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1.
Sci Rep ; 14(1): 10528, 2024 05 08.
Artículo en Inglés | MEDLINE | ID: mdl-38719861

RESUMEN

The current study aimed to assess the effect of the germination process of wild mustard seeds on the phenolic profile, antioxidant, antibacterial, and antidiabetic properties, and some relevant enzyme activities. The total phenolic and flavonoid contents increased 5- and 10-fold, respectively, and were maximized on 5-days sprouts. One new phenolic compound was identified on 5-days sprout extract using HPLC. The concentrations of the identified phenolic compounds increased 1.5-4.3 folds on 5-days sprouts compared with dry seeds. The total antioxidant activity multiplied 17- and 21-fold on 5-days sprouts using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) assays, respectively. The activity of carbohydrate-cleaving, phenolic-synthesizing and antioxidant enzymes also increased during germination. On 5-days sprouts, there was a substantial correlation between the highest ß-glucosidase and peroxidase activities with highest phenolic and flavonoid levels and maximum antioxidant activity. The phenolic extract of 5-days sprouts exhibited antimicrobial activities against Escherichia coli and Staphylococcus aureus and showed potent antidiabetic activity established by its inhibitory effect against α-amylase and α-glucosidase compared to dry seeds.


Asunto(s)
Antioxidantes , Germinación , Planta de la Mostaza , Fenoles , Extractos Vegetales , Semillas , Fenoles/análisis , Fenoles/farmacología , Fenoles/química , Antioxidantes/farmacología , Antioxidantes/química , Germinación/efectos de los fármacos , Semillas/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Planta de la Mostaza/química , Antibacterianos/farmacología , Antibacterianos/química , Flavonoides/análisis , Flavonoides/farmacología , Flavonoides/química , Hipoglucemiantes/farmacología , Hipoglucemiantes/química , Cromatografía Líquida de Alta Presión
2.
Int J Mol Sci ; 25(9)2024 Apr 26.
Artículo en Inglés | MEDLINE | ID: mdl-38731940

RESUMEN

Amyloid fibroproliferation leads to organ damage and is associated with a number of neurodegenerative diseases affecting populations worldwide. There are several ways to protect against fibril formation, including inhibition. A variety of organic compounds based on molecular recognition of amino acids within the protein have been proposed for the design of such inhibitors. However, the role of macrocyclic compounds, i.e., thiacalix[4]arenes, in inhibiting fibrillation is still almost unknown. In the present work, the use of water-soluble thiacalix[4]arene derivatives for the inhibition of hen egg-white lysozyme (HEWL) amyloid fibrillation is proposed for the first time. The binding of HEWL by the synthesized thiacalix[4]arenes (logKa = 5.05-5.13, 1:1 stoichiometry) leads to the formation of stable supramolecular systems capable of stabilizing the protein structure and protecting against fibrillation by 29-45%. The macrocycle conformation has little effect on protein binding strength, and the native HEWL secondary structure does not change via interaction. The synthesized compounds are non-toxic to the A549 cell line in the range of 0.5-250 µg/mL. The results obtained may be useful for further investigation of the anti-amyloidogenic role of thiacalix[4]arenes, and also open up future prospects for the creation of new ways to prevent neurodegenerative diseases.


Asunto(s)
Ácidos Carboxílicos , Muramidasa , Muramidasa/química , Humanos , Ácidos Carboxílicos/química , Ácidos Carboxílicos/farmacología , Animales , Células A549 , Amiloide/química , Amiloide/metabolismo , Amiloide/antagonistas & inhibidores , Unión Proteica , Fenoles/química , Fenoles/farmacología , Calixarenos/química , Calixarenos/farmacología , Sulfuros
3.
Int J Mol Sci ; 25(9)2024 Apr 27.
Artículo en Inglés | MEDLINE | ID: mdl-38731987

RESUMEN

Contemporary living is continuously leading to poor everyday choices resulting in the manifestation of various diseases. The benefits of plant-based nutrition are undeniable and research on the topic is rising. Modern man is now aware of the possibilities that plant nutrition can provide and is seeking ways to benefit from it. Dietary phenolic compounds are among the easily accessible beneficial substances that can exhibit antioxidant, anti-inflammatory, antitumor, antibacterial, antiviral, antifungal, antiparasitic, analgesic, anti-diabetic, anti-atherogenic, antiproliferative, as well as cardio-and neuroprotective activities. Several industries are exploring ways to incorporate biologically active substances in their produce. This review is concentrated on presenting current information about the dietary phenolic compounds and their contribution to maintaining good health. Additionally, this content will demonstrate the importance and prosperity of natural compounds for various fields, i.e., food industry, cosmetology, and biotechnology, among others.


