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1.
Drug Des Devel Ther ; 14: 27-41, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32021089

RESUMO

Background: Naproxen (NP) is a non-steroidal anti-inflammatory drug with poor aqueous solubility and low oral bioavailability, which may lead to therapeutic failure. NP causes crucial GIT irritation, bleeding, and peptic and duodenal ulcers. Purpose of the study: This study aimed to engineer and characterize polymer hybrid enteric microspheres using an integrated (experimental and molecular modelling) approach with further development to solid dosage form with modified drug release kinetics and improved bioavailability. Materials and methods: NP loaded polymer hybrid enteric microspheres (PHE-Ms) were fabricated by using a modified solvent evaporation technique coupled with molecular modelling (MM) approach. The PHE-Ms were characterized by particle size, distribution, morphology, crystallinity, EE, drug-polymer compatibility, and DSC. The optimized NP loaded PHE-Ms were further subjected to downstream procedures including tablet dosage form development, stability studies and comparative in vitro-in vivo evaluation. Results: The hydrophobic polymer EUD-L100 and hydrophilic polymer HPMC-E5 delayed and modified drug release at intestinal pH while imparting retardation of NP release at gastric pH to diminish the gastric side effects. The crystallinity of the NP loaded PHE-Ms was established through DSC and P (XRD). The particle size for the developed formulations of PEH-Ms (M1-M5) was in the range from 29.06 ±7.3-74.31 ± 17.7 µm with Span index values of 0.491-0.69, respectively. The produced NP hybrid microspheres demonstrated retarded drug release at pH 1.2 and improved dissolution at pH 6.8. The in vitro drug release patterns were fitted to various release kinetic models and the best-followed model was the Higuchi model with a release exponent "n" value > 0.5. Stability studies at different storage conditions confirmed stability of the NP loaded PHE-Ms based tablets (P<0.05). The molecular modelling (MM) study resulted in adequate binding energy of co-polymer complex SLS-Eudragit-HPMC-Naproxen (-3.9 kcal/mol). In contrast to the NP (unprocessed) and marketed formulations, a significant increase in the Cmax of PHE-MT1 (44.41±4.43) was observed. Conclusion: The current study concludes that developing NP loaded PHE-Ms based tablets could effectively reduce GIT consequences with restored therapeutic effects. The modified release pattern could improve the dissolution rate and enhancement of oral bioavailability. The MM study strengthens the polymer-drug relationship in microspheres.

2.
Artigo em Inglês | MEDLINE | ID: mdl-31827560

RESUMO

Background: Rosmarinus officinalis (R. officinalis) is a medicinal plant called rosemary, largely used in the Mediterranean diet for many decades ago. Objective: The aim of the present study was to investigate the polyphenolic content, the antioxidant activity, and the antiproliferative effect against human prostate cancer cell lines (LNCaP) of carnosol and carnosic acid as bioactive compounds contained in R. officinalis growing in Morocco. Materials and Methods: Polyphenolic content of R. officinalis ethanolic extract was studied using colorimetric assay. Carnosol and carnosic acid contained in R. officinalis extract were quantified using high-performance liquid chromatography (HPLC). The antiproliferative effect of the studied extracts on LNCaP was evaluated by WST-1 bioassay, and the antioxidant activity was assessed using DPPH assay. Results: The extracts of R. officinalis showed an important polyphenolic content ranging from 74.15 µg·GAE/mg to 146.63 µg·GAE/mg. The percentage of carnosol and carnosic acid in rosemary crops ranges from 11.7 to 17.3% and 1.09% to 3%, respectively. The extracts of R. officinalis exhibited a promoting antioxidant activity with IC50 ranging from 0.236 mg/mL to 0.176 mg/mL. Regarding the antiproliferative effect, the WST-1 assay revealed that all the tested extracts reduced notably the cell viability with IC50 values ranging from 14.15 to 15. 04 µg/mL. Conclusion: In the current work, carnosol and carnosic acid exhibit antioxidant and antiproliferative activities in a concentration-dependent manner.

