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Medicinas Complementárias
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1.
BMC Oral Health ; 23(1): 852, 2023 11 11.
Artículo en Inglés | MEDLINE | ID: mdl-37951865

RESUMEN

BACKGROUND: The continuously increasing demand for removable denture appliances and the importance of adequate denture cleaning have led to the development of various denture cleansing products. The aim of this study was to evaluate the efficacy of two novel denture cleansing agents (GE and TM) and three commonly available cleansers (0.5% sodium hypochlorite; NaClO, 0.12% chlorhexidine gluconate; CHX, and Polident®; POL) on multispecies microbial biofilm formation, stain removal and physical properties of dentures. METHODS: The antimicrobial activities of denture cleansing agents were determined against major oral opportunistic pathogens including Streptococcus mutans, Staphylococcus aureus, Escherichia coli and Candida albicans, using time-kill assays. Multispecies microbial biofilms grown on acrylic resins for 72 h were generated to determine the antibiofilm effects of cleansing agents by confocal laser scanning microscopy (CLSM). Evaluations of the tea and coffee stain removal properties and the alterations in the physical properties of dentures were also performed. The toxicity of cleanser residues released from denture acrylics to fibroblast cells was investigated using MTT assay. RESULTS: All denture cleansing agents tested could effectively kill oral bacteria and Candida albicans. Furthermore, after immersion for more than 3 h, the cleansers Polident®, GE and TM could efficiently penetrate and inhibit multispecies denture biofilms with effects similar to 10 min of immersion in 0.5% NaClO. However, immersion in 0.12% CHX for 20 min showed less antibiofilm activity. The NaClO solution had the highest efficacy for removing stains from the artificial teeth. Conversely, the CHX solution enhanced tea and coffee staining, and the teeth immersed in this solution showed clinically unacceptable colour changes (ΔE > 5.5). However, the colour differences of teeth stained and immersed in POL, GE and TM cleansers were in the clinically acceptable range. There was no significant difference among the POL, GE and TM cleansers in terms of stain removal efficacy. The cleansers GE and TM did not alter the surface roughness and colour of the materials, moreover the residues of both cleansers did not exhibit cytotoxicity. CONCLUSION: Two novel denture cleansing agents containing natural products, GE and TM exhibited effective antimicrobial activity, antibiofilm and stain removal capabilities without toxicity or disturbance of the physical properties of acrylics.


Asunto(s)
Antiinfecciosos , Limpiadores de Dentadura , Humanos , Limpiadores de Dentadura/farmacología , Limpiadores de Dentadura/química , Colorantes/farmacología , Café , Detergentes/farmacología , Candida albicans , Antiinfecciosos/farmacología , Dentaduras , Biopelículas , , Propiedades de Superficie
2.
Molecules ; 28(21)2023 Oct 24.
Artículo en Inglés | MEDLINE | ID: mdl-37959658

RESUMEN

Liver fibrosis refers to a complex inflammatory response caused by multiple factors, which is a known cause of liver cirrhosis and even liver cancer. As a valuable medicine food homology herb, saffron has been widely used in the world. Saffron is commonly used in liver-related diseases and has rich therapeutic and health benefits. The therapeutic effect is satisfactory, but its mechanism is still unclear. In order to clarify these problems, we planned to determine the pharmacological effects and mechanisms of saffron extract in preventing and treating liver fibrosis through network pharmacology analysis combined with in vivo validation experiments. Through UPLC-Q-Exactive-MS analysis, a total of fifty-six nutrients and active ingredients were identified, and nine of them were screened to predict their therapeutic targets for liver fibrosis. Then, network pharmacology analysis was applied to identify 321 targets for saffron extract to alleviate liver fibrosis. Functional and pathway enrichment analysis showed that the putative targets of saffron for the treatment of hepatic fibrosis are mainly involved in the calcium signaling pathway, the HIF-1 signaling pathway, endocrine resistance, the PI3K/Akt signaling pathway, lipid and atherosclerosis, and the cAMP signaling pathway. Based on the CCl4-induced liver fibrosis mice model, we experimentally confirmed that saffron extract can alleviate the severity and pathological changes during the progression of liver fibrosis. RT-PCR and Western blotting analysis confirmed that saffron treatment can prevent the CCl4-induced upregulation of HIF-1α, VEGFA, AKT, and PI3K, suggesting that saffron may regulate AKT/HIF-1α/VEGF and alleviate liver fibrosis.


Asunto(s)
Crocus , Medicamentos Herbarios Chinos , Ratones , Animales , Proteínas Proto-Oncogénicas c-akt/metabolismo , Factor A de Crecimiento Endotelial Vascular/metabolismo , Crocus/metabolismo , Fosfatidilinositol 3-Quinasas/metabolismo , Transducción de Señal , Cirrosis Hepática/inducido químicamente , Cirrosis Hepática/tratamiento farmacológico , Colorantes/farmacología , Medicamentos Herbarios Chinos/farmacología
3.
Sci Prog ; 106(4): 368504231215593, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37993993