Asunto(s)
Antioxidantes , Fenoles , Humanos , Fenoles/química , Fenoles/farmacología , Antioxidantes/farmacología , Antioxidantes/química , Animales , Dieta
4.
Int J Mol Sci ; 25(9)2024 Apr 29.
Artículo en Inglés | MEDLINE | ID: mdl-38732062

RESUMEN

Prunella vulgaris (PV) is one of the most commonly used nutraceuticals as it has been proven to have anti-inflammatory and antioxidant properties. The aim of this study was to evaluate the phytochemical composition of PV and its in vivo antioxidant properties. A phytochemical analysis measuring the total phenolic content (TPC), the identification of phenolic compounds by HPLC-DAD-ESI, and the evaluation of the in vitro antioxidant activity by the DPPH assay of the extract were performed. The antioxidant effects on inflammation induced by turpentine oil were experimentally tested in rats. Seven groups with six animals each were used: a control group, the experimental inflammation treatment group, the experimental inflammation and diclofenac sodium (DS) treatment group, and four groups with their inflammation treated using different dilutions of the extract. Serum redox balance was assessed based on total oxidative status (TOS), nitric oxide (NO), malondialdehyde (MDA), total antioxidant capacity (TAC), total thiols, and an oxidative stress index (OSI) contents. The TPC was 0.28 mg gallic acid equivalents (GAE)/mL extract, while specific representatives were represented by caffeic acid, p-coumaric acid, dihydroxybenzoic acid, gentisic acid, protocatechuic acid, rosmarinic acid, vanillic acid, apigenin-glucuronide, hesperidin, kaempferol-glucuronide. The highest amount (370.45 µg/mL) was reported for hesperidin, which is a phenolic compound belonging to the flavanone subclass. The antioxidant activity of the extracts, determined using the DPPH assay, was 27.52 mmol Trolox/mL extract. The PV treatment reduced the oxidative stress by lowering the TOS, OSI, NO, and MDA and by increasing the TAC and thiols. In acute inflammation, treatment with the PV extract reduced oxidative stress, with lower concentrations being more efficient and having a better effect than DS.


Asunto(s)
Antioxidantes , Inflamación , Estrés Oxidativo , Fitoquímicos , Extractos Vegetales , Prunella , Animales , Antioxidantes/farmacología , Antioxidantes/química , Ratas , Prunella/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Fitoquímicos/farmacología , Fitoquímicos/química , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Estrés Oxidativo/efectos de los fármacos , Masculino , Antiinflamatorios/farmacología , Antiinflamatorios/química , Fenoles/farmacología , Fenoles/análisis , Ratas Wistar
5.
Drug Des Devel Ther ; 18: 1439-1457, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38707616

RESUMEN

Background: Acteoside, an active ingredient found in various medicinal herbs, is effective in the treatment of diabetic kidney disease (DKD); however, the intrinsic pharmacological mechanism of action of acteoside in the treatment of DKD remains unclear. This study utilizes a combined approach of network pharmacology and experimental validation to investigate the potential molecular mechanism systematically. Methods: First, acteoside potential targets and DKD-associated targets were aggregated from public databases. Subsequently, utilizing protein-protein interaction (PPI) networks, alongside GO and KEGG pathway enrichment analyses, we established target-pathway networks to identify core potential therapeutic targets and pathways. Further, molecular docking facilitated the confirmation of interactions between acteoside and central targets. Finally, the conjectured molecular mechanisms of acteoside against DKD were verified through experimentation on unilateral nephrectomy combined with streptozotocin (STZ) rat model. The underlying downstream mechanisms were further investigated. Results: Network pharmacology identified 129 potential intersected targets of acteoside for DKD treatment, including targets such as AKT1, TNF, Casp3, MMP9, SRC, IGF1, EGFR, HRAS, CASP8, and MAPK8. Enrichment analyses indicated the PI3K-Akt, MAPK, Metabolic, and Relaxin signaling pathways could be involved in this therapeutic context. Molecular docking revealed high-affinity binding of acteoside to PIK3R1, AKT1, and NF-κB1. In vivo studies validated the therapeutic efficacy of acteoside, demonstrating reduced blood glucose levels, improved serum Scr and BUN levels, decreased 24-hour urinary total protein (P<0.05), alongside mitigated podocyte injury (P<0.05) and ameliorated renal pathological lesions. Furthermore, this finding indicates that acteoside inhibits the expression of pyroptosis markers NLRP3, Caspase-1, IL-1ß, and IL-18 through the modulation of the PI3K/AKT/NF-κB pathway. Conclusion: Acteoside demonstrates renoprotective effects in DKD by regulating the PI3K/AKT/NF-κB signaling pathway and alleviating pyroptosis. This study explores the pharmacological mechanism underlying acteoside's efficacy in DKD treatment, providing a foundation for further basic and clinical research.


Asunto(s)
Diabetes Mellitus Experimental , Nefropatías Diabéticas , Glucósidos , Simulación del Acoplamiento Molecular , Farmacología en Red , Fenoles , Polifenoles , Estreptozocina , Nefropatías Diabéticas/tratamiento farmacológico , Nefropatías Diabéticas/metabolismo , Animales , Ratas , Glucósidos/farmacología , Glucósidos/química , Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Experimental/metabolismo , Masculino , Fenoles/farmacología , Fenoles/química , Ratas Sprague-Dawley
6.
Integr Cancer Ther ; 23: 15347354241253846, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38721848

