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1.
Mol Divers ; 25(2): 763-776, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-32100245

RESUMO

The present research paper reports the convenient synthesis, successful characterization, in vitro antibacterial, antifungal, antioxidant potency and biocompatibility of N-acyl-morpholine-4-carbothioamides (5a-5j). The biocompatible derivatives were found to be highly active against the tested bacterial and fungal strains. Moreover, some of the screened N-acyl-morpholine-4-carbothioamides exhibited excellent antioxidant potential. Docking simulation provided additional information about possibilities of their inhibitory potential against RNA. It has been predicted by in silico investigation of the binding pattern that compounds 5a and 5j can serve as the potential surrogate for design of novel and potent antibacterial agents. The results for the in vitro bioassays were promising with the identification of compounds 5a and 5j as the lead and selective candidate for RNA inhibition. Results of the docking computations further ascertained the inhibitory potential of compound 5a. Based on the in silico studies, it can be suggested that compounds 5a and 5j can serve as a structural model for the design of antibacterial agents with better inhibitory potential. Binding mode of compound 5j inside the active site of RNA in 3D space. 5j displayed highest antibacterial potential than the reference drug ampicillin with ZOI 10.50 mm against Staphylococcus aureus. 5j also displayed highest antifungal potential than the reference drug amphotericin B with ZOI 18.20 mm against Fusarium solani.


Assuntos
Antibacterianos , Antifúngicos , Antioxidantes , Morfolinas , Tioamidas , Antibacterianos/síntese química , Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/síntese química , Antifúngicos/química , Antifúngicos/farmacologia , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/farmacologia , Aspergillus flavus/efeitos dos fármacos , Aspergillus flavus/crescimento & desenvolvimento , Aspergillus niger/efeitos dos fármacos , Aspergillus niger/crescimento & desenvolvimento , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Compostos de Bifenilo/química , Células Cultivadas , Eritrócitos/efeitos dos fármacos , Fusarium/efeitos dos fármacos , Fusarium/crescimento & desenvolvimento , Hemólise/efeitos dos fármacos , Humanos , Simulação de Acoplamento Molecular , Morfolinas/síntese química , Morfolinas/química , Morfolinas/farmacologia , Picratos/química , RNA/química , Tioamidas/síntese química , Tioamidas/química , Tioamidas/farmacologia
2.
Chem Biodivers ; 17(3): e1900509, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31943755

RESUMO

The present study reports the convenient synthesis, spectroscopic characterization, bio-assays and computational evaluation of a novel series of N-acyl-1H-imidazole-1-carbothioamides. The screened derivatives displayed excellent antioxidant activity, moderate antibacterial and antifungal potential. The screened derivatives were found to be highly biocompatible against hRBCs. Molecular docking ascertained the mechanism and mode of action towards the molecular target delineating that ligands and complexes were stabilized at the active site by electrostatic and hydrophobic forces in accordance to the corresponding experimental results. Docking simulation provided additional information about the possibilities of inhibitory potential of the compounds against RNA. Computational evaluation predicted that N-acyl-1H-imidazole-1-carbothioamides 5c and 5g can serve as potential surrogates for hit to lead generation and design of novel antioxidant and antibacterial agents.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Materiais Biocompatíveis/farmacologia , Imidazóis/farmacologia , Simulação de Acoplamento Molecular , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Antioxidantes/síntese química , Antioxidantes/química , Materiais Biocompatíveis/síntese química , Materiais Biocompatíveis/química , Compostos de Bifenilo/antagonistas & inibidores , Relação Dose-Resposta a Droga , Desenho de Fármacos , Eritrócitos/efeitos dos fármacos , Humanos , Imidazóis/síntese química , Imidazóis/química , Estrutura Molecular , Picratos/antagonistas & inibidores , Relação Estrutura-Atividade
3.
Open Life Sci ; 16(1): 14-30, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33817294

