Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 25
Filtrar
Mais filtros










Base de dados
Intervalo de ano de publicação
1.
Sci Total Environ ; 899: 165726, 2023 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-37495153

RESUMO

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.


Assuntos
Metais Pesados , Poluentes do Solo , Humanos , Cromo/metabolismo , Biodegradação Ambiental , Metais Pesados/metabolismo , Plantas/metabolismo , Poluentes do Solo/análise , Solo
2.
ACS Omega ; 8(21): 18940-18950, 2023 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-37273635

RESUMO

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.
Artigo em Inglês | MEDLINE | ID: mdl-35888280

RESUMO

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.
Artigo em Inglês | MEDLINE | ID: mdl-34832332

RESUMO

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.
Artigo em Inglês | MEDLINE | ID: mdl-34343667

RESUMO

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.


Assuntos
Grafite , Nanocompostos , Fotoquimioterapia , Óxido de Zinco , Antibacterianos/farmacologia , Escherichia coli , Fotoquimioterapia/métodos , Fármacos Fotossensibilizantes
6.
Bioresour Bioprocess ; 8(1): 23, 2021 Mar 23.
Artigo em Inglês | MEDLINE | ID: mdl-38650208

RESUMO

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.
Artigo em Inglês | MEDLINE | ID: mdl-32841752

RESUMO

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.


Assuntos
Nanopartículas Metálicas , Nanocompostos , Fotoquimioterapia , Humanos , Fotoquimioterapia/métodos , Fármacos Fotossensibilizantes , Extratos Vegetais , Folhas de Planta , Prata
8.
Eur J Med Chem ; 198: 112322, 2020 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-32361064

RESUMO

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.


Assuntos
Antineoplásicos/síntese química , Benzamidas/química , Neoplasias do Colo/tratamento farmacológico , Quinase 2 Dependente de Ciclina/antagonistas & inibidores , Histona Desacetilases/metabolismo , Inibidores de Proteínas Quinases/síntese química , Purinas/química , Animais , Antineoplásicos/farmacocinética , Antineoplásicos/uso terapêutico , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Humanos , Masculino , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos ICR , Camundongos Nus , Simulação de Acoplamento Molecular , Neoplasias Experimentais , Inibidores de Proteínas Quinases/farmacocinética , Inibidores de Proteínas Quinases/uso terapêutico , Relação Estrutura-Atividade
9.
J Photochem Photobiol B ; 205: 111821, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32131044

RESUMO

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.


Assuntos
Antibacterianos , Compostos Férricos , Nanopartículas , Extratos Vegetais/química , Tamaricaceae , Antibacterianos/administração & dosagem , Antibacterianos/química , Antibacterianos/efeitos da radiação , Bacillus subtilis/efeitos dos fármacos , Bacillus subtilis/crescimento & desenvolvimento , Catálise , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Compostos Férricos/administração & dosagem , Compostos Férricos/química , Compostos Férricos/efeitos da radiação , Química Verde , Luz , Azul de Metileno/química , Azul de Metileno/efeitos da radiação , Nanopartículas/administração & dosagem , Nanopartículas/química , Nanopartículas/efeitos da radiação , Fotólise
10.
Nanomedicine (Lond) ; 15(8): 809-828, 2020 04.
Artigo em Inglês | MEDLINE | ID: mdl-32207379

RESUMO

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.


Assuntos
Antiprotozoários , Leishmania , Leishmaniose , Nanopartículas Metálicas , Antiprotozoários/farmacologia , Humanos , Leishmaniose/tratamento farmacológico
11.
Eur J Med Chem ; 189: 112073, 2020 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-31991336

RESUMO

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.


Assuntos
Antineoplásicos/farmacologia , Benzamidas/farmacologia , Neoplasias do Colo/tratamento farmacológico , Quinases Ciclina-Dependentes/antagonistas & inibidores , Descoberta de Drogas , Inibidores de Histona Desacetilases/farmacologia , Histona Desacetilases/química , Inibidores de Proteínas Quinases/farmacologia , Animais , Antineoplásicos/química , Apoptose , Benzamidas/química , Ciclo Celular , Proliferação de Células , Neoplasias do Colo/enzimologia , Neoplasias do Colo/patologia , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Inibidores de Histona Desacetilases/química , Humanos , Técnicas In Vitro , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos ICR , Camundongos Nus , Inibidores de Proteínas Quinases/química , Células Tumorais Cultivadas , Ensaios Antitumorais Modelo de Xenoenxerto
12.
J Photochem Photobiol B ; 203: 111743, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31864091

RESUMO

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.


Assuntos
Antibacterianos/síntese química , Luz , Nanocompostos/química , Selênio/química , Óxido de Zinco/química , Antibacterianos/farmacologia , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Nanocompostos/toxicidade , Nanomedicina , Espécies Reativas de Oxigênio/metabolismo , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/efeitos da radiação , Temperatura
13.
J Photochem Photobiol B ; 199: 111632, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31610431

RESUMO

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.


