Rivista e Edizione

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Dettagli della rivista
Formato
Rivista
eISSN
1846-9558
Pubblicato per la prima volta
28 Feb 2007
Periodo di pubblicazione
4 volte all'anno
Lingue
Inglese

Cerca

Volume 71 (2021): Edizione 3 (September 2021)

Dettagli della rivista
Formato
Rivista
eISSN
1846-9558
Pubblicato per la prima volta
28 Feb 2007
Periodo di pubblicazione
4 volte all'anno
Lingue
Inglese

Cerca

12 Articoli
Accesso libero

Computer-aided approaches reveal trihydroxychroman and pyrazolone derivatives as potential inhibitors of SARS-CoV-2 virus main protease

Pubblicato online: 31 Dec 2020
Pagine: 325 - 333

Astratto

Abstract

COVID-19 was declared a pandemic by the World Health Organization (WHO) in March 2020. The disease is caused by severe acute respiratory syndrome coronavirus 2 (SARSCoV-2). The aim of this study is to target the SARS-CoV-2 virus main protease (Mpro) via structure-based virtual screening. Consequently, > 580,000 ligands were processed via several filtration and docking steps, then the top 21 compounds were analysed extensively via MM-GBSA scoring and molecular dynamic simulations. Interestingly, the top compounds showed favorable binding energies and binding patterns to the protease enzyme, forming interactions with several key residues. Trihydroxychroman and pyrazolone derivatives, SN02 and SN18 ligands, exhibited very promising binding modes along with the best MM-GBSA scoring of –40.9 and –41.2 kcal mol−1, resp. MD simulations of 300 ns for the ligand-protein complexes of SN02 and SN18 affirmed the previously attained results of the potential inhibition activity of these two ligands. These potential inhibitors can be the starting point for further studies to pave way for the discovery of new antiviral drugs for SARS-CoV-2.

Parole chiave

  • COVID-19
  • M
  • SARS-COV-2
  • antiviral
  • virtual screening
  • docking
Accesso libero

Melatonin as a powerful antioxidant

Pubblicato online: 31 Dec 2020
Pagine: 335 - 354

Astratto

Abstract

Melatonin is a hormone that has many body functions and, for several decades, its antioxidant potential has been increasingly talked about. There is a relationship between failure in melatonin production in the pineal gland, an insufficient supply of this hormone to the body, and the occurrence of free radical etiology diseases such as neurodegenerative diseases, cardiovascular diseases, diabetes, cancer and others. Despite the development of molecular biology, numerous in vitro and in vivo studies, the exact mechanism of melatonin antioxidant activity is still unknown. Nowadays, the use of melatonin supplementation is more and more common, not only to prevent insomnia, but also to slow down the aging process and provide protection against diseases. The aim of this study is to get acquainted with current reports on melatonin, antioxidative mechanisms and their importance in diseases of free radical etiology.

Parole chiave

  • melatonin
  • antioxidants
  • lipid peroxidation
  • free radicals
  • oxidative stress
Accesso libero

Cannabigerol and cannabichromene in Cannabis sativa L.

Pubblicato online: 31 Dec 2020
Pagine: 355 - 364

Astratto

Abstract

In addition to delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD), other phytocannabinoids, such as cannabigerol (CBG) and cannabichromene (CBC), also have beneficial effects on human health. A high content of CBG is found in plants with the B0 genotype, whereas CBC is independent of the allelic chemotype locus B. In basic research models such as mice or rats, CBG has demonstrated anticancer properties, particularly against breast cancer. CBG has shown anti-inflammatory effects on murine colitis and on inflammatory bowel disease as well as stimulatory effects on the feeding behaviors of mice. It has also exhibited inhibition of aldose reductase, which is known to cause an accumulation of sorbitol and increase glucose levels in the blood, which may lead to diabetes. Cannabinoid CBC has also shown anti-inflammatory effects and reduced hypermobility in the gut and has displayed potential in vitro effect on adult neural stem progenitor cells. CBC also exerts modest analgesic properties in rodents, as well as anti-fungal, anti-bacterial, pro-apoptotic, and anti-proliferative effects in tumor cells.

