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1.
Sci Total Environ ; 899: 165726, 2023 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-37495153

RESUMEN

Chromium (Cr) is released into the environment through anthropogenic activities and has gained significant attention in the recent decade as environmental pollution. Its contamination has adverse effects on human health and the environment e.g. decreases soil fertility, alters microbial activity, and reduces plant growth. It can occur in different oxidation states, with Cr(VI) being the most toxic form. Cr contamination is a significant environmental and health issue, and phytoremediation offers a promising technology for remediating Cr-contaminated soils. Globally, over 400 hyperaccumulator plant species from 45 families have been identified which have the potential to remediate Cr-contaminated soils through phytoremediation. Phytoremediation can be achieved through various mechanisms, such as phytoextraction, phytovolatilization, phytodegradation, phytostabilization, phytostimulation, and rhizofiltration. Understanding the sources and impacts of Cr contamination, as well as the factors affecting Cr uptake in plants and remediation techniques such as phytoremediation and mechanisms behind it, is crucial for the development of effective phytoremediation strategies. Overall, phytoremediation offers a cost-effective and sustainable solution to the problem of Cr pollution. Further research is needed to identify plant species that are more efficient at accumulating Cr and to optimize phytoremediation methods for specific environmental conditions. With continued research and development, phytoremediation has the potential to become a widely adopted technique for the remediation of heavy metal-contaminated soils.


Asunto(s)
Metales Pesados , Contaminantes del Suelo , Humanos , Cromo/metabolismo , Biodegradación Ambiental , Metales Pesados/metabolismo , Plantas/metabolismo , Contaminantes del Suelo/análisis , Suelo
2.
ACS Omega ; 8(21): 18940-18950, 2023 May 30.
Artículo en Inglés | MEDLINE | ID: mdl-37273635

RESUMEN

Heavy metal contamination in soil, such as cadmium (Cd), poses a serious threat to global food security and human health. It must be managed using environmentally friendly and cost-effective technologies. Plants with high resistance to Cd stress and high biomass production could be potential candidates for the phytoremediation of Cd-contaminated soils to improve Cd phytoextraction. In this regard, the present study was carried out to determine the effect of gibberellic acid (GA3), indole acetic acid (IAA), and fertilizers (N, P, and K) on Parthenium hysterophorus growth and biomass production as well as Cd phytoextraction capabilities. A pot experiment was conducted with various combinations of PGRs and fertilizers, with treatments arranged in five replicates using a completely randomized design. After harvesting, each plant was divided into various parts such as stems, roots, and leaves, and different growth, physiological, and biochemical parameters were recorded. Results showed that under Cd stress, growth, physiological, and biochemical parameters were all significantly decreased. With the combined application of plant growth regulators (GA3 and IAA) and nutrients, Cd stress was alleviated and all parameters significantly improved. In comparison to the control treatment, the combined application of N + P + K + GA3 + IAA resulted in the highest fresh and dry biomass production of the root (12.31 and 5.11 g pot-1), shoot (19. 69 and 6.99 g pot-1), leaves (16.56 and 7.09 g pot-1), and entire plant (48.56 and 19.19 g pot-1). Similarly, the same treatment resulted in higher chlorophyll a and b and total chlorophyll contents under Cd stress, which were 2.19, 2.03, and 3.21 times higher than the control, which was Cd stress without any treatment. The combination of N + P + K + GA3 + IAA also resulted in the highest proline and phenolic contents. In the case of different enzyme activities, the combined application of N + P + K + GA3 + IAA under Cd stress led to a high increase in catalase (2.5 times), superoxide (3.5 times), and peroxidase (3.7 times) compared to the control. With the combined application of N+ P+ K + GA3 + IAA, the maximum values of BCF (8.25), BAC (2.6), and RF (5.14%) were measured for phytoextraction potential. On the basis of these findings, it is concluded that P. hysterophorus has a high potential to grow, produce the most biomass, and act as a Cd hyperaccumulator in Cd-contaminated soil.

