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Détails du magazine
Format
Magazine
eISSN
1846-9558
Première publication
28 Feb 2007
Période de publication
4 fois par an
Langues
Anglais

Chercher

Volume 65 (2015): Edition 3 (September 2015)

Détails du magazine
Format
Magazine
eISSN
1846-9558
Première publication
28 Feb 2007
Période de publication
4 fois par an
Langues
Anglais

Chercher

10 Articles
Accès libre

Novel 4-aminoquinazoline derivatives as new leads for anticancer drug discovery

Publié en ligne: 30 Sep 2015
Pages: 299 - 309

Résumé

Abstract

A novel series of quinazoline derivatives 2-8, 10-12 were designed and synthesized. Structures of the newly synthesized compounds were confirmed by elemental analyses, IR, 1H and 13C NMR spectral data. All the newly synthesized compounds were evaluated for in vitro cytotoxic activity against the breast cancer cell line MCF-7. Seven of the novel compounds exhibited higher activity than the reference drug doxorubicin. The corresponding compounds 3, 4, 5, 8, 10, 11 and 12 exhibited higher activity with IC50 values from 22.75 to 43.44 μmol L−1, compared to the reference drug doxorubicin with IC50 value of 47.90 μmol L−1. Also, compounds 1, 6, and 9 are nearly as active as doxorubicin with IC50 values of 48.31, 48.90, and 48.91 μmol L−1, respectively, while compounds 2 and 7 exhibited a moderate activity with IC50 values of 50.44 and 52.37 μmol L−1. In addition, compound 13 showed no activity. Cytotoxic screening of the tested copmpounds offered an encouraging framework that may lead to the discovery of potent anti-breast cancer activity.

Mots clés

  • 4-aminoquinazoline derivatives
  • synthesis
  • anti-breast cancer activity
Accès libre

Synthesis of pyranopyrazolo N-glycoside and pyrazolopyranopyrimidine C-glycoside derivatives as promising antitumor and antimicrobial agents

Publié en ligne: 30 Sep 2015
Pages: 215 - 233

Résumé

Abstract

As a part of systematic investigation of the synthesis and biological activities of pyrazole analogues linked to various heterocyclic systems, a new series of pyrazolo-N-glycoside derivatives, pyrazolopyranopyrimidine and C-glycoside of pyrazolopyranotriazolo-pyrimidine derivatives was synthesized through the reaction of the key intermediate 6-amino-3-methyl-4-(substituted-phenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile (3a,b) with different reagents. Structures of the newly synthesized compounds were elucidated by elemental microanalysis and spectroscopic methods. The compounds were subjected to in vitro antitumor evaluation using the MTT assay. N-(β-D-ribofuranosyl)- and N-(β-D-xylofuranosyl)-6{[(1E)-4-chlorophenyl)-methylene] amino}4-(4-florophenyl)-3-methyl-1,4-dihydropyrano[2,3-c]-pyrazole-5-carbonitrile (6a,b) were the most active compounds against three human cancer cell lines. Also, most of the newly synthesized compounds exhibited high activity towards Gram-negative and Gram-positive bacteria. Compound 6a exhibited excellent activity towards bacteria compared to ofloxacine as the reference drug.

Mots clés

  • -nucleoside of pyranopyrazole
  • -glycoside of pyrazolopyranotriazolopyrimidine
  • anticancer activity
  • antimicrobial activity
Accès libre

Investigation of the effects of vitamin D and calcium on intestinal motility: In vitro tests and implications for clinical treatment

Publié en ligne: 30 Sep 2015
Pages: 343 - 349

Résumé

Abstract

The presence of vitamin D receptors in small intestine muscle cells may lead one to think that vitamin D may act locally, influencing intracellular calcium concentration and contributing to the contraction-relaxation regulation of the intestinal smooth muscle cells. This study investigates the potential effects of vitamin D and calcium on intestinal motility using an in vitro test.