RESUMEN

This research investigates the viability of using Syzygium aromaticum (clove) as a natural dye for wool yarn through the application of microwave treatment and optimization using central composite design (CCD). As concerns grow over the environmental impact of synthetic dyes and their detrimental disposal in water bodies, the search for eco-friendly alternatives becomes imperative to revolutionize the textile industry. Microwave-assisted extraction of the colorant from clove powder is explored as an efficient and sustainable method, minimizing solvent usage and energy consumption compared to conventional techniques. To enhance colorfastness properties while eliminating the need for toxic mordants, green alternatives such as Al, Fe, and tannic acid, combined with plant phenolics from red sumac, pomegranate rind, and weld, are employed. According to the analysis of CCD, the higher color strength value 18.1653 was achieved using pH = 3, time = 50 min, temperature = 70 °C, and salt concentration = 1.5 g/100 mL. The optimized dyeing conditions also showed a maximum level of colorfastness properties of 5 for light, 5 for wash, 5 for dry rubbing, and 4 for wet rubbing. The findings from Fourier-transform infrared spectroscopy and scanning electron microscopy analyses provide valuable insights into the chemical and morphological changes induced by microwave treatment and dyeing with clove extract. The results affirm the presence of eugenol as a potential active molecule responsible for the captivating color of clove flower buds, validating its suitability as a natural dye source for wool. This study highlights the promising potential of microwave-assisted extraction and plant-based biomolecules as innovative and environmentally friendly approaches in natural dyeing, paving the way for a more sustainable future in the textile industry. Embracing these eco-friendly practices allows the textile sector to reduce its ecological footprint and contribute to a cleaner and greener environment. Further research and implementation of these techniques can foster a more harmonious coexistence with nature, ensuring a healthier ecosystem for all.


Asunto(s)
Syzygium , Lana , Animales , Colorantes/química , Colorantes/farmacología , Syzygium/química , Microondas , Ecosistema
4.
Phytomedicine ; 106: 154424, 2022 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-36126544

RESUMEN

BACKGROUND: Dengue virus (DENV) is considered one of the most important pathogens in the world causing 390 million infections each year. Currently, the development of vaccines against DENV presents some shortcomings and there is no antiviral therapy available for its infection. An important challenge is that both treatments and vaccines must be effective against all four DENV serotypes. Nordihydroguaiaretic acid (NDGA), isolated from Larrea divaricata Cav. (Zygophyllaceae) has shown a significant inhibitory effect on a broad spectrum of viruses, including DENV serotypes 2 and 4. PURPOSE: We evaluated the in vitro virucidal and antiviral activity of NDGA on DENV serotype 1 (DENV1), including the study of its mechanism of action, to provide more evidence on its antiviral activity. METHODS: The viability of viral particles was quantified by the plaque-forming unit reduction method. NDGA effects on DENV1 genome and viral proteins were evaluated by qPCR and immunofluorescence, respectively. Lysosomotropic activity was assayed using acridine orange and neutral red dyes. RESULTS: NDGA showed in vitro virucidal and antiviral activity against DENV1. The antiviral effect would be effective within the first 2 h after viral internalization, when the uncoating process takes place. In addition, we determined by qPCR that NDGA decreases the amount of intracellular RNA of DENV1 and, by immunofluorescence, the number of cells infected. These results indicate that the antiviral effect of NDGA would have an intracellular mechanism of action, which is consistent with its ability to be incorporated into host cells. Considering the inhibitory activity of NDGA on the cellular lipid metabolism, we compared the antiviral effect of two inhibitors acting on two different pathways of this type of metabolism: 1) resveratrol that inhibits the sterol regulatory element of binding proteins, and 2) caffeic acid that inhibits the 5-lipoxygenase (5-LOX) enzyme. Only caffeic acid produced an inhibitory effect on DENV1 infection. We studied the lysosomotropic activity of NDGA on host cells and found, for the first time, that this compound inhibited the acidification of cell vesicles which would prevent DENV1 uncoating process. CONCLUSION: The present work contributes to the knowledge of NDGA activity on DENV. We describe its activity on DENV1, a serotype different to those that have been already reported. Moreover, we provide evidence on which stage/s of the viral replication cycle NDGA exerts its effects. We suggest that the mechanism of action of NDGA on DENV1 is related to its lysosomotropic effect, which inhibits the viral uncoating process.


Asunto(s)
Virus del Dengue , Naranja de Acridina/farmacología , Antivirales/farmacología , Araquidonato 5-Lipooxigenasa/genética , Ácidos Cafeicos , Colorantes/farmacología , Virus del Dengue/fisiología , Masoprocol/farmacología , Rojo Neutro/farmacología , ARN , Resveratrol/farmacología , Serogrupo , Esteroles/farmacología , Proteínas Virales , Replicación Viral
5.
Microbiol Spectr ; 10(5): e0299022, 2022 10 26.
Artículo en Inglés | MEDLINE | ID: mdl-36121287

