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1.
Cureus ; 16(6): e62197, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-39006606

RESUMO

Aim To assess the antimicrobial activity of herbal, homeopathic, and conventional dentifrices against oral microorganisms. Methodology Mueller Hilton agar was used to cultivate distinct strains of Streptococcus mutans and Enterococcus faecalis, whereas Candida albicans was cultured on a potato dextrose agar medium. Diffusion ratios of 1:5, 1:10, and 1:15 were obtained by diluting 1 gram of each dentifrice (KP Namboodiri, Homeodent, and Colgate Strong Teeth) in 4 ml, 9 ml, and 14 ml of distilled water, respectively. The culture medium was filled with sterile discs. Twenty µl of each dilution of prepared dentifrice formulations were incorporated using a micropipette. The agar plates were incubated for 24 hours at 37ºC. Result The findings indicate that there was a higher zone of inhibition against Streptococcus mutans with herbal dentifrice at 10 mm, 8 mm, and 6.5 mm, followed by conventional dentifrice at 10 mm, 7.5 mm, and 7 mm, and the lowest with homeopathic dentifrice at 8 mm, 7 mm, and 7 mm at 1:5, 1:10 and 1:15 dilutions, respectively. Conventional dentifrice was found to inhibit Enterococcus faecalis at 9 mm, 8 mm, and 7 mm with 1:5, 1:10, and 1:15 dilutions followed by herbal dentifrice at 9 mm, 7 mm with 1:5, 1:10 dilutions, and no inhibition at 1:15 dilution. In contrast, homeopathic dentifrice displayed no inhibition at 1:5, 1:10, and 1:15 dilutions. Neither homeopathic nor conventional dentifrices inhibited Candida albicans, but herbal dentifrices showed a 10 mm zone of inhibition at 1:10 dilution. Conclusion Conventional and herbal dentifrices were found to be more effective against Streptococcus mutans than the homeopathic dentifrice used in the study, whereas herbal dentifrice was more effective against Candida albicans when compared to conventional and homeopathic dentifrices.

2.
J Pharm Bioallied Sci ; 16(Suppl 2): S1515-S1521, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38882729

RESUMO

Periodontitis and oral squamous cell carcinoma (OSCC) are prevalent oral diseases with distinct etiologies, yet they share certain molecular and biological characteristics. Gene expression datasets from the gene expression omnibus (GEO) repository (GSE30784 for OSCC and GSE10334 for periodontitis) were analyzed. Data preprocessing and differential gene expression analysis using GEO2R identified common differentially expressed genes (DEGs), and FunRich software facilitated the construction of a protein-protein interaction (PPI) network on the STRING database. Cytoscape, coupled with the CytoHubba plugin, identified Cluster of Differentiation 19 (CD19) and Von Willebrand Factor (VWF) as the top hub genes, with Complement C3 (C3) also highly ranked. Functional enrichment analysis highlighted pathways such as the B-cell receptor signaling pathway, complement and coagulation cascades, and hematopoietic cell lineage. Additionally, miRNet analysis identified key miRNAs, including hsa-mir-26a-5p, hsa-mir-129-2-3p, and hsa-mir-27a-3p, associated with these pathways. These findings suggested an association of molecular mechanisms between periodontitis and OSCC, with identified hub genes and miRNAs potentially serving as therapeutic targets.

3.
Mol Divers ; 2023 Jun 20.
Artigo em Inglês | MEDLINE | ID: mdl-37338672

RESUMO

NF-κB has become a predominant regulator responsible for multiple physiological and pathological processes. NF-κB signaling pathway has canonical and non-canonical components which strategize the cancer-related metabolic processes. Non-canonical NF-κB pathways are known to contribute towards the chemoresistance of cancer cells. Consequently, NF-κB can be utilized as a potential therapeutic target for modifying the behaviour of tumor cells. In view of this, we herein report a series of pyrazolone-based bioactive ligands that potentially target NF- κB and, thereby, unveil their anticancer properties. The pharmacological screening of the synthesized compounds were carried out using various virtual screening techniques. The anticancer studies of synthesized pyrazolones showed that APAU exhibited the most potent effect against the MCF-7 cells with an IC50 value of 30 µg/ml. Molecular docking studies revealed that the pyrazolones inhibited cell proliferation by targeting the NFκB signaling pathway. The molecular dynamics simulation studies predicted the stability and flexibility of pyrazolone-based bioactive ligands.