RESUMO

Nanotechnology is the fabrication, characterization, and potential application of various materials at the nanoscale. Over the past few decades, nanomaterials have attracted researchers from different fields because of their high surface-to-volume ratio and other unique and remarkable properties. Cobalt and cobalt oxide nanoparticles (NPs) have various biomedical applications because of their distinctive antioxidant, antimicrobial, antifungal, anticancer, larvicidal, antileishmanial, anticholinergic, wound healing, and antidiabetic properties. In addition to biomedical applications, cobalt and cobalt oxide NPs have been widely used in lithium-ion batteries, pigments and dyes, electronic thin film, capacitors, gas sensors, heterogeneous catalysis, and for environmental remediation purposes. Different chemical and physical approaches have been used to synthesize cobalt and cobalt oxide NPs; however, these methods could be associated with eco-toxicity, cost-effectiveness, high energy, and time consumption. Recently, an eco-friendly, safe, easy, and simple method has been developed by researchers, which uses biotic resources such as plant extract, microorganisms, algae, and other biomolecules such as starch and gelatin. Such biogenic cobalt and cobalt oxide NPs offer more advantages over other physicochemically synthesized methods. In this review, we have summarized the recent literature for the understanding of green synthesis of cobalt and cobalt oxide NPs, their characterization, and various biomedical applications.

4.
Nanomedicine (Lond) ; 15(5): 467-488, 2020 02.
Artigo em Inglês | MEDLINE | ID: mdl-32063095

RESUMO

Aim: To demonstrate synthesis of cerium oxide nanoparticles (CeO2 NPs) by a green method using Hyphaene thebaica, and investigate their therapeutic applications. Materials & methods: Structural, vibrational and luminescent properties were established using x-ray diffraction, Fourier transformed infrared spectroscopy, Raman spectroscopy, ultraviolet absorption spectroscopy, selected area electron diffraction, electron microscopy and photolumincence spectroscopy. Therapeutic properties were established using different in vitro assays. Results: CeO2 NPs were determined to be crystalline in nature with a grain size of approximately 14 nm. They had characteristic Ce-O vibration at 481 cm-1. Photoluminescence spectra revealed broad bands at 463 and 600 nm. ζ potential was recorded as -17.2 mV. Potent antimicrobial and antiviral properties with hemocompatibility were reported. Conclusion: Biosynthesized CeO2 NPs revealed multifunctional therapeutic properties.


Assuntos
Anti-Infecciosos/farmacologia , Antivirais/farmacologia , Cério/farmacologia , Nanopartículas Metálicas , Química Verde , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
5.
Mater Sci Eng C Mater Biol Appl ; 112: 110890, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32409045

RESUMO

Maghemite (Fe2O3-NPs) nanoparticles were synthesized by a convenient, green and cost effective method using aqueous fruit extracts of Hyphaene thebaica. Different techniques like FTIR, XRD, UV-Vis, Raman, HR-TEM, EDS. SAED, Zeta potential were used to establish the nature of Fe2O3-NPs, while the therapeutic properties were studied using different biological assays including antiviral, antibacterial, antifungal, antioxidant and enzyme inhibition assays. XRD pattern revealed sharp peaks and a crystalline nature of Fe2O3-NPs. HR-TEM revealed quasi-spherical and cuboidal morphologies, while the particle size in ~10 nm. FTIR indicated a sharp peak centered at ~444 cm-1 which is the characteristic FeO band vibration. SAED pattern indicated the crystalline nature while EDS also confirmed the synthesis of Fe2O3 NPs. Zeta potential was obtained in different solvents and physiological buffers indicating highest value in water (-26.5 mV) and lowest in DMSO (-15.8 mV). Tested bacterial strains, Bacillus subtilis was found to be inhibited significantly. Aspergillus flavus appeared to be susceptible to all of the tested concentration of Fe2O3 NPs. Maximum 40.78% FRSA was obtained at 400 µg/mL. Cell culture based studies on RD cells and L20B cells indicated reduction in viability of cells with increase concentration of Fe2O3 NPs. Moderate inhibition of polio virus-1 and polio virus-2 was observed, after culturing the virus in the L20B cells. Excellent Protein Kinase (PK) inhibition was revealed. Hemolytic potential and cytotoxic potential was indicated to be dose dependent. In conclusion, the present report for the first time reports the synthesis of Fe2O3 NPs from H. thebaica fruits and reveals their biomedical potential including antiviral potential.