RESUMEN

Bacterial efflux pumps in the resistance-nodulation-cell division (RND) family of Gram-negative bacteria contribute significantly to the development of antimicrobial resistance by many pathogens. In this study, we selected the MtrD transporter protein of Neisseria gonorrhoeae as it is the sole RND pump possessed by this strictly human pathogen and can export multiple antimicrobials, including antibiotics, bile salts, detergents, dyes, and antimicrobial peptides. Using knowledge from our previously published structures of MtrD in the presence or absence of bound antibiotics as a model and the known ability of MtrCDE to export cationic antimicrobial peptides, we hypothesized that cationic peptides could be accommodated within MtrD binding sites. Furthermore, we thought that MtrD-bound peptides lacking antibacterial action could sensitize bacteria to an antibiotic normally exported by the MtrCDE efflux pump or other similar RND-type pumps possessed by different Gram-negative bacteria. We now report the identification of a novel nonantimicrobial cyclic cationic antimicrobial peptide, which we termed CASP (cationic antibiotic-sensitizing peptide). By single-particle cryo-electron microscopy, we found that CASP binds within the periplasmic cleft region of MtrD using overlapping and distinct amino acid contact sites that interact with another cyclic peptide (colistin) or a linear human cationic antimicrobial peptide derived from human LL-37. While CASP could not sensitize Neisseria gonorrhoeae to an antibiotic (novobiocin) that is a substrate for RND pumps, it could do so against multiple Gram-negative, rod-shaped bacteria. We propose that CASP (or future derivatives) could serve as an adjuvant for the antibiotic treatment of certain Gram-negative infections previously thwarted by RND transporters. IMPORTANCE RND efflux pumps can export numerous antimicrobials that enter Gram-negative bacteria, and their action can reduce the efficacy of antibiotics and provide decreased susceptibility to various host antimicrobials. Here, we identified a cationic antibiotic-sensitizing peptide (CASP) that binds within the periplasmic cleft of an RND transporter protein (MtrD) produced by Neisseria gonorrhoeae. Surprisingly, CASP was able to render rod-shaped Gram-negative bacteria, but not gonococci, susceptible to an antibiotic that is a substrate for the gonococcal MtrCDE efflux pump. CASP (or its future derivatives) could be used as an adjuvant to treat infections for which RND efflux contributes to multidrug resistance.


Asunto(s)
Antiinfecciosos , Colistina , Humanos , Colistina/metabolismo , Novobiocina/metabolismo , Microscopía por Crioelectrón , Detergentes/metabolismo , Detergentes/farmacología , Proteínas Bacterianas/genética , Neisseria gonorrhoeae , Antibacterianos/farmacología , Antibacterianos/uso terapéutico , Antiinfecciosos/farmacología , División Celular , Aminoácidos/metabolismo , Ácidos y Sales Biliares/metabolismo , Colorantes/metabolismo , Colorantes/farmacología , Farmacorresistencia Bacteriana Múltiple
6.
Molecules ; 27(3)2022 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-35164210

RESUMEN

Color is an important characteristic of food products. This characteristic is related to consumer acceptability. To use the entire rhizome of Curcuma longa (CL) as a food colorant, a novel gel alike stable suspension (CLS) was previously developed using cellulose nanofibers (CNFs). Therefore, the present study was conducted to evaluate the CLS as a color additive on a stirred yogurt. Three concentrations of CLS were studied (0.1, 0.125, and 0.15 wt. %) and compared to yogurt without CLS. The obtained yogurts were characterized through the determination of pH, titratable acidity, syneresis, color and curcumin content after 1, 7, 14, and 21 days of storage. Additionally, rheological and sensory measurements were performed on the samples after one day of storage. Results show that the addition of CLS does not affect the pH and titratable acidity of the samples, but all the yogurts showed an increase in their syneresis during the storage time, showing a breakdown of the gel structure. Furthermore, the CLS suspension has the ability to impart a yellow color to yogurts, a characteristic that was stable during storage. Finally, the addition of 1 wt. % or 1.25 wt. % of CLS allows the development of a yogurt with adequate sensory perception.


Asunto(s)
Colorantes/farmacología , Curcuma/química , Manipulación de Alimentos/métodos , Extractos Vegetales/farmacología , Sensación/efectos de los fármacos , Gusto/efectos de los fármacos , Yogur/análisis , Humanos , Reología
7.
Environ Sci Pollut Res Int ; 29(57): 86308-86319, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-35040048

RESUMEN

Borassus flabellifer leaf extract has been used for rapid biogenic synthesis of zinc oxide nanoparticles (ZnO-NPs) due to rich source of bioactive compounds. The synthesized ZnO-NPs were preliminarily confirmed by UV-visible spectroscopy adsorption peak range at 365 nm. The XRD (X-ray diffraction) confirms purity of ZnO-NPs that were crystalline in nature. The analysis of FT-IR (Fourier-transform infrared spectroscopy) confirms the presence of the following functional group such as alcohol, phenols, carboxylic acids, primary amides, secondary amides, and alkyl halide. The Field Emission Scanning Electron Microscope (FE-SEM) analysis indicated that ZnO-NPs were in spherical shape, followed by EDX analysis which confirmed the presence of Zn-element. Antimicrobial effect of ZnO-NPs was investigated using different clinical pathogens like bacteria Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Klebsiella Pneumonia, and Pseudomonas aeruginosa and fungi Aspergillus flavus, Candida albicans, and Penicillium expansum which confirmed ZnO-NPs efficiency as an antimicrobial agent. ZnO-NP antimicrobial efficiency was observed in higher zone of inhibition at 50 µg/mL concentrations. Antioxidant activity was ascertained to be used for several biomedical applications. The ZnO-NPs efficiently degraded the environmental toxic dyes (methylene blue and crystal violet) under sunlight, and up to 95% higher degradation was achieved in both dyes. In support of photo light degradation, the study was progressed to understand the ZnO-dye interaction stability using molecular mechanism, and it shows efficient bonding features in the NPs environment. Overall, this investigation has great potential for being an effective and eco-friendly material used in environmental applications.


