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1.
Molecules ; 27(4)2022 Feb 16.
Artigo em Inglês | MEDLINE | ID: mdl-35209121

RESUMO

This study aimed at fabricating gold (Au), iron (Fe) and selenium (Se) nanoparticles (NPs) using various natural plant extracts from the Fertile Crescent area and evaluating their potential application as antioxidant and biocompatible agents to be used in the pharmaceutical field, especially in drug delivery. The Au-NPs were synthesized using Ephedra alata and Pistacia lentiscus extracts, whereas the Fe-NPs and Se-NPs were synthesized using peel, fruit and seed extracts of Punica granatum. The phytofabricated NPs were characterized by the UV-visible spectroscopy, scanning electron microscope, Fourier transform infrared spectroscopy, X-ray diffraction (XRD) and energy-dispersive X-ray (EDS) spectroscopy. Scanning electron microscope technique showed that the synthesized NPs surface was spherical, and the particle size analysis confirmed a particle size of 50 nm. The crystalline nature of the NPs was confirmed by the XRD analysis. All synthesized NPs were found to be biocompatible in the fibroblast and human erythroleukemic cell lines. Se-NPs showed a dose-dependent antitumor activity as evidenced from the experimental results with breast cancer (MCF-7) cells. A dose-dependent, free-radical scavenging effect of the Au-NPs and Se-NPs was observed in the DPPH (2,2-Diphenyl-1-picrylhydrazyl) assay, with the highest effect recorded for Au-NPs.


Assuntos
Complexos de Coordenação/síntese química , Complexos de Coordenação/farmacologia , Ouro/química , Química Verde , Ferro/química , Nanopartículas Metálicas/química , Compostos Fitoquímicos/química , Selênio/química , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Antioxidantes/síntese química , Antioxidantes/farmacologia , Complexos de Coordenação/química , Humanos , Células MCF-7 , Nanopartículas Metálicas/ultraestrutura , Análise Espectral
2.
Biomed Res Int ; 2022: 5562849, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35047637

RESUMO

The silver nanoparticles (AgNPs) were synthesized via green synthesis approach using Euporbia serpens Kunth aqueous extract. The synthesized AgNPs were characterized by UV-visible spectroscopy and Furrier Transformer Infra-Red spectroscopy to justify the reduction and stabilization of AgNPs from its precursors. AgNPs characteristic absorption peak was observed at 420 nm in the UV-visible spectrum. The SEM and TEM analysis demonstrated the spherical shape of the synthesized nanoparticles with particle sizes ranging from 30 nm to 80 nm. FTIR transmission bands at 2920 cm-1, 1639 cm-1, 1410 cm-1, 3290 cm-1, and 1085 cm-1 were attributed to C-H, C=O, C-C, N-H, and C-N functional groups, respectively. XRD peaks could be attributed to (111), (200), (220), and (311) crystalline plane of the faced-centered cube (FCC) crystalline structure of the metallic silver nanoparticles. The AgNPs showed good antibacterial activity against all the tested bacteria at each concentration. The particles were found to be more active against Escherichia coli (E. coli) with 20 ± 06 mm and Salmonella typhi (S. typhi) with 18 ± 0.5 mm zone of inhibition in reference to standard antibiotic amoxicillin with 23 ± 0.3 mm and 20 ± 0.4 mm zone of inhibition, respectively. Moderate antifungal activities were observed against Candida albicans (C. albicans) and Alternaria alternata (A. alternata) with zone of inhibitions 16.5 mm and 15 mm, respectively, compared to the standard with 23 mm of inhibition. Insignificant antifungal inhibition of 7.5 mm was observed against Fusarium gramium (F. gramium). All the tested concentrations of AgNPs showed comparable % RSA with the standard reference ascorbic acid in the range sixty percent to seventy five percent. The percent motility at 3 hours postincubation showed quick response and most Tetramorium caespitum were found deceased or paralyzed. Similarly, the percent mortality showed a linear response at concentration and time. It was observed that 1 µg/mL to 2 µg/mL concentration of AgNPs displayed a significant cytotoxic activity against Artemia salina with LD50 of 5.37 and 5.82, respectively.


Assuntos
Anti-Infecciosos , Antioxidantes , Citotoxinas , Euphorbia/química , Nanopartículas Metálicas , Extratos Vegetais/química , Prata , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/farmacologia , Citotoxinas/síntese química , Citotoxinas/química , Citotoxinas/farmacologia , Nanopartículas Metálicas/química , Nanopartículas Metálicas/uso terapêutico , Testes de Sensibilidade Microbiana , Prata/química , Prata/farmacologia
3.
Nucleosides Nucleotides Nucleic Acids ; 40(12): 1159-1197, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34612797