4.
Ayu ; 40(2): 114-119, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-32398912

RESUMO

BACKGROUND: Stress is a potential contributer to chronic hyperglycemia. Pitta Prakriti (body constitution) individuals are more prone to stress and the prevalence of type 2 diabetes in stressed out individuals is much more. Aim of study was to evaluate the role of stress in hyperglycemia in individuals of Pitta predominant constitution and to assess the effectiveness of Mahatiktaka Kashaya in stress-induced hyperglycemia. METHODOLOGY: A cross-sectional study was carried out in 100 Pitta predominant patients having fasting blood sugar level greater than 140 mg/dl, to find the association of stress and hyperglycemia, using International Stress Management Association questionnaire followed by open lebelled clinical trial with Mahatiktaka Kashaya (Decoction). Trial drug was administered at a dose of 15 ml twice daily for 14 days. Assessment was done before and after the treatment. OBSERVATION AND ANALYSIS: 80% of Pitta predominant individuals have reported stress-associated hyperglycemia. Overall effect of Mahatiktaka Kashaya in major domains of Stress Assessment Questionnaire, i.e., symptoms, stability and strategies was significant. Furthermore, the trial drug showed significant improvement in biochemical parameters of diabetes. CONCLUSION: The study concludes that there is significant association between stress and hyperglycemia in the individuals of Pitta constitution. Mahatiktaka Kashaya is found to be highly significant in stress-associated hyperglycemia in the above said group.

5.
RSC Adv ; 8(37): 20630-20636, 2018 Jun 05.
Artigo em Inglês | MEDLINE | ID: mdl-35542326

RESUMO

We studied the conductivity relaxation originating from a glass-former composed of cations and anions, and the relation to the structural α-relaxation at temperatures above and below the glass transition temperature. The material chosen was amorphous amlodipine besylate (AMB), which is also a pharmaceutical with a complex chemical structure. Measurements were made using differential scanning calorimetry (DSC), broadband dielectric spectroscopy (BDS) and X-ray diffraction, and the characterization was assisted using density functional theory (DFT). The X-ray diffraction pattern confirms the amorphous nature of vitrified AMB. Both the ionic and dipolar aspects of the dynamics of AMB were examined using these measurements and were used to probe the nature of the secondary conductivity and dipolar relaxations and their relation to the conductivity α-relaxation and the structural α-relaxation. The coupling model predictions and quantum mechanical simulations were used side by side to reveal the properties and nature of the secondary conductivity relaxation and the secondary dipolar relaxation. Remarkably, the two secondary relaxations have the same relaxation times, and are one and the same process performing dual roles in conductivity and dipolar relaxations. This is caused by the translation-rotation coupling of the AMB molecule. Thus, AMB has both conductivity α- and ß-relaxations, and application of the coupling model shows that these two relaxations are related in the same way as the structural α-relaxation and the Johari-Goldstein ß-relaxation are. This important result has an impact on the fundamental understanding of the dynamics of ionic conductivity.