3.
Materials (Basel) ; 15(14)2022 Jul 10.
Artículo en Inglés | MEDLINE | ID: mdl-35888280

RESUMEN

The use of medical devices for therapeutic and diagnostic purpose is globally increasing; however, bacterial colonization on therapeutic devices can occur, causing severe infections in the human body. It has become an issue for public health. It is necessary to develop a nanomaterial based on photothermal treatment to kill toxic bacterial strains. Appropriately, high photothermal conversion and low-cost powerful photothermal agents have been investigated. Recently, gold nanocomposites have attracted great interest in biological applications. Here, we prepared rod-shaped Se-Te@Au nanocomposites of about 200 nm with uniform shape and surface-coated with gold nanoparticles for the first time showing high anti-bacterial and anti-cancer activities. Se-Te@Au showed proper structural consistency and natural resistance to bacterial and cancer cells. The strong absorption and high photothermal conversion efficacy made it a good photothermal agent material for the photothermal treatment of bacterial and cancer cells. The Se-Te@Au rod showed excellent anti-bacterial efficacy against Gram-negative Escherichia coli and Gram-positive Staphylococcus aureus, with highest recorded inhibition zones of 25 ± 2 mm and 22 ± 2 mm, respectively. More than 99% of both types of strains were killed after 5 min with a near-infrared (NIR) laser at the very low concentration of 48 µg/mL. The Se-Te@Au rod's explosion in HeLa cells was extensively repressed and demonstrated high toxicity at 100 µg/mL for 5 min when subjected to an NIR laser. As a result of its high photothermal characteristics, the exceptional anti-bacterial and anti-cancer effects of the Se-Te@Au rod are considerably better than those of other methods previously published in articles. This study could open a new framework for sterilization applications on the industrial level.

4.
Materials (Basel) ; 14(22)2021 Nov 16.
Artículo en Inglés | MEDLINE | ID: mdl-34832332

RESUMEN

Innovations in nanotechnology have had an immense impact on medicine, such as in drug delivery, tissue engineering, and medical devices that combat different pathogens. The pathogens that may cause biofilm-associated nosocomial diseases are multidrug-resistant (MDR) bacteria, such as Escherichia coli (E. coli), Pseudomonas aeruginosa (P. aeruginosa), Staphylococcus aureus (S. aureus), including both Gram-positive and Gram-negative bacterial species. About 65-80% of infections are caused by biofilm-associated pathogens creating a move in the international community toward developing antimicrobial therapies to eliminate such pathogenic infections. Several nanomaterials (NMs) have been discovered and significantly employed in various antipathogenic therapies. These NMs have unique properties of singlet oxygen production, high absorption of near-infrared irradiation, and reasonable conversion of light to heat. In this review, functionalized NPs that combat different pathogenic infections are introduced. This review highlights NMs that combat infections caused by multidrug-resistant (MDR) and other pathogenic microorganisms. It also highlights the biomedical application of NPs with regard to antipathogenic activities.

5.
Photodiagnosis Photodyn Ther ; 35: 102471, 2021 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-34343667

RESUMEN

Nanotechnologyapplications in the field of biomedicine like drug delivery, cell labeling, and bacterial inhibition are growing . New nano-materials having less toxicity and excellent antibacterial activity attract research interest. In the current study, while taking advantage of green synthesis we have decorated zinc oxide on the surface of grephene oxide forming Zno@GO nanocomposite. The Transmission electron microscopy (TEM) study showed successfully synthesized trigonal small sizes ZnO on the surface of GO nanosheets. The as-synthesized ZnO@GO was used against MDR gram-negative pathogen E-coli (BL21 DE3) and showed excellent antibacterial activity killing about 95 % toxic bacteria within 5 h due to electrostatic interaction between cell membrane of E. coli (BL21 DE3) and ZnO@GO complex. Hence the nano composite subsequently penetrated into the cytoplasm by damaging the cell membrane of bacteria, as a result production of ROS into the cytoplasm led to imbalance of metabolic system in the cell. Moreover, the cell membrane damage of gram-negative bacteria verified through zeta potential and propidium iodide (PI) study. Thus, our study develops a way to solve the challenge of efficient design of a drug delivery system for dissolution enhancement according to the need for required drug release.


Asunto(s)
Grafito , Nanocompuestos , Fotoquimioterapia , Óxido de Zinc , Antibacterianos/farmacología , Escherichia coli , Fotoquimioterapia/métodos , Fármacos Fotosensibilizantes
6.
Bioresour Bioprocess ; 8(1): 23, 2021 Mar 23.
Artículo en Inglés | MEDLINE | ID: mdl-38650208

RESUMEN

BACKGROUND: Sixty five percent of procyanidins in grape seeds is polymeric procyanidins (PPC), and they could not be assimilated directly by human. To enhance procyanidin assimilation, steam explosion treatment (SE) was used to facilitate the preparation of oligomeric procyanidins (OPC) from grape seeds. RESULTS: The results indicate that SE treatment made grape seeds loose and porous, and decreased the mean degree of polymerization (mDP) of procyanidins. The procyanidins content and total phenolic content (TPC) were decreased with the increase of SE severity, while the amount of catechin (CA), epicatechin (EC) and epicatechin-3-O-gallate (ECG) were increased, resulting in significant increase of antioxidant activity. CONCLUSIONS: Although SE treatment could depolymerize PPC and produce CA/EC/ECG with high yield, it caused the yield loss of total procyanidins. SE treatment is a potential effective method to prepare procyanidins with low degree of polymerization and high antioxidant activity. However, it still needs to study further how to balance the yield of total procyanidins and catechin monomers (CA/EC/ECG).