RESUMEN

Vikil 20 is an herbal formula produced in Ghana and is widely marketed as a product to boost immunity as well as for general well-being. However, the pharmacological effect of this herbal preparation has not been proven scientifically. Therefore, this study was aimed at investigating the antioxidative as well as the anti-prostate cancer effects of the product. To assess the antioxidative effect of Vikil 20, the DPPH and ABTS activities were investigated. The total phenolic content was investigated using the Folin-Ciocalteu method. The cytotoxic effect of Vikil 20 against prostate cancer (PC-3) cells as well as normal (RAW 264.7) cells was investigated using the MTT assay whereas its anti-metastatic effect was analyzed using the cell migration assay. The effect of Vikil 20 on cell adhesion was analyzed via the cell adhesion assay whereas its effect on TNF-α secretion was investigated using a TNF-α detection kit. Vikil 20 demonstrated significant antioxidant effects by suppressing 57.61% and 92.88% respectively of DPPH and ABTS radicals at 1000 µg/mL with total phenolic contents of 140.45 mg GAE/g. Vikil 20 suppressed the proliferation of PC-3 cells by reducing the number of viable cells to 49.5% while sparing the RAW, 264.7 cells. Further, Vikil 20 significantly suppressed both cellular migration and adhesion of prostate cancer cells. Finally, suppression of cellular migration and adhesion is associated with a reduction in TNF-α secretion by PC-3 cells. Taken together, Vikil 20 was found to possess significant antioxidant and anti-prostate cancer effects in vitro.


Asunto(s)
Antioxidantes , Movimiento Celular , Proliferación Celular , Extractos Vegetales , Neoplasias de la Próstata , Masculino , Humanos , Neoplasias de la Próstata/tratamiento farmacológico , Neoplasias de la Próstata/patología , Proliferación Celular/efectos de los fármacos , Células PC-3 , Antioxidantes/farmacología , Movimiento Celular/efectos de los fármacos , Ratones , Animales , Células RAW 264.7 , Radicales Libres/metabolismo , Extractos Vegetales/farmacología , Adhesión Celular/efectos de los fármacos , Línea Celular Tumoral , Factor de Necrosis Tumoral alfa/metabolismo , Fenoles/farmacología
7.
Med Oncol ; 41(6): 144, 2024 May 08.
Artículo en Inglés | MEDLINE | ID: mdl-38717574

RESUMEN

Peganum harmala has been extensively employed in Algerian traditional medicine practices. This study aimed to explore the impact of n-butanol (n-BuOH) extract sourced from Peganum harmala seeds on cell proliferation, cell migration, and angiogenesis inhibition. Cytotoxic potential of n-BuOH extract was evaluated using MTT (3-(4,5-dimethylthiazol-2-yl) 2,5 diphenyltetrazolium bromide) assay against human breast adenocarcinoma MCF-7 cells, cell migration was determined using scratch assay, and anti-angiogenic effect was evaluated through macroscopic and histological examinations conducted on chick embryo chorioallantoic membrane. Additionally, this research estimated the phytochemical profile of n-BuOH extract. Fifteen phenolic compounds were identified using Ultra-performance liquid chromatography UPLC-ESI-MS-MS analysis. In addition, the n-BuOH extract of P. harmala exhibited potent antioxidant and free radical scavenging properties. The n-BuOH extract showed potent cytotoxicity against MCF-7 cell with an IC50 value of 8.68 ± 1.58 µg/mL. Furthermore, n-BuOH extract significantly reduced migration. A strong anti-angiogenic activity was observed in the groups treated with n-BuOH extract in comparison to the negative control. Histological analysis confirmed the anti-angiogenic effect of the n-BuOH extract. This activity is probably a result of the synergistic effects produced by different polyphenolic classes.


Asunto(s)
Inhibidores de la Angiogénesis , Movimiento Celular , Peganum , Fenoles , Extractos Vegetales , Humanos , Movimiento Celular/efectos de los fármacos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Peganum/química , Embrión de Pollo , Fenoles/farmacología , Fenoles/análisis , Inhibidores de la Angiogénesis/farmacología , Células MCF-7 , Animales , Proliferación Celular/efectos de los fármacos , Fitoquímicos/farmacología , Fitoquímicos/química , Antioxidantes/farmacología , Antioxidantes/química , Antineoplásicos Fitogénicos/farmacología , Membrana Corioalantoides/efectos de los fármacos , Membrana Corioalantoides/irrigación sanguínea
8.
Int J Mol Sci ; 25(9)2024 May 06.
Artículo en Inglés | MEDLINE | ID: mdl-38732269

RESUMEN

New antimicrobial molecules effective against Pseudomonas aeruginosa, known as an antibiotic-resistant "high-priority pathogen", are urgently required because of its ability to develop biofilms related to healthcare-acquired infections. In this study, for the first time, the anti-biofilm and anti-virulence activities of a polyphenolic extract of extra-virgin olive oil as well as purified oleocanthal and oleacein, toward P. aeruginosa clinical isolates were investigated. The main result of our study was the anti-virulence activity of the mixture of oleacein and oleocanthal toward multidrug-resistant and intermediately resistant strains of P. aeruginosa isolated from patients with ventilator-associated pneumonia or surgical site infection. Specifically, the mixture of oleacein (2.5 mM)/oleocanthal (2.5 mM) significantly inhibited biofilm formation, alginate and pyocyanin production, and motility in both P. aeruginosa strains (p < 0.05); scanning electron microscopy analysis further evidenced its ability to inhibit bacterial cell adhesion as well as the production of the extracellular matrix. In conclusion, our results suggest the potential application of the oleacein/oleocanthal mixture in the management of healthcare-associated P. aeruginosa infections, particularly in the era of increasing antimicrobial resistance.