Parole chiave

  • cannabinoids
  • chemotype
  • health effects
  • hemp
  • receptors
Accesso libero

Preparation, characterization and antimicrobial assessment of selected ciprofloxacin salts

Pubblicato online: 31 Dec 2020
Pagine: 365 - 382

Astratto

Abstract

The formation of salts is considered a simple strategy to modify the physicochemical properties of active pharmaceutical ingredients. In this study, seven novel binary and ternary organic salts of ciprofloxacin (CP) were prepared with benzoic acid (BA), acetylsalicylic acid (ASA), p-coumaric acid (PCMA) and p-aminosalicylic acid (PASA). They were characterized by spectroscopic techniques and differential scanning calorimetry. Solubility and partition coefficients values were also measured. Evaluation of the antimicrobial activity of the organic salts against Staphylococcus aureus and Staphylococcus epidermidis revealed that most of the new salts had higher antimicrobial activity than CPHCl against both strains. The most active compounds against S. epidermidis and S. aureus were CP-PASA and CPPCMA, resp., which were up to fourteen times more potent than parent CP-HCl. Our findings indicated a strong correlation between the lipophilicity of the formed salts and their antimicrobial activity and showed that an optimum value of lipophilicity (log P = 0.75) seemed to be necessary to maximize the antimicrobial activity. These findings highlighted the improved physical, thermal and antimicrobial properties of the new salts of CP that can aid in providing higher bioavailability than CP-HCl.

Parole chiave

  • ciprofloxacin
  • salts
  • partition coefficient
  • Staphylococcus aureus
  • Staphylococcus epidermidis
Accesso libero

Ilex paraguariensis extract as an alternative to pain medications

Pubblicato online: 31 Dec 2020
Pagine: 383 - 398

Astratto

Abstract

Pain is a common and distressing symptom of many diseases and its clinical treatment generally involves analgesics and anti-inflammatory drugs. This study evaluated the toxicity of Ilex paraguariensis A. St.-Hil. (Aquifoliaceae) aqueous extract (leaves, petioles and branches) and its performance in a nociceptive response. Hepatotoxicity, psycho-stimulant test and evaluation of enzyme markers for liver damage were also tested. Chromatographic analysis by UPLC-MS demonstrated a series of isomeric monocaffeoylquinic acids, isomers of dicaffeoylquinic acid, flavonol glycosides, and saponins. Phase I and II of nociception were obtained for meloxicam, dexamethasone and aqueous Ilex paraguariensis extract. Ilex paraguariensis extract concentration was negatively correlated (R = –0.887) with alanine aminotransferase (p < 0.05) in acetaminophen-induced hepatotoxicity test, indicating hepatoprotective activity of this extract. Ilex paraguariensis extract also presented analgesic properties equivalent to drugs that already have proven efficacy. Notably, the administration of multiple doses of Ilex paraguariensis extract was considered safe from the therapeutic point of view.

Parole chiave

  • nociception
  • pain
  • hepatoprotection
  • toxicity
  • aqueous extract
  • UPLCMS
Accesso libero

Screening of six medicinal plant species for antileishmanial activity

Pubblicato online: 31 Dec 2020
Pagine: 399 - 414

Astratto

Abstract

This study is aimed to investigate the in vitro anti-leishmanial activity of ethanolic, aqueous or dichloromethane extracts of leaves, flowers, fruits or roots, of six medicinal plant species, namely, Nectandra megapotamica, Brunfelsia uniflora, Myrcianthes pungens, Anona muricata, Hymenaea stigonocarpa and Piper corcovandesis. After isolation and analysis of chemical components by ultra-high performance liquid chromatography-high-resolution tandem mass spectrometry (UHPLC-HRMS/MS), the extracts were also tested for toxicity in J774.A1 macrophages and human erythrocytes. Phenolic acids, flavonoids, acetogenins, alkaloids and lignans were identified in these extracts. Grow inhibition of promastigotes forms of Leishmania amazonensis and Leishmania braziliensis and the cytotoxicity in J774.A1 macrophages were estimated by the XTT method. The most promising results for L. amazonensis and L. braziliensis were shown by the ethanolic extract of the fruits of Hymenaea stigonocarpa and dichloromethane extract of the roots of Piper corcovadensis, with IC50 of 160 and 150 μg mL−1, resp. Ethanolic extracts of A. muricata (leaf), B. uniflora (flower and leaf), M. pungens (fruit and leaf), N. megapotamica (leaf), and aqueous extract of H. stigonocarpa (fruit) showed IC50 > 170 μg mL−1 for L. amazonensis and > 200 μg mL−1 for L. braziliensis. The extracts exhibited low cytotoxicity towards J774.A1 macrophages with CC50 > 1000 μg mL−1 and hemolytic activity from 0 to 46.1 %.