7.
Photodiagnosis Photodyn Ther ; 32: 101970, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32841752

RESUMEN

Noble metal/metal oxide nanocomposites are pet and spellbound candidates in biomedical and catalytic fields because of their awestruck properties. This report put forward the facile and environmentally friendly fabrication of Ag/Fe2O3 nanocomposite using the eqeous extract of Algaia Monozyga leaves. The Ag/ Fe2O3 bimetallic nanocomposite was prepared using AgNO3, FeCl3 (anhydrous) and plant leaves extract as a natural source for reduction and stabilization of this nanocomposite. We prepared a separate solution of Silver and Iron salts and upon addition of this solution to the plant extract, the conversion of colour to brown appears within 10 min at constant stirring at 350 rpm. To confirm the synthesis of nanocomposite, UV-vis spectroscopy, Scanning electron microscopy (SEM), EDX and X-ray diffraction spectroscopy were used. The as prepared nanocomposite was used for photocatalytic activity in degradation of Methylene Blue (MB) in the presence of light which shows effective photocatalytic activity. The antimicrobial activities were also determined for nanocomposite which were found to be efficient against human pathogenic multidrug resistant bacteria. The Ag/Fe2O3 nanocomposite significantly preventing the growth of Staphylococcus aureus, E.coli QH4 and Pseudomonas putida with zones of inhibition 23 (±0.5), 21 (±0.4) and 19 (±0.4) mm, respectively.The eco-benignly synthesized Ag/Fe2O3 nanocomposite could be a desired material for efficient remediation of toxic organic pollutants and microbes.


Asunto(s)
Nanopartículas del Metal , Nanocompuestos , Fotoquimioterapia , Humanos , Fotoquimioterapia/métodos , Fármacos Fotosensibilizantes , Extractos Vegetales , Hojas de la Planta , Plata
8.
Eur J Med Chem ; 198: 112322, 2020 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-32361064

RESUMEN

In the current study, we have designed and synthesized a series of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent kinase2 (CDK2) dual inhibitors by integrating purine-based pharmacophore into the recognition cap group of CS055. The representative compound 14d with excellent antiproliferative activities towards five solid cancer cells, showed potent inhibitory activities against HDAC1, HDAC2 and CDK2 with IC50 values of 70.7 nM, 23.1 nM and 0.80 µM, respectively. Besides, compound 14d could effectively block the cell cycle in the G2/M phase and induce apoptosis, which might be related to increasing intracellular ROS levels. Importantly, compound 14d exhibited desirable pharmacokinetic (PK) properties with the intraperitoneal bioavailability of 50.8% in ICR mice, and potent in vivo antitumor activity in the HCT116 xenograft model. Therefore, compound 14d could be considered as a promising lead compound for the development of multitargeting anticancer agents.


Asunto(s)
Antineoplásicos/síntesis química , Benzamidas/química , Neoplasias del Colon/tratamiento farmacológico , Quinasa 2 Dependiente de la Ciclina/antagonistas & inhibidores , Histona Desacetilasas/metabolismo , Inhibidores de Proteínas Quinasas/síntesis química , Purinas/química , Animales , Antineoplásicos/farmacocinética , Antineoplásicos/uso terapéutico , Apoptosis/efectos de los fármacos , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Diseño de Fármacos , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Humanos , Masculino , Ratones Endogámicos BALB C , Ratones Endogámicos ICR , Ratones Desnudos , Simulación del Acoplamiento Molecular , Neoplasias Experimentales , Inhibidores de Proteínas Quinasas/farmacocinética , Inhibidores de Proteínas Quinasas/uso terapéutico , Relación Estructura-Actividad
9.
Nanomedicine (Lond) ; 15(8): 809-828, 2020 04.
Artículo en Inglés | MEDLINE | ID: mdl-32207379

RESUMEN

Leishmaniasis, a category 1 disease, has remained neglected for decades, and therefore, has developed into a severe health problem worldwide. Unfortunately, the available antileishmanial drugs are limited, and the parasites have shown an inevitable resistance toward most of these drugs. All these factors pose a barrier to control the parasite at present. Hence, new strategies are needed to develop more effective and less toxic nanomedicines that could treat and manage the Leishmania parasite. One of these effective strategies is to construct nanometals with biologically active molecules that could possess dynamic antileishmanial activities with desirable biocompatibility. In this review paper, antileishmanial potencies of different metal nanoparticles, with particular emphasis on biogenic metal nanoparticles from 2011 to 2019, are summarized. The mechanisms by which metal-based nanomedicines kill Leishmania are also discussed.


