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1.
Pak J Pharm Sci ; 37(1): 147-154, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38741411

RESUMO

Zeravschania khorasanica, a species endemic to the eastern part of Iran, possesses distinct characteristics that distinguish it from its two closely related species. This research employed five different extraction techniques to identify the active components, total phenolic content and in vitro antioxidant activity of the extract. Furthermore, hydro-distillation was utilized for GC/MS analysis to determine the composition of the essential oil. The total phenolic content was estimated using the Folin-Ciocalteu assay and the antioxidant capacity was evaluated using the DPPH radical scavenging test. The findings revealed that ethanolic Soxhlet extraction yielded the highest efficiency in extracting total phenolic content (88.19 ±1.99 gallic acid mg/100g). In contrast, water maceration extraction demonstrated the highest antioxidant activity (68.1 ±5.4%). Interestingly, the study uncovered that there is no significant positive correlation between the phenolic content and the antioxidant activity of the plant. Additionally, HPLC analysis identified three phenolic constituents in the extract. The Soxhlet extraction method yielded the highest levels of chlorogenic acid (5.8 ppm), caffeic acid (4.1 ppm) and salicylic acid (10.3 ppm). As per the GC/MS analysis, a total of eleven compounds were identified. The predominant compounds were elemicin at 58.19% and trans--bergamotene at 25.78%.


Assuntos
Antioxidantes , Apiaceae , Cromatografia Gasosa-Espectrometria de Massas , Fenóis , Extratos Vegetais , Solventes , Antioxidantes/isolamento & purificação , Antioxidantes/análise , Antioxidantes/farmacologia , Antioxidantes/química , Fenóis/análise , Fenóis/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Irã (Geográfico) , Solventes/química , Apiaceae/química , Cromatografia Líquida de Alta Pressão , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Óleos Voláteis/farmacologia , Compostos de Bifenilo/química , Picratos/química , Ácidos Cafeicos/isolamento & purificação , Ácidos Cafeicos/análise
2.
Chem Pharm Bull (Tokyo) ; 71(10): 766-774, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37779078

RESUMO

One of the most lethal cancers, glioblastoma (GBM), affects 14.5% of all central nervous system (CNS) tumors. Patients diagnosed with GBM have a meager median overall survival (OS) of 15 months. Extensive genetic analysis has shown that many dysregulated pathways, including the Wnt/ß-catenin signaling system, contribute to the pathogenicity of GBM. Paclitaxel (PTX) and temozolomide (TMZ) are recognized to have therapeutic potential in several types of cancer, including GBM. This work aimed to examine the impact of PTX and TMZ on the human glioma cell lines U251 and T98G using molecular docking simulations and gene expression profiles in the Wnt/ß-catenin signaling pathway. Standard procedure for Molecular Docking simulation, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay, and Flow Cytometry assay was used. Genes implicated in the Wnt/ß-catenin signaling pathway, including Dvl, Axin, APC, ß-catenin, and glycogen synthase kinase3-ß (GSK3ß), were subjected to real-time PCR. The estimated parameters for targets revealed that the average binding energy and inhibition constant (Ki) for the DVL, ß-Catenin, and GSK3ß, when targeted by PTX, were - 5.01 kcal/mol, - 5.4 kcal/mol, and - 9.06 kcal/mol, respectively. This energy range was - 6.34 kcal/mol for DVL, - 5.52 kcal/mol for ß-Catenin, and - 5.66 kcal/mol for GSK3ß as a result of TMZ's inhibitory actions. Gene expression analyses indicated that PTX and PTX/TMZ suppressed GSK3ß (p < 0.05). GSK3ß from the Wnt/ß-catenin signaling pathway was significantly targeted by PTX alone, and adding TMZ to PTX may improve the efficacy of glioblastoma treatment. In addition, the GSK3ß gene may help GBM therapy strategies as a potential PTX target.


Assuntos
Glioblastoma , Humanos , Temozolomida/farmacologia , Temozolomida/uso terapêutico , Glioblastoma/tratamento farmacológico , Simulação de Acoplamento Molecular , beta Catenina/genética , beta Catenina/metabolismo , beta Catenina/uso terapêutico , Glicogênio Sintase Quinase 3 beta/genética , Glicogênio Sintase Quinase 3 beta/metabolismo , Via de Sinalização Wnt , Paclitaxel/farmacologia , Linhagem Celular Tumoral , Resistencia a Medicamentos Antineoplásicos , Expressão Gênica , Proliferação de Células
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