Parole chiave

  • Piper corcovadensis
  • Hymenaea stigonocarpa
  • antileishmanial
  • Leishmania amazonensis
  • Leishmania braziliensis
  • cytotoxicity
  • hemolysis
Accesso libero

Quantitative analysis and pharmacokinetic study of a novel diarylurea EGFR inhibitor (ZCJ14) in rat plasma using a validated LC-MS/MS method

Pubblicato online: 31 Dec 2020
Pagine: 415 - 428

Astratto

Abstract

1-(4-(Pyrrolidin-1-yl-methyl)phenyl)-3-(4-((3-(trifluoromethyl) phenyl)amino)quinazolin-6-yl)urea (ZCJ14), a novel epidermal growth factor receptor (EGFR) inhibitor, with diarylurea moiety, displays anticancer effect. In the present study, an LCMS/MS method was established to determine the concentration of ZCJ14 in rat plasma. Furthermore, the method was applied to investigate the pharmacokinetic characteristics of ZCJ14. Chromatographic separation of ZCJ14 and internal standard (IS) [1-phenyl-3-(4-((3-(trifluoromethyl)phenyl)amino) quinazolin-6-yl)urea] was accomplished by gradient elution using the Kromasil C18 column. The selected reaction monitoring transitions were performed at m/z 507.24→436.18 and 424.13→330.96 for ZCJ14 and IS, resp. The established method was linear over the concentration range of 10–1000 ng mL−1. The intra- and inter-day precisions were < 11.0 % (except for LLOQ which was up to 14.3 %) and the respective accuracies were within the range of 87.5–99.0 %. The extraction recovery and matrix effect were within the range of 88.4–104.5 % and 87.3–109.9 %, resp. ZCJ14 was stable under all storage conditions. The validated method was successfully applied to the pharmacokinetic study of ZCJ14 in rats, and the pharmacokinetic parameters have been determined. The oral bioavailability of ZCJ14 was found to be 46.1 %. Overall, this accurate and reliable quantification method might be useful for other diarylurea moiety-containing drugs.

Parole chiave

  • ZCJ14
  • epidermal growth factor receptor inhibitor
  • LC-MS/MS
  • pharmacokinetics
  • bioavailability
Accesso libero

Determination of carbohydrates in the herbal antidiabetic mixtures by GC-MC

Pubblicato online: 31 Dec 2020
Pagine: 429 - 443

Astratto

Abstract

Due to the wide range of biologically active substances, the herbal mixtures can influence the development of diabetes mellitus and its complications. Carbohydrates attract particular attention due to their hypoglycemic, hypolipidemic, anticholesterolemic, antioxidant, antiinflammatory and detoxifying activities. The aim of this study was to investigate the content of carbohydrates through their monomeric composition in the herbal mixture samples: a) Urtica dioica leaf, Cichorium intybus roots, Rosa majalis fruits, Elymys repens rhizome, Taraxacum officinale roots, b) Arctium lappa roots, Elymys repens rhizome, Zea mays columns with stigmas, Helichrysum arenarium flowers, Rosa majalis fruits, c) Inula helenium rhizome with roots, Helichrysi arenarium flowers, Zea mays columns with stigmas, Origanum vulgare herb, Rosa majalis fruits, Taraxacum officinale roots, d) Cichorium intybus roots, Elymys repens rhizome, Helichrysum arenarium flowers, Rosa majalis fruits, Zea mays columns with stigmas and e) Urtica dioica leaf, Taraxacum officinale roots, Vaccinium myrtillus leaf, Rosa majalis fruits, Mentha piperita herb, which were used in Ukrainian folk medicine for the prevention and treatment of diabetes mellitus type 2.

The carbohydrates were separated by gas chromatography-mass spectrometry after conversion into volatile aldononitrile acetate derivatives. The monomeric composition of polysaccharides was studied after their hydrolysis to form monosaccharides and poly-alcohols.

Quantitative analyses of free carbohydrates showed that the predominant sugars were fructose, glucose and disaccharide – sucrose, in all samples. Concerning the determination of polysaccharide monomers after hydrolysis, glucose was the most abundant in all samples. The chromatographic study revealed a number of polyalcohols that are important for the treatment and prevention of progression of diabetes mellitus and its complications, namely, mannitol, pinitol and myo-inositol.

Parole chiave

  • carbohydrates
  • herbal antidiabetic mixtures
  • GC-MS
  • monosaccharides
Accesso libero

Simplex lattice design for optimization of the mass ratio of Curcuma longa L., Curcuma zedoaria (Christm.) Roscoe and Curcuma aromatica Salisb. to maximize curcuminoids content and antioxidant activity

Pubblicato online: 31 Dec 2020
Pagine: 445 - 457

Astratto

Abstract

The aim of this work was to optimize the mass ratio of three Curcuma plants’ rhizomes to obtain the highest curcuminoid content and antioxidant activity using the simplex lattice design. The selected Curcuma plants were C. longa, C. zedoaria and C. aromatica. The simplex lattice design was applied in the work. The individual curcuminoids (curcumin, demethoxycurcumin and bis-demethoxycurcumin) and total curcuminoid content were determined using high-performance liquid chromatography. Curcuma longa alone provided the highest content of bis-demethoxycurcumin and demethoxycurcumin. A mixture of C. longa and C. aromatica in the mass ratio of 72:28 % provided the highest curcumin content. The results showed that C. longa alone exhibited the highest antioxidant activity.