Asunto(s)
Antiprotozoarios , Leishmania , Leishmaniasis , Nanopartículas del Metal , Antiprotozoarios/farmacología , Humanos , Leishmaniasis/tratamiento farmacológico
10.
J Photochem Photobiol B ; 205: 111821, 2020 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-32131044

RESUMEN

Iron oxide nanoparticles (Fe2O3NPs) are an interested and attractive area of research as they have numerous effective environmental and biomedical applications. Herein we have reported a simple and eco-benign synthesis Fe2O3NPs using Tamarix aphylla extract. The extract of the Tamarix aphylla acts both as a reducing and capping agent which leads to the fast and successful eco-benign synthesis of Fe2O3NPs.UV/Vis spectroscopy, XRD, EDX, SEM and TEM techniques were used to characterize and explore different features of Fe2O3NPs. UV/Vis studies showed asharppeak at 390 nm due to surface plasmon resonance absorption of Fe2O3NPs. XRD studies indicated that Fe2O3NPs were crystalline in nature. Structural features, elemental composition and geometry of Fe2O3NPswere confirmed by SEM, EDX and TEM. The as synthesized Fe2O3NPs showed efficient efficacy to degrade 100% of Methylene blue (MB) dye by 4 mg/25 ml MB and revealed 90% scavenging of the more stable DPPH free radical(1 mg/ml). Furthermore, Fe2O3NPs showed excellent antimicrobial activity against pathogenic multidrug resistant bacterial strains. The results of the present study explored the potential reducing, capping property of Tamarix aphylla extract, photocatalytic and biomedical applications of eco-benignly synthesized Fe2O3NPs which could be an alternative material for effective remediation of lethal organic pollutants and microbes.


Asunto(s)
Antibacterianos , Compuestos Férricos , Nanopartículas , Extractos Vegetales/química , Tamaricaceae , Antibacterianos/administración & dosificación , Antibacterianos/química , Antibacterianos/efectos de la radiación , Bacillus subtilis/efectos de los fármacos , Bacillus subtilis/crecimiento & desarrollo , Catálisis , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Escherichia coli/crecimiento & desarrollo , Compuestos Férricos/administración & dosificación , Compuestos Férricos/química , Compuestos Férricos/efectos de la radiación , Tecnología Química Verde , Luz , Azul de Metileno/química , Azul de Metileno/efectos de la radiación , Nanopartículas/administración & dosificación , Nanopartículas/química , Nanopartículas/efectos de la radiación , Fotólisis
11.
Eur J Med Chem ; 189: 112073, 2020 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-31991336

RESUMEN

In the current study, we reported a series of novel 1-H-pyrazole-3-carboxamide-based inhibitors targeting histone deacetylase (HDAC) and cyclin-dependent kinase (CDK). The representative compounds N-(4-((2-aminophenyl)carbamoyl)benzyl)-4-(2,6-dichlorobenzamido)-1H-pyrazole-3-carboxamide (7c) and N-(4-(2-((2-aminophenyl)amino)-2-oxoethyl)phenyl)-4-(2,6-dichlorobenzamido)-1H-pyrazole-3-carboxamide (14a) with potent antiproliferative activities towards five solid cancer cell lines, showed excellent inhibitory activities against HDAC2 (IC50 = 0.25 and 0.24 nM respectively) and CDK2 (IC50 = 0.30 and 0.56 nM respectively). In addition, compounds 7c and 14a significantly inhibited the migration of A375 and H460 cells. Further studies revealed that compounds 7c and 14a could arrest cell cycle in G2/M phase and promote apoptosis in A375, HCT116, H460 and Hela cells, which was associated with increasing the intracellular reactive oxygen species (ROS) levels. More importantly, compound 7c possessed favorable pharmacokinetic properties with the intraperitoneal bioavailability of 63.6% in ICR mice, and potent in vivo antitumor efficacy in the HCT116 xenograft model. Our study demonstrated that compound 7c provides a promising strategy for the treatment of malignant tumors.


Asunto(s)
Antineoplásicos/farmacología , Benzamidas/farmacología , Neoplasias del Colon/tratamiento farmacológico , Quinasas Ciclina-Dependientes/antagonistas & inhibidores , Descubrimiento de Drogas , Inhibidores de Histona Desacetilasas/farmacología , Histona Desacetilasas/química , Inhibidores de Proteínas Quinasas/farmacología , Animales , Antineoplásicos/química , Apoptosis , Benzamidas/química , Ciclo Celular , Proliferación Celular , Neoplasias del Colon/enzimología , Neoplasias del Colon/patología , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Inhibidores de Histona Desacetilasas/química , Humanos , Técnicas In Vitro , Ratones , Ratones Endogámicos BALB C , Ratones Endogámicos ICR , Ratones Desnudos , Inhibidores de Proteínas Quinasas/química , Células Tumorales Cultivadas , Ensayos Antitumor por Modelo de Xenoinjerto
12.
J Photochem Photobiol B ; 203: 111743, 2020 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-31864091