Assuntos
Arecaceae/química , Nanopartículas Magnéticas de Óxido de Ferro/química , Extratos Vegetais/química , Animais , Antibacterianos/síntese química , Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/síntese química , Antifúngicos/química , Antifúngicos/farmacologia , Antivirais/síntese química , Antivirais/química , Antivirais/farmacologia , Arecaceae/metabolismo , Aspergillus flavus/efeitos dos fármacos , Bacillus subtilis/efeitos dos fármacos , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Frutas/química , Frutas/metabolismo , Química Verde , Hemólise/efeitos dos fármacos , Humanos , Nanopartículas Magnéticas de Óxido de Ferro/toxicidade , Oxirredução , Tamanho da Partícula , Poliovirus/efeitos dos fármacos , Poliovirus/fisiologia
6.
Nanomedicine (Lond) ; 15(17): 1653-1669, 2020 07.
Artigo em Inglês | MEDLINE | ID: mdl-32669064

RESUMO

Aim: The biosynthesis of chromium oxide nanoparticles (Cr2O3 NPs), using Hyphaene thebaica as a bioreductant, for assessment of their potential nanomedicinal applications. Materials & methods: Biosynthesized Cr2O3 NPs were characterized by x-ray diffraction, Fourier-transform infrared spectroscopy, energy dispersive x-ray spectroscopy, scanning and transmission electron microscopy, selected area electron diffraction, UV-Vis spectroscopy and ζ-potential measurement. In vitro assays were used to assess the biological properties of Cr2O3 NPs. Results: Nanoparticles with size approximately 25-38 nm were obtained with a characteristic Cr-O vibration at 417 cm-1. A broad spectrum antimicrobial potential and antioxidant nature is reported. Slight inhibition of polio virus and biocompatibility at low doses was observed. Conclusion: We conclude a multifunctional nature of biogenic Cr2O3 NPs.


Assuntos
Anti-Infecciosos , Nanopartículas Metálicas , Extratos Vegetais , Antibacterianos , Espectrometria por Raios X , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
7.
Biomolecules ; 10(1)2019 12 27.
Artigo em Inglês | MEDLINE | ID: mdl-31892257

RESUMO

The rising burden of cancer worldwide calls for an alternative treatment solution. Herbal medicine provides a very feasible alternative to western medicine against cancer. This article reviews the selected plant species with active phytochemicals, the animal models used for these studies, and their regulatory aspects. This study is based on a meticulous literature review conducted through the search of relevant keywords in databases, Web of Science, Scopus, PubMed, and Google Scholar. Twenty plants were selected based on defined selection criteria for their potent anticancer compounds. The detailed analysis of the research studies revealed that plants play an indispensable role in fighting different cancers such as breast, stomach, oral, colon, lung, hepatic, cervical, and blood cancer cell lines. The in vitro studies showed cancer cell inhibition through DNA damage and activation of apoptosis-inducing enzymes by the secondary metabolites in the plant extracts. Studies that reported in vivo activities of these plants showed remarkable results in the inhibition of cancer in animal models. Further studies should be performed on exploring more plants, their active compounds, and the mechanism of anticancer actions for use as standard herbal medicine.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Neoplasias/tratamento farmacológico , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Animais , Antineoplásicos Fitogênicos/química , Proliferação de Células/efeitos dos fármacos , Modelos Animais de Doenças , Medicina Herbária , Humanos , Neoplasias/metabolismo , Neoplasias/patologia , Compostos Fitoquímicos/química , Extratos Vegetais/química
8.
AMB Express ; 9(1): 200, 2019 Dec 12.
Artigo em Inglês | MEDLINE | ID: mdl-31832797

RESUMO

Biosynthesis of bismuth vanadate (BiVO4) nanorods was performed using dried fruit extracts of Hyphaene thebaica as a cost effective reducing and stabilizing agent. XRD, DRS, FTIR, zeta potential, Raman, HR-SEM, HR-TEM, EDS and SAED were used to study the main physical properties while the biological properties were established by performing diverse assays. The zeta potential is reported as - 5.21 mV. FTIR indicated Bi-O and V-O vibrations at 640 cm-1 and 700 cm-1/1120 cm-1. Characteristic Raman modes were observed at 166 cm-1, 325 cm-1 and 787 cm-1. High resolution scanning and transmission electron micrographs revealed a rod like morphology of the BiVO4. Bacillus subtilis, Klebsiella pneumonia, Fusarium solani indicated highest susceptibility to the different doses of BiVO4 nanorods. Significant protein kinase inhibition is reported for BiVO4 nanorods which suggests their potential anticancer properties. The nanorods revealed good DPPH free radical scavenging potential (48%) at 400 µg/mL while total antioxidant capacity of 59.8 µg AAE/mg was revealed at 400 µg/mL. No antiviral activity is reported on sabin like polio virus. Overall excellent biological properties are reported. We have shown that green synthesis can replace well established processes for synthesizing BiVO4 nanorods.

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