.05) α-glucosidase and α-amylase inhibitory activities with IC50 values of 2.89 ± 0.46 and 97.51 ± 5.72 μg mL-1, respectively. Enzyme kinetic studies indicated that the butanol fraction is a non-competitive inhibitor for α-glucosidase with an inhibition binding constant Ki of 1.30 μg mL-1 and a competitive inhibitor of α-amylase with a Ki of 7.50 μg mL-1. GC-MS analysis revealed that the butanol fraction contained two chromones, p-anilinophenol and 3-ethyl-5-(3- ethyl-(3H)-benzothiazol-2-ylidene)-2-(p-tolylvinylamino)- 4-thiazolidinone. Data obtained in the study suggest that the butanol fraction derived from the ethanolic extract of K. senegalensis root possessed excellent antioxidative as well as α-glucosidase and a-amylase inhibitory activities while chromones and/or p-anilinophenol could be the main bioactive compounds responsible for the observed activities.

Palabras clave

  • Khaya senegalensis (Meliaceae)
  • type-2 diabetes
  • α-glucosidase
  • α-amylase
  • oxidative stress
Acceso abierto

Analysis of Active Components in Salvia Miltiorrhiza Injection Based on Vascular Endothelial Cell Protection

Publicado en línea: 08 Oct 2014
Páginas: 325 - 334

Resumen

Abstract

Correlation analysis based on chromatograms and pharmacological activities is essential for understanding the effective components in complex herbal medicines. In this report, HPLC and measurement of antioxidant properties were used to describe the active ingredients of Salvia miltiorrhiza injection (SMI). HPLC results showed that tanshinol, protocatechuic aldehyde, rosmarinic acid, salvianolic acid B, protocatechuic acid and their metabolites in rat serum may contribute to the efficacy of SMI. Assessment of antioxidant properties indicated that differences in the composition of serum powder of SMI caused differences in vascular endothelial cell protection. When bivariate correlation was carried out it was found that salvianolic acid B, tanshinol and protocatechuic aldehyde were active components of SMI because they were correlated to antioxidant properties.

Palabras clave

  • Salvia miltiorrhiza injection
  • HPLC
  • antioxidant activity
  • correlation analysis
  • salvianolic acid
Acceso abierto

Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial Agents

Publicado en línea: 08 Oct 2014
Páginas: 335 - 344

Resumen

Abstract

A series of pyrazole derivatives 9-22 were designed and synthesized. All the newly synthesized compounds were assayed for their antimicrobial activity against the Grampositive bacteria Staphyllococcus aureus and Bacillius subtilis and the Gram-negative bacteria Escherichia coli, Pseudomonas aeruginosa, in addition to the fungi organisms, Candida albicans, C. parapsilosis and C. tropicalis. Ethyl 5-(2,5-dimethylthiophen- 3-yl)-1-phenyl-1H-pyrazole-3-carboxylate (21) (MICE.coli = 0.038 μmol mL-1, MICP. aerug. = 0.067 μmol mL-1) is nearly as active as ampicillin (MIC = 0.033 and 0.067 μmol mL-1), respectively. Ethyl 5-(4-bromo-2-chlorophenyl)- 1-phenyl-1H-pyrazole-3-carboxylate (16) (MIC = 0.015 μmol mL-1) is more active than fluconazole (0.020 μmol mL-1) as a reference drug against C. parapsilosis.

Palabras clave

  • pyrazole-3-carboxylates
  • antimicrobial activity
Acceso abierto

Rosuvastatin, Sildenafil and Their Combination in Monocrotaline-Induced Pulmonary Hypertension in Rat

Publicado en línea: 08 Oct 2014
Páginas: 345 - 353

Resumen

Abstract

There is considerable interest in the pleiotropic effects of statins and their potential role in the treatment of pulmonary hypertension. Previous experimental findings indicate that a combination of lipophilic statins with phosphodiesterase type-5 inhibitor, sildenafil, can offer preventive effects on rat monocrotaline-induced pulmonary hypertension. The present study is aimed to assess whether therapeutic regimen provides any benefits. Seven days after pulmonary hypertension induction, hydrophilic rosuvastatin and sildenafil were given for 14 days to male Wistar outbred rats. Right ventricular pressure, right ventricle mass and three biomarkers were evaluated after 21 days: brain natriuretic peptide, high-density lipoprotein cholesterol and vascular endothelial growth factor. The present study demonstrates that administration of hydrophilic statin with sildenafil results in reduction of pulmonary vascular remodeling and right ventricular pressure. The results of biochemical measurements may suggest that statins play a positive role in right ventricle function or the process of angiogenesis in pulmonary hypertension development.