RESUMEN

The designing of new antibacterial agents with high and long-lasting activities are urgently needed in order to cope with the fast-emerging bacterial resistance. Zinc oxide nanoparticles (ZnO) have shown a significant promise as broad-spectrum antibacterial agents, and are efficient material in compromising bacterial membrane stability that leads to an increased cell permeability to nano-products. However, further engineering is required to improve their biological activities and to minimize their toxicity to healthy cells. In an attempt to resolve this issue, two semiconductor materials, ZnO and selenium (Se), were fabricated into a unique structural composite by a newly developed facile green method, and the designed composite was applied as an antibacterial nanomedicine. The developed methodology involves the initial preparation of ZnO, followed by its fabrication with Se at different temperatures (70 °C to 95 °C). Our experimental data showed that well defined interpenetrated crystalline Se network on ZnO (ZnO-Se) can be obtained at 80 °C for 180 min. The as-prepared ZnO-Se showed promising results in inhibiting the challenged bacterial strains under light irradiation (visible light) as compared to free ZnO. The enhanced biocidal property of ZnO-Se could be ascribed to its improved light-harvesting ability for sustainable induction of reactive oxygen species (ROS) and an active contact killing mechanism. Thus, ZnO-Se composite with a novel architecture could be a promising material in the treatment of bacterial infections by a mutual antibacterial synergy from the incorporated elements. Interestingly, the ZnO-Se has the ability to scavenge the overproduction of hydroxyl radicals, thus protecting the healthy cells from oxidative damage.


Asunto(s)
Antibacterianos/síntesis química , Luz , Nanocompuestos/química , Selenio/química , Óxido de Zinc/química , Antibacterianos/farmacología , Pruebas Antimicrobianas de Difusión por Disco , Nanocompuestos/toxicidad , Nanomedicina , Especies Reactivas de Oxígeno/metabolismo , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/efectos de la radiación , Temperatura
13.
J Photochem Photobiol B ; 199: 111632, 2019 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-31610431

RESUMEN

The development of eco-benign experimental procedures for the synthesis of nanomaterials is a fundamental developing branch of green nanotechnology. In this paper, green synthetic route was followed to synthesize novel Au@Fe2O3nanocomposite using Citrus sinensis fruit extract as a reducing and stabilizing agent. The as synthesized Au@Fe2O3nanocomposite was successfully characterized by UV-visible spectroscopy, X-ray diffraction (XRD), Scanning electron microscope (SEM), Energy-dispersive X-ray (EDX), Fourier transform infrared (FT1R) spectrophotometry and Zeta potential. UV-vis spectroscopy showed two SPR peaks for Fe2O3 and coated Au at 290 and 520 nm respectively. XRD confirmed the crystallinity of Au@Fe2O3. Au@Fe2O3 nanocomposite showed better antioxidant activity to effectively scavenge DPPH. The Au@Fe2O3 has been also tested for antibacterial activity which showed an effective antibacterial activity against multi drug resistant E.coli and Bacillus subtilis. Furthermore, Au@Fe2O3 also demonstrated better photo catalytic activity for methylene blue (MB) degradation. We proposed that the existence of organic acids (citric acids) also played a significant role in the stabilization of Au@Fe2O3, and plant (Citrus sinensis Var Kozan yerly) containing such component may be more effective for the green synthesis of Au@Fe2O3 nanocomposite. The findings of this study prove the overwhelming therapeutic and photocatalytic potential of bio-inspired Au@Fe2O3nanocomposite which can be a novel candidate for the effective remediation of microbes and toxic organic pollutants.


Asunto(s)
Antibacterianos/síntesis química , Antioxidantes/síntesis química , Citrus sinensis/química , Compuestos Férricos/química , Oro/química , Nanocompuestos/química , Procesos Fotoquímicos , Extractos Vegetales/química , Bacillus subtilis/efectos de los fármacos , Catálisis , Ácido Cítrico/química , Escherichia coli/efectos de los fármacos , Tecnología Química Verde/métodos , Luz , Azul de Metileno/química , Pruebas de Sensibilidad Microbiana/métodos , Oxidación-Reducción , Propiedades de Superficie , Contaminación Química del Agua
14.
Eur J Med Chem ; 176: 195-207, 2019 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-31103900

RESUMEN

Previously, we focused on a series of 2-aminobenzamide-based histone deacetylase (HDAC) inhibitors, compound 9 of which displayed potent HDAC inhibitory activity against HDAC1 and HDAC2, and moderate anti-proliferative activity against several cancer cell lines. In the current study, we have designed and synthesized a series of novel HDAC inhibitors based on thioether moiety with 9 as a lead compound. Representative compounds12 g and 12 h showed apparently potent anti-proliferative activities against five solid cancer cell lines: A549, HCT116, Hela, A375 and SMMC7721, and low cytotoxicity against NIH 3T3 normal cells. Especially, 12 g and 12 h also revealed potent HDAC inhibitory activity against HDAC1, 2 and 3. In addition, the two compounds could arrest cell cycle in G2/M phase and promote cell apoptosis. Moreover, they showed extended inhibition of colony formation and effectively blocked cell migration towards A549 cancer cells. Furthermore, 12 g and 12 h possessed better pharmacokinetic properties than the lead compound 9. Benefiting from these results, we also explored 12 g and 12 h in the A549 xenografts model for in vivo antitumor activity. The in vivo experiment indicated that 12 g and 12 h could evidently augment antitumor activity (TGI = 56.9% and 62.7% respectively).