Asunto(s)
Antiinfecciosos , Nanopartículas del Metal , Óxido de Zinc , Óxido de Zinc/química , Antioxidantes/farmacología , Pruebas de Sensibilidad Microbiana , Espectroscopía Infrarroja por Transformada de Fourier , Nanopartículas del Metal/química , Antibacterianos/química , Escherichia coli , Antiinfecciosos/farmacología , Difracción de Rayos X , Extractos Vegetales/farmacología , Extractos Vegetales/química , Colorantes/farmacología , Amidas
8.
J Am Chem Soc ; 143(43): 17891-17909, 2021 11 03.
Artículo en Inglés | MEDLINE | ID: mdl-34677069

RESUMEN

The emergence of multi-drug-resistant pathogens threatens the healthcare systems world-wide. Recent advances in phototherapy (PT) approaches mediated by photo-antimicrobials (PAMs) provide new opportunities for the current serious antibiotic resistance. During the PT treatment, reactive oxygen species or heat produced by PAMs would react with the cell membrane, consequently leaking cytoplasm components and effectively eradicating different pathogens like bacteria, fungi, viruses, and even parasites. This Perspective will concentrate on the development of different organic photo-antimicrobials (OPAMs) and their application as practical therapeutic agents into therapy for local infections, wound dressings, and removal of biofilms from medical devices. We also discuss how to design highly efficient OPAMs by modifying the chemical structure or conjugating with a targeting component. Moreover, this Perspective provides a discussion of the general challenges and direction for OPAMs and what further needs to be done. It is hoped that through this overview, OPAMs can prosper and will be more widely used for microbial infections in the future, especially at a time when the global COVID-19 epidemic is getting more serious.


Asunto(s)
Antiinfecciosos/química , Diseño de Fármacos , Fototerapia/métodos , Animales , Antiinfecciosos/farmacología , Antiinfecciosos/uso terapéutico , Bacterias/efectos de los fármacos , Biopelículas/efectos de los fármacos , Biopelículas/efectos de la radiación , Colorantes/química , Colorantes/farmacología , Equipos y Suministros/microbiología , Equipos y Suministros/virología , Escherichia coli/efectos de los fármacos , Escherichia coli/fisiología , Oftalmopatías/tratamiento farmacológico , Oftalmopatías/patología , Hongos/efectos de los fármacos , Grafito/química , Luz , Nanopartículas/química , Nanopartículas/toxicidad , Fármacos Fotosensibilizantes/química , Fármacos Fotosensibilizantes/farmacología , Fármacos Fotosensibilizantes/uso terapéutico , Teoría Cuántica , Especies Reactivas de Oxígeno/metabolismo , Virus/efectos de los fármacos
9.
Eur J Pharm Biopharm ; 169: 1-11, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-34461213

RESUMEN

Abundant existence of extracellular matrix biological hydrogels in solid tumors precludes most therapeutics to arrive at intracellular target sites, which is probably one of the threatened reasons of pancreatic ductal adenocarcinoma (PDAC) for public health. In this study, we designed a rod-shaped protocell nanoparticle loading with doxorubicin hydrochloride (Dox) and indocyanine green (ICG), denoted as Dox/ICG-RsPNs, for enhanced chemo-photothermal PDAC treatment. The enhanced therapeutic efficacy was achieved by successively enhancing penetration across matrix hydrogels, endocytosis, increasing local temperature under laser irradiation and hyperthermia-triggered Dox release to nucleus. We found that RsPNs with rod shape could easily penetrate across matrix hydrogel, exerting excellent tumor accumulation. Then RsPNs was internalized effectively by BxPC-3 cells via a caveolin-mediated endocytosis pathway. In addition, ICG endowed the Dox/ICG-RsPNs with photothermal effect and the photothermal conversion efficiency was calculated for 16.2%. Under irradiation, a great number of Dox transported to the nucleus via hyperthermia-induced release. Furthermore, we found that the relative tumor volume of Dox/ICG-RsPNs was merely 1.37 under irradiation at the end of pharmacodynamic studies, which was significantly lower than that of other groups. These findings will provide a promise on the rational design of drug delivery system for effective chemo-photothermal combination therapy to treat PDAC.


Asunto(s)
Doxorrubicina/farmacología , Quimioterapia/métodos , Hipertermia Inducida/métodos , Verde de Indocianina/farmacología , Terapia Fototérmica/métodos , Animales , Antibióticos Antineoplásicos/farmacología , Células Artificiales , Disponibilidad Biológica , Línea Celular Tumoral , Colorantes/farmacología , Matriz Extracelular , Humanos , Ratones , Sistema de Administración de Fármacos con Nanopartículas/farmacología , Neoplasias Pancreáticas , Resultado del Tratamiento , Neoplasias Pancreáticas
10.
Molecules ; 26(9)2021 May 10.
Artículo en Inglés | MEDLINE | ID: mdl-34068613

RESUMEN

Nowadays, natural dyes are expected by the cosmetic and food industries. In contrast to synthetic dyes, colorants derived from natural sources are more environmentally friendly and safer for human health. In this work, plant extracts from Gomphrena globasa L., Clitoria ternatea L., Carthamus tinctorius L., Punica granatum L. and Papaver rhoeas L. as the natural and functional dyes for the cosmetics industry were assessed. Cytotoxicity on keratinocyte and fibroblast cell lines was determined as well as antioxidant and anti-aging properties by determining their ability to inhibit the activity of collagenase and elastase enzymes. In addition, the composition of the extracts was determined. The obtained extracts were also applied in face cream formulation and color analyses were performed. It has been shown that the obtained extracts were characterized by no cytotoxicity and a high antioxidant potential. The extracts also show strong ability to inhibit the activity of collagenase and moderate ability to inhibit elastase and provide effective and long-lasting hydration after their application on the skin. Application analyses showed that the extracts of P. rhoeas L., C. ternatea L. and C. tinctorius L. can be used as effective cosmetic dyes that allow for attainment of an intense and stable color during the storage of the product. The extracts of P. granatum L. and G. globasa L., despite their beneficial effects as active ingredients, did not work effectively as cosmetic dyes, because cosmetic emulsions with these extracts did not differ significantly in color from emulsions without the extract.