Parole chiave

  • curcuminoids
  • HPLC
  • simplex lattice design
  • optimization
  • antioxidant activity
Accesso libero

Amygdalin isolated from Amygdalus mongolica protects against hepatic fibrosis in rats

Pubblicato online: 31 Dec 2020
Pagine: 459 - 471

Astratto

Abstract

The aim of this research was to investigate the effect of amygdalin on hepatic fibrosis in rats. Amygdalin was purified and identified from the seeds of Amygdalus mongo lica. Sprague Dawley rats in the control and model groups were administered water. Sprague Dawley rats were divided into the low-, middle-, and high-dose amygdalin groups that received 20, 40, and 80 mg kg−1 amygdalin, respectively. whereas the silymarin group was treated with 50 mg kg−1 silymarin. The control and model groups were administered water. Liver tissue analysis revealed significantly lower activities of ALT, AST, ALP, SOD, and MDA in the drug-treated groups compared to the model group. Serum analysis revealed significantly lower HYC and C-IV in the middle-dose amygdalin-treated group compared to the model group. The histopathological changes were less severe in the drug-treated groups as observed by the formation of pseudolobuli and decreased collagen fiber deposition. Hepatic fibrosis-related genes were expressed at significantly lower levels in the amygdalin-treated groups than in the model group. Amygdalin from A. mongolica represents a therapeutic candidate for hepatic fibrosis prevention and treatment.

Parole chiave

  • amygdalin
  • hepatic fibrosis
  • rat model
  • traditional Chinese medicine
Accesso libero

Effect of sacubitril/valsartan on inflammation and oxidative stress in doxorubicin-induced heart failure model in rabbits

Pubblicato online: 31 Dec 2020
Pagine: 473 - 484

Astratto

Abstract

Our study evaluates the effects of sacubitril/valsartan (SAC/VAL) in the rabbit model of doxorubicin-induced heart failure. Twenty rabbits (5 per group) were administered with doxorubicin (DOX, 1.5 mg kg−1, i.v.) to induce heart failure. Specific biomarkers such as BNP, CnT, CRP and ROMs were determined. The cardiac enzymatic anti-oxidant systems were recorded with their electrographic profiles. HR, SBP, DBP and MAP were restored at 5 or 10 mg kg−1 (p.o.) of SAC/VAL compared to DOX, followed by reduced levels of creatinine and BNP (p < 0.001). Significant improvements (p < 0.05) compared to DOX were also noticed in CAT, SOD and LPO with the same doses of SAC/VAL. Specific biomarkers such as BNP, CnT, CRP and ROMs descended significantly (p < 0.001) with treatment when compared to their baseline values. Our findings implied that SAC/VAL treatment reduced the inflammation and oxidative stress to improve the cardiac function.

Parole chiave

  • sacubitril
  • valsartan
  • doxorubicin-heart failure
  • inflammation
  • oxidative stress
  • natriuretic peptide
Accesso libero

Esters of quinoxaline-7-carboxylate-1,4-di-N-oxide as Trichomonas vaginalis triosephosphate isomerase inhibitors

Pubblicato online: 31 Dec 2020
Pagine: 485 - 495

Astratto

Abstract

Trichomoniasis is a public health problem worldwide. Trichomoniasis treatment consists of the use of nitroimidazole derivatives; however, therapeutic ineffectiveness occurs in 5 to 20 % of the cases. Therefore, it is essential to propose new pharmacological agents against this disease. In this work, esters of quinoxaline-7-carboxylate-1,4-di-N-oxide (EQX-NO) were evaluated in in vitro assays as novel trichomonicidal agents. Additionally, an in vitro enzyme assay and molecular docking analysis against triosephosphate isomerase of Trichomonas vaginalis to confirm their mechanism of action were performed. Ethyl (compound 12) and n-propyl (compound 37) esters of quinoxaline-7-carboxy-late-1,4-di-N-oxide derivatives showed trichomonicidal activity comparable to nitazoxanide, whereas five methyl (compounds 5, 15, 19, 20 and 22), four isopropyl (compounds 28, 29, 30 and 34), three ethyl (compounds 4, 13 and 23) and one npropyl (compound 35) ester derivatives displayed activity comparable to albendazole. Compounds 6 and 20 decreased 100 % of the enzyme activity of recombinant protein triosephosphate isomerase.