6.
Biotechnol Prog ; 29(5): 1222-9, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23804494

RESUMO

Nylon 6 capillary-channeled polymer (C-CP) fibers are investigated as an alternative support/stationary phase for downstream processing of macromolecules. Ionizable amine and carboxylic acid end groups on the native fiber surface allow for ion exchange chromatography (IEC). The low cost and ability to operate at high linear velocities and low back pressures are practical advantages of C-CP fibers for preparative-scale macromolecule separations. The lack of fiber porosity ensures facile adsorption/desorption that is conducive to high throughput and recoveries/yields. Described here is a preliminary investigation of the processing characteristics of lysozyme on nylon 6 fibers with an eye toward downstream processing applications. Fibers were packed into microbore (0.8 mm i.d.) and analytical-size (2.1 mm i.d.) columns for the evaluation of the role of linear velocity on pressure drop, frontal throughput, and yield. Protein isolation by frontal development involved three steps: loading of the column to breakthrough, an aqueous wash, and a salt wash to recover the protein. Frontal throughput was evaluated with different salt concentrations (0-1000 mM NaCl) and different linear velocities (6-24 mm s(-1)). The observed throughput values are in the range of 0.12-0.20 mg min(-1) when 0.25 mg mL(-1) lysozyme (in 20 mM Tris-HCl) is loaded onto 78 mg of C-CP fiber in 0.52 mL volume analytical columns. Increased throughput and yield were found when protein was loaded and eluted at high linear velocity. Results of this study lend credence to the further development of C-CP fibers for biomacromolecule processing on larger scales.


Assuntos
Caprolactama/análogos & derivados , Polímeros/química , Proteínas/química , Adsorção , Ação Capilar , Caprolactama/química , Cromatografia por Troca Iônica , Estudos de Avaliação como Assunto , Muramidase/metabolismo , Porosidade , Sais
7.
BMC Biotechnol ; 13: 37, 2013 Apr 26.
Artigo em Inglês | MEDLINE | ID: mdl-23622112

RESUMO

BACKGROUND: Recent research on nanoparticles in a number of crops has evidenced for enhanced germination and seedling growth, physiological activities including photosynthetic activity and nitrogen metabolism, mRNA expression and protein level, and also positive changes in gene expression indicating their potential use in crop improvement. We used a medicinally rich vegetable crop, bitter melon, as a model to evaluate the effects of seed treatment with a carbon-based nanoparticle, fullerol [C60(OH)20], on yield of plant biomass and fruit characters, and phytomedicine contents in fruits. RESULTS: We confirmed the uptake, translocation and accumulation of fullerol through bright field imaging and Fourier transform infra-red spectroscopy. We observed varied effects of seed treatment at five concentrations, including non-consequential and positive, on plant biomass yield, fruit yield and its component characters, and content of five phytomedicines in fruits. Fullerol-treatment resulted in increases up to 54% in biomass yield and 24% in water content. Increases of up to 20% in fruit length, 59% in fruit number, and 70% in fruit weight led to an improvement up to 128% in fruit yield. Contents of two anticancer phytomedicines, cucurbitacin-B and lycopene, were enhanced up to 74% and 82%, respectively, and contents of two antidiabetic phytomedicines, charantin and insulin, were augmented up to 20% and 91%, respectively. Non-significant correlation inter se plant biomass, fruit yield, phytomedicine content and water content evidenced for separate genetic control and biosynthetic pathways for production of plant biomass, fruits, and phytomedicines in fruits, and also no impact of increased water uptake. CONCLUSIONS: While our results indicated possibility of improving crop yield and quality by using proper concentrations of fullerol, extreme caution needs to be exercised given emerging knowledge about accumulation and toxicity of nanoparticles in bodily tissues.


Assuntos
Biomassa , Fulerenos/química , Momordica charantia/crescimento & desenvolvimento , Nanotecnologia , Carotenoides/biossíntese , Frutas/química , Frutas/metabolismo , Fulerenos/metabolismo , Fulerenos/farmacologia , Germinação/efeitos dos fármacos , Glucosídeos/biossíntese , Insulina/genética , Insulina/metabolismo , Licopeno , Momordica charantia/metabolismo , Plântula/efeitos dos fármacos , Plântula/metabolismo , Espectroscopia de Infravermelho com Transformada de Fourier , Distribuição Tecidual , Triterpenos/metabolismo , Água/metabolismo
8.
J Sep Sci ; 35(23): 3270-80, 2012 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-23109248

