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1.
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
2.
Molecules ; 24(18)2019 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-31491967

RESUMO

Alzheimer's disease (AD) is a widespread dynamic neurodegenerative malady. Its etiology is still not clear. One of the foremost pathological features is the extracellular deposits of Amyloid-beta (Aß) peptides in senile plaques. The interaction of Aß and the receptor for advanced glycation end products at the blood-brain barrier is also observed in AD, which not only causes the neurovascular anxiety and articulation of proinflammatory cytokines, but also directs reduction of cerebral bloodstream by upgrading the emission of endothelin-1 to induce vasoconstriction. In this process, RAGE is deemed responsible for the influx of Aß into the brain through BBB. In the current study, we predicted the interaction potential of the natural compounds vincamine, ajmalicine and emetine with the Aß peptide concerned in the treatment of AD against the standard control, curcumin, to validate the Aß peptide-compounds results. Protein-protein interaction studies have also been carried out to see their potential to inhibit the binding process of Aß and RAGE. Moreover, the current study verifies that ligands are more capable inhibitors of a selected target compared to positive control with reference to ΔG values. The inhibition of Aß and its interaction with RAGE may be valuable in proposing the next round of lead compounds for effective Alzheimer's disease treatment.


Assuntos
Peptídeos beta-Amiloides/química , Produtos Biológicos/química , Modelos Moleculares , Doença de Alzheimer , Aminoácidos , Peptídeos beta-Amiloides/antagonistas & inibidores , Peptídeos beta-Amiloides/metabolismo , Proteínas Amiloidogênicas/antagonistas & inibidores , Proteínas Amiloidogênicas/química , Sítios de Ligação , Produtos Biológicos/farmacologia , Humanos , Ligações de Hidrogênio , Ligantes , Conformação Molecular , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Ligação Proteica , Relação Estrutura-Atividade
3.
Bioorg Med Chem Lett ; 29(4): 623-630, 2019 02 15.
Artigo em Inglês | MEDLINE | ID: mdl-30595445

RESUMO

In the present investigation, new chloroquinoline derivatives bearing vinyl benzylidene aniline substituents at 2nd position were synthesized and screed for biofilm inhibitory, antifungal and antibacterial activity. The result of biofilm inhibition of C. albicans suggested that compounds 5j (IC50 value = 51.2 µM) and 5a (IC50 value = 66.2 µM) possess promising antibiofilm inhibition when compared with the standard antifungal drug fluconazole (IC50 = 40.0 µM). Two compounds 5a (MIC = 94.2 µg/mL) and 5f (MIC = 98.8 µg/mL) also exhibited good antifungal activity comparable to standard drug fluconazole (MIC = 50.0 µg/mL). The antibacterial screening against four strains of bacteria viz. E. coli, P. aeruginosa, B. subtilis, and S. aureus suggested their potential antibacterial activity and especially all the compounds except 5g were found more active than the standard drug ciprofloxacin against B. subtilis. To further gain insights into the possible mechanism of these compounds in biofilm inhibition through the agglutinin like protein (Als), molecular docking and molecular dynamics simulation studies were carried out. Molecular modeling studies suggested the clear role in inhibition of this protein and the resulting biofilm inhibitory activity.

4.
Biomed Res Int ; 2013: 985259, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23984426

RESUMO

Guar Gum is a natural polysaccharide that, due to its physicochemical properties, is extensively investigated for biomedical applications as a matrix for modified drug delivery, but it is also used in the food industry as well as in cosmetics. A commercial sample of Guar Gum was sonicated for different periods of time, and the reduction in the average molecular weight was monitored by means of viscometric measurements. At the same time, the rheological behaviour was also followed, in terms of viscoelasticity range, flow curves, and mechanical spectra. Sonicated samples were used for the preparation of gels in the presence of borate ions. The effect of borax on the new samples was investigated by recording mechanical spectra, flow curves, and visible absorption spectra of complexes with Congo Red. The anisotropic elongation, observed in previous studies with tablets of Guar Gum and borax, was remarkably reduced when the sonicated samples were used for the preparation of the gels.


Assuntos
Fenômenos Químicos , Sistemas de Liberação de Medicamentos , Galactanos/química , Mananas/química , Gomas Vegetais/química , Sonicação/métodos , Boratos/química , Cromatografia em Gel , Elasticidade , Espectroscopia de Ressonância Magnética , Conformação Molecular , Peso Molecular , Reologia , Soluções , Fatores de Tempo , Viscosidade , Água/química
5.
Molecules ; 17(3): 2283-97, 2012 Feb 24.
Artigo em Inglês | MEDLINE | ID: mdl-22367024

RESUMO

Scleroglucan is a natural polysaccharide that has been proposed for various applications. However there is no investigation on its property variations when the molecular weight of this polymer is reduced. Scleroglucan was sonicated at two different polymer concentrations for different periods of time and the effect of sonication was investigated with respect to molecular weight variations and rheological properties. Molar mass, estimated by viscometric measurements, was drastically reduced already after a sonication for a few min. Sonicated samples were used for the preparation of gels in the presence of borate ions. The effect of borax on the new samples was investigated by recording the mechanical spectra and the flow curves. A comparison with the system prepared with the dialysed polymer was also carried out. The anisotropic elongation, observed with tablets of scleroglucan and borax, was remarkably reduced when the sonicated samples were used for the preparation of the gels.


Assuntos
Glucanos/química , Hidrogéis/química , Anisotropia , Boratos/química , Elasticidade , Peso Molecular , Reologia , Sonicação , Viscosidade , Água , Molhabilidade
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