Asunto(s)
Antioxidantes/farmacología , Colorantes/farmacología , Cosméticos/farmacología , Citoprotección , Desecación , Flores/química , Extractos Vegetales/farmacología , Benzotiazoles/química , Compuestos de Bifenilo/química , Muerte Celular/efectos de los fármacos , Colagenasas/metabolismo , Color , Citoprotección/efectos de los fármacos , Células HaCaT , Humanos , Cinética , Inhibidores de la Metaloproteinasa de la Matriz/farmacología , Oxazinas/metabolismo , Elastasa Pancreática/antagonistas & inhibidores , Elastasa Pancreática/metabolismo , Picratos/química , Plantas/química , Crema para la Piel/farmacología , Ácidos Sulfónicos/química , Rayos Ultravioleta , Pérdida Insensible de Agua/efectos de los fármacos , Xantenos/metabolismo
11.
Carbohydr Polym ; 257: 117612, 2021 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-33541643

RESUMEN

Interest in environment-friendly textile processing techniques has been augmenting in recent years. Natural dyes are environment friendly, low toxic and less allergenic owing to the existence of large number of structurally diverse active compounds which makes natural colourants promising options for the development of antimicrobial and ultra-violet (UV) protective textiles. The purpose of the present study was to investigate the effect of biopolymer and dyeing treatment with natural dye on the functional properties (antibacterial and UV protection) of cotton fabric and the assessment was done using standard test method. It was found that the chitosan treated onion skin dyed cotton fabric showed 97.20 percent and 98.03 % reduction in the growth of E. coli and S. aureus bacteria respectively. The chitosan treated dyed cotton fabric showed the higher ultra-violet protection factor (UPF) value (84.80) as compared to alum treated dyed cotton fabric (66.70) depicting that the chitosan treated dyed cotton fabric provided more ultraviolet protection than the alum treated dyed fabric.


Asunto(s)
Antibacterianos/farmacología , Celulosa/química , Quitosano/química , Colorantes/farmacología , Fibra de Algodón , Cebollas/metabolismo , Antibacterianos/química , Biopolímeros/química , Escherichia coli/efectos de los fármacos , Gossypium , Concentración de Iones de Hidrógeno , Pruebas de Sensibilidad Microbiana , Staphylococcus aureus/efectos de los fármacos , Temperatura , Textiles , Rayos Ultravioleta
12.
Toxicol Appl Pharmacol ; 402: 115124, 2020 09 01.
Artículo en Inglés | MEDLINE | ID: mdl-32652086

RESUMEN

Atypical antipsychotics (AAPs) have the tendency of inducing severe metabolic alterations like obesity, diabetes mellitus, insulin resistance, dyslipidemia and cardiovascular complications. These alterations have been attributed to altered hypothalamic appetite regulation, energy sensing, insulin/leptin signaling, inflammatory reactions and active reward anticipation. Line of evidence suggests that transient receptor potential vanilloid type 1 and 3 (TRPV1 and TRPV3) channels are emerging targets in treatment of obesity, diabetes mellitus and could modulate feed intake. The present study was aimed to investigate the putative role TRPV1/TRPV3 in olanzapine-induced metabolic alterations in mice. Female BALB/c mice were treated with olanzapine for six weeks to induce metabolic alterations. Non-selective TRPV1/TRPV3 antagonist (ruthenium red) and selective TRPV1 (capsazepine) and TRPV3 antagonists (2,2-diphenyltetrahydrofuran or DPTHF) were used to investigate the involvement of TRPV1/TRPV3 in chronic olanzapine-induced metabolic alterations. These metabolic alterations were differentially reversed by ruthenium red and capsazepine, while DPTHF didn't show any significant effect. Olanzapine treatment also altered the mRNA expression of hypothalamic appetite-regulating and nutrient-sensing factors, inflammatory genes and TRPV1/TRPV3, which were reversed with ruthenium red and capsazepine treatment. Furthermore, olanzapine treatment also increased expression of TRPV1/TRPV3 in nucleus accumbens (NAc), TRPV3 expression in ventral tegmental area (VTA), which were reversed by the respective antagonists. However, DPTHF treatment showed reduced feed intake in olanzapine treated mice, which might be due to TRPV3 specific antagonism and reduced hedonic feed intake. In conclusion, our results suggested the putative role TRPV1 in hypothalamic dysregulations and TRPV3 in the mesolimbic pathway; both regulate feeding in olanzapine treated mice.