RESUMO

Novel and synthetically essential flavonoids compounds containing the organosulfur moiety from Schiff bases, as well as their copper complexes, were synthesized from chrysin and 2-(phenylthio)aniline. These complexes were characterized using elemental analysis, mass spectrometry, electronic absorption spectroscopy, IR, 1H, and 13C NMR spectroscopy techniques. All the Cu(II) complexes exhibit square planar geometry. The in vitro antimicrobial activities of the investigated compounds were tested against the bacterial species, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus epidermidis, and Klebsiella pneumoniae and fungal species, Aspergillus niger, Fusarium solani, Culvularia lunata, Rhizoctonia bataicola, and Candida albicans by serial dilution method. The DNA binding and DNA cleavage properties of copper complexes were studied. Free radical scavenging, superoxide dismutase, glutathione peroxidase, and antioxidant activities of the copper complexes have also been studied. In addition, using the egg albumin process, the in vitro anti-inflammatory efficacy of metal chelates was examined. Anti-tuberculosis and α-glucosidase inhibition activity were carried out from the prepared metal complexes. The flavonoid compounds containing the organosulfur moiety of Cu(II) complexes (1-8) exhibited better therapeutic agent.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Complexos de Coordenação/farmacologia , DNA/efeitos dos fármacos , Animais , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Antioxidantes/síntese química , Antioxidantes/química , Ascomicetos/efeitos dos fármacos , Aspergillus niger/efeitos dos fármacos , Compostos de Bifenilo/antagonistas & inibidores , Candida albicans/efeitos dos fármacos , Bovinos , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , Cobre/química , Cobre/farmacologia , Clivagem do DNA/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Flavonoides/química , Flavonoides/farmacologia , Fusarium/efeitos dos fármacos , Klebsiella pneumoniae/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Picratos/antagonistas & inibidores , Pseudomonas aeruginosa/efeitos dos fármacos , Rhizoctonia/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus epidermidis/efeitos dos fármacos
4.
Pharm Dev Technol ; 26(9): 953-966, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34374616

RESUMO

The study aims at formulation and optimization of resveratrol and humic acid co-encapsulated colloidal polymeric nanocarriers to improve stability, oral bioavailability, and antiradical activity of water-insoluble, resveratrol. The eudragit E100 polymeric material was used to fabricate resveratrol and humic acid co-encapsulated oral colloidal polymeric nanocarriers (Res-HA-co-CPNs) using emulsification-diffusion-evaporation method. Taguchi orthogonal array design was employed to check the effect of formulation factors on in vitro physicochemical characteristics. The optimized formulation was further evaluated for oral bioavailability as well as for antiradical potential. Optimized Res-HA-co-CPNs demonstrated spherical and smooth surface including mean particle size, 120.56 ± 18.8 nm; polydispersity index, 0.122; zeta potential, +38.25 mV; and entrapment efficiency, 82.37 ± 1.49%. Solid-state characterization confirmed the amorphous characteristic of optimized Res-HA-co-CPNs. In vitro release profile of Res-HA-co-CPNs showed sustained release behavior up to 48 h and CPNs were found to remain stable at the refrigerated condition for 6 months. In vivo pharmacokinetic studies revealed significant (p < 0.05) improvement of ∼62.76-fold in oral bioavailability. The radical-scavenging activity was found to be increased with time and after 72 h, it was analogous to pure Res. IC50 values were reported to be decreased with time. Henceforth, developed Res-HA-co-CPNs was proven to be a proficient dosage form to increase stability, oral bioavailability, and antiradical activity of resveratrol.HighlightsResveratrol-humic acid co-encapsulated colloidal polymeric nanocarriers (Res-HA-co-CPNs) were fabricated by emulsification-diffusion-evaporation method and optimized by Taguchi orthogonal array design.The Res-HA-co-CPNs revealed favorable mean particle size and percent encapsulation efficiency with a spherical and smooth surface.The Res-HA-co-CPNs showed diffusion-controlled release of Res and were found to be stable at the refrigerated condition for 6 months.The optimized Res-HA-co-CPNs demonstrated significantly (p < 0.05) higher oral bioavailability with respect to pure Res and PM.The optimized Res-HA-co-CPNs demonstrated higher radical-scavenging activity with respect to time.


Assuntos
Portadores de Fármacos/síntese química , Composição de Medicamentos/métodos , Substâncias Húmicas , Nanopartículas/química , Polímeros/síntese química , Resveratrol/síntese química , Administração Oral , Animais , Antioxidantes/síntese química , Antioxidantes/metabolismo , Quelantes/síntese química , Quelantes/metabolismo , Coloides , Portadores de Fármacos/metabolismo , Avaliação Pré-Clínica de Medicamentos/métodos , Feminino , Masculino , Nanopartículas/metabolismo , Tamanho da Partícula , Polímeros/metabolismo , Ratos , Resveratrol/metabolismo
5.
Molecules ; 26(15)2021 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-34361702

RESUMO

Neurodegenerative diseases have a complex nature which highlights the need for multitarget ligands to address the complementary pathways involved in these diseases. Over the last decade, many innovative curcumin-based compounds have been designed and synthesized, searching for new derivatives having anti-amyloidogenic, inhibitory of tau formation, as well as anti-neuroinflammation, antioxidative, and AChE inhibitory activities. Regarding our experience studying 3-substituted coumarins with interesting properties for neurodegenerative diseases, our aim was to synthesize a new series of curcumin-coumarin hybrid analogues and evaluate their activity. Most of the 3-(7-phenyl-3,5-dioxohepta-1,6-dien-1-yl)coumarin derivatives 11-18 resulted in moderated inhibitors of hMAO isoforms and AChE and BuChE activity. Some of them are also capable of scavenger the free radical DPPH. Furthermore, compounds 14 and 16 showed neuroprotective activity against H2O2 in SH-SY5Y cell line. Nanoparticles formulation of these derivatives improved this property increasing the neuroprotective activity to the nanomolar range. Results suggest that by modulating the substitution pattern on both coumarin moiety and phenyl ring, ChE and MAO-targeted derivatives or derivatives with activity in cell-based phenotypic assays can be obtained.