RESUMO

Polypropylene (PP) capillary-channeled polymer (C-CP) fiber stationary phases are investigated for applications in HPLC. Specifically, the roles that fiber size and shape, linear velocity, interstitial fraction, and column inner diameter play in separation efficiency were evaluated using a uracil and butylparaben mixture eluted under isocratic conditions. Four fiber types, having nominal diameters ranging from 30 to 65 µm, were used in 250 mm × 2.1 mm columns. Optimum flow characteristics, as judged by plate height and resolution, were observed for 40 µm diameter PP C-CP fibers packed at an interstitial fraction of ~0.63, over a broad range of linear velocities (~2 to 37 mm/s). The influence of column inner diameter was studied on 1.5, 2.1, and 4.6 mm columns packed at the optimal interstitial fraction. The best performing column in terms of plate height and resolution was the 2.1 mm inner diameter. C-CP columns were also evaluated for the separation of a protein mixture composed of ribonuclease A, cytochrome c, and transferrin. Results obtained with the biomacromolecules mixture validate the optimal structural and operative conditions determined with the small solutes, laying the groundwork towards biomacromolecule applications, focusing more on the chemical aspects of separations.


Assuntos
Cromatografia Líquida de Alta Pressão/instrumentação , Cromatografia Líquida de Alta Pressão/métodos , Citocromos c/isolamento & purificação , Polipropilenos/química , Ribonuclease Pancreático/isolamento & purificação , Transferrina/isolamento & purificação , Citocromos c/química , Humanos , Ribonuclease Pancreático/química , Transferrina/química
9.
Anal Bioanal Chem ; 404(3): 721-9, 2012 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-22736228

RESUMO

The performance of microbore columns with polypropylene (PP) capillary-channeled polymer (C-CP) fibers as the support/stationary phase for separation of macromolecules has been investigated. Polypropylene C-CP fibers (40 µm diameter) were packed in fluorinated ethylene propylene (FEP) tubing of inner diameter 0.8 mm and lengths of 40, 60, 80, and 110 cm. The performance of PP fiber packed microbore columns (peak width, peak capacity, and resolution) was evaluated for separation of a three-protein mixture of ribonuclease A, cytochrome c, and transferrin under reversed-phase gradient conditions. The low backpressure characteristics of C-CP fiber columns enable operation at high linear velocities (up to 75 mm s(-1) at 1.5 mL min(-1)). In contrast with the performance of other phases, such velocities enable enhanced resolution of the three-protein mixture, because peak widths decrease with velocity. Increased column length resulted in increased resolution, because the peak widths remained essentially constant, although retention times increased. In addition, it was found that the peak capacity increased with column length and linear velocity. Radial compression of the microbore tubing enhanced the homogeneity of the packing and, thereby, separation efficiency and resolution. Radial compression of columns resulted in a decrease in the interstitial fraction (~5%), but increased resolution of ~14% between ribonuclease A and cytochrome c. Even so, a linear velocity of 75 mm s(-1) required a backpressure of 9.5 MPa only. It is clear that the fluid and solute-transport properties of the C-CP fiber microbore columns afford far better performance than is obtainable by use of standard format columns. The ability to achieve high separation efficiencies, rapidly and with low volume flow rates, holds promise for high-capacity protein separations in proteomics applications.


Assuntos
Cromatografia Líquida de Alta Pressão/instrumentação , Cromatografia de Fase Reversa/instrumentação , Polipropilenos/química , Adsorção , Animais , Bovinos , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia de Fase Reversa/métodos , Citocromos c/química , Halogenação , Humanos , Teste de Materiais , Ribonuclease Pancreático/química , Transferrina/química
10.
Metallomics ; 3(10): 1027-34, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21904748