Asunto(s)
Aldehídos , Antibacterianos , Biopelículas , Monoterpenos Ciclopentánicos , Aceite de Oliva , Fenoles , Pseudomonas aeruginosa , Biopelículas/efectos de los fármacos , Biopelículas/crecimiento & desarrollo , Pseudomonas aeruginosa/efectos de los fármacos , Aceite de Oliva/química , Aceite de Oliva/farmacología , Fenoles/farmacología , Fenoles/química , Aldehídos/farmacología , Aldehídos/química , Antibacterianos/farmacología , Antibacterianos/química , Humanos , Pruebas de Sensibilidad Microbiana , Infecciones por Pseudomonas/tratamiento farmacológico , Infecciones por Pseudomonas/microbiología , Adhesión Bacteriana/efectos de los fármacos
9.
Nutrients ; 16(9)2024 Apr 25.
Artículo en Inglés | MEDLINE | ID: mdl-38732529

RESUMEN

The Mediterranean diet, renowned for its health benefits, especially in reducing cardiovascular risks and protecting against diseases like diabetes and cancer, emphasizes virgin olive oil as a key contributor to these advantages. Despite being a minor fraction, the phenolic compounds in olive oil significantly contribute to its bioactive effects. This review examines the bioactive properties of hydroxytyrosol and related molecules, including naturally occurring compounds (-)-oleocanthal and (-)-oleacein, as well as semisynthetic derivatives like hydroxytyrosyl esters and alkyl ethers. (-)-Oleocanthal and (-)-oleacein show promising anti-tumor and anti-inflammatory properties, which are particularly underexplored in the case of (-)-oleacein. Additionally, hydroxytyrosyl esters exhibit similar effectiveness to hydroxytyrosol, while certain alkyl ethers surpass their precursor's properties. Remarkably, the emerging research field of the effects of phenolic molecules related to virgin olive oil on cell autophagy presents significant opportunities for underscoring the anti-cancer and neuroprotective properties of these molecules. Furthermore, promising clinical data from studies on hydroxytyrosol, (-)-oleacein, and (-)-oleocanthal urge further investigation and support the initiation of clinical trials with semisynthetic hydroxytyrosol derivatives. This review provides valuable insights into the potential applications of olive oil-derived phenolics in preventing and managing diseases associated with cancer, angiogenesis, and atherosclerosis.


Asunto(s)
Inhibidores de la Angiogénesis , Aceite de Oliva , Fenoles , Alcohol Feniletílico , Aceite de Oliva/química , Humanos , Fenoles/farmacología , Inhibidores de la Angiogénesis/farmacología , Alcohol Feniletílico/análogos & derivados , Alcohol Feniletílico/farmacología , Dieta Mediterránea , Aterosclerosis/prevención & control , Aterosclerosis/tratamiento farmacológico , Monoterpenos Ciclopentánicos , Neoplasias/prevención & control , Neoplasias/tratamiento farmacológico , Catecoles/farmacología , Aldehídos/farmacología , Animales , Antineoplásicos/farmacología , Antiinflamatorios/farmacología
10.
Nutrients ; 16(9)2024 Apr 26.
Artículo en Inglés | MEDLINE | ID: mdl-38732549

RESUMEN

Oleocanthal (OC) is a monophenol of extra-virgin olive oil (EVOO) endowed with antibiotic, cardioprotective and anticancer effects, among others, mainly in view of its antioxidant and anti-inflammatory properties. OC has been largely investigated in terms of its anticancer activity, in Alzheimer disease and in collagen-induced arthritis; however, the possibility that it can also affect muscle biology has been totally overlooked so far. This study is the first to describe that OC modulates alterations induced in C2C12 myotubes by stimuli known to induce muscle wasting in vivo, namely TNF-α, or in the medium conditioned by the C26 cachexia-inducing tumor (CM-C26). C2C12 myotubes were exposed to CM-C26 or TNF-α in the presence or absence of OC for 24 and 48 h and analyzed by immunofluorescence and Western blotting. In combination with TNF-α or CM-C26, OC was revealed to be able to restore both the myotube's original size and morphology and normal levels of both atrogin-1 and MuRF1. OC seems unable to impinge on the autophagic-lysosomal proteolytic system or protein synthesis. Modulations towards normal levels of the expression of molecules involved in myogenesis, such as Pax7, myogenin and MyHC, were also observed in the myotube cultures exposed to OC and TNF-α or CM-C26. In conclusion, the data presented here show that OC exerts a protective action in C2C12 myotubes exposed to TNF-α or CM-C26, with mechanisms likely involving the downregulation of ubiquitin-proteasome-dependent proteolysis and the partial relief of myogenic differentiation impairment.