Assuntos
Antioxidantes/síntese química , Inibidores da Colinesterase/síntese química , Cumarínicos/síntese química , Curcumina/análogos & derivados , Inibidores da Monoaminoxidase/síntese química , Fármacos Neuroprotetores/síntese química , Acetilcolinesterase/metabolismo , Animais , Antioxidantes/farmacologia , Compostos de Bifenilo/antagonistas & inibidores , Butirilcolinesterase/metabolismo , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Inibidores da Colinesterase/farmacologia , Cumarínicos/farmacologia , Curcumina/farmacologia , Proteínas Ligadas por GPI/metabolismo , Humanos , Peróxido de Hidrogênio/antagonistas & inibidores , Peróxido de Hidrogênio/farmacologia , Monoaminoxidase/metabolismo , Inibidores da Monoaminoxidase/farmacologia , Córtex Motor/citologia , Córtex Motor/enzimologia , Nanopartículas/química , Neurônios/citologia , Neurônios/efeitos dos fármacos , Neurônios/enzimologia , Fármacos Neuroprotetores/farmacologia , Picratos/antagonistas & inibidores , Cultura Primária de Células , Ratos , Relação Estrutura-Atividade
6.
Molecules ; 26(15)2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-34361812

RESUMO

Metal oxide nanoparticles synthesized by the biological method represent the most recent research in nanotechnology. This study reports the rapid and ecofriendly approach for the synthesis of CeO2 nanoparticles mediated using the Abelmoschus esculentus extract. The medicinal plant extract acts as both a reducing and stabilizing agent. The characterization of CeO2 NPs was performed by scanning electron microscopy (SEM), X-ray diffraction (XRD), ultraviolet-visible spectroscopy (UV-Vis), and Fourier transform infrared spectroscopy (FTIR). The in vitro cytotoxicity of green synthesized CeO2 was assessed against cervical cancerous cells (HeLa). The exposure of CeO2 to HeLa cells at 10-125 µg/mL caused a loss in cellular viability against cervical cancerous cells in a dose-dependent manner. The antibacterial activity of the CeO2 was assessed against S. aureus and K. pneumonia. A significant improvement in wound-healing progression was observed when cerium oxide nanoparticles were incorporated into the chitosan hydrogel membrane as a wound dressing.


Assuntos
Abelmoschus/química , Antioxidantes/síntese química , Extratos Vegetais/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Antibacterianos/química , Antibacterianos/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Proliferação de Células/efeitos dos fármacos , Cério/química , Química Verde/tendências , Células HeLa , Humanos , Nanopartículas Metálicas/química , Microscopia Eletrônica de Varredura , Extratos Vegetais/química , Espectroscopia de Infravermelho com Transformada de Fourier , Staphylococcus aureus/patogenicidade , Cicatrização/efeitos dos fármacos
7.
Molecules ; 26(16)2021 Aug 17.
Artigo em Inglês | MEDLINE | ID: mdl-34443574

RESUMO

Natural extracts are a rich source of biomolecules that are useful not only as antioxidant drugs or diet supplements but also as complex reagents for the biogenic synthesis of metallic nanoparticles. The natural product components can act as strong reducing and capping substrates guaranteeing the stability of formed NPs. The current work demonstrates the suitability of extracts of Camellia sinensis, Ilex paraguariensis, Salvia officinalis, Tilia cordata, Levisticum officinale, Aegopodium podagraria, Urtica dioica, Capsicum baccatum, Viscum album, and marine algae Porphyra Yezoensis for green synthesis of AgNPs. The antioxidant power of methanolic extracts was estimated at the beginning according to their free radical scavenging activity by the DPPH method and reducing power activity by CUPRAC and SNPAC (silver nanoparticle antioxidant capacity) assays. The results obtained by the CUPRAC and SNAPC methods exhibited excellent agreement (R2~0.9). The synthesized AgNPs were characterized by UV-vis spectroscopy, Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), energy dispersive X-ray analysis (EDX), dynamic light scattering (DLS) particle size, and zeta potential. The UV-vis absorption spectra showed a peak at 423 nm confirming the presence of AgNPs. The shapes of extract-mediated AgNPs were mainly spherical, spheroid, rod-shaped, agglomerated crystalline structures. The NPs exhibited a high negative zeta potential value in the range from -49.8 mV to -56.1 mV, proving the existence of electrostatic stabilization. FTIR measurements indicated peaks corresponding to different functional groups such as carboxylic acids, alcohol, phenol, esters, ethers, aldehydes, alkanes, and proteins, which were involved in the synthesis and stabilization of AgNPs. Among the examined extracts, green tea showed the highest activity in all antioxidant tests and enabled the synthesis of the smallest nanoparticles, namely 62.51, 61.19, and 53.55 nm, depending on storage times of 30 min, 24 h, and 72 h, respectively. In turn, the Capsicum baccatum extract was distinguished by the lowest zeta potential, decreasing with storage time from -66.0 up to -88.6 mM.


