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1.
Pharmaceuticals (Basel) ; 16(1)2022 Dec 22.
Artigo em Inglês | MEDLINE | ID: mdl-36678510

RESUMO

Alzheimer's disease (AD) is a devastating neurodegenerative disorder without a cure. Hence, developing an effective treatment or protective agent is crucial for public health. The present study aims to characterize orange peel extract (OPE) through in vitro and in silico studies. Furthermore, it examines the protective effect of OPE against experimentally-induced Alzheimer's disease in rats. The total phenolic and flavonoid content of OPE was 255.86 ± 1.77 and 52.06 ± 1.74 (mg/100 g), respectively. Gallic acid, the common polyphenol in OPE detected by HPLC was 3388.60 µg/100 g. OPE antioxidant IC50 was 67.90 ± 1.05, 60.48 ± 0.91, and 63.70 ± 0.30 by DPPH, ABTS and Hydroxyl radical scavenging activity methods, respectively. In vitro anti-acetylcholinesterase (AChE) IC50 was 0.87 ± 0.025 mg/mL for OPE and 2.45 ± 0.001 mg/mL for gallic acid. Molecular docking analysis for human AChE (4EY7) with donepezil, gallic acid, and acetylcholine showed binding energy ΔG values of -9.47, -3.72, and -5.69 Kcal/mol, respectively. Aluminum chloride injection (70 mg/Kg/day for 6 weeks) induced Alzheimer's-like disease in male rats. OPE (100 and 200 mg/kg/d) and gallic acid (50 mg/kg/d) were administered orally to experimental animals for 6 weeks in addition to aluminum chloride injection (as protective). OPE was found to protect against aluminum chloride-induced neuronal damage by decreasing both gene expression and activity of acetylcholinesterase (AChE) and a decrease in amyloid beta (Aß42) protein level, thiobarbituric acid-reactive substances (TBARS), and nitric oxide (NO), and increased reduced glutathione (GSH) level and activity of the antioxidant enzymes in the brain tissues. Additionally, gene expressions for amyloid precursor protein (APP) and beta secretase enzyme (BACE1) were downregulated, whereas those for presinilin-2 (PSEN2) and beta cell lymphoma-2 (BCL2) were upregulated. Furthermore, the reverse of mitochondrial alternation and restored brain ultrastructure might underlie neuronal dysfunction in AD. In conclusion, our exploration of the neuroprotective effect of OPE in vivo reveals that OPE may be helpful in ameliorating brain oxidative stress, hence protecting from Alzheimer's disease progression.

2.
Sci Rep ; 11(1): 6224, 2021 03 18.
Artigo em Inglês | MEDLINE | ID: mdl-33737634

RESUMO

In plants, Fruits and their wastes are the main sources of bioactive compounds. Currently, Annona fruits have attracted the attention of people interested in health-promoting foods due to their phytochemical content that their activities were not studied before. This study aimed to explore the potential antioxidant, antimicrobial, and in vitro anticancer activity of two cultivars Annona squamosa (Annona b. and Annona h.) seed, peel, and pulp. We also meausred phenolic, flavonoid, sulfated polysaccharide, tannins, and triterpenoids. Polyphenol identification was determined using RP-HPLC. Results of the antioxidant activity revealed that the highest activity was observed for Annona h. seed extract using DPPH and ABTS assays with IC50 6.07 ± 0.50 and 9.58 ± 0.53 µg/ml, respectively. The antimicrobial activity against various pathogenic strains revealed that the peel extracts of both Annona b. and Annona h. exhibited the best antimicrobial activity. We also assessed the IC50 values for anticancer activity in all six Annona b. and Annona h samples against four cancer cell lines colon (Caco-2), prostate (PC3), liver (HepG-2), and breast (MCF-7) using MTT assay. Annona b. and Annona h seed extracts had the lowest IC50 values for four cancer cell lines with 7.31 ± 0.03 and 15.99 ± 1.25 for PC-3 and MCF-7, respectively. Both seed extracts, Annona b. and Annona h., showed significantly down-regulated mRNA expression of Bcl-2 and up-regulated p53 in all treated cell lines. Apoptosis was evaluated using nuclear staining, flow cytometric analysis, and immunohistochemistry of the proliferation marker (Ki-67). Additional studies are required to characterize the bioactive compounds responsible for the observed activities of Annona seed and determine its mechanism as an anticancer drug.


Assuntos
Annona/química , Anti-Infecciosos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Flavonoides/farmacologia , Triterpenos/farmacologia , Anti-Infecciosos/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Apoptose/efeitos dos fármacos , Apoptose/genética , Benzotiazóis/antagonistas & inibidores , Compostos de Bifenilo/antagonistas & inibidores , Células CACO-2 , Candida/efeitos dos fármacos , Candida/crescimento & desenvolvimento , Flavonoides/isolamento & purificação , Frutas/química , Expressão Gênica/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/crescimento & desenvolvimento , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/crescimento & desenvolvimento , Células Hep G2 , Humanos , Concentração Inibidora 50 , Antígeno Ki-67/genética , Antígeno Ki-67/metabolismo , Células MCF-7 , Células PC-3 , Fenóis/isolamento & purificação , Fenóis/farmacologia , Picratos/antagonistas & inibidores , Extratos Vegetais/química , Polissacarídeos/isolamento & purificação , Polissacarídeos/farmacologia , Proteínas Proto-Oncogênicas c-bcl-2/genética , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Sementes/química , Ácidos Sulfônicos/antagonistas & inibidores , Taninos/isolamento & purificação , Taninos/farmacologia , Triterpenos/isolamento & purificação , Proteína Supressora de Tumor p53/genética , Proteína Supressora de Tumor p53/metabolismo
3.
Toxins (Basel) ; 12(12)2020 11 27.
Artigo em Inglês | MEDLINE | ID: mdl-33260849

RESUMO

Pomegranate, similar to other fruits, has juice-extraction by-products. Pomegranate seed oil (PGO) is a non-traditional oil with health benefits, rich in bioactive components. This study was aimed to assess PGO phytochemicals and their influence as bioactive components to reduce mycotoxin secretion. The encapsulation was applied in micro and nanoforms to protect the quality and enhance the efficacy of the oil. The PGO was extracted using ultrasound-assisted methods. Carotenoids, tocochromanols, sterols, phenolic, flavonoid, antioxidant, and antimicrobial activity were determined. The fatty acid profile was analyzed by the GC-MS, while mycotoxin was determined utilizing the HPLC apparatus. The toxicity and protective action of oil were examined using the hepatocytes' cell line. The resultant oil acts as oleoresin that is rich in bioactive molecules. Phenolics and antioxidant potency recorded higher values compared to traditional vegetable oils, whereas polyunsaturated fatty acids were 87.51%. The major fatty acid was conjugated punicic acid (81.29%), which has high biological effects. Application of the PGO on fungal media reduced aflatoxins secretion up to 63%, and zearalenone up to 78.5%. These results confirm the bio-functionality of oil to regulate the fungal secondary metabolites process. The PGO is a unique prospective non-traditional oil and has several functionalities in food, which achieve nutritional, antioxidant, and anti-mycotoxigenic activities.


Assuntos
Fungos/efeitos dos fármacos , Micotoxinas/metabolismo , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Punica granatum/química , Animais , Anti-Infecciosos/farmacologia , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Linhagem Celular , Hepatócitos/efeitos dos fármacos , Camundongos , Testes de Sensibilidade Microbiana
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