Asunto(s)
Antineoplásicos/uso terapéutico , Benzamidas/uso terapéutico , Inhibidores de Histona Desacetilasas/uso terapéutico , Sulfuros/uso terapéutico , Animales , Antineoplásicos/síntesis química , Antineoplásicos/farmacocinética , Antineoplásicos/toxicidad , Apoptosis/efectos de los fármacos , Benzamidas/síntesis química , Benzamidas/farmacocinética , Benzamidas/toxicidad , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Diseño de Fármacos , Ensayos de Selección de Medicamentos Antitumorales , Puntos de Control de la Fase G2 del Ciclo Celular/efectos de los fármacos , Inhibidores de Histona Desacetilasas/síntesis química , Inhibidores de Histona Desacetilasas/farmacocinética , Inhibidores de Histona Desacetilasas/toxicidad , Humanos , Ratones , Simulación del Acoplamiento Molecular , Células 3T3 NIH , Sulfuros/síntesis química , Sulfuros/farmacocinética , Sulfuros/toxicidad , Ensayos Antitumor por Modelo de Xenoinjerto
15.
Eur J Med Chem ; 173: 185-202, 2019 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-31003060

RESUMEN

A series of novel 2-aminobenzamide derivatives decorated with thioquinazolinone were designed and synthesized as histone deacetylase (HDAC) inhibitors. These derivatives were evaluated for their antiproliferative activities against several human cancer cell lines including A375, Hela, A549, HCT116 and SMMC7721. It's significantly indicated that some inhibitors exhibited potent antiproliferative activities towards all the studied cancer cell lines. Compounds 7a, 4i, 4o, and 4p exhibited higher antiproliferative activities towards three cancer cell lines: A375, A549 and SMMC7721 compared to CS055, MS275, and CI994. Compound 4p showed more than 4000-fold the isoform selectivity for HDAC1 and more than 250-fold selectivity for HDAC2 compared with HDAC6. The molecular docking analysis reasonably explained the HDAC inhibitory activity and isoform selectivity. In addition, compounds 7a, 4i, 4o, and 4p showed potent inhibitory activities in migration assay and colony formation analysis, and also promoted cell apoptosis. Moreover, compounds 7a, 4i, and 4o inhibited the growth of SMMC7721 cells at S phase of the cell cycle. The immunofluorometric analysis indicated that compounds 7a, 4i, 4o, and 4p could increase the acetylation status of H3K9. Furthermore, in vivo anticancer efficacy of compound 4p was assessed in the A549 xenograft models, and 4p demonstrated potent antitumor activity (TGI = 62.5%). This study provided an effective strategy for further development of tumor-targeting therapy.


Asunto(s)
Antineoplásicos/farmacología , Diseño de Fármacos , Inhibidores de Histona Desacetilasas/farmacología , Histona Desacetilasas/metabolismo , Quinazolinonas/farmacología , ortoaminobenzoatos/farmacología , Animales , Antineoplásicos/síntesis química , Antineoplásicos/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Inhibidores de Histona Desacetilasas/síntesis química , Inhibidores de Histona Desacetilasas/química , Humanos , Ratones , Ratones Endogámicos BALB C , Ratones Desnudos , Estructura Molecular , Neoplasias Experimentales/tratamiento farmacológico , Neoplasias Experimentales/metabolismo , Neoplasias Experimentales/patología , Quinazolinonas/química , Relación Estructura-Actividad , ortoaminobenzoatos/síntesis química , ortoaminobenzoatos/química
16.
J Photochem Photobiol B ; 193: 31-38, 2019 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-30802773