Different calcium concentrations added to the tissue not pre-treated with 1,25-dihydroxycholecalciferol [1α,25(OH)2D3] produced no response at low doses (1.25 × 10−3 and 2.0 × 10−3 mol L−1) and only a very weak response at higher concentration (3.0 × 10−3 mol L−1). The addition of 1α,25(OH)2D3 (1.44 × 10−10 mol L−1) had no effect on isolated ileum motility. When calcium (3.0 × 10−3 mol L−1) was added after at least 3 hours, it evoked evident and persistent contractions for 60–90 minutes. The contractions were at about 40 % of the peak produced by acetylcholine. Thus, simultaneous intake of vitamin D and calcium might be a useful co-adjuvant in intestinal atony therapy aimed to stimulate normal gut motility in humans. These findings imply that supplemental vitamin D may be important in all cases where calcium has to be prescribed.

Mots clés

  • vitamin D
  • calcium
  • intestinal motility
  • tests
Accès libre

Dissolution profiles of perindopril and indapamide in their fixed-dose formulations by a new HPLC method and different mathematical approaches

Publié en ligne: 30 Sep 2015
Pages: 235 - 252

Résumé

Abstract

A new HPLC method was introduced and validated for simultaneous determination of perindopril and indapamide. Validation procedure included specificity, sensitivity, robustness, stability, linearity, precision and accuracy. The method was used for the dissolution test of perindopril and indapamide in three fixed-dose formulations. The dissolution procedure was optimized using different media, different pH of the buffer, surfactants, paddle speed and temperature. Similarity of dissolution profiles was estimated using different model-independent and model-dependent methods and, additionally, by principal component analysis (PCA). Also, some kinetic models were checked for dissolved amounts of drugs as a function of time.

Mots clés

  • perindopril
  • indapamide
  • dissolution profiles
  • model-independent methods
  • model-dependent methods
  • PCA
Accès libre

Development of a high-throughput screening system for identification of novel reagents regulating DNA damage in human dermal fibroblasts

Publié en ligne: 30 Sep 2015
Pages: 331 - 341

Résumé

Abstract

Ultraviolet (UV) radiation is a major inducer of skin aging and accumulated exposure to UV radiation increases DNA damage in skin cells, including dermal fibroblasts. In the present study, we developed a novel DNA repair regulating material discovery (DREAM) system for the high-throughput screening and identification of putative materials regulating DNA repair in skin cells. First, we established a modified lentivirus expressing the luciferase and hypoxanthine phosphoribosyl transferase (HPRT) genes. Then, human dermal fibroblast WS-1 cells were infected with the modified lentivirus and selected with puromycin to establish cells that stably expressed luciferase and HPRT (DREAM-F cells). The first step in the DREAM protocol was a 96-well-based screening procedure, involving the analysis of cell viability and luciferase activity after pretreatment of DREAM-F cells with reagents of interest and post-treatment with UVB radiation, and vice versa. In the second step, we validated certain effective reagents identified in the first step by analyzing the cell cycle, evaluating cell death, and performing HPRT-DNA sequencing in DREAM-F cells treated with these reagents and UVB. This DREAM system is scalable and forms a time-saving high-throughput screening system for identifying novel anti-photoaging reagents regulating DNA damage in dermal fibroblasts.

Mots clés

  • human dermal fibroblasts
  • DNA damage
  • high-throughput screening
  • aging
Accès libre

Contribution to diagnostics/prognostics of tuberculosis in children. I. New methods of assaying zinc and simultaneously copper and zinc in diluted sera by flame atomic-absorption spectrometry

Publié en ligne: 30 Sep 2015
Pages: 311 - 320

Résumé

Abstract

In an attempt to provide a reliable status of metal ions in children, new methods of analysis of children’s sera are proposed. New flame atomic-absorption spectrometric (FAAS) methods are simple, cost- and time-effective and, above all, labor-, reagent- and sample-saving. Two methods were suggested: method A for simultaneous determination of Cu and Zn from 5-fold diluted sera, and method B, for assaying zinc alone in 10-fold diluted samples. Both methods are based on a single-step sample pretreatment (deproteinization with 3 mol dm–3 HCl). Method A uses a single-step calibration with a mixed standard. The main advantage of method B is an additional reduction in sample consumption. Both methods were fully validated against reference methods. Accuracy, sensitivity and precision have proven them to be comparable to the reference methods in terms of analytical performance, and applicable to analyses of children’s sera.