Assuntos
Antioxidantes/síntese química , Antioxidantes/farmacologia , Nanopartículas Metálicas , Extratos Vegetais/química , Prata/química , Prata/farmacologia , Antioxidantes/química , Compostos de Bifenilo/química , Técnicas de Química Sintética , Química Verde , Picratos/química
8.
Bioorg Chem ; 114: 105080, 2021 09.
Artigo em Inglês | MEDLINE | ID: mdl-34225164

RESUMO

Antioxidants with high efficacy and low toxicity have the potential to treat cerebral ischemia reperfusion injury (CIRI). Dienone monocarbonyl curcumin analogs (DMCA) capable of overcoming the instability and pharmacokinetic defects of curcumin possess notable antioxidant activity but are found to be significantly toxic. In this study, a novel skeleton of the monoenone monocarbonyl curcumin analogue sAc possessing reduced toxicity and improved stability was designed on the basis of the DMCA skeleton. Moreover, 32 sAc analogs were obtained by applying a green, simple, and economical synthetic method. Multiple sAc analogs with an antioxidant protective effect in PC12 cells were screened using an H2O2-induced oxidative stress damage model, and quantitative evaluation of structure-activity relationship (QSAR) model with regression coefficient of R2 = 0.918921 was built through random forest algorithm (RF). Among these compounds, the optimally active compound sAc15 elicited a potent protective effect on cell growth of PC12 cells by effectively eliminating ROS generation in response to oxidative stress injury by activating the Nrf2/HO-1 antioxidant signaling pathway. In addition, sAc15 exhibited good protection against CIRI in the mice middle cerebral artery occlusion (MCAO) model. In this paper, we provide a novel class of antioxidants and a potential compound for stroke treatment.


Assuntos
Antioxidantes/farmacologia , Curcumina/farmacologia , Química Verde , Infarto da Artéria Cerebral Média/tratamento farmacológico , Substâncias Protetoras/farmacologia , Traumatismo por Reperfusão/tratamento farmacológico , Animais , Antioxidantes/síntese química , Antioxidantes/química , Células Cultivadas , Curcumina/análogos & derivados , Curcumina/química , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Desenho de Fármacos , Avaliação Pré-Clínica de Medicamentos , Infarto da Artéria Cerebral Média/patologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Estrutura Molecular , Estresse Oxidativo/efeitos dos fármacos , Células PC12 , Substâncias Protetoras/síntese química , Substâncias Protetoras/química , Ratos , Traumatismo por Reperfusão/patologia , Relação Estrutura-Atividade
9.
AAPS PharmSciTech ; 22(5): 167, 2021 Jun 02.
Artigo em Inglês | MEDLINE | ID: mdl-34080078

RESUMO

In developing countries, populations have employed herbal medicines for primary health care because they are believed to be more appropriate to the human body and have less side effects than chemically synthesized drugs. The present study aimed to develop and evaluate herbal tablets incorporated with a Thai traditional medicinal extract, U-pa-ri-waat (URW), using microwave-assisted extraction (MAE). The extraction efficiency for URW using MAE and traditional solvent extraction was compared based on the percent yield after spray drying. URW tablets were prepared using the dry granulation method. The optimized products were assessed using standard characterization methods based on the United States and British Pharmacopeias. DPPH and ABTS radical scavenging assays were performed to analyze the antioxidant capacity of the microwave-assisted extracts. The results revealed that the flowability of the dry granule with added maltodextrin was improved compared to a granule without additives, as indicated by an angle of repose of 33.69 ± 2.0°, a compressibility index of 15.38 ± 0.66, and a Hausner's ratio of 1.18 ± 0.06. The resulting formulation produced flat tablets with uniform weight variation, hardness, thickness, friability, and optimum disintegration time. The URW extracts showed antioxidant activity and MAE with maltodextrin carrier displayed the strongest DPPH and ABTS radical activities with IC50 values of 1.60 ± 0.02 µg/mL and 4.02 ± 0.24 µg/mL, respectively. The URW tablet formulation passed the quality control tests. Storage of the formulation tablets for 90 days under accelerated conditions had minimal effects on tablet characteristics.