Asunto(s)
Catecoles , Monoterpenos Ciclopentánicos , Fibras Musculares Esqueléticas , Proteínas Musculares , Atrofia Muscular , Factor de Necrosis Tumoral alfa , Animales , Fibras Musculares Esqueléticas/efectos de los fármacos , Fibras Musculares Esqueléticas/metabolismo , Ratones , Factor de Necrosis Tumoral alfa/metabolismo , Atrofia Muscular/prevención & control , Atrofia Muscular/metabolismo , Proteínas Musculares/metabolismo , Monoterpenos Ciclopentánicos/farmacología , Catecoles/farmacología , Línea Celular , Proteínas Ligasas SKP Cullina F-box/metabolismo , Proteínas Ligasas SKP Cullina F-box/genética , Desarrollo de Músculos/efectos de los fármacos , Proteínas de Motivos Tripartitos/metabolismo , Proteínas de Motivos Tripartitos/genética , Ubiquitina-Proteína Ligasas/metabolismo , Autofagia/efectos de los fármacos , Fenoles/farmacología , Caquexia/prevención & control , Medios de Cultivo Condicionados/farmacología , Aldehídos
11.
Nutrients ; 16(9)2024 Apr 30.
Artículo en Inglés | MEDLINE | ID: mdl-38732606

RESUMEN

Currently, a clear interest has been given to berries due to their richness in active metabolites, including anthocyanins and non-coloured phenolics. Therefore, the main aim of the present work is to investigate the phenolic profile, antioxidant abilities, and antiproliferative effects on normal human dermal fibroblasts (NHDF) and human colon carcinoma cell line (Caco-2) cells of phenolic-rich extracts from three red fruits highly appreciated by consumers: two species of blackberries (Rubus fruticosus and Rubus ulmifolius) and one species of mulberry (Morus nigra). A total of 19 different phenolics were identified and quantified by HPLC-DAD-ESI/MSn and HPLC-DAD, respectively. Focusing on the biological potential of the phenolic-rich extracts, all of them revealed notable scavenging abilities. Concerning the antiproliferative properties, R. fruticosus presented a cytotoxic selectivity for Caco-2 cells compared to NHDF cells. To deeper explore the biological potential, combinations with positive controls (ascorbic acid and 5-fluorouracil) were also conducted. Finally, the obtained data are another piece of evidence that the combination of phenolic-rich extracts from natural plants with positive controls may reduce clinical therapy costs and the possible toxicity of chemical drugs.


Asunto(s)
Antioxidantes , Proliferación Celular , Frutas , Morus , Estrés Oxidativo , Fenoles , Extractos Vegetales , Rubus , Humanos , Células CACO-2 , Extractos Vegetales/farmacología , Rubus/química , Morus/química , Fenoles/farmacología , Fenoles/análisis , Estrés Oxidativo/efectos de los fármacos , Antioxidantes/farmacología , Proliferación Celular/efectos de los fármacos , Frutas/química , Antineoplásicos Fitogénicos/farmacología , Cromatografía Líquida de Alta Presión
12.
Pak J Pharm Sci ; 37(1): 25-32, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-38741397

RESUMEN

In the present study, antioxidant activity and inhibition of acetylcholinesterase (AChE) and paraoxonase (hPON 1) of Alchemilla lithophila extracts were evaluated for the first time. Besides, there is no research on the contents of phenolic compounds except for fatty acids. In this context, phenolic compounds of A. lithophila were investigated by liquid chromatography/ mass spectrometry (LC-MS/MS). The methanol extract of the A. lithophila exhibited significant inhibition on the AChE (IC50 value for methanol extract 0.162 ± 0.25 mg /mL, R2:0.992). Besides, antioxidant activities of the A. lithophila extracts were examined using by the methods ABTS•+ and DPPH• free radical scavenging potentials, FRAP and CUPRAC metal-reducing activities. ABTS•+ and DPPH• scavenging activities were found for methanol extract at 70.67% and water extract at 75.38%, respectively. Also, FRAP and CUPRAC metal-reducing were determined for water extract 0.796 and hexane extract 1.570 as absorbance. According to LC-MS/MS analyses, the amounts of ellagic acid, catechin hydrate, gallic acid, fumaric acid, luteolin, quercetin, kaempferol, acetohydroxamic acid, caffeic acid, syringic acid, hydroxybenzoic acid and salicylic acid were determined by LC-MS/MS, respectively. As a consequence, this study will be a useful resource for determining bioactivity and phenolic compound profile for natural medicine research.


Asunto(s)
Acetilcolinesterasa , Antioxidantes , Arildialquilfosfatasa , Inhibidores de la Colinesterasa , Fenoles , Extractos Vegetales , Inhibidores de la Colinesterasa/farmacología , Fenoles/análisis , Fenoles/farmacología , Antioxidantes/farmacología , Antioxidantes/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Acetilcolinesterasa/metabolismo , Acetilcolinesterasa/efectos de los fármacos , Arildialquilfosfatasa/metabolismo , Arildialquilfosfatasa/antagonistas & inhibidores , Espectrometría de Masas en Tándem
13.
Molecules ; 29(9)2024 Apr 26.
Artículo en Inglés | MEDLINE | ID: mdl-38731494