Mots clés

  • copper
  • zinc
  • flame atomic-absorption spectrometry
  • single-step analysis
  • children’s serum
Accès libre

Contribution to diagnostics/prognostics of tuberculosis in children. II. Indicative value of metal ions and biochemical parameters in serum

Publié en ligne: 30 Sep 2015
Pages: 321 - 329

Résumé

Abstract

Newly introduced methods of assaying simultaneously copper and zinc and zinc alone in serum by flame atomic-absorption spectrometry are simple and economical, especially in saving the consumption of serum material. Along with biochemical parameters, they have been successfully applied to diagnostics/prognostics of tuberculosis in children, through analyses of sera from pediatric patients with lung tuberculosis or suspected tuberculosis, enabling the follow-up of therapeutic efficiency. The prognostic strength of Cu and Cu/Zn ratio together with C-reactive protein, complement components C3 and C4, and erythrocyte sedimentation rate have been documented.

Mots clés

  • copper
  • zinc
  • Cu/Zn ratio
  • biochemical parameters
  • children’s serum
  • lung tuberculosis
Accès libre

Conventional versus ultrasound and microwave assisted synthesis: Some new environmentally friendly functionalized picolinium-based ionic liquids with potential antibacterial activity

Publié en ligne: 30 Sep 2015
Pages: 253 - 270

Résumé

Abstract

A green chemistry approach has been adopted for the synthesis of thirty-four new picolinium-based ionic liquids using microwave (MW) and ultrasound (US) irradiation as well as conventional thermal heating. Their structures were confirmed by FT-IR, 1H NMR, 13C NMR, 11B NMR, 19F NMR, 31P NMR, mass spectra and elemental analyses. The antimicrobial profile of the novel ionic liquids was evaluated and the minimum inhibitory concentration (MIC) showed their moderate to low antimicrobial activity against eight types of human pathogens.

Mots clés

  • picolinium-based ionic liquids
  • ultrasound irradiation
  • microwave irradiation
  • green procedure
  • antibacterial activity
Accès libre

Curcumin phytosomal softgel formulation: Development, optimization and physicochemical characterization

Publié en ligne: 30 Sep 2015
Pages: 285 - 297

Résumé

Abstract

Curcumin, a naturally occurring lipophilic molecule can exert multiple and diverse bioactivities. However, its limited aqueous solubility and extensive presystemic metabolism restrict its bioavailability. Curcumin phytosomes were prepared by a simple solvent evaporation method where free flowing powder was obtained in addition to a newly developed semisolid formulation to increase curcumin content in softgels. Phytosomal powder was characterized in terms of drug content and zeta potential. Thirteen different softgel formulations were developed using oils such as Miglyol 812, castor oil and oleic acid, a hydrophilic vehicle such as PEG 400 and bioactive surfactants such as Cremophor EL and KLS P 124. Selected formulations were characterized in terms of curcumin in vitro dissolution. TEM analysis revealed good stability and a spherical, self-closed structure of curcumin phytosomes in complex formulations. Stability studies of chosen formulations prepared using the hydrophilic vehicle revealed a stable curcumin dissolution pattern. In contrast, a dramatic decrease in curcumin dissolution was observed in case of phytosomes formulated in oily vehicles.