Palabras clave

  • rosuvastatin
  • sildenafil
  • combination therapy
  • pulmonary hypertension
  • hemodynamic parameters
Acceso abierto

Influence of Process Parameters on Content Uniformity of a Low Dose Active Pharmaceutical Ingredient in a Tablet Formulation According to GMP

Publicado en línea: 08 Oct 2014
Páginas: 355 - 367

Resumen

Abstract

The article describes the development and production of tablets using direct compression of powder mixtures. The aim was to describe the impact of filler particle size and the time of lubricant addition during mixing on content uniformity according to the Good Manufacturing Practice (GMP) process validation requirements. Processes are regulated by complex directives, forcing the producers to validate, using sophisticated methods, the content uniformity of intermediates as well as final products. Cutting down of production time and material, shortening of analyses, and fast and reliable statistic evaluation of results can reduce the final price without affecting product quality. The manufacturing process of directly compressed tablets containing the low dose active pharmaceutical ingredient (API) warfarin, with content uniformity passing validation criteria, is used as a model example. Statistic methods have proved that the manufacturing process is reproducible. Methods suitable for elucidation of various properties of the final blend, e.g., measurement of electrostatic charge by Faraday pail and evaluation of mutual influences of researched variables by partial least square (PLS) regression, were used. Using these methods, it was proved that the filler with higher particle size increased the content uniformity of both blends and the ensuing tablets. Addition of the lubricant, magnesium stearate, during the blending process improved the content uniformity of blends containing the filler with larger particles. This seems to be caused by reduced sampling error due to the suppression of electrostatic charge.

Palabras clave

  • content uniformity
  • warfarin
  • validation
  • narrow therapeutic index
  • Faraday pail
  • PLS regression
Acceso abierto

Evaluation of the Antioxidant Activity of Coreopsis Tinctoria Nuff. and Optimisation of Isolation by Response Surface Methodology

Publicado en línea: 08 Oct 2014
Páginas: 369 - 378

Resumen

Abstract

The aim of the present study was to determine the antioxidant activity of Coreopsis tinctoria flowering tops (CTFT). Studies were conducted to obtain suitable extraction conditions for chlorogenic acid, quercetin, luteolin, apigenin and kaempferol, which were identified and quantified by HPLC. Response surface methodology was employed to optimise the ultrasound-assisted extraction conditions including extraction time, ethanol concentration and liquid-solid ratio. The antioxidant activity of the extracts was analysed using various antioxidant models, such as DPPH, ABTS and hydroxyl radical scavenging assay. CTFT extracted for 15.0 min with ethanol at a concentration of 60.4 % and with liquidsolid ratio 27.5:1 possessed a considerable amounts of total flavonoids and polyphenols (18.9 %). This extract showed higher scavenging activity of ABTS and hydroxyl radical activity than rutin, however not in the DPPH test. We may assume that CTFT possess antioxidant and free radical scavenging potentials.

Palabras clave

  • Coreopsis tinctoria (Asteraceae)
  • flavonoids
  • polyphenols
  • antioxidant activity
  • response surface methodology
  • HPLC
Acceso abierto

Potential of the Essential Oil from Pimenta Pseudocaryophyllus as an Antimicrobial Agent

Publicado en línea: 08 Oct 2014
Páginas: 379 - 385

Resumen

Abstract

This study evaluated the effectiveness of the essential oil of Pimenta pseudocaryophyllus in inhibiting the growth of the main bacteria responsible for bad perspiration odor (Staphylococcus epidermidis, Proteus hauseri, Micrococcus yunnanensis and Corynebacterium xerosis). The chemical profile of the essential oil was evaluated by high-resolution gas chromatography (HR-GC) and four constituents were identified, eugenol being the major component (88.6 %). The antimicrobial activity was evaluated by means of the turbidimetric method, using the microdilution assay. The minimum inhibitory concentration (MIC) values of the essential oil ranged from 500 to 1,000 μg mL-1. Scanning electron microscope (SEM) observations confirmed the physical damage and morphological alteration of the test bacteria treated with the essential oil, reference drugs and eugenol. The findings of the study demonstrated that this essential oil can be used in the formulation of personal care products.

Palabras clave

  • Pimenta pseudocaryophyllus (Myrtaceae)
  • essential oil
  • eugenol
  • antimicrobial activity
  • scanning electron microscopy

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