Parole chiave

  • quinoxaline 1
  • 4-di--oxide
  • trichomoniasis
  • triosephosphate isomerase inhibitor
12 Articoli
Accesso libero

Computer-aided approaches reveal trihydroxychroman and pyrazolone derivatives as potential inhibitors of SARS-CoV-2 virus main protease

Pubblicato online: 31 Dec 2020
Pagine: 325 - 333

Astratto

Abstract

COVID-19 was declared a pandemic by the World Health Organization (WHO) in March 2020. The disease is caused by severe acute respiratory syndrome coronavirus 2 (SARSCoV-2). The aim of this study is to target the SARS-CoV-2 virus main protease (Mpro) via structure-based virtual screening. Consequently, > 580,000 ligands were processed via several filtration and docking steps, then the top 21 compounds were analysed extensively via MM-GBSA scoring and molecular dynamic simulations. Interestingly, the top compounds showed favorable binding energies and binding patterns to the protease enzyme, forming interactions with several key residues. Trihydroxychroman and pyrazolone derivatives, SN02 and SN18 ligands, exhibited very promising binding modes along with the best MM-GBSA scoring of –40.9 and –41.2 kcal mol−1, resp. MD simulations of 300 ns for the ligand-protein complexes of SN02 and SN18 affirmed the previously attained results of the potential inhibition activity of these two ligands. These potential inhibitors can be the starting point for further studies to pave way for the discovery of new antiviral drugs for SARS-CoV-2.

Parole chiave

  • COVID-19
  • M
  • SARS-COV-2
  • antiviral
  • virtual screening
  • docking
Accesso libero

Melatonin as a powerful antioxidant

Pubblicato online: 31 Dec 2020
Pagine: 335 - 354

Astratto

Abstract

Melatonin is a hormone that has many body functions and, for several decades, its antioxidant potential has been increasingly talked about. There is a relationship between failure in melatonin production in the pineal gland, an insufficient supply of this hormone to the body, and the occurrence of free radical etiology diseases such as neurodegenerative diseases, cardiovascular diseases, diabetes, cancer and others. Despite the development of molecular biology, numerous in vitro and in vivo studies, the exact mechanism of melatonin antioxidant activity is still unknown. Nowadays, the use of melatonin supplementation is more and more common, not only to prevent insomnia, but also to slow down the aging process and provide protection against diseases. The aim of this study is to get acquainted with current reports on melatonin, antioxidative mechanisms and their importance in diseases of free radical etiology.

Parole chiave

  • melatonin
  • antioxidants
  • lipid peroxidation
  • free radicals
  • oxidative stress
Accesso libero

Cannabigerol and cannabichromene in Cannabis sativa L.

Pubblicato online: 31 Dec 2020
Pagine: 355 - 364

Astratto

Abstract

In addition to delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD), other phytocannabinoids, such as cannabigerol (CBG) and cannabichromene (CBC), also have beneficial effects on human health. A high content of CBG is found in plants with the B0 genotype, whereas CBC is independent of the allelic chemotype locus B. In basic research models such as mice or rats, CBG has demonstrated anticancer properties, particularly against breast cancer. CBG has shown anti-inflammatory effects on murine colitis and on inflammatory bowel disease as well as stimulatory effects on the feeding behaviors of mice. It has also exhibited inhibition of aldose reductase, which is known to cause an accumulation of sorbitol and increase glucose levels in the blood, which may lead to diabetes. Cannabinoid CBC has also shown anti-inflammatory effects and reduced hypermobility in the gut and has displayed potential in vitro effect on adult neural stem progenitor cells. CBC also exerts modest analgesic properties in rodents, as well as anti-fungal, anti-bacterial, pro-apoptotic, and anti-proliferative effects in tumor cells.

Parole chiave

  • cannabinoids
  • chemotype
  • health effects
  • hemp
  • receptors
Accesso libero

Preparation, characterization and antimicrobial assessment of selected ciprofloxacin salts

Pubblicato online: 31 Dec 2020
Pagine: 365 - 382

Astratto

Abstract

The formation of salts is considered a simple strategy to modify the physicochemical properties of active pharmaceutical ingredients. In this study, seven novel binary and ternary organic salts of ciprofloxacin (CP) were prepared with benzoic acid (BA), acetylsalicylic acid (ASA), p-coumaric acid (PCMA) and p-aminosalicylic acid (PASA). They were characterized by spectroscopic techniques and differential scanning calorimetry. Solubility and partition coefficients values were also measured. Evaluation of the antimicrobial activity of the organic salts against Staphylococcus aureus and Staphylococcus epidermidis revealed that most of the new salts had higher antimicrobial activity than CPHCl against both strains. The most active compounds against S. epidermidis and S. aureus were CP-PASA and CPPCMA, resp., which were up to fourteen times more potent than parent CP-HCl. Our findings indicated a strong correlation between the lipophilicity of the formed salts and their antimicrobial activity and showed that an optimum value of lipophilicity (log P = 0.75) seemed to be necessary to maximize the antimicrobial activity. These findings highlighted the improved physical, thermal and antimicrobial properties of the new salts of CP that can aid in providing higher bioavailability than CP-HCl.