Mots clés

  • curcumin
  • phospholipid
  • phytosomes
  • bioavailability
  • lipids
  • softgels
Accès libre

Anti-breast cancer activity of some novel quinoline derivatives

Publié en ligne: 30 Sep 2015
Pages: 271 - 283

Résumé

Abstract

To discover new bioactive lead compounds for medicinal purposes, 2-cyano-3-(4-substituted)-N-(quinolin-3-yl) acrylamide derivatives 2–24, chromenes 25, 26 and benzochromenes 27, 28 were synthesized. The structures of the newly synthesized compounds were confirmed by elemental analyses, IR, 1H NMR and 13C NMR spectroscopies. In addition, the structure of compound 1 was confirmed through X-ray crystallography. All the newly synthesized compounds were evaluated for their cytotoxic activity against the breast cancer cell line MCF7. The corresponding 2-cyano-3-(4-hydroxy-3-methoxyphenyl)-N-(quinolin-3-yl) acrylamide (15), 3-oxo-N-(quinolin-3-yl)-3H-benzol[f] chromene-2-carboxamide (27), 2-cyano-3-(4-fluorophenyl-N-(quinolin-3-yl) acrylamide (7), 2-cyano-5-(4-(dimethyl-amino) phenyl)-N-(quinolin-3-yl) penta-2,4-dienamide (19) exhibited higher activity compared to doxorubicin (with IC50 value of 47.9 μmol L−1) as a reference drug, with IC50 values of 29.8, 39.0, 40.0, 40.4 μmol L−1, resp. Also, quinoline acrylamides containing 2,3,4-trimethoxyphenyl 17, 2-chlorophenyl 10, benzo[d][1,3]dioxol 12, 2-methoxynaphthalen 22, 2,4-dichlorophenyl 18 and quinoline carrying a chromene-3-carboxamide moiety 25 were nearly as active as doxorubicin, while quinoline acrylamides incorporating unsubstituted phenyl 2, p-tolyl 3, 2,4-dienamide 8, 3-nitrophenyl 13, 4-nitrophenyl 14, 3,4-dimethoxyphenyl 16 and chromene 26 exhibited a moderate activity. In addition, quinoline with acetamide 1, 4-hydroxyphenyl 4, 4-dimethylaminophenyl 9, 4-chlorophenyl 11, 3-bromophenyl 20, 4-bromophenyl 21 and 3-thienyl moiety 24 showed less activity than doxorubicin. On the other hand, quinoline having 2-methoxyphenyl 5, 4-methoxyphenyl 6, 4-metho xynaphthalene 23 and chromene-2-carboxamide 28 showed no activity.

Mots clés

  • quinolineacrylamides
  • chromenes
  • benzochromenes
  • anti-breast cancer activity
10 Articles
Accès libre

Novel 4-aminoquinazoline derivatives as new leads for anticancer drug discovery

Publié en ligne: 30 Sep 2015
Pages: 299 - 309

Résumé

Abstract

A novel series of quinazoline derivatives 2-8, 10-12 were designed and synthesized. Structures of the newly synthesized compounds were confirmed by elemental analyses, IR, 1H and 13C NMR spectral data. All the newly synthesized compounds were evaluated for in vitro cytotoxic activity against the breast cancer cell line MCF-7. Seven of the novel compounds exhibited higher activity than the reference drug doxorubicin. The corresponding compounds 3, 4, 5, 8, 10, 11 and 12 exhibited higher activity with IC50 values from 22.75 to 43.44 μmol L−1, compared to the reference drug doxorubicin with IC50 value of 47.90 μmol L−1. Also, compounds 1, 6, and 9 are nearly as active as doxorubicin with IC50 values of 48.31, 48.90, and 48.91 μmol L−1, respectively, while compounds 2 and 7 exhibited a moderate activity with IC50 values of 50.44 and 52.37 μmol L−1. In addition, compound 13 showed no activity. Cytotoxic screening of the tested copmpounds offered an encouraging framework that may lead to the discovery of potent anti-breast cancer activity.