Assuntos
Química Farmacêutica/métodos , Micro-Ondas , Compostos Fitoquímicos/síntese química , Preparações de Plantas/síntese química , Administração Oral , Antioxidantes/administração & dosagem , Antioxidantes/síntese química , Antioxidantes/farmacocinética , Avaliação Pré-Clínica de Medicamentos/métodos , Sequestradores de Radicais Livres/administração & dosagem , Sequestradores de Radicais Livres/síntese química , Sequestradores de Radicais Livres/farmacocinética , Medicina Herbária/métodos , Humanos , Compostos Fitoquímicos/administração & dosagem , Compostos Fitoquímicos/farmacocinética , Preparações de Plantas/administração & dosagem , Preparações de Plantas/farmacocinética , Comprimidos , Tailândia
10.
J Chem Neuroanat ; 116: 101990, 2021 10.
Artigo em Inglês | MEDLINE | ID: mdl-34146667

RESUMO

Cisplatin (CP) is a chemotherapy agent used in the treatment of cancer, but it has various side effects, in particular, neurotoxicity. Zinc oxide nanoparticles (ZnO NPs) are a potent antioxidant. However, there is limited knowledge about the protective effects of ZnO NPs against CP-induced hippocampal toxicity. The present study aimed to explore the potential protective effects of ZnO NPs against CP-induced oxidative stress, loss of neurotrophins support, and tissue damage in the hippocampus of the rats. Eighty adult male Wistar rats were dividing into ten groups including: control (Con), sham, ZnO Bulk (ZnB), chemical ZnO NPs (ChZnO NPs), Green ZnO NPs (GrZnO NPs), CP, CP + ZnB, CP + ChZnO NPs, CP + GrZnO NPs and CP + AE. CP was administrated (5 mg/kg/weekly) for four weeks, and animals were treated simultaneously with different forms of ZnO (5 mg/kg/day). At the end of the experiment, the activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), malondialdehyde (MDA), changes of reduced glutathione (GSH), oxidized glutathione (GSSG) and GSH/GSSG ratio, histological changes, expression of brain-derived neurotrophic factor (BDNF) and nerve growth factor (NGF) genes were assessed in the hippocampus. The results revealed that a decrease in BDNF and NGF mRNA expression, GSH concentration and GSH/GSSG ratio, increasing of GSSG and MDA levels, and neuronal loss in the CP-treated rats were reversed following the administration of different forms of ZnO, especially Gr ZnO NPs and ch ZnO NPs. Co-administration of ZnO NPs to CP-treated rats restored the suppressive effects of CP on activities of antioxidant enzymes (SOD, GPX, CAT). The results showed that in most of the evaluated factors, Gr ZnO NPs showed a greater protective effect than other forms of ZnO. The results suggest that ZnO NPs, in particular Green ZnO NPs (GrZnO NPs) had more potential protective effects against CP-induced oxidative stress, inadequate support neurotrophin and tissue damage in rat hippocampus.


Assuntos
Antioxidantes/farmacologia , Cisplatino/toxicidade , Hipocampo/metabolismo , Nanopartículas/administração & dosagem , Fatores de Crescimento Neural/biossíntese , Óxido de Zinco/farmacologia , Aloe , Animais , Antineoplásicos/toxicidade , Antioxidantes/síntese química , Química Verde/métodos , Hipocampo/efeitos dos fármacos , Masculino , Nanopartículas/química , Estresse Oxidativo/efeitos dos fármacos , Estresse Oxidativo/fisiologia , Extratos Vegetais/síntese química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Óxido de Zinco/síntese química
11.
Sci Rep ; 11(1): 13507, 2021 06 29.
Artigo em Inglês | MEDLINE | ID: mdl-34188065

RESUMO

Selenium nanoparticles (SeNPs) are gaining importance in the field of medicines due to their high surface area and unique properties than their other forms of selenium. In this study, biogenic selenium nanoparticles (B-SeNPs) were synthesized using cyanobacteria and their bioactivities (antioxidant, antimicrobial, anticancer and biocompatibility) were determined for comparison with commercially available chemically synthesized selenium nanoparticles (C-SeNPs). Color change of reaction mixture from sky blue to orange-red indicated the synthesis of biogenic SeNPs (B-SeNPs). UV-Vis spectra of the reaction mixture exhibited peak at 266 nm. During optimization, 30 °C of temperature, 24 h of time and 1:2 concentration ratio of sodium selenite and cell extract represented the best condition for SeNPs synthesis. Various functional groups and biochemical compounds present in the aqueous extract of Anabaena variabilis NCCU-441, which may have possibly influenced the reduction process of SeNPs were identified by FT-IR spectrum and GC-MS. The synthesized cyanobacterial SeNPs were orange red in color, spherical in shape, 10.8 nm in size and amorphous in nature. The B-SeNPs showed better anti-oxidant (DPPH, FRAP, SOR and ABTS assays), anti-microbial (antibacterial and antifungal) and anti-cancer activitities along with its biocompatibility in comparison to C-SeNPs suggesting higher probability of their biomedical application.


Assuntos
Anabaena variabilis/química , Antioxidantes , Nanopartículas Metálicas/química , Selênio/química , Antioxidantes/síntese química , Antioxidantes/química
12.
Artif Cells Nanomed Biotechnol ; 49(1): 354-366, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33792441