Assuntos
Antibacterianos/síntese química , Antioxidantes/síntese química , Citrus sinensis/química , Compostos Férricos/química , Ouro/química , Nanocompostos/química , Processos Fotoquímicos , Extratos Vegetais/química , Bacillus subtilis/efeitos dos fármacos , Catálise , Ácido Cítrico/química , Escherichia coli/efeitos dos fármacos , Química Verde/métodos , Luz , Azul de Metileno/química , Testes de Sensibilidade Microbiana/métodos , Oxirredução , Propriedades de Superfície , Poluição Química da Água
14.
Eur J Med Chem ; 176: 195-207, 2019 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-31103900

RESUMO

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).


Assuntos
Antineoplásicos/uso terapêutico , Benzamidas/uso terapêutico , Inibidores de Histona Desacetilases/uso terapêutico , Sulfetos/uso terapêutico , Animais , Antineoplásicos/síntese química , Antineoplásicos/farmacocinética , Antineoplásicos/toxicidade , Apoptose/efeitos dos fármacos , Benzamidas/síntese química , Benzamidas/farmacocinética , Benzamidas/toxicidade , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos , Inibidores de Histona Desacetilases/síntese química , Inibidores de Histona Desacetilases/farmacocinética , Inibidores de Histona Desacetilases/toxicidade , Humanos , Camundongos , Simulação de Acoplamento Molecular , Células NIH 3T3 , Sulfetos/síntese química , Sulfetos/farmacocinética , Sulfetos/toxicidade , Ensaios Antitumorais Modelo de Xenoenxerto
15.
Eur J Med Chem ; 173: 185-202, 2019 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-31003060

RESUMO

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.


Assuntos
Antineoplásicos/farmacologia , Desenho de Fármacos , Inibidores de Histona Desacetilases/farmacologia , Histona Desacetilases/metabolismo , Quinazolinonas/farmacologia , ortoaminobenzoatos/farmacologia , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Inibidores de Histona Desacetilases/síntese química , Inibidores de Histona Desacetilases/química , Humanos , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Estrutura Molecular , Neoplasias Experimentais/tratamento farmacológico , Neoplasias Experimentais/metabolismo , Neoplasias Experimentais/patologia , Quinazolinonas/química , Relação Estrutura-Atividade , ortoaminobenzoatos/síntese química , ortoaminobenzoatos/química
16.
J Photochem Photobiol B ; 193: 31-38, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30802773

RESUMO

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.


Assuntos
Antibacterianos/farmacologia , Arisaema/química , Escherichia coli/efeitos dos fármacos , Nanopartículas Metálicas/química , Extratos Vegetais/química , Prata/química , Antibacterianos/síntese química , Antibacterianos/química , Arisaema/metabolismo , Catálise , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Escherichia coli/genética , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Química Verde , Luz , Nanopartículas Metálicas/toxicidade , Microscopia Eletrônica de Transmissão , Tubérculos/química , Tubérculos/metabolismo , Espectroscopia de Infravermelho com Transformada de Fourier , Ressonância de Plasmônio de Superfície , Difração de Raios X
17.
Microb Pathog ; 125: 150-157, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30217515

RESUMO

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.


Assuntos
Antibacterianos/metabolismo , Glucosamina/metabolismo , Nanopartículas Metálicas/ultraestrutura , Paládio/metabolismo , Substâncias Redutoras/metabolismo , Membrana Celular/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Excipientes/metabolismo , Redes e Vias Metabólicas/efeitos dos fármacos , Nanopartículas Metálicas/química , Espécies Reativas de Oxigênio/metabolismo , Espectrometria por Raios X , Análise Espectral , Ressonância de Plasmônio de Superfície , Difração de Raios X
18.
Artif Cells Nanomed Biotechnol ; 46(sup3): S471-S480, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30198334

RESUMO

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).


Assuntos
Antibacterianos , Apoptose/efeitos dos fármacos , Misturas Complexas/química , Cianobactérias/química , Escherichia coli/crescimento & desenvolvimento , Nanopartículas Metálicas/química , Prata , Staphylococcus aureus/crescimento & desenvolvimento , Antibacterianos/química , Antibacterianos/farmacologia , Células HeLa , Humanos , Prata/química , Prata/farmacologia
19.
Dalton Trans ; 47(35): 12253-12263, 2018 Sep 11.
Artigo em Inglês | MEDLINE | ID: mdl-30106404

RESUMO

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.
Artigo em Inglês | MEDLINE | ID: mdl-29763756

RESUMO

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.


Assuntos
Antibacterianos/química , Grafite/química , Nanopartículas Metálicas/química , Nanocompostos/química , Prata/química , Tobramicina/química , Antibacterianos/síntese química , Antibacterianos/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Parede Celular/química , Parede Celular/efeitos dos fármacos , Sinergismo Farmacológico , Escherichia coli/efeitos dos fármacos , Células HEK293 , Humanos , Microscopia de Força Atômica , Microscopia Eletrônica de Transmissão , Nanocompostos/toxicidade , Óxidos/química , Espécies Reativas de Oxigênio/metabolismo , Espectroscopia de Infravermelho com Transformada de Fourier , Tobramicina/farmacologia
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...