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1.
ACS Appl Bio Mater ; 7(3): 1790-1800, 2024 Mar 18.
Artigo em Inglês | MEDLINE | ID: mdl-38424007

RESUMO

A sustainable approach for pharmaceutically important pyrimidine derivatives is achieved by using biogenically produced single-phase δ-MnO2 NPs under external ligand-free conditions. The phytochemicals that comprise the extract of Areca Nut Husk (ANH) have been discovered to serve as reducing agents. The role of phytochemicals is not only to aid in the reduction of Mn(VII) into Mn(IV), but they also have an important role in stabilizing the catalyst. The establishment of δ-MnO2 NPs was confirmed inveterate by FE-SEM, p-XRD, ICP-OES (Mn content = 43.17% w/w), EDX, and with an active Mn content of 43.17% w/w. A series of pyrimidine derivatives were prepared in good yields using a one-pot multicomponent synthesis approach under atmospheric conditions. In addition, hot filtration tests, control experiments, gram-scale synthesis, and mechanistic investigations were demonstrated. Additionally, antimicrobial activity studies of δ-MnO2 NPs and pyrimidine derivatives against the Gram-negative bacteria E. coli, growth curve and minimum inhibitory concentration were studied.


Assuntos
Anti-Infecciosos , Nanopartículas , Escherichia coli , Compostos de Manganês/farmacologia , Óxidos , Nanopartículas/uso terapêutico , Pirimidinas/farmacologia , Anti-Infecciosos/farmacologia
2.
Artigo em Inglês | MEDLINE | ID: mdl-37688693

RESUMO

The present study reports highly stable polymeric nanoparticles comprising curcumin and polyvinylpyrrolidone, and then conjugated with gold nanoparticles, resulting in C-PVP and C-PVP-Au, respectively. The synthesized conjugates C-PVP and C-PVP-Au were investigated for amyloid aggregation inhibition activity, antimicrobial activity, and wound healing applications. The anti-amyloidogenic capacity of nanoconjugates were studied for model protein, hen egg-white lysozyme (HEWL). The ThT binding assay, fibril size measurement, and electron microscopy results revealed that conjugates suppress fibrillogenesis in HEWL. The highest amyloid inhibition activity obtained against C-PVP and C-PVP-Au was 31 µg.mL-1 and 30 µg.mL-1, respectively. The dissociation activity for amyloid aggregation was observed against Q-PVP and Q-PVP-Au at 29 µg.mL-1 and 27 µg.mL-1, respectively. The antibacterial studies show significant efficacy against Escherichia coli (E. coli) in the presence of C-PVP and C-PVP-Au. The substantial antibacterial potential of C-PVP@PVA and C-PVP-Au@PVA membranes shows promising wound healing applications. The PVA membranes with nanoparticles promote the antibacterial activity and wound healing activity in the Drosophila model. C-PVP-Au@PVA membrane healed the wound faster than the C-PVP@PVA, and it can be used for better results in wound healing. Thus, C-PVP-Au and C-PVP have higher bioavailability and stability and can act as multifunctional therapeutic agents for amyloid-related diseases and as wound healing agents. Graphical abstract C-PVP, and C-PVP-Au conjugates for inhibition of HEWL aggregation, antibacterial and wound healing activity.

3.
RSC Adv ; 12(36): 23661-23674, 2022 Aug 16.
Artigo em Inglês | MEDLINE | ID: mdl-36090438

RESUMO

Quercetin is an abundant plant polyphenol effective against several diseases due to its antioxidant and anti-inflammatory activity. Herein, we report novel polymeric quercetin nanorods and the former decorated with gold nanoparticles for the first time. The prepared conjugates quercetin-polyvinylpyrrolidone (Q-PVP) and quercetin-polyvinylpyrrolidone-gold nanoparticles (Q-PVP-Au) were characterized by UV-visible spectroscopy, Fourier transform infrared, dynamic light scattering, and zeta potential measurements. The surface morphology of conjugates was analyzed by field emission scanning electron microscopy. These conjugates exhibit harmonized rod-like morphology with a narrow size distribution. Furthermore, the quercetin conjugates with nanorod morphology exhibited enhanced and prolonged drug release over a long period. The synthesized conjugates were investigated for lysozyme aggregation kinetics. ThT binding assay, fibril size measurement, and electron microscopy results revealed that conjugates could suppress fibrillogenesis in lysozyme. The highest amyloid aggregation inhibition activity (IC50) was obtained against Q-PVP and Q-PVP-Au at 32 µg mL-1 and 30 µg mL-1 respectively. The amyloid aggregate disintegration activity (DC50) obtained against Q-PVP and Q-PVP-Au was 27 µg mL-1 and 29 µg mL-1 respectively. The present quercetin conjugates exhibit enhanced bioavailability and stability. They were potent inhibitors of lysozyme aggregation that may find applications as a therapeutic agent in neurological diseases like Alzheimer's and Parkinson's.

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