RESUMO

This study reports the synthesis of silver nanoparticles (AgNPs) from silver nitrate by leaf extract of a medicinal plant Ziziphus nummularia. The leaf extract acts as a reducing and stabilizing agent for the formation of nanoparticles. The green synthesized AgNPs were characterized by ultraviolet-visible (UV-vis) spectroscopy, Fourier transform infrared (FITR) spectroscopy, Thermogravimetric analysis (TGA), X-ray diffraction (XRD), transmission electron microscopy (TEM) analysis and evaluated their antimicrobial, antioxidant, cytotoxic and genotoxic potential. The UV-Vis spectroscopy showed a characteristic absorption peak at 430 nm due to surface plasma resonance. TEM analysis showed that synthesized AgNPs were spherical and oval with an average size of 25.96 nm. AgNPs showed effective antimicrobial activity (lowest MIC-0.625 µg/mL against Escherichia coli), synergistic antimicrobial activity (lowest ΣFIC 0.09 with chlormaphenicol against Corynebacterium rubrum) and antibiofilm activity. AgNPs showed strong DPPH activity with IC50 - 520 µg/mL and ABTS activity IC50 - 55 µg/mL and reducing capacity assessment. In vitro cytotoxic effect was evaluated by MTT assay against HeLa cells, breast cells and fibroblast cells. Genotoxic effect was evaluated by comet assay. AgNPs displayed dose-dependent cytotoxic and genotoxic effect. Our findings indicated that synthesized AgNPs could be considered as multifunctional and have great potential for use in biomedical applications.HighlightsSilver nanoparticles were synthesized using leaf extract of Ziziphus nummulariaCharacterization was done by various spectral techniquesAntimicrobial efficacy was demonstrated against an array of bacteriaAgNPs exhibited significant cytotoxic effect against HeLa cell lineAgNPs showed cytotoxicity and genotoxicity in a dose-dependent manner.


Assuntos
Nanopartículas Metálicas/química , Extratos Vegetais/química , Folhas de Planta/química , Prata/química , Prata/farmacologia , Ziziphus/química , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/farmacologia , Células HeLa , Humanos , Mutagênicos/síntese química , Mutagênicos/química , Mutagênicos/farmacologia
13.
Biomolecules ; 11(3)2021 03 22.
Artigo em Inglês | MEDLINE | ID: mdl-33809976

RESUMO

The current work aimed to synthesize selenium and zinc nanoparticles using the aqueous extract of Ephedra aphylla as a valuable medicinal plant. The prepared nanoparticles were characterized by TEM, zeta potential, and changes in the phytochemical constituents. Hence, the phenolic, flavonoid, and tannin contents were reduced in the case of the prepared samples of nanoparticles than the original values in the aqueous extract. The prepared extract of Ephedra aphylla and its selenium and zinc nanoparticles showed high potency as antioxidant agents as a result of the DPPH• assay. The samples were assessed as anticancer agents against six tumor cells and a normal lung fibroblast (WI-38) cell line. The selenium nanoparticles of Ephedra aphylla extract revealed very strong cytotoxicity against HePG-2 cells (inhibitory concentration (IC50) = 7.56 ± 0.6 µg/mL), HCT-116 cells (IC50 = 10.02 ± 0.9 µg/mL), and HeLa cells (IC50 = 9.23 ± 0.8 µg/mL). The samples were evaluated as antimicrobial agents against bacterial and fungal strains. Thus, selenium nanoparticles showed potent activities against Gram-negative strains (Salmonella typhimurium, Pseudomonas aeruginosa, Klebsiella pneumoniae, and Escherichia coli), Gram-positive strains (Bacillus cereus, Listeria monocytogenes, Staphylococcus aureus, and Staphylococcus epidermidis), and the fungal strain Candida albicans. In conclusion, the preparation of nanoparticles of either selenium or zinc is crucial for improved biological characteristics.


Assuntos
Anti-Infecciosos/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Ephedra/química , Nanopartículas Metálicas/química , Extratos Vegetais/química , Zinco/química , Antibacterianos/química , Antibacterianos/farmacologia , Anti-Infecciosos/síntese química , Antineoplásicos/química , Antioxidantes/síntese química , Candida albicans/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Staphylococcus aureus/efeitos dos fármacos
14.
Molecules ; 26(9)2021 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-33925409

RESUMO

A simple and efficient route for the synthesis of new glycoconjugates has been developed. The approach acts as a model for a mini-library of compounds with a deoxy-selenosugar core joined to a polyphenolic moiety with well-known antioxidant properties. An unexpected stereocontrol detected in the Mitsunobu key reaction led to the most attractive product showing a natural d-configuration. Thus, we were able to obtain the target molecules from the commercially available d-ribose via a shorter and convenient sequence of reactions.


Assuntos
Antioxidantes/síntese química , Glicoconjugados/síntese química , Compostos Organosselênicos/síntese química , Selênio/química , Antioxidantes/química , Glicoconjugados/química , Humanos , Compostos Organosselênicos/química
15.
Eur J Med Chem ; 220: 113475, 2021 Aug 05.
Artigo em Inglês | MEDLINE | ID: mdl-33901898