Mots clés

  • 4-aminoquinazoline derivatives
  • synthesis
  • anti-breast cancer activity
Accès libre

Synthesis of pyranopyrazolo N-glycoside and pyrazolopyranopyrimidine C-glycoside derivatives as promising antitumor and antimicrobial agents

Publié en ligne: 30 Sep 2015
Pages: 215 - 233

Résumé

Abstract

As a part of systematic investigation of the synthesis and biological activities of pyrazole analogues linked to various heterocyclic systems, a new series of pyrazolo-N-glycoside derivatives, pyrazolopyranopyrimidine and C-glycoside of pyrazolopyranotriazolo-pyrimidine derivatives was synthesized through the reaction of the key intermediate 6-amino-3-methyl-4-(substituted-phenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile (3a,b) with different reagents. Structures of the newly synthesized compounds were elucidated by elemental microanalysis and spectroscopic methods. The compounds were subjected to in vitro antitumor evaluation using the MTT assay. N-(β-D-ribofuranosyl)- and N-(β-D-xylofuranosyl)-6{[(1E)-4-chlorophenyl)-methylene] amino}4-(4-florophenyl)-3-methyl-1,4-dihydropyrano[2,3-c]-pyrazole-5-carbonitrile (6a,b) were the most active compounds against three human cancer cell lines. Also, most of the newly synthesized compounds exhibited high activity towards Gram-negative and Gram-positive bacteria. Compound 6a exhibited excellent activity towards bacteria compared to ofloxacine as the reference drug.

Mots clés

  • -nucleoside of pyranopyrazole
  • -glycoside of pyrazolopyranotriazolopyrimidine
  • anticancer activity
  • antimicrobial activity
Accès libre

Investigation of the effects of vitamin D and calcium on intestinal motility: In vitro tests and implications for clinical treatment

Publié en ligne: 30 Sep 2015
Pages: 343 - 349

Résumé

Abstract

The presence of vitamin D receptors in small intestine muscle cells may lead one to think that vitamin D may act locally, influencing intracellular calcium concentration and contributing to the contraction-relaxation regulation of the intestinal smooth muscle cells. This study investigates the potential effects of vitamin D and calcium on intestinal motility using an in vitro test.

Different calcium concentrations added to the tissue not pre-treated with 1,25-dihydroxycholecalciferol [1α,25(OH)2D3] produced no response at low doses (1.25 × 10−3 and 2.0 × 10−3 mol L−1) and only a very weak response at higher concentration (3.0 × 10−3 mol L−1). The addition of 1α,25(OH)2D3 (1.44 × 10−10 mol L−1) had no effect on isolated ileum motility. When calcium (3.0 × 10−3 mol L−1) was added after at least 3 hours, it evoked evident and persistent contractions for 60–90 minutes. The contractions were at about 40 % of the peak produced by acetylcholine. Thus, simultaneous intake of vitamin D and calcium might be a useful co-adjuvant in intestinal atony therapy aimed to stimulate normal gut motility in humans. These findings imply that supplemental vitamin D may be important in all cases where calcium has to be prescribed.

Mots clés

  • vitamin D
  • calcium
  • intestinal motility
  • tests
Accès libre

Dissolution profiles of perindopril and indapamide in their fixed-dose formulations by a new HPLC method and different mathematical approaches

Publié en ligne: 30 Sep 2015
Pages: 235 - 252

Résumé

Abstract

A new HPLC method was introduced and validated for simultaneous determination of perindopril and indapamide. Validation procedure included specificity, sensitivity, robustness, stability, linearity, precision and accuracy. The method was used for the dissolution test of perindopril and indapamide in three fixed-dose formulations. The dissolution procedure was optimized using different media, different pH of the buffer, surfactants, paddle speed and temperature. Similarity of dissolution profiles was estimated using different model-independent and model-dependent methods and, additionally, by principal component analysis (PCA). Also, some kinetic models were checked for dissolved amounts of drugs as a function of time.

Mots clés

  • perindopril
  • indapamide
  • dissolution profiles
  • model-independent methods
  • model-dependent methods
  • PCA
Accès libre

Development of a high-throughput screening system for identification of novel reagents regulating DNA damage in human dermal fibroblasts