RESUMEN

Figs are the edible fruits of the fig tree, Ficus carica L., that have been used for centuries for human consumption and in traditional medicine, to treat skin problems, inflammation, and gastrointestinal disorders. Our previous study investigated the presence of phenolic compounds in aqueous extracts of two Algerian popular fig varieties, azendjar (Az) and taamriouth (Ta), as well as their in vitro antioxidant activity. In this study, we assessed hydroethanolic extracts of these fig varieties. The total phenolic content was measured, along with the phenolic profile. Rutin was determined to be the dominant phenolic compound, followed by vanillic acid, 3,4-dihydroxybenzoic acid, quercetin, 4-hydroxybenzoic acid, rosmarinic acid (in Az only), and cinnamic acid. The antioxidant activity of the extracts was evaluated both in vitro (DPPH and FRAP assays) and in vivo, in rats intoxicated with carbon tetrachloride. In all assays, the fig extract-especially the dark-peeled fig variety azendjar-showed antioxidant potency. The administration of fig extract resulted in a reduction in liver damage, expressed by both different biochemical markers and histopathological study (less degraded liver architecture, reduced fibrosis, and only mild inflammation). A dose-dependent therapeutic effect was observed. The extract from the dark-peeled fig variety, Az, was characterized by a higher phenolic content and a stronger antioxidant activity than the extract from the light-peeled variety-Ta. Our study justifies the use of figs in traditional healing and shows the potential of using fig extracts in natural medicines and functional foods.


Asunto(s)
Antioxidantes , Tetracloruro de Carbono , Ficus , Estrés Oxidativo , Extractos Vegetales , Animales , Ficus/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Antioxidantes/farmacología , Antioxidantes/química , Ratas , Estrés Oxidativo/efectos de los fármacos , Fenoles/farmacología , Fenoles/química , Masculino , Hígado/efectos de los fármacos , Hígado/metabolismo , Hígado/patología , Ratas Wistar
14.
Molecules ; 29(9)2024 Apr 27.
Artículo en Inglés | MEDLINE | ID: mdl-38731503

RESUMEN

This current article was dedicated to the determination of the composition of phenolic compounds in extracts of four species of the genus Filipendula in order to establish a connection between the composition of polyphenols and biological effects. A chemical analysis revealed that the composition of the extracts studied depended both on the plant species and its part (leaf or flower) and on the extractant used. All four species of Filipendula were rich sources of phenolic compounds and contained hydrolyzable tannins, condensed tannins, phenolic acids and their derivatives, and flavonoids. The activities included data on those that are most important for creating functional foods with Filipendula plant components: the influence on blood coagulation measured by prothrombin and activated partial thromboplastin time, and on the activity of the digestive enzymes (pancreatic amylase and lipase). It was established that plant species, their parts, and extraction methods contribute meaningfully to biological activity. The most prominent result is as follows: the plant organ determines the selective inhibition of either amylase or lipase; thus, the anticoagulant activities of F. camtschatica and F. stepposa hold promise for health-promoting food formulations associated with general metabolic disorders.


Asunto(s)
Fenoles , Extractos Vegetales , Extractos Vegetales/química , Extractos Vegetales/farmacología , Fenoles/química , Fenoles/análisis , Fenoles/farmacología , Lipasa/antagonistas & inhibidores , Lipasa/metabolismo , Flavonoides/química , Flavonoides/farmacología , Flavonoides/análisis , Polifenoles/química , Polifenoles/farmacología , Polifenoles/análisis , Amilasas/antagonistas & inhibidores , Amilasas/metabolismo , Coagulación Sanguínea/efectos de los fármacos , Humanos , Anticoagulantes/farmacología , Anticoagulantes/química , Hojas de la Planta/química
15.
Molecules ; 29(9)2024 Apr 29.
Artículo en Inglés | MEDLINE | ID: mdl-38731544

RESUMEN

Berberis vulgaris (L.) has remarkable ethnopharmacological properties and is widely used in traditional medicine. The present study investigated B. vulgaris stem bark (Berberidis cortex) by extraction with 50% ethanol. The main secondary metabolites were quantified, resulting in a polyphenols content of 17.6780 ± 3.9320 mg Eq tannic acid/100 g extract, phenolic acids amount of 3.3886 ± 0.3481 mg Eq chlorogenic acid/100 g extract and 78.95 µg/g berberine. The dried hydro-ethanolic extract (BVE) was thoroughly analyzed using Ultra-High-Performance Liquid Chromatography coupled with High-Resolution Mass Spectrometry (UHPLC-HRMS/MS) and HPLC, and 40 bioactive phenolic constituents were identified. Then, the antioxidant potential of BVE was evaluated using three methods. Our results could explain the protective effects of Berberidis cortex EC50FRAP = 0.1398 mg/mL, IC50ABTS = 0.0442 mg/mL, IC50DPPH = 0.2610 mg/mL compared to ascorbic acid (IC50 = 0.0165 mg/mL). Next, the acute toxicity and teratogenicity of BVE and berberine-berberine sulfate hydrate (BS)-investigated on Daphnia sp. revealed significant BS toxicity after 24 h, while BVE revealed considerable toxicity after 48 h and induced embryonic developmental delays. Finally, the anticancer effects of BVE and BS were evaluated in different tumor cell lines after 24 and 48 h of treatments. The MTS assay evidenced dose- and time-dependent antiproliferative activity, which was higher for BS than BVE. The strongest diminution of tumor cell viability was recorded in the breast (MDA-MB-231), colon (LoVo) cancer, and OSCC (PE/CA-PJ49) cell lines after 48 h of exposure (IC50 < 100 µg/mL). However, no cytotoxicity was reported in the normal epithelial cells (HUVEC) and hepatocellular carcinoma (HT-29) cell lines. Extensive data analysis supports our results, showing a significant correlation between the BVE concentration, phenolic compounds content, antioxidant activity, exposure time, and the viability rate of various normal cells and cancer cell lines.