RESUMO

Harnessing the antioxidant cellular machinery has sparked considerable interest as an efficient anticancer strategy. Activating Nrf2, the master switch of the cellular redox system, suppresses ROS, alleviates oxidative stress, and halts cancer progression. 1,2,4-oxadiazoles are iconic direct Nrf2 activators that disrupt Nrf2 interaction with its endogenous repressor Keap1. This study introduces rationally designed 1,2,4-oxadiazole derivatives that inhibit other Nrf2 suppressors (TrxR1, IKKα, and NF-kB) thus enhancing Nrf2 activation for preventing oxidative stress and carcinogenesis. Preliminary screening showed that the phenolic oxadiazoles 11, 15, and 19 were comparable to ascorbic acid (ROS scavenging) and EDTA (iron chelation), and superior to doxorubicin against HepG-2, MDA-MB231, and Caco-2 cells. They suppressed ROS by 3 folds and activated Nrf2 by 2 folds in HepG-2 cells. Mechanistically, they inhibited TrxR1 (IC50; 13.19, 17.89, and 9.21 nM) and IKKα (IC50; 11.0, 15.94, and 19.58 nM), and downregulated NF-κB (7.6, 1.4 and 1.9 folds in HepG-2), respectively. They inhibited NADPH oxidase (IC50; 16.4, 21.94, and 10.71 nM, respectively) that potentiates their antioxidant activities. Docking studies predicted their important structural features. Finally, they recorded drug-like in silico physicochemical properties, ADMET, and ligand efficiency metrics.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Oxidiazóis/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Antioxidantes/síntese química , Antioxidantes/química , Compostos de Bifenilo/antagonistas & inibidores , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Oxidiazóis/síntese química , Oxidiazóis/química , Picratos/antagonistas & inibidores , Relação Estrutura-Atividade
16.
Biometals ; 34(4): 815-829, 2021 08.
Artigo em Inglês | MEDLINE | ID: mdl-33895912

RESUMO

Aqueous glutathione selenium nano-incorporation (GSH-SeN-Inco) was prepared by gamma radiation in presence of microbial glutathione (GSH) and selenium dioxide. The novel prepared GSH-SeN-Inco are validated by UV-vis spectroscopy, TEM (17.5 nm), DLS, XRD, EDX and FTIR spectrum reveals the presence of GSH moiety that coating the selenium nanoparticles (SeNPs) forming GSH-SeN-Inco. The XRD analysis verified the presence of metallic SeNPs. The nucleation and radiolysis mechanism of GSH-SeN-Inco formation are also discussed. The size GSH-SeN-Inco (17.5 nm) is affected by certain factors such as concentration of GSH, selenium dioxide, and absorbed dose of gamma radiation. The present study explored the positive role of GSH-SeN-Inco as an antitumor activity against HepG-2 and MCF-7, with IC50 at a concentration of 1.00 and 0.9 mM, respectively. The GSH-SeN-Inco show significant scavenging activity at 33%. The GSH-SeN-Inco shows antimicrobial potential against Gram-negative and Gram-positive bacteria with significant MIC especially Escherichia coli ATCC 25922 at 5.20 µg/ml.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Glutationa/farmacologia , Nanopartículas/química , Selênio/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Antioxidantes/síntese química , Antioxidantes/química , Compostos de Bifenilo/antagonistas & inibidores , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Glutationa/química , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Tamanho da Partícula , Picratos/antagonistas & inibidores , Selênio/química
17.
Biosci Biotechnol Biochem ; 85(3): 476-480, 2021 Feb 24.
Artigo em Inglês | MEDLINE | ID: mdl-33624772

RESUMO

Caffeic acid ß-phenethyl ester (CAPE), an antioxidative bioactive catechol isolated from propolis, was semisynthesized from chlorogenic acid and related compounds in an extract of raw (unroasted) Robusta coffee (Coffea canephora) beans in 5 steps and a total yield of 31%. Oxidative degradation of the intermediates and target molecule was prevented by alkaline hydrolysis of the chlorogenic acids in the presence of sodium dithionite (Na2S2O4) and deprotection of the catecholic diacetate precursor by Candida antarctica lipase B-mediated transesterification as the final step.


Assuntos
Antioxidantes/síntese química , Ácidos Cafeicos/síntese química , Coffea/química , Álcool Feniletílico/análogos & derivados , Extratos Vegetais/síntese química , Própole/química , Esterificação , Álcool Feniletílico/síntese química
18.
J Mater Chem B ; 9(6): 1592-1603, 2021 02 14.
Artigo em Inglês | MEDLINE | ID: mdl-33471014

RESUMO

Many coating materials are commercially available to combat microbial infections. However, these coatings are difficult to synthesize, and are mostly composed of toxic chemicals. Lignin is an under-explored natural biopolymer with multifaceted potential. Lignin, with adhesive, UV resistant, and antimicrobial properties, is a suitable candidate to develop coating materials. Here we report a smart method to fabricate a sustainable nanospray coating from lignin which does not require any toxic chemicals or additives during synthesis. Initially, we have developed stable lignin nanospheres in a single step in aqueous medium, which were later utilized as a lignin nanospray (LNSR). The LNSR was characterized by dynamic light scattering, scanning electron microscopy, FTIR and other analytical techniques. This LNSR showed remarkable UV blocking, antioxidant and light-activated antimicrobial properties. Interestingly, for the first time, the LNSR demonstrated photoluminescence, making it useful for bioimaging. Moreover, singlet oxygen generation potential was observed in the LNSR, which could render it useful in phototheranostic applications (i.e. light assisted imaging and photodynamic therapy). Further, the LNSR was directly utilized to fabricate a sustainable coating. The nanospray coating exhibited maximum light-induced cell killing when applied to common microbes as detected by live-dead cell imaging. Taken together, the lignin nanospray coating developed via a direct pathway holds great promise to disinfect microbes in the presence of light.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Materiais Revestidos Biocompatíveis/farmacologia , Luz , Lignina/farmacologia , Nanopartículas/química , Antibacterianos/síntese química , Antibacterianos/química , Antioxidantes/síntese química , Antioxidantes/química , Bacillus megaterium/efeitos dos fármacos , Materiais Revestidos Biocompatíveis/síntese química , Materiais Revestidos Biocompatíveis/química , Desenvolvimento de Medicamentos , Escherichia coli/efeitos dos fármacos , Lignina/síntese química , Lignina/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Tamanho da Partícula , Fotoquimioterapia , Propriedades de Superfície
19.
Int J Mol Sci ; 22(2)2021 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-33419098