Parole chiave

  • ciprofloxacin
  • salts
  • partition coefficient
  • Staphylococcus aureus
  • Staphylococcus epidermidis
Accesso libero

Ilex paraguariensis extract as an alternative to pain medications

Pubblicato online: 31 Dec 2020
Pagine: 383 - 398

Astratto

Abstract

Pain is a common and distressing symptom of many diseases and its clinical treatment generally involves analgesics and anti-inflammatory drugs. This study evaluated the toxicity of Ilex paraguariensis A. St.-Hil. (Aquifoliaceae) aqueous extract (leaves, petioles and branches) and its performance in a nociceptive response. Hepatotoxicity, psycho-stimulant test and evaluation of enzyme markers for liver damage were also tested. Chromatographic analysis by UPLC-MS demonstrated a series of isomeric monocaffeoylquinic acids, isomers of dicaffeoylquinic acid, flavonol glycosides, and saponins. Phase I and II of nociception were obtained for meloxicam, dexamethasone and aqueous Ilex paraguariensis extract. Ilex paraguariensis extract concentration was negatively correlated (R = –0.887) with alanine aminotransferase (p < 0.05) in acetaminophen-induced hepatotoxicity test, indicating hepatoprotective activity of this extract. Ilex paraguariensis extract also presented analgesic properties equivalent to drugs that already have proven efficacy. Notably, the administration of multiple doses of Ilex paraguariensis extract was considered safe from the therapeutic point of view.

Parole chiave

  • nociception
  • pain
  • hepatoprotection
  • toxicity
  • aqueous extract
  • UPLCMS
Accesso libero

Screening of six medicinal plant species for antileishmanial activity

Pubblicato online: 31 Dec 2020
Pagine: 399 - 414

Astratto

Abstract

This study is aimed to investigate the in vitro anti-leishmanial activity of ethanolic, aqueous or dichloromethane extracts of leaves, flowers, fruits or roots, of six medicinal plant species, namely, Nectandra megapotamica, Brunfelsia uniflora, Myrcianthes pungens, Anona muricata, Hymenaea stigonocarpa and Piper corcovandesis. After isolation and analysis of chemical components by ultra-high performance liquid chromatography-high-resolution tandem mass spectrometry (UHPLC-HRMS/MS), the extracts were also tested for toxicity in J774.A1 macrophages and human erythrocytes. Phenolic acids, flavonoids, acetogenins, alkaloids and lignans were identified in these extracts. Grow inhibition of promastigotes forms of Leishmania amazonensis and Leishmania braziliensis and the cytotoxicity in J774.A1 macrophages were estimated by the XTT method. The most promising results for L. amazonensis and L. braziliensis were shown by the ethanolic extract of the fruits of Hymenaea stigonocarpa and dichloromethane extract of the roots of Piper corcovadensis, with IC50 of 160 and 150 μg mL−1, resp. Ethanolic extracts of A. muricata (leaf), B. uniflora (flower and leaf), M. pungens (fruit and leaf), N. megapotamica (leaf), and aqueous extract of H. stigonocarpa (fruit) showed IC50 > 170 μg mL−1 for L. amazonensis and > 200 μg mL−1 for L. braziliensis. The extracts exhibited low cytotoxicity towards J774.A1 macrophages with CC50 > 1000 μg mL−1 and hemolytic activity from 0 to 46.1 %.