Asunto(s)
Regulación del Apetito/efectos de los fármacos , Inflamación/metabolismo , Olanzapina/farmacología , Canales Catiónicos TRPV/metabolismo , Animales , Capsaicina/administración & dosificación , Capsaicina/análogos & derivados , Capsaicina/farmacología , Colorantes/administración & dosificación , Colorantes/farmacología , Metabolismo Energético/efectos de los fármacos , Metabolismo Energético/fisiología , Femenino , Furanos/administración & dosificación , Furanos/farmacología , Regulación de la Expresión Génica/efectos de los fármacos , Prueba de Tolerancia a la Glucosa , Hipoglucemiantes/administración & dosificación , Hipoglucemiantes/farmacología , Hipotálamo/efectos de los fármacos , Inflamación/genética , Metformina/administración & dosificación , Metformina/farmacología , Ratones , Ratones Endogámicos BALB C , Actividad Motora , Rojo de Rutenio/administración & dosificación , Rojo de Rutenio/farmacología , Fármacos del Sistema Sensorial/administración & dosificación , Fármacos del Sistema Sensorial/farmacología , Canales Catiónicos TRPV/genética
13.
Vet Med Sci ; 6(3): 441-446, 2020 08.
Artículo en Inglés | MEDLINE | ID: mdl-32323476

RESUMEN

Staining, as a valuable method for sperm morphological assessment, has been used to determine sperm abnormalities, fertilization capability and sperm suitability during freezing-thawing process. Synthetic dyes have been used for sperm viability and morphological evaluation. However, most of them have been made from chemical substances and have a perilous effect on the environment. In the current study, we evaluated three different natural dyes as the natural sources of dye for sperm staining. Bull frozen semen was used and prepared on slides for staining. Aqueous extract dye of black mulberry (BM), henna (HA), safflower (SA) and eosin-nigrosine (control group) were used for sperm staining. Additionally, the effect of staining dyes on viability and some morphological parameters (head area: HR, head abnormality: HB and tail abnormality: TA) were evaluated. Although none of the natural dyes could detect viability of the sperm cells, safflower stain (HR: 26.55 µm, HB: 0% TA: 28%) and black mulberry stain (HR: 25.07 µm, HB: 2% TA: 3%) compared to control group (HR: 34.29 µm, HB: 4%, TA: 4%) provoked a strong reaction in the sperm cells, so that the sperms were observed yellow and red respectively. The reaction of sperm cells to the henna dye was very poor and it did not stain the sperm cells. Thus, the present study demonstrated that SA and BM dyes are able to stain the spermatozoa and with further modification could be used as alternative dyes for sperm staining in the study of sperm morphology, but not viability. Staining with these dyes can be an alternative to current costly chemical staining methods.


Asunto(s)
Colorantes/farmacología , Preparaciones de Plantas/farmacología , Análisis de Semen/veterinaria , Espermatozoides/fisiología , Animales , Carthamus tinctorius/química , Bovinos , Masculino , Morus/química , Naftoquinonas/química , Análisis de Semen/métodos , Coloración y Etiquetado/veterinaria
14.
Biomolecules ; 10(2)2020 02 02.
Artículo en Inglés | MEDLINE | ID: mdl-32024305

RESUMEN

Cotton has the shortcomings of having no antibacterial, antioxidant and ultraviolet (UV) protection properties, which are of great importance for health protection purposes. In the present study, grape seed extract (GSE) mainly composed of proanthocyanins (tannins) was employed to simultaneously import pale colors and the three aforementioned functions to cotton fabric. The tests on the application conditions of GSE showed that pH and GSE concentration had great impact on the color depth of cotton fabric, and the color hue of dyed fabric could be controlled in the absence of pH regulators due to the weakly acidic nature of GSE solution. The fabric dyed with 10%owf (on the weight of fabric) GSE exhibited an excellent inhibition effect towards Escherichia coli, whereas the one dyed with 20%owf GSE had high antioxidant activity of 97%. The fabric dyed with 5%owf GSE offered excellent UV protection. This study reveals that GSE can be used as a functional finishing agent for health protection in cotton textiles in addition to coloration capability.


Asunto(s)
Fibra de Algodón , Extracto de Semillas de Uva/química , Proantocianidinas/química , Textiles , Antibacterianos/química , Antibacterianos/farmacología , Antioxidantes/química , Colorantes/farmacología , Escherichia coli/efectos de los fármacos , Gossypium , Concentración de Iones de Hidrógeno , Pruebas de Sensibilidad Microbiana , Taninos/química , Rayos Ultravioleta
15.
Mol Pharm ; 17(3): 748-756, 2020 03 02.
Artículo en Inglés | MEDLINE | ID: mdl-31990564

RESUMEN

Mechanistic-understanding-based selection of excipients may improve formulation development strategies for generic drug products and potentially accelerate their approval. Our study aimed at investigating the effects of molecular excipients present in orally administered FDA-approved drug products on the intestinal efflux transporter, BCRP (ABCG2), which plays a critical role in drug absorption with potential implications on drug safety and efficacy. We determined the interactions of 136 oral molecular excipients with BCRP in isolated membrane vesicles and identified 26 excipients as BCRP inhibitors with IC50 values less than 5 µM using 3H-cholecystokinin octapeptide (3H-CCK8). These BCRP inhibitors belonged to three functional categories of excipients: dyes, surfactants, and flavoring agents. Compared with noninhibitors, BCRP inhibitors had significantly higher molecular weights and SLogP values. The inhibitory effects of excipients identified in membrane vesicles were also evaluated in BCRP-overexpressing HEK293 cells at similar concentrations. Only 1 of the 26 inhibitors of BCRP identified in vesicles inhibited BCRP-mediated 3H-oxypurinol uptake by more than 50%, consistent with the notion that BCRP inhibition depends on transmembrane or intracellular availability of the inhibitors. Collectively, the results of this study provide new information on excipient selection during the development of drug products with active pharmaceutical ingredients that are BCRP substrates.