RESUMO

This study deals with the green synthesis of chromium oxide (Cr2O3) nanoparticles using a leaf extract of Abutilon indicum (L.) Sweet as a reducing and capping agent. Different characterization techniques were used to characterize the synthesized nanoparticles such as X-ray diffraction (XRD), Scanning electron microscope (SEM), Transmission electron microscope (TEM), Energy-dispersive X-ray (EDX), Fourier transform infrared (FTIR), X-ray photoelectron spectroscopy (XPS), and ultraviolet-visible (UV-VIS) spectroscopy. The X-ray diffraction technique confirmed the purity and crystallinity of the Cr2O3 nanoparticles. The average size of the nanoparticles ranged from 17 to 42 nm. The antibacterial activity of the green synthesized nanoparticles was evaluated against four different bacterial strains, E. coli, S. aureus, B. bronchiseptica, and B. subtilis using agar well diffusion and a live/dead staining assay. The anticancer activities were determined against Michigan Cancer Foundation-7 (MCF-7) cancer cells using MTT and a live/dead staining assay. Antioxidant activity was investigated in the linoleic acid system. Moreover, the cytobiocompatibility was analyzed against the Vero cell lines using MTT and a live/dead staining assay. The results demonstrated that the green synthesized Cr2O3 nanoparticles exhibited superior antibacterial activity in terms of zones of inhibition (ZOIs) against Gram-positive and Gram-negative bacteria compared to plant extracts and chemically synthesized Cr2O3 nanoparticles (commercial), but comparable to the standard drug (Leflox). The green synthesized Cr2O3 nanoparticles exhibited significant anticancer and antioxidant activities against MCF-7 cancerous cells and the linoleic acid system, respectively, compared to chemically synthesized Cr2O3 nanoparticles. Moreover, cytobiocompatibility analysis displayed that they presented excellent biocompatibility with Vero cell lines than that of chemically synthesized Cr2O3 nanoparticles. These results suggest that the green synthesized Cr2O3 nanoparticles' enhanced biological activities might be attributed to a synergetic effect. Hence, green synthesized Cr2O3 nanoparticles could prove to be promising candidates for future biomedical applications.


Assuntos
Antibacterianos/química , Antineoplásicos/química , Antioxidantes/química , Materiais Biocompatíveis/química , Compostos de Cromo/química , Nanopartículas Metálicas/química , Animais , Antibacterianos/síntese química , Antibacterianos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Antioxidantes/síntese química , Antioxidantes/farmacologia , Bactérias/classificação , Bactérias/efeitos dos fármacos , Materiais Biocompatíveis/síntese química , Materiais Biocompatíveis/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Chlorocebus aethiops , Química Verde/métodos , Humanos , Células MCF-7 , Nanopartículas Metálicas/ultraestrutura , Testes de Sensibilidade Microbiana/métodos , Microscopia Eletrônica , Oxirredução/efeitos dos fármacos , Espectroscopia de Infravermelho com Transformada de Fourier , Células Vero , Difração de Raios X
20.
J Antibiot (Tokyo) ; 74(4): 233-243, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33441970

RESUMO

Addressed herein a series of thioureas starting from various amines and nicotinic acid have been synthesized. Notably, thiourea based scaffolds are increasingly employed in medicinal chemistry owing to their tunable physicochemical and structural properties. As well-known from the literature, the pyridine ring contains various biological properties, especially antimicrobial activity. Therefore, we performed the synthesis of biologically important thiourea derivatives containing pyridine ring. The structures of the synthesized compounds were characterized by 1H NMR, 13C NMR and FT-IR. In the second part of the study, newly synthesized compounds were also tested in order to demonstrate their antimicrobial and antioxidant properties. All compounds exhibited moderate activity against all tested bacteria known to cause nosocomial infections, which have acquired resistance to many antibiotics, as compared to the standard antibiotics and also strong antioxidant properties. Therefore, they can be evaluated as possible seeds of agents in the treatment of bacterial infections and many health problems related to aging such as cancer, and neurodegenerative diseases.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Tioureia/química , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Antioxidantes/síntese química , Antioxidantes/química , Desenho de Fármacos , Avaliação Pré-Clínica de Medicamentos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Espectroscopia de Infravermelho com Transformada de Fourier
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