3.
J Photochem Photobiol B ; 201: 111643, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31698218

RESUMO

Diabetes is a major emerging health consequence across the world which directly associated with the obesity. Contemporary anti-diabetic drugs have numeral limitations, and investigation of herbal remedies for diabetes give novel guide for the expansion of new drugs that can be used as harmonizing to present anti-diabetic allopathic medications. Gold nanoparticles (AuNPs) of 21 nm have been formerly well portrayed in vitro for their capability to intend active uptake in cell. Our present study was dealing with the synthesis of gold nanoparticles by means of Smilax glabra rhizome amend the anti-obesity constraints in high-fat diet by streptozotocin provoked obese diabetes in rat model. Characterization studies like UV -Spectroscopy, XRD analysis, SEM, TEM microscopy, Energy Dispersive X-Ray Spectroscopy, and FT-IR investigation confirms the availability of dimension, shape and size. Biochemical parameters like blood glucose and insulin sufferance and its release, lipid profile, aterogenic & coronary index, liver markers, inflammatory markers, hormones like leptin, resistin, adiponectin indicates the therapeutic effect of gold nanoparticles harvested from Smilax glabra on obese and diabetic rats. Histopathological examinations displayed the disturbed internal structures of obese and diabetic rats liver and heart tissues. Whereas, treatment with gold nanoparticles synthesized from Smilax glabra restored the internal membrane, nuclei and cytoplasm. All these findings confirmed the anti-obesity and anti-diabetic effect of synthesized gold nanoparticles from Smilax glabra.


Assuntos
Diabetes Mellitus Experimental/patologia , Dieta Hiperlipídica , Ouro/química , Nanopartículas Metálicas/química , Smilax/química , Animais , Glicemia/análise , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Coração/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Masculino , Nanopartículas Metálicas/uso terapêutico , Nanopartículas Metálicas/toxicidade , Miocárdio/metabolismo , Miocárdio/patologia , Extratos Vegetais/química , Ratos , Ratos Wistar , Rizoma/química , Rizoma/metabolismo , Smilax/metabolismo , Estreptozocina/toxicidade
4.
J Photochem Photobiol B ; 201: 111657, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31706085

RESUMO

Parkinson's disease (PD) is a general neurodegenerative disorder which largely has an effect on the society of the aged populations. PD is distinguishedwith loss of dopaminergic (DA) neurons in the substantia nigra. The exceptional properties of gold nanoparticles (AuNPs) have fascinated great attention in biomedical applications. In this present study, we explored theprospective beneficial effects of AuNPs synthesized from Cinnamomum verum on PD. PD rat models were established through MPTP injection treatment and AuNPs was administered. Administration of AuNPs reduces effect of MPTP-induced oxidative stress and motor abnormalities observed in PD rats. In addition ELISA analysis demonstrated that AuNPs treatment significantly attenuates Tumor Necrosis Factor-α (TNF-α), Interleukin-1ß (IL-1ß) and Interleukin-6 (IL-6) expression levels. Consequently, we investigated TLR/NF-κB pathway to examine the function of AuNPs on MPTP- induced PD rats. We found that AuNPs suppressed the alterations in the pathway of TLR/NF-κB associated molecules in MPTP stimulated PD rats. Hence, our results suggest that AuNPs attenuates MPTP introduced motor disorders, oxidative stress, activated inflammatory cytokines and activated TLR/NF-κB signaling in PD rats. In conclusion, AuNPs ease PD symptoms by the inhibition of TLR/NF-κB signaling pathway and recommend promise approach in the treatment of neurodegenerative diseases such as PD.


Assuntos
Cinnamomum zeylanicum/química , Ouro/química , Intoxicação por MPTP/tratamento farmacológico , Nanopartículas Metálicas/uso terapêutico , Animais , Cinnamomum zeylanicum/metabolismo , Citocinas/metabolismo , Química Verde , Intoxicação por MPTP/patologia , Masculino , Nanopartículas Metálicas/química , Nanopartículas Metálicas/toxicidade , Camundongos , NF-kappa B/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley , Transdução de Sinais/efeitos dos fármacos , Receptores Toll-Like/metabolismo
5.
Chem Biol Drug Des ; 94(4): 1750-1759, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31145839

RESUMO

In continuation with our research program on the development of novel bioactive molecules, we report herein the design and synthesis of a series of diversified heterocycles (4-22). The synthesized compounds were evaluated for their anti-inflammatory activity. The chemical structures of the newly synthesized compounds have been confirmed by NMR, FTIR, and microanalysis.

6.
Artigo em Inglês | MEDLINE | ID: mdl-31029221

RESUMO

Thiouracil, 2-sulfanylidene-1H-pyrimidin-4-one, has been used as anti-thyroid, coronary vasodilator, and in congestive heart failure. It was found to cause agranulocytosis and it is suspected to be teratogenic and carcinogenic. Owing to its high frequency of adverse reactions, especially agranulocytosis, its use was abandoned in favor of other, less toxic drugs, such as propylthiouracil and methimazole. Thiouracil refers both to a specific molecule consisting of a sulfated uracil and a family of molecules based upon the structure. An important member of this family is propylthiouracil, which is a thiourea antithyroid drug that acts by blocking the production of thyroid hormones; it also inhibits the peripheral deiodination of thyroxine to tri-iodothyronine. This profile is prepared to discuss and explain physical and chemical properties, proprietary and nonproprietary names of thiouracil and propylthiouracil. It also includes uses and applications, methods of preparation, thermal and spectral behavior and methods of analysis. In addition, metabolism, excretion and pharmacology of propylthiouracil are also discussed.


Assuntos
Antitireóideos/farmacologia , Tiouracila/farmacologia , Antitireóideos/química , Metimazol , Propiltiouracila , Tiouracila/química , Tiroxina
7.
Artigo em Inglês | MEDLINE | ID: mdl-31029222

RESUMO

Topiramate, 2,3:4,5-di-O-isopropylidene-ß-d-fructopyranose sulfamate, is a potent antiepileptic drug with a broad spectrum of activity. It is effective in both partial and generalized seizures. Topiramate was also found to have significant efficacy in migraine prevention with considerable reductions in the frequency of migraine headaches. The most common adverse events, which may accompany the use of topiramate, are paresthesia, fatigue, decreased appetite, nausea, diarrhea, weight decrease and taste perversion. The weight loss observed with the use of topiramate in obese, epileptic patients, afforded the approval of this drug as an anti-obesity medication. This action is thought to be based on the selective inhibition of mitochondrial carbonic anhydrase isoforms. This profile is prepared to discuss and explain physical characteristics, proprietary and nonproprietary names of topiramate. It also includes methods of preparation, thermal and spectral behavior and methods of analysis. Pharmacokinetics, metabolism, excretion and pharmacology together with its uses and applications are also discussed.


Assuntos
Anticonvulsivantes/farmacologia , Topiramato/farmacologia , Anticonvulsivantes/química , Epilepsia/tratamento farmacológico , Humanos , Transtornos de Enxaqueca/tratamento farmacológico , Topiramato/química
8.
Biomed Res Int ; 2019: 9873146, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31950062