Parole chiave

  • Piper corcovadensis
  • Hymenaea stigonocarpa
  • antileishmanial
  • Leishmania amazonensis
  • Leishmania braziliensis
  • cytotoxicity
  • hemolysis
Accesso libero

Quantitative analysis and pharmacokinetic study of a novel diarylurea EGFR inhibitor (ZCJ14) in rat plasma using a validated LC-MS/MS method

Pubblicato online: 31 Dec 2020
Pagine: 415 - 428

Astratto

Abstract

1-(4-(Pyrrolidin-1-yl-methyl)phenyl)-3-(4-((3-(trifluoromethyl) phenyl)amino)quinazolin-6-yl)urea (ZCJ14), a novel epidermal growth factor receptor (EGFR) inhibitor, with diarylurea moiety, displays anticancer effect. In the present study, an LCMS/MS method was established to determine the concentration of ZCJ14 in rat plasma. Furthermore, the method was applied to investigate the pharmacokinetic characteristics of ZCJ14. Chromatographic separation of ZCJ14 and internal standard (IS) [1-phenyl-3-(4-((3-(trifluoromethyl)phenyl)amino) quinazolin-6-yl)urea] was accomplished by gradient elution using the Kromasil C18 column. The selected reaction monitoring transitions were performed at m/z 507.24→436.18 and 424.13→330.96 for ZCJ14 and IS, resp. The established method was linear over the concentration range of 10–1000 ng mL−1. The intra- and inter-day precisions were < 11.0 % (except for LLOQ which was up to 14.3 %) and the respective accuracies were within the range of 87.5–99.0 %. The extraction recovery and matrix effect were within the range of 88.4–104.5 % and 87.3–109.9 %, resp. ZCJ14 was stable under all storage conditions. The validated method was successfully applied to the pharmacokinetic study of ZCJ14 in rats, and the pharmacokinetic parameters have been determined. The oral bioavailability of ZCJ14 was found to be 46.1 %. Overall, this accurate and reliable quantification method might be useful for other diarylurea moiety-containing drugs.

Parole chiave

  • ZCJ14
  • epidermal growth factor receptor inhibitor
  • LC-MS/MS
  • pharmacokinetics
  • bioavailability
Accesso libero

Determination of carbohydrates in the herbal antidiabetic mixtures by GC-MC

Pubblicato online: 31 Dec 2020
Pagine: 429 - 443

Astratto

Abstract

Due to the wide range of biologically active substances, the herbal mixtures can influence the development of diabetes mellitus and its complications. Carbohydrates attract particular attention due to their hypoglycemic, hypolipidemic, anticholesterolemic, antioxidant, antiinflammatory and detoxifying activities. The aim of this study was to investigate the content of carbohydrates through their monomeric composition in the herbal mixture samples: a) Urtica dioica leaf, Cichorium intybus roots, Rosa majalis fruits, Elymys repens rhizome, Taraxacum officinale roots, b) Arctium lappa roots, Elymys repens rhizome, Zea mays columns with stigmas, Helichrysum arenarium flowers, Rosa majalis fruits, c) Inula helenium rhizome with roots, Helichrysi arenarium flowers, Zea mays columns with stigmas, Origanum vulgare herb, Rosa majalis fruits, Taraxacum officinale roots, d) Cichorium intybus roots, Elymys repens rhizome, Helichrysum arenarium flowers, Rosa majalis fruits, Zea mays columns with stigmas and e) Urtica dioica leaf, Taraxacum officinale roots, Vaccinium myrtillus leaf, Rosa majalis fruits, Mentha piperita herb, which were used in Ukrainian folk medicine for the prevention and treatment of diabetes mellitus type 2.

The carbohydrates were separated by gas chromatography-mass spectrometry after conversion into volatile aldononitrile acetate derivatives. The monomeric composition of polysaccharides was studied after their hydrolysis to form monosaccharides and poly-alcohols.

Quantitative analyses of free carbohydrates showed that the predominant sugars were fructose, glucose and disaccharide – sucrose, in all samples. Concerning the determination of polysaccharide monomers after hydrolysis, glucose was the most abundant in all samples. The chromatographic study revealed a number of polyalcohols that are important for the treatment and prevention of progression of diabetes mellitus and its complications, namely, mannitol, pinitol and myo-inositol.

Parole chiave

  • carbohydrates
  • herbal antidiabetic mixtures
  • GC-MS
  • monosaccharides
Accesso libero

Simplex lattice design for optimization of the mass ratio of Curcuma longa L., Curcuma zedoaria (Christm.) Roscoe and Curcuma aromatica Salisb. to maximize curcuminoids content and antioxidant activity

Pubblicato online: 31 Dec 2020
Pagine: 445 - 457

Astratto

Abstract

The aim of this work was to optimize the mass ratio of three Curcuma plants’ rhizomes to obtain the highest curcuminoid content and antioxidant activity using the simplex lattice design. The selected Curcuma plants were C. longa, C. zedoaria and C. aromatica. The simplex lattice design was applied in the work. The individual curcuminoids (curcumin, demethoxycurcumin and bis-demethoxycurcumin) and total curcuminoid content were determined using high-performance liquid chromatography. Curcuma longa alone provided the highest content of bis-demethoxycurcumin and demethoxycurcumin. A mixture of C. longa and C. aromatica in the mass ratio of 72:28 % provided the highest curcumin content. The results showed that C. longa alone exhibited the highest antioxidant activity.