RESUMO

The analysis of metal-binding proteins requires careful sample manipulation to ensure that the metal-protein complex remains in its native state and the metal retention is preserved during sample preparation or analysis. Chemical analysis for the metal content in proteins typically involves some type of liquid chromatography/electrophoresis separation step coupled with an atomic (i.e., inductively coupled plasma-optical emission spectroscopy or -mass spectrometry) or molecular (i.e., electrospray ionization-mass spectrometry) analysis step that requires altered-solvent introduction techniques. UV-VIS absorbance is employed here to monitor the iron content in human holo-transferrin (Tf) under various solvent conditions, changing polarity, pH, ionic strength, and the ionic and hydrophobic environment of the protein. Iron loading percentages (i.e. 100% loading equates to 2 Fe(3+):1 Tf) were quantitatively determined to evaluate the effect of solvent composition on the retention of Fe(3+) in Tf. Maximum retention of Fe(3+) was found in buffered (20 mM Tris) solutions (96 ± 1%). Exposure to organic solvents and deionized H(2)O caused release of ~23-36% of the Fe(3+) from the binding pocket(s) at physiological pH (7.4). Salt concentrations similar to separation conditions used for ion exchange had little to no effect on Fe(3+) retention in holo-Tf. Unsurprisingly, changes in ionic strength caused by additions of guanidine HCl (0-10 M) to holo-Tf resulted in unfolding of the protein and loss of Fe(3+) from Tf; however, denaturing and metal loss was found not to be an instantaneous process for additions of 1-5 M guanidinium to Tf. In contrast, complete denaturing and loss of Fe(3+) was instantaneous with ≥6 M additions of guanidinium, and denaturing and loss of iron from Tf occurred in parallel proportions. Changes to the hydrophobicity of Tf (via addition of 0-14 M urea) had less effect on denaturing and release of Fe(3+) from the Tf binding pocket compared to changes in ionic strength.


Assuntos
Ferro/metabolismo , Transferrina/metabolismo , Cromatografia de Fase Reversa , Dicroísmo Circular , Humanos , Ligação Proteica , Desnaturação Proteica , Espectrofotometria Ultravioleta , Transferrina/química
11.
Pharm Dev Technol ; 9(3): 265-75, 2004 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-15458232

RESUMO

The objectives of the present study were to undertake activities toward the development of an aqueous-based formulation of propofol (2,6-diisopropyl phenol), using sulfobutylether 7-beta-cyclodextrin (SBECD). Preformulation studies, including high performance liquid chromatography (HPLC) method development and phase-solubility evaluation in the presence of SBECD were conducted. It was determined that equilibrium solubility has been reached by 4-day and 7-day phase-solubility analysis at 30 degrees C and 37 degrees C. The apparent binding constants and various thermodynamic parameters were calculated from this data. These results suggest that "nonclassical hydrophobic effects" are the driving forces for inclusion complex formation. Compounding and lyophilization of the formulation with 20% SBECD yielded a product with propofol concentration of 10 mg/mL. The formulation properties were probed by using techniques that included modulated differential scanning calorimetry (MDSC) and Karl Fischer analysis. MDSC showed that propofol, SBECD, and the Propofol-SBECD complex displayed thermal properties at widely varying temperatures, suggesting the formation of a new solid form. The active pharmaceutical ingredient in the liquid formulation and lyophilized product was determined by the newly developed and qualified HPLC method. Short-term stability studies of the liquid formulation showed that they were stable for a month at 4 degrees C. Short-term stability studies of the freeze-dried cakes showed that the product was stable for over a month at 4 degrees C, 37 degrees C, and 50 degrees C. Based on these preliminary results, we believe that an aqueous based injectable formulation of propofol with sulfobutylether 7-beta-cyclodextrin can be successfully developed.


Assuntos
Anestésicos Intravenosos/química , Propofol/análogos & derivados , Propofol/química , beta-Ciclodextrinas/química , Algoritmos , Anestésicos Intravenosos/administração & dosagem , Varredura Diferencial de Calorimetria , Química Farmacêutica , Cromatografia Líquida de Alta Pressão , Formas de Dosagem , Estabilidade de Medicamentos , Liofilização , Injeções , Propofol/administração & dosagem , Reprodutibilidade dos Testes , Água/análise
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