RESUMEN

Metal nanoparticles, synthesized using Phyto-constituents are the most economically and environmentally benign materials ever. Biogenic silver nanoparticles (AgNPs) from three fractions of Arisaema flavum tuber extract were synthesized and characterized by UV-visible spectroscopy, XRD (X-rays diffraction), FT-IR (Fourier transform infrared spectroscopy) TEM (transmission electron microscopy) and EDX (Energy dispersive Microscopy). XRD pattern show the face centred cubic crystalline (Fcc) structure of AgNPs. FTIR spectra confirmed the presence of different Polyphenolic compounds capping the AgNps. UV-visible spectroscopy result confirmed the presence of Ag because of the particular surface plasmon Resonance (SPR) in the area of 400-430 nm. The electron microscope studies revealed the formation of spherical AgNPs with diameter ranging from 12 nm to 20 nm. Strong signals of AgNPs were confirmed with EDX analysis. The antibacterial properties of the AgNPs prepared with various extracts were tested against multi-drug resistant bacteria. Which showed significant antibacterial activity against all the multidrug resistant bacterial strains and especially multidrug resistant engineered E.ColiQH4. AgNPs synthesized by methanolic, Ethyl Acetate and aqueous Extracts of Areseama Flavum exhibited significant Photocatalytic activity to reduce methylene blue. Small size, spherical shape and high dispersion are the key properties due to which the AgNPs are having significant biological and photocatalytic activity. To the best of our knowledge, it is the first report of biogenic AgNPs regarding antibacterial activity against multidrug resistant Engineered E.Coli QH4.


Asunto(s)
Antibacterianos/farmacología , Arisaema/química , Escherichia coli/efectos de los fármacos , Nanopartículas del Metal/química , Extractos Vegetales/química , Plata/química , Antibacterianos/síntesis química , Antibacterianos/química , Arisaema/metabolismo , Catálisis , Pruebas Antimicrobianas de Difusión por Disco , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Escherichia coli/genética , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Tecnología Química Verde , Luz , Nanopartículas del Metal/toxicidad , Microscopía Electrónica de Transmisión , Tubérculos de la Planta/química , Tubérculos de la Planta/metabolismo , Espectroscopía Infrarroja por Transformada de Fourier , Resonancia por Plasmón de Superficie , Difracción de Rayos X
17.
Artif Cells Nanomed Biotechnol ; 46(sup3): S471-S480, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-30198334

RESUMEN

Utilizing novel approaches for the green synthesis of metal nanoparticles are of great importance. Therefore, we reported biogenic synthesis of silver nanoparticles (AgNPs) using extracts of Leptolyngbya strain JSC-1, and their significant applications against pathogenic bacteria and cancerous HeLa cell line. The biofabricated AgNPs were characterized by UV-visible spectroscopy, FTIR, SEM, TEM, DLS and zeta-potential. The as prepared AgNPs were assessed for inhibition of bacterial growth and induction of apoptosis in HeLa cells by different doses of AgNPs was evaluated. UV-visible spectroscopy and FTIR of AgNPs demonstrated the surface plasmon resonance at 413 nm and interaction among extract and nanoparticles, respectively. Electron microscopy revealed the morphology and DLS demonstrated size distribution of the particles (10-100 nm). Zeta potential values were between -47 and 0 mV, indicating stability of the particles. Proliferation of HeLa cells was significantly inhibited and severe cytotoxicity with higher intracellular uptake were observed after applying high concentration of AgNPs. Efficient inhibition zones (17 ± 2 and 21 ± 2 mm) were produced at maximum concentration (100 µl from 1 mg ml-1 stock of AgNPs) for Staphylococcus aureus and Escherichia coli, respectively. These findings reveal that the biofabricated AgNPs possess strong antibacterial activity and ability to induce apoptosis in cancer cell line (HeLa).


Asunto(s)
Antibacterianos , Apoptosis/efectos de los fármacos , Mezclas Complejas/química , Cianobacterias/química , Escherichia coli/crecimiento & desarrollo , Nanopartículas del Metal/química , Plata , Staphylococcus aureus/crecimiento & desarrollo , Antibacterianos/química , Antibacterianos/farmacología , Células HeLa , Humanos , Plata/química , Plata/farmacología
18.
Microb Pathog ; 125: 150-157, 2018 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-30217515

RESUMEN

Low cost and an easy technique for the synthesis of palladium nanoparticles (PdNPs) was developed. Glucosamine was used to stabilize palladium precursor (PdCl2) into palladium nanoparticles. Several analytical techniques were used for the determination of morphology, crystalline structure; size, capping, and composition of synthesize palladium nanoparticles. The UV-visible spectroscopy SPR peak (Surface Plasmon Resonance) at 284 nm revealed synthesis of PdNPs. Energy dispersive X-ray (EDX) and X-ray diffraction (XRD) studies proved the elemental composition and crystalline structure of the synthesized palladium nanoparticles respectively. The average particle sizes (5.5 nm) were obtained by using the 1 M glucosamine solution, with a fixed amount of PdCl2 (4 mM). Moreover, the as synthesized PdNPs was evaluated against Gram negative bacterial E. which shows tremendous antibacterial activity as compare to tobramycin standard antibiotics. It's mechanistically found that PdNPs damage cell membrane and caused imbalance of metabolism system of the cell as a result production of reactive oxygen species (ROS). Thus, these finding revealed that cells become leaky and all organelles come out from cells, finally caused death of the E. coli. Addition, the as prepared PdNPs also showed excellent catalytic activities toward reduction of methylene blue and 4-nitrophenol.Thus, glucosamine mediated PdNPs having dual functions biomedical as well as intoxicating catalyst for industries.