Parole chiave

  • curcuminoids
  • HPLC
  • simplex lattice design
  • optimization
  • antioxidant activity
Accesso libero

Amygdalin isolated from Amygdalus mongolica protects against hepatic fibrosis in rats

Pubblicato online: 31 Dec 2020
Pagine: 459 - 471

Astratto

Abstract

The aim of this research was to investigate the effect of amygdalin on hepatic fibrosis in rats. Amygdalin was purified and identified from the seeds of Amygdalus mongo lica. Sprague Dawley rats in the control and model groups were administered water. Sprague Dawley rats were divided into the low-, middle-, and high-dose amygdalin groups that received 20, 40, and 80 mg kg−1 amygdalin, respectively. whereas the silymarin group was treated with 50 mg kg−1 silymarin. The control and model groups were administered water. Liver tissue analysis revealed significantly lower activities of ALT, AST, ALP, SOD, and MDA in the drug-treated groups compared to the model group. Serum analysis revealed significantly lower HYC and C-IV in the middle-dose amygdalin-treated group compared to the model group. The histopathological changes were less severe in the drug-treated groups as observed by the formation of pseudolobuli and decreased collagen fiber deposition. Hepatic fibrosis-related genes were expressed at significantly lower levels in the amygdalin-treated groups than in the model group. Amygdalin from A. mongolica represents a therapeutic candidate for hepatic fibrosis prevention and treatment.

Parole chiave

  • amygdalin
  • hepatic fibrosis
  • rat model
  • traditional Chinese medicine
Accesso libero

Effect of sacubitril/valsartan on inflammation and oxidative stress in doxorubicin-induced heart failure model in rabbits

Pubblicato online: 31 Dec 2020
Pagine: 473 - 484

Astratto

Abstract

Our study evaluates the effects of sacubitril/valsartan (SAC/VAL) in the rabbit model of doxorubicin-induced heart failure. Twenty rabbits (5 per group) were administered with doxorubicin (DOX, 1.5 mg kg−1, i.v.) to induce heart failure. Specific biomarkers such as BNP, CnT, CRP and ROMs were determined. The cardiac enzymatic anti-oxidant systems were recorded with their electrographic profiles. HR, SBP, DBP and MAP were restored at 5 or 10 mg kg−1 (p.o.) of SAC/VAL compared to DOX, followed by reduced levels of creatinine and BNP (p < 0.001). Significant improvements (p < 0.05) compared to DOX were also noticed in CAT, SOD and LPO with the same doses of SAC/VAL. Specific biomarkers such as BNP, CnT, CRP and ROMs descended significantly (p < 0.001) with treatment when compared to their baseline values. Our findings implied that SAC/VAL treatment reduced the inflammation and oxidative stress to improve the cardiac function.

Parole chiave

  • sacubitril
  • valsartan
  • doxorubicin-heart failure
  • inflammation
  • oxidative stress
  • natriuretic peptide
Accesso libero

Esters of quinoxaline-7-carboxylate-1,4-di-N-oxide as Trichomonas vaginalis triosephosphate isomerase inhibitors

Pubblicato online: 31 Dec 2020
Pagine: 485 - 495

Astratto

Abstract

Trichomoniasis is a public health problem worldwide. Trichomoniasis treatment consists of the use of nitroimidazole derivatives; however, therapeutic ineffectiveness occurs in 5 to 20 % of the cases. Therefore, it is essential to propose new pharmacological agents against this disease. In this work, esters of quinoxaline-7-carboxylate-1,4-di-N-oxide (EQX-NO) were evaluated in in vitro assays as novel trichomonicidal agents. Additionally, an in vitro enzyme assay and molecular docking analysis against triosephosphate isomerase of Trichomonas vaginalis to confirm their mechanism of action were performed. Ethyl (compound 12) and n-propyl (compound 37) esters of quinoxaline-7-carboxy-late-1,4-di-N-oxide derivatives showed trichomonicidal activity comparable to nitazoxanide, whereas five methyl (compounds 5, 15, 19, 20 and 22), four isopropyl (compounds 28, 29, 30 and 34), three ethyl (compounds 4, 13 and 23) and one npropyl (compound 35) ester derivatives displayed activity comparable to albendazole. Compounds 6 and 20 decreased 100 % of the enzyme activity of recombinant protein triosephosphate isomerase.

Parole chiave

  • quinoxaline 1
  • 4-di--oxide
  • trichomoniasis
  • triosephosphate isomerase inhibitor

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