Asunto(s)
Transportador de Casetes de Unión a ATP, Subfamilia G, Miembro 2/metabolismo , Colorantes/metabolismo , Excipientes/metabolismo , Aromatizantes/metabolismo , Proteínas de Neoplasias/metabolismo , Tensoactivos/metabolismo , Transportador de Casetes de Unión a ATP, Subfamilia G, Miembro 2/antagonistas & inhibidores , Transportador de Casetes de Unión a ATP, Subfamilia G, Miembro 2/genética , Administración Oral , Colorantes/química , Colorantes/farmacología , Composición de Medicamentos/métodos , Evaluación Preclínica de Medicamentos/métodos , Excipientes/química , Excipientes/farmacología , Femenino , Aromatizantes/química , Aromatizantes/farmacología , Células HEK293 , Humanos , Concentración 50 Inhibidora , Absorción Intestinal/efectos de los fármacos , Peso Molecular , Proteínas de Neoplasias/antagonistas & inhibidores , Proteínas de Neoplasias/genética , Transducción de Señal/genética , Tensoactivos/química , Tensoactivos/farmacología , Transfección
16.
J Mater Chem B ; 8(5): 935-944, 2020 02 07.
Artículo en Inglés | MEDLINE | ID: mdl-31912837

RESUMEN

Multifunctional nanotheranostic systems with both therapeutic and imaging functions are highly desired for the development of more effective and less toxic anti-tumor drugs. Herein, a simple but effective method is reported to fabricate a novel PCN-CuS-FA-ICG-based nanoplatform for dual-modal imaging-guided synergistic photothermal/photodynamic therapy. Porphyrinic metal-organic frameworks with CuS NPs are obtained in aqueous solution via a simple post-synthesis strategy. Furthermore, to obtain a more effective therapy, indocyanine green (ICG) was incorporated into the multifunctional theranostic platform to promote the photothermal therapeutic effect. The as-prepared PCN-CuS-FA-ICG not only exhibits an excellent 1O2 generation efficiency under 650 nm irradiation to achieve remarkable photodynamic cell killing, but also presents outstanding photothermal conversion under 808 nm irradiation to destroy tumor tissues by hyperthermia. In particular, the nanotherapeutic agent realized fluorescence and thermal imaging dual-modal imaging-guided cancer treatment. Meanwhile, in vivo experiments confirmed the evident accumulation of nanoparticles (NPs) at local tumors, and tumor growth was inhibited obviously via synergistic photothermal/photodynamic therapy with negligible side effects.


Asunto(s)
Antineoplásicos/farmacología , Colorantes/farmacología , Hipertermia Inducida , Estructuras Metalorgánicas/farmacología , Nanopartículas/química , Fotoquimioterapia , Antineoplásicos/síntesis química , Antineoplásicos/química , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Colorantes/síntesis química , Colorantes/química , Cobre/química , Cobre/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Verde de Indocianina/química , Verde de Indocianina/farmacología , Rayos Infrarrojos , Ensayo de Materiales , Estructuras Metalorgánicas/síntesis química , Estructuras Metalorgánicas/química , Imagen Óptica , Tamaño de la Partícula , Oxígeno Singlete/análisis , Oxígeno Singlete/metabolismo , Propiedades de Superficie , Células Tumorales Cultivadas
17.
Medicine (Baltimore) ; 99(2): e18467, 2020 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-31914018

RESUMEN

BACKGROUND: Curcumin, a controversial "panacea," has been broadly studied. Its bioactivities including antioxidant, anti-inflammatory, and especially antineoplastic activities have been documented. However, due to its extensive bioactivities, some scientists hold a skeptical point of view toward curcumin and described curcumin as a "deceiver" to chemists. The objective of this study was to explore curcumin's another possibility as a potential supplementary leading compound to cancer treatments. METHODS: Literature searches were conducted using electronic databases. Search terms such as "curcumin," "curcumin analogues," and so on were used. The literatures were collected and summarized. In this article, reported targets of curcumin are reviewed. The limitations of a curcumin as a therapeutic anticancer product including low bioavailability and poor targeting are mentioned. Furthermore, modified curcumin analogues and antitumor mechanisms are listed and discussed in the aspects of cell death and tumor microenvironment including angiogenesis, tissue hypoxia status, and energy metabolism. RESULTS: Several possible modification strategies were presented by analyzing the relationships between the antitumor activity of curcumin analogues and their structural characteristics, including the introduction of hydrophilic group, shortening of redundant hydrocarbon chain, the introduction of extra chemical group, and so on. CONCLUSIONS: From our perspective, after structural modification curcumin could be more effective complementary product for cancer therapies by the enhancement of targeting abilities and the improvement of bioavailability.