Asunto(s)
Antioxidantes , Berberis , Corteza de la Planta , Extractos Vegetales , Berberis/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Antioxidantes/farmacología , Antioxidantes/química , Corteza de la Planta/química , Humanos , Línea Celular Tumoral , Animales , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos Fitogénicos/química , Supervivencia Celular/efectos de los fármacos , Fenoles/farmacología , Fenoles/química , Cromatografía Líquida de Alta Presión , Tallos de la Planta/química
16.
Molecules ; 29(9)2024 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-38731583

RESUMEN

Xanthorrhizol, an important marker of Curcuma xanthorrhiza, has been recognized for its different pharmacological activities. A green strategy for selective xanthorrhizol extraction is required. Herein, natural deep eutectic solvents (NADESs) based on glucose and organic acids (lactic acid, malic acid, and citric acid) were screened for the extraction of xanthorrhizol from Curcuma xanthorrhiza. Ultrasound-assisted extraction using glucose/lactic acid (1:3) (GluLA) gave the best yield of xanthorrhizol. The response surface methodology with a Box-Behnken Design was used to optimize the interacting variables of water content, solid-to-liquid (S/L) ratio, and extraction to optimize the extraction. The optimum conditions of 30% water content in GluLA, 1/15 g/mL (S/L), and a 20 min extraction time yielded selective xanthorrhizol extraction (17.62 mg/g) over curcuminoids (6.64 mg/g). This study indicates the protective effect of GluLA and GluLA extracts against oxidation-induced DNA damage, which was comparable with those obtained for ethanol extract. In addition, the stability of the xanthorrhizol extract over 90 days was revealed when stored at -20 and 4 °C. The FTIR and NMR spectra confirmed the hydrogen bond formation in GluLA. Our study reported, for the first time, the feasibility of using glucose/lactic acid (1:3, 30% water v/v) for the sustainable extraction of xanthorrhizol.


Asunto(s)
Antioxidantes , Curcuma , Fenoles , Extractos Vegetales , Rizoma , Curcuma/química , Antioxidantes/química , Antioxidantes/farmacología , Antioxidantes/aislamiento & purificación , Rizoma/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Fenoles/química , Fenoles/aislamiento & purificación , Fenoles/farmacología , Disolventes Eutécticos Profundos/química , Ondas Ultrasónicas
17.
Molecules ; 29(9)2024 May 02.
Artículo en Inglés | MEDLINE | ID: mdl-38731598

RESUMEN

Obtaining high-added value compounds from agricultural waste receives increasing attention, as it can both improve resource utilization efficiency and reduce waste generation. In this study, polysaccharides are extracted from the discarded roots of Abelmoschus manihot (L.) by the high-efficiency ultrasound-assisted extraction (UAE). The optimized condition was determined as solid-liquid ratio SL ratio = 1:20, temperature T = 30 °C and time T = 40 min, achieving an extraction yield of 13.41%. Composition analysis revealed that glucose (Glc, 44.65%), rhamnose (Rha, 26.30%), galacturonic acid (GalA, 12.50%) and galactose (Gal, 9.86%) are the major monosaccharides of the extract. The extract showed a low degree of esterification (DE) value of 40.95%, and its Fourier-transform infrared (FT-IR) spectrum exhibited several characteristic peaks of polysaccharides. Inspired by the wide cosmetic applications of polysaccharides, the skincare effect of the extract was evaluated via the moisture retention, total phenolic content (TPC) quantification, 2,2-Diphenyl-1-picrylhydrazyl (DPPH)-free radical scavenging activity, anti-hyaluronidase and anti-elastase activity experiments. The extract solutions demonstrated a 48 h moisture retention rate of 10.75%, which is superior to that of commercially available moisturizer hyaluronic acid (HA). Moreover, both the TPC value of 16.16 mg GAE/g (dw) and DPPH-free radical scavenging activity of 89.20% at the concentration of 2 mg/mL indicated the strong anti-oxidant properties of the extract. Furthermore, the anti-hyaluronidase activity and moderate anti-elastase activity were determined as 72.16% and 42.02%, respectively. In general, in vitro skincare effect experiments suggest moisturizing, anti-oxidant, anti-radical and anti-aging activities of the A. manihot root extract, indicating its potential applications in the cosmetic industry.