Publié en ligne: 30 Sep 2015
Pages: 331 - 341

Résumé

Abstract

Ultraviolet (UV) radiation is a major inducer of skin aging and accumulated exposure to UV radiation increases DNA damage in skin cells, including dermal fibroblasts. In the present study, we developed a novel DNA repair regulating material discovery (DREAM) system for the high-throughput screening and identification of putative materials regulating DNA repair in skin cells. First, we established a modified lentivirus expressing the luciferase and hypoxanthine phosphoribosyl transferase (HPRT) genes. Then, human dermal fibroblast WS-1 cells were infected with the modified lentivirus and selected with puromycin to establish cells that stably expressed luciferase and HPRT (DREAM-F cells). The first step in the DREAM protocol was a 96-well-based screening procedure, involving the analysis of cell viability and luciferase activity after pretreatment of DREAM-F cells with reagents of interest and post-treatment with UVB radiation, and vice versa. In the second step, we validated certain effective reagents identified in the first step by analyzing the cell cycle, evaluating cell death, and performing HPRT-DNA sequencing in DREAM-F cells treated with these reagents and UVB. This DREAM system is scalable and forms a time-saving high-throughput screening system for identifying novel anti-photoaging reagents regulating DNA damage in dermal fibroblasts.

Mots clés

  • human dermal fibroblasts
  • DNA damage
  • high-throughput screening
  • aging
Accès libre

Contribution to diagnostics/prognostics of tuberculosis in children. I. New methods of assaying zinc and simultaneously copper and zinc in diluted sera by flame atomic-absorption spectrometry

Publié en ligne: 30 Sep 2015
Pages: 311 - 320

Résumé

Abstract

In an attempt to provide a reliable status of metal ions in children, new methods of analysis of children’s sera are proposed. New flame atomic-absorption spectrometric (FAAS) methods are simple, cost- and time-effective and, above all, labor-, reagent- and sample-saving. Two methods were suggested: method A for simultaneous determination of Cu and Zn from 5-fold diluted sera, and method B, for assaying zinc alone in 10-fold diluted samples. Both methods are based on a single-step sample pretreatment (deproteinization with 3 mol dm–3 HCl). Method A uses a single-step calibration with a mixed standard. The main advantage of method B is an additional reduction in sample consumption. Both methods were fully validated against reference methods. Accuracy, sensitivity and precision have proven them to be comparable to the reference methods in terms of analytical performance, and applicable to analyses of children’s sera.

Mots clés

  • copper
  • zinc
  • flame atomic-absorption spectrometry
  • single-step analysis
  • children’s serum
Accès libre

Contribution to diagnostics/prognostics of tuberculosis in children. II. Indicative value of metal ions and biochemical parameters in serum

Publié en ligne: 30 Sep 2015
Pages: 321 - 329

Résumé

Abstract

Newly introduced methods of assaying simultaneously copper and zinc and zinc alone in serum by flame atomic-absorption spectrometry are simple and economical, especially in saving the consumption of serum material. Along with biochemical parameters, they have been successfully applied to diagnostics/prognostics of tuberculosis in children, through analyses of sera from pediatric patients with lung tuberculosis or suspected tuberculosis, enabling the follow-up of therapeutic efficiency. The prognostic strength of Cu and Cu/Zn ratio together with C-reactive protein, complement components C3 and C4, and erythrocyte sedimentation rate have been documented.

Mots clés

  • copper
  • zinc
  • Cu/Zn ratio
  • biochemical parameters
  • children’s serum
  • lung tuberculosis
Accès libre

Conventional versus ultrasound and microwave assisted synthesis: Some new environmentally friendly functionalized picolinium-based ionic liquids with potential antibacterial activity

Publié en ligne: 30 Sep 2015
Pages: 253 - 270

Résumé

Abstract

A green chemistry approach has been adopted for the synthesis of thirty-four new picolinium-based ionic liquids using microwave (MW) and ultrasound (US) irradiation as well as conventional thermal heating. Their structures were confirmed by FT-IR, 1H NMR, 13C NMR, 11B NMR, 19F NMR, 31P NMR, mass spectra and elemental analyses. The antimicrobial profile of the novel ionic liquids was evaluated and the minimum inhibitory concentration (MIC) showed their moderate to low antimicrobial activity against eight types of human pathogens.