Asunto(s)
Antibacterianos/metabolismo , Glucosamina/metabolismo , Nanopartículas del Metal/ultraestructura , Paladio/metabolismo , Sustancias Reductoras/metabolismo , Membrana Celular/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Excipientes/metabolismo , Redes y Vías Metabólicas/efectos de los fármacos , Nanopartículas del Metal/química , Especies Reactivas de Oxígeno/metabolismo , Espectrometría por Rayos X , Análisis Espectral , Resonancia por Plasmón de Superficie , Difracción de Rayos X
19.
Dalton Trans ; 47(35): 12253-12263, 2018 Sep 11.
Artículo en Inglés | MEDLINE | ID: mdl-30106404

RESUMEN

In this paper, we present the fabrication of an expanded-perlite (EP)-based floating photocatalyst comprising CdS and Ag nanoparticles. In the Ag-CdS/EP nanocomposite, Ag-CdS was introduced as the photocatalytically active components and EP was employed as a low cost and sustainable support to reduce the problem of easy aggregation and improve the floating behavior of the designed catalyst. The Ag-CdS/EP photocatalyst was characterized via transmission electron microscopy (TEM), high-resolution transmission electron microscopy (HR-TEM), scanning electron microscopy (SEM), X-ray diffraction (XRD), UV-vis diffuse spectroscopy (UV-vis DRS), energy dispersive spectroscopy (EDS), X-ray photoelectron spectroscopy (XPS), and photoluminescence (PL) and photoelectrochemical measurements. The XRD and HR-TEM results confirmed the formation of cubic crystalline silver nanoparticles anchored on the surface of EP-immobilized hexagonal cubic CdS. The significantly enhanced photocatalytic activities of the Ag-CdS/EP nanocomposite with varying Ag contents were investigated for the degradation of rhodamine B (RhB) and phenol under visible light irradiation, and it was found that the photocatalytic reaction proceeds via first order kinetics. Furthermore, the desirable cycling ability (5 runs) of the Ag-CdS/EP photocatalyst indicates its promising stability and reusability. The designed novel photocatalyst also conforms to the development of green chemistry since no organic solvents were required.

20.
J Photochem Photobiol B ; 183: 342-348, 2018 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-29763756

RESUMEN

Graphene-based materials have attracted a significant attention in constructing hybrid systems for drug delivery with enhanced antimicrobial activities. In our work, we demonstrated the formation of silver nanoparticles (AgNPs) on graphene oxide (GO) using tobramycin (TOB), an aminoglycoside antibiotic, as reducing and decorating agent. The TOB decorated GO AgNPs (TOB-GO-Ag) composite was used as an antibacterial agent against multi-drug resistant Gram-negative E-coli (BL21 DE3). The reversal of surface potential from -30 mV (GO) to +20 mV confirms the successful reduction of GO by TOB. Atomic force microscopy (AFM) and high-resolution transmission electron microscopic (HRTEM) analyses confirmed the formation of uniformly distributed AgNPs on the reduced GO with an approximate particle size of 5 nm. The as-synthesized nanocomposite displayed significant antibacterial activity as compared to pure AgNPs and TOB. The positively charged TOB-GO-Ag interacts with the negatively charged E. coli membrane and inhibit bacterial growth by the antibacterial actions of the released silver, GO and tobramycin from the TOB-GO-Ag composite. The significant loss of bacterial membrane potential from -52 ±â€¯2 mV (control) to -2 ±â€¯1 mV (treated) indicates a severe cell wall damage caused by TOB-GO-Ag composite. Furthermore, fluorescence study also demonstrated a severe membrane disruption in bacterial cells treated with TOB-GO-Ag composite as compared to pure AgNPs and GO. In conclusion, the development of such hybrid systems would help in enhancing the efficacy of available drugs and eradicating the emerging bacterial resistance.


Asunto(s)
Antibacterianos/química , Grafito/química , Nanopartículas del Metal/química , Nanocompuestos/química , Plata/química , Tobramicina/química , Antibacterianos/síntesis química , Antibacterianos/farmacología , Supervivencia Celular/efectos de los fármacos , Pared Celular/química , Pared Celular/efectos de los fármacos , Sinergismo Farmacológico , Escherichia coli/efectos de los fármacos , Células HEK293 , Humanos , Microscopía de Fuerza Atómica , Microscopía Electrónica de Transmisión , Nanocompuestos/toxicidad , Óxidos/química , Especies Reactivas de Oxígeno/metabolismo , Espectroscopía Infrarroja por Transformada de Fourier , Tobramicina/farmacología
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