Asunto(s)
Abelmoschus , Antioxidantes , Extractos Vegetales , Raíces de Plantas , Polisacáridos , Polisacáridos/química , Polisacáridos/farmacología , Polisacáridos/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/farmacología , Raíces de Plantas/química , Abelmoschus/química , Antioxidantes/química , Antioxidantes/farmacología , Espectroscopía Infrarroja por Transformada de Fourier , Cuidados de la Piel/métodos , Ramnosa/química , Galactosa , Ácidos Hexurónicos/química , Fenoles/química , Fenoles/análisis , Fenoles/farmacología , Humanos
18.
Molecules ; 29(9)2024 May 03.
Artículo en Inglés | MEDLINE | ID: mdl-38731619

RESUMEN

This study aims to investigate the vegetative buds from Picea abies (spruce), naturally found in a central region of Romania, through a comprehensive analysis of the chemical composition to identify bioactive compounds responsible for pharmacological properties. Using HPLC/derivatization technique of GC-MS and quantitative spectrophotometric assays, the phenolic profile, and main components of an ethanolic extract from the buds were investigated. The essential oil was characterized by GC-MS. Moreover, the antioxidant activity with the DPPH method, and the antimicrobial activity were tested. Heavy metal detection was performed by graphite furnace atomic absorption spectrometry. The main components of the alcoholic extract were astragalin, quercetin, kaempferol, shikimic acid, and quinic acid. A total content of 25.32 ± 2.65 mg gallic acid equivalent per gram of dry plant (mg GAE/g DW) and of 10.54 ± 0.083 mg rutin equivalents/g of dry plant (mg RE/g DW) were found. The essential oil had D-limonene, α-cadinol, δ-cadinene, 13-epimanool, and δ-3-carene as predominant components. The spruce vegetative buds exhibited significant antioxidant activity (IC50 of 53 µg/mL) and antimicrobial effects against Staphylococcus aureus. Furthermore, concentrations of heavy metals Pb and Cd were below detection limits, suggesting that the material was free from potentially harmful contaminants. The results confirmed the potential of this indigenous species to be used as a source of compounds with pharmacological utilities.


Asunto(s)
Antiinfecciosos , Antioxidantes , Aceites Volátiles , Fitoquímicos , Picea , Extractos Vegetales , Picea/química , Antioxidantes/farmacología , Antioxidantes/química , Fitoquímicos/farmacología , Fitoquímicos/química , Antiinfecciosos/farmacología , Antiinfecciosos/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Aceites Volátiles/farmacología , Aceites Volátiles/química , Pruebas de Sensibilidad Microbiana , Cromatografía de Gases y Espectrometría de Masas , Rumanía , Fenoles/análisis , Fenoles/farmacología , Fenoles/química
19.
Int J Mol Sci ; 25(9)2024 Apr 30.
Artículo en Inglés | MEDLINE | ID: mdl-38732097

RESUMEN

The olive oil sector is a fundamental food in the Mediterranean diet. It has been demonstrated that the consumption of extra virgin olive oil (EVOO) with a high content of phenolic compounds is beneficial in the prevention and/or treatment of many diseases. The main objective of this work was to study the relationship between the content of phenolic compounds and the in vitro neuroprotective and anti-inflammatory activity of EVOOs from two PDOs in the province of Granada. To this purpose, the amounts of phenolic compounds were determined by liquid chromatography coupled to mass spectrometry (HPLC-MS) and the inhibitory activity of acetylcholinesterase (AChE) and cyclooxygenase-2 (COX-2) enzymes by spectrophotometric and fluorimetric assays. The main families identified were phenolic alcohols, secoiridoids, lignans, flavonoids, and phenolic acids. The EVOO samples with the highest total concentration of compounds and the highest inhibitory activity belonged to the Picual and Manzanillo varieties. Statistical analysis showed a positive correlation between identified compounds and AChE and COX-2 inhibitory activity, except for lignans. These results confirm EVOO's compounds possess neuroprotective potential.


Asunto(s)
Fármacos Neuroprotectores , Aceite de Oliva , Fenoles , Aceite de Oliva/química , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/química , Fenoles/análisis , Fenoles/química , Fenoles/farmacología , España , Ciclooxigenasa 2/metabolismo , Acetilcolinesterasa/metabolismo , Cromatografía Líquida de Alta Presión , Inhibidores de la Colinesterasa/farmacología , Inhibidores de la Colinesterasa/química , Inhibidores de la Ciclooxigenasa 2/farmacología , Inhibidores de la Ciclooxigenasa 2/química , Flavonoides/análisis , Flavonoides/farmacología , Flavonoides/química
20.
J Colloid Interface Sci ; 668: 282-292, 2024 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-38678884

RESUMEN

Metal-phenolic networks (MPNs) have emerged as a versatile and multifunctional platform applied in bioimaging, disease treatment, electrocatalysis, and water purification. The synthesis of MPNs with mesoporous frameworks and ultra-small diameters (<200 nm), crucial for post-modification, cargo loading, and mass transport, remains a formidable challenge. Inspired by mussel chemistry, mesoporous metal-phenolic nanospheres (MMPNs) are facilely prepared by direct deposition of the metal-polyphenol complex on the interface of oil nano-droplets composed of block copolymers/1,3,5-trimethylbenzene followed by a spontaneous template-removal process. Due to the penetrable and stable networks, the oil nano-droplets gradually leak from the networks driven by shear stress during the stirring process. As a result, MMPNs are obtained without additional template removal procedures such as solvent extraction or high-temperature calcination. The materials have a large pore size (∼12.1 nm), uniform spherical morphology with a small particle size (∼99 nm), and a large specific surface area (49.8 m2 g-1). Due to the abundant phenolic hydroxyl groups, the MMPNs show excellent antioxidative property. The MMPNs also have excellent photothermal property, