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1.
ACS Omega ; 8(18): 15920-15931, 2023 May 09.
Artigo em Inglês | MEDLINE | ID: mdl-37179630

RESUMO

Cancer treatment development is hampered by chemotherapy side effects, drug resistance, and tumor metastasis, giving cancer patients a gloomy prognosis. Nanoparticles (NPs) have developed as a promising medicinal delivery technique in the last 10 years. The zinc oxide (ZnO) NPs can precisely and captivatingly promote the apoptosis of cancer cells in cancer treatment. There is also an urgent need to discover novel anti-cancer therapies, and current research suggests that ZnO NPs hold significant promise. ZnO NPs have been tested for phytochemical screening and in vitro chemical efficiency. The green synthesis method was employed for the preparation of ZnO NPs from Sisymbrium irio (L.) (Khakshi). An alcoholic and aqueous extract of S. irio was prepared using the Soxhlet method. Various chemical compounds were revealed in the methanolic extract through qualitative analysis. The results of quantitative analysis showed that the total phenolic content has the highest amount (42.7861 mgGAE/g), while the resultant amounts of (5.72175 mgAAE/g) and (15.20725 mgAAE/g) were obtained in total flavonoid content and antioxidant property, respectively. ZnO NPs were prepared using a 1:1 ratio. The synthesized ZnO NPs were identified to have a hexagonal wurtzite crystal arrangement. The nanomaterial was characterized by scanning electron microscopy, transmission electron microscopy, and UV-visible spectroscopy. The ZnO-NPs' morphology exhibited an absorbance at 350-380 nm. Furthermore, different fractions were prepared and assessed for anticancer activity. As a result of this anticancer activity, all fractions exhibited cytotoxic activity against both BHK and HepG2 human cancer cell lines. The methanol fraction showed the highest activity of 90% (IC50 = 0.4769 mg/mL), followed by the hexane fraction that showed 86.72%, ethyl acetate showed 85%, and chloroform fraction showed 84% against BHK and HepG2 cell lines. These findings suggested that synthesized ZnO-NPs have anticancer potential.

2.
Drug Dev Res ; 82(8): 1169-1181, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-33983647

RESUMO

Urease plays a significant role in the pathogenesis of urolithiasis pyelonephritis, urinary catheter encrustation, hepatic coma, hepatic encephalopathy, and peptic acid duodenal ulcers. Salvinia molesta was explored to identify new bioactive compounds with particular emphasis on urease inhibitors. The aqueous methanol extract was fractionated using solvents of increasing polarity. A series of column chromatography and later HPLC were performed on butanol extract. The structures of the resulting pure compounds were resolved using NMR (1D and 2D), infrared, and mass spectroscopy. The novel isolate was evaluated for antioxidant activity (using DPPH, superoxide anion radical scavenging, oxidative burst, and Fe+2 chelation assays), anti-glycation behavior, anticancer activity, carbonic anhydrase inhibition, phosphodiesterase inhibition, and urease inhibition. One new glucopyranose derivative 6'-O-(3,4-dihydroxybenzoyl)-4'-O-(4-hydroxybenzoyl)-α/ß-D-glucopyranoside (1) and four known glycosides were identified. Glycoside 1 demonstrated promising antioxidant potential with IC50 values of 48.2 ± 0.3, 60.3 ± 0.6, and 42.1 ± 1.8 µM against DPPH, superoxide radical, and oxidative burst, respectively. Its IC50 in the Jack bean urease inhibition assay was 99.1 ± 0.8 µM. The mechanism-based kinetic studies presented that compound 1 is a mixed-type inhibitor of urease with a Ki value of 91.8 ± 0.1 µM. Finally, molecular dynamic simulations exploring the binding mode of compound 1 with urease provided quantitative agreement between estimated binding free energies and the experimental results. The studies corroborate the use of compound 1 as a lead for QSAR studies as an antioxidant and urease inhibitor. Moreover, it needs to be further evaluated through the animal model, that is, in vivo or tissue culture-based ex-vivo studies, to establish their therapeutic potential against oxidative stress phosphodiesterase-II and urease-induced pathologies.


Assuntos
Antioxidantes/isolamento & purificação , Extratos Vegetais/análise , Traqueófitas/química , Urease/antagonistas & inibidores , Antioxidantes/farmacologia , Inibidores Enzimáticos/isolamento & purificação , Medições Luminescentes , Simulação de Acoplamento Molecular , Inibidores de Fosfodiesterase/isolamento & purificação , Urease/química
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