RESUMO

Background: Prickly pear (Opuntia spp.), called Barbary fig, is a cultivated species springing from family Cactaceae. It is native to Mexico and has been naturalized in other continents, especially the Mediterranean countries (North Africa). The aim of the study was to investigate the physical, physicochemical, and biochemical criteria of peels of three Moroccan prickly pear varieties (Aakria, Derbana, and Mles) growing in the Rhamna regions (dry area). Material and Methods: Both physicochemical characteristics (humidity, water activity, Brix, ash content, pH, and total titratable acidity) and biochemical characteristics (total carotenoid content, betalain content, total polyphenolic content, and ascorbic acid content) were were studied according to previously reported methods. Results: Regarding the physiochemical criteria, the moisture of the fresh peels of studied varieties ranged from 81.59 ± 0.02 to 83.47 ± 0.02%. The water activity (aw) ranged from 0.862 ± 0.001 to 0.872 ± 0.001. The values of Brix varied from 14.69 ± 0.05° Bx to 15.80 ± 0.03° Bx. pH values varied from 5.13 ± 0.01 to 5.32. The total titratable acidity values ranged from 0.130 ± 0.008 to 0.196 ± 0.014 g of citric acid/100 g of FM (fresh matter). The ash content values ranged from 8.92 ± 0.10 to 11.04 ± 0.06 g/100 g of FM. Regarding the biochemical criteria, the total carotenoid content ranged from 2.29 ± 0.01 to 2.87 ± 0.01 µg/g of FM. The total betalain content ranged from 6213.46 ± 58.86 to 8487.19 ± 51.71 µg/100 g of FM. The total polyphenolic content varied from 160 ± 3.55 to 243.79 ± 5.55 mg GA E/100 g of FM. The ascorbic content ranged from 58.21 ± 0.24 to 74.72 ± 0.17 mg/100 g of FM. Conclusion: The findings of physicochemical and biochemical criteria of the investigated varieties growing in Moroccan drylands showed promising results in terms of studied parameters.

9.
Front Chem ; 6: 294, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30073161

RESUMO

Formyl glycals are the versatile synthetic intermediates and can serves as precursor for the synthesis of various C and N-nucleosides. Due to the presence of electron donating and electron withdrawing character on formyl sugars which makes the molecule more susceptible to nucleophilic attack. Utilizing same strategy, we propose the synthesis of diversified C-nucleosides (3-14) by reaction with N,N dinucleophiles. These nucleoside analogs were than tested against viral, bacterial and fungal strains.

10.
J Nat Prod ; 80(6): 1900-1908, 2017 06 23.
Artigo em Inglês | MEDLINE | ID: mdl-28581290

RESUMO

Teucrium yemense (Defl), locally known as Reehal Fatima, is a medicinal plant commonly grown in Saudi Arabia and Yemen. Phytochemical investigation of the aerial parts of T. yemense yielded six new neoclerodane diterpenoids, namely fatimanol A-E (1, 2, 3, 5, and 6) and fatimanone (4), and the known teulepicephin (7). As both the Teucrium genus and the related Lamiaceae family have previously been widely reported to possess anthelmintic and antimicrobial activities, the structural and biological characterization of the seven diterpenoids was pursued. The structures of the new compounds were elucidated from their 2D NMR and MS profiles and by comparison to related compounds. The structure of fatimanol D (5) was confirmed by X-ray crystallographic analysis. The new structures contribute to the breadth of knowledge of secondary metabolites in this genus.


Assuntos
Diterpenos/isolamento & purificação , Lamiaceae/química , Plantas Medicinais/química , Teucrium/química , Candida albicans/efeitos dos fármacos , Cristalografia por Raios X , Diterpenos/química , Diterpenos Clerodânicos , Escherichia coli/efeitos dos fármacos , Células Hep G2 , Humanos , Testes de Sensibilidade Microbiana , Conformação Molecular , Estrutura Molecular , Mycobacterium smegmatis/efeitos dos fármacos , Ressonância Magnética Nuclear Biomolecular , Pseudomonas aeruginosa/efeitos dos fármacos , Arábia Saudita , Staphylococcus aureus/efeitos dos fármacos
13.
Acta Crystallogr Sect E Struct Rep Online ; 68(Pt 2): o487, 2012 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-22347090

RESUMO

The title ketal, C(12)H(14)FNO(3), crystallized with two independent molecules in the asymmetric unit. In each molecule the fused ring system is essentially planar [maximum deviations of 0.0169 (11) and 0.0402 (13) Å]. The mol-ecules are each hydrogen bonded across a center of inversion into a dimer; adjacent dimers are linked by another N-H⋯O hydrogen bond, forming a chain running along [100].

14.
Acta Crystallogr Sect E Struct Rep Online ; 68(Pt 2): o491, 2012 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-22347093

RESUMO

In the title compound, C(14)H(15)NO, the torsion angle about the two Csp(3) atoms adopts a partially eclipsed conformation [-61.5 (1)°]. The dihedral angle between the two rings is 48.1 (1)°. In the crystal, the mol-ecules are connected by O-H⋯N and N-H⋯O hydrogen bonds into zigzag chains running along [010]. One of the amino H atoms is not involved in hydrogen bonding.