Asunto(s)
Colorantes/metabolismo , Colorantes/farmacología , Curcumina/metabolismo , Curcumina/farmacología , Antineoplásicos , Disponibilidad Biológica , Muerte Celular/efectos de los fármacos , Terapias Complementarias , Curcumina/química , Humanos , Neoplasias/tratamiento farmacológico , Microambiente Tumoral/efectos de los fármacos
18.
Homeopathy ; 109(2): 79-86, 2020 05.
Artículo en Inglés | MEDLINE | ID: mdl-31604351

RESUMEN

BACKGROUND: The mechanism by which highly diluted and agitated solutions have their effect is still unknown, but the development in recent years of new methods identifying changes in water and solute dipole moments is providing insights into potential modes of action. OBJECTIVE: The objective of the current study was to compare the biological effects of Antimonium crudum (AC) previously obtained by our group and already described in the literature with now measurable physico-chemical effects on solvatochromic dyes. METHODS: Different dilutions of AC and succussed water have been characterized with respect to their effect on the visible spectra of the solvatochromic dyes methylene violet (MV), a pyridinium phenolate (ET33), and a dimethylamino naphthalenone (BDN) compared with in-vitro action against Leishmania amazonensis-infected macrophages. RESULTS: Dye responses varied according to the dye used and the level of AC dilution and results were found to corroborate previously published in-vivo and in-vitro effects of AC. In addition, a very significant enhancement in the absorbance increase of MV was seen using the supernatant from AC 200cH-treated cells (15%; p < 0.0001) over that seen with AC 200cH itself (4%; p = 0.034), suggesting the amplification of ultra-high dilution effects by biological systems. Furthermore, supernatants from AC-treated cells increased the range of dilutions of AC that were capable of producing effects on the spectra of MV. The effect of AC dilutions on dye ET33 was eliminated by a weak electric current passed through potency solutions. CONCLUSION: The data confirm a correspondence between the biological effects of dilutions of AC in-vitro and physico-chemical effects on solvatochromic dyes as measured by changes in their visible spectra. Results also indicate high dilutions of AC are sensitive to exposure to electric currents and biological systems.


Asunto(s)
Antimonio/química , Antimonio/farmacología , Colorantes/química , Homeopatía , Solventes/química , Colorantes/farmacología , Leishmania mexicana/efectos de los fármacos , Macrófagos , Solventes/farmacología , Espectrofotometría Ultravioleta
19.
J Photochem Photobiol B ; 200: 111631, 2019 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-31630045

RESUMEN

In this work, over the course of four seasons (12 months), we have monitored the fluorescence quantum efficiency (η) from two sets (S1 and S2) of fresh natural dye extracts from the leaves of Tradescantia pallida purpurea. The natural dye was extracted in aqueous solutions from leaves collected from regions with a predominance of shade (S1) and sun (S2) during the day. The thermo-optical parameter fractional thermal load (φ) was measured using conical diffraction (CD) patterns caused by thermally driven self-phase modulation, for η determination in both sets of solutions. Fluorescence measurements corroborate the CD results, and the η values are, on average, slightly higher (~ 11%) in the summer than in the other seasons for both sets of samples (S1 and S2). In addition, the experimental results are presented using natural dye extracted from Tradescantia pallida purpurea as a fungicide probe in Fusarium solani, Sclerotinia sclerotiorum, and Colletotrichum gloeosporioides fungi. The promising fungicide results obtained for the aqueous natural dye extract were compared with those obtained for other natural dyes and fungi. The fungi tested are of the necrotrophic group and constitute important pathosystems in Brazil, causing diseases in several crops that synthetic fungicides often cannot control or do so with low efficiency.


Asunto(s)
Antifúngicos/química , Colorantes/química , Extractos Vegetales/química , Tradescantia/química , Antifúngicos/aislamiento & purificación , Antifúngicos/farmacología , Colorantes/aislamiento & purificación , Colorantes/farmacología , Hongos/efectos de los fármacos , Hojas de la Planta/química , Hojas de la Planta/metabolismo , Refractometría , Estaciones del Año , Tradescantia/metabolismo
20.
Food Chem ; 298: 125014, 2019 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-31260973

RESUMEN

Natural red purple dye, Betanin, was extracted from the beetroot, purified by aqueous two- phase extraction and gel permeation column chromatography, and used as a reducing agent for the synthesis of silver-betanin core-shell triangular nanodisks for the first time. Spectroscopic data show that the nanoparticle structure is core@shell like with Ag as core and betanin as shell. Langmuir monolayer model (qm = 32.4 mg/g, RL = 0.99 and R2 = 0.997) was the best fit adsorption isotherm for the dye removal. Adsorption kinetics is well explained by pseudo-second-order equation. Gibbs free energy (ΔG0 = -2.59 kJ mol-1), enthalpy (ΔH0 = 18.05 kJ mol-1), and entropy (ΔS0 = 68.92 J/K/mol) were calculated and discussed. The antibacterial activity of betanin-AgNPs were determined against Escherichia coli MTCC-450 (E. coli) and Staphylococcus aureus MTCC-3160 (S. aureus) bacteria.


Asunto(s)
Antibacterianos/farmacología , Beta vulgaris/química , Betacianinas/farmacología , Colorantes/farmacología , Nanopartículas del Metal/química , Plata/química , Adsorción , Antibacterianos/química , Betacianinas/química , Betacianinas/aislamiento & purificación , Colorantes/química , Colorantes/aislamiento & purificación , Entropía , Escherichia coli/efectos de los fármacos , Cinética , Staphylococcus aureus/efectos de los fármacos , Termodinámica
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