Mots clés

  • picolinium-based ionic liquids
  • ultrasound irradiation
  • microwave irradiation
  • green procedure
  • antibacterial activity
Accès libre

Curcumin phytosomal softgel formulation: Development, optimization and physicochemical characterization

Publié en ligne: 30 Sep 2015
Pages: 285 - 297

Résumé

Abstract

Curcumin, a naturally occurring lipophilic molecule can exert multiple and diverse bioactivities. However, its limited aqueous solubility and extensive presystemic metabolism restrict its bioavailability. Curcumin phytosomes were prepared by a simple solvent evaporation method where free flowing powder was obtained in addition to a newly developed semisolid formulation to increase curcumin content in softgels. Phytosomal powder was characterized in terms of drug content and zeta potential. Thirteen different softgel formulations were developed using oils such as Miglyol 812, castor oil and oleic acid, a hydrophilic vehicle such as PEG 400 and bioactive surfactants such as Cremophor EL and KLS P 124. Selected formulations were characterized in terms of curcumin in vitro dissolution. TEM analysis revealed good stability and a spherical, self-closed structure of curcumin phytosomes in complex formulations. Stability studies of chosen formulations prepared using the hydrophilic vehicle revealed a stable curcumin dissolution pattern. In contrast, a dramatic decrease in curcumin dissolution was observed in case of phytosomes formulated in oily vehicles.

Mots clés

  • curcumin
  • phospholipid
  • phytosomes
  • bioavailability
  • lipids
  • softgels
Accès libre

Anti-breast cancer activity of some novel quinoline derivatives

Publié en ligne: 30 Sep 2015
Pages: 271 - 283

Résumé

Abstract

To discover new bioactive lead compounds for medicinal purposes, 2-cyano-3-(4-substituted)-N-(quinolin-3-yl) acrylamide derivatives 2–24, chromenes 25, 26 and benzochromenes 27, 28 were synthesized. The structures of the newly synthesized compounds were confirmed by elemental analyses, IR, 1H NMR and 13C NMR spectroscopies. In addition, the structure of compound 1 was confirmed through X-ray crystallography. All the newly synthesized compounds were evaluated for their cytotoxic activity against the breast cancer cell line MCF7. The corresponding 2-cyano-3-(4-hydroxy-3-methoxyphenyl)-N-(quinolin-3-yl) acrylamide (15), 3-oxo-N-(quinolin-3-yl)-3H-benzol[f] chromene-2-carboxamide (27), 2-cyano-3-(4-fluorophenyl-N-(quinolin-3-yl) acrylamide (7), 2-cyano-5-(4-(dimethyl-amino) phenyl)-N-(quinolin-3-yl) penta-2,4-dienamide (19) exhibited higher activity compared to doxorubicin (with IC50 value of 47.9 μmol L−1) as a reference drug, with IC50 values of 29.8, 39.0, 40.0, 40.4 μmol L−1, resp. Also, quinoline acrylamides containing 2,3,4-trimethoxyphenyl 17, 2-chlorophenyl 10, benzo[d][1,3]dioxol 12, 2-methoxynaphthalen 22, 2,4-dichlorophenyl 18 and quinoline carrying a chromene-3-carboxamide moiety 25 were nearly as active as doxorubicin, while quinoline acrylamides incorporating unsubstituted phenyl 2, p-tolyl 3, 2,4-dienamide 8, 3-nitrophenyl 13, 4-nitrophenyl 14, 3,4-dimethoxyphenyl 16 and chromene 26 exhibited a moderate activity. In addition, quinoline with acetamide 1, 4-hydroxyphenyl 4, 4-dimethylaminophenyl 9, 4-chlorophenyl 11, 3-bromophenyl 20, 4-bromophenyl 21 and 3-thienyl moiety 24 showed less activity than doxorubicin. On the other hand, quinoline having 2-methoxyphenyl 5, 4-methoxyphenyl 6, 4-metho xynaphthalene 23 and chromene-2-carboxamide 28 showed no activity.

Mots clés

  • quinolineacrylamides
  • chromenes
  • benzochromenes
  • anti-breast cancer activity

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