15.
Acta Crystallogr Sect E Struct Rep Online ; 68(Pt 2): o492, 2012 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-22347094

RESUMO

The dihedral angle between the two phenyl rings in the title compound, C(15)H(17)NO, is 52.9 (1)°. In the crystal, the mol-ecules are connected by O-H⋯N hydrogen bonds into centrosymmetric dimers. The amino H atom is not involved in hydrogen bonding.

16.
Artigo em Inglês | MEDLINE | ID: mdl-22259388

RESUMO

The title compound, C(13)H(12)N(6)O, is a functionalized ditriazoloquinazoline with substituted eth-oxy and methyl groups attached at the 2-position of each triazole spacer. The fused-ring system is essentially planar [r.m.s. deviation = 0.016 (2) Å]. In the crystal, a weak C-H⋯N hydrogen bond connects the mol-ecules into a chain along [101].

17.
Acta Crystallogr Sect E Struct Rep Online ; 67(Pt 3): o693, 2011 Feb 23.
Artigo em Inglês | MEDLINE | ID: mdl-21522438

RESUMO

In the title mol-ecule, C(14)H(15)N(3)O(4)S, the pyrazole ring is aligned at a dihedral angle of 55.5 (1)° with respect to the benzene ring; the mean planes of the acetyl substituents are twisted by 13.4 (3) and 30.1 (3)° with respect to the pyrazole ring. Inter-molecular classical N-H⋯O and weak C-H⋯O hydrogen bonding links the mol-ecules, forming a three-dimensional network architecture in the crystal structure.

18.
Acta Crystallogr Sect E Struct Rep Online ; 67(Pt 3): o694, 2011 Feb 23.
Artigo em Inglês | MEDLINE | ID: mdl-21522439

RESUMO

In the title compound, C(27)H(21)N(3)O(2), the non-H atoms of the meth-oxy-phenyl-acryloyl substitutent of the pyrazolyl ring are almost co-planar (r.m.s. deviation = 0.070 Å), and the mean plane is twisted by 18.7 (1)° with respect to the pyrazolyl ring. The phenyl and tolyl substituents are aligned at 48.9 (1) and 44.5 (1)° with respect to the pyrazolyl ring. Weak inter-molecular C-H⋯O and C-H⋯N hydrogen bonding is present in the crystal structure.

19.
Acta Crystallogr Sect E Struct Rep Online ; 67(Pt 3): o695, 2011 Feb 23.
Artigo em Inglês | MEDLINE | ID: mdl-21522440

RESUMO

In the crystal structure of the title compound, C(30)H(24)N(4)O(2)S, the dihydro-quinoxaline fused-ring system is disordered over three orientations in a 0.358 (2):0.318 (3):0.324 (3) ratio; the mean planes of the non-H atoms of the disorder components are aligned at 4.0 (3), 11.8 (4) and 41.7 (2)° with respect to the pyrazole ring. The rings of the phenyl and tolyl substituents are aligned at 64.0 (1) and 43.7 (1)° with respect to the pyrazole ring. Weak intermolecular C-H⋯O hydrogen bonding links the mol-ecules, forming supra-molecular chains running along the a axis.

20.
Acta Crystallogr Sect E Struct Rep Online ; 67(Pt 3): o696, 2011 Feb 23.
Artigo em Inglês | MEDLINE | ID: mdl-21522441

RESUMO

In the title compound, C(11)H(9)BrO(3), the benzofuran fused-ring system is almost planar, with a maximum atomic deviation of 0.024 (5) Å; the carboxyl -CO(2) fragment is aligned at 4.8 (7)° with respect to the fused-ring plane. Weak inter-molecular C-H⋯O hydrogen bonding is present in the crystal structure. π-π stacking is also observed between parallel mol-ecules, the centroid-centroid distance between benzene and furan rings of adjacent mol-ecules being 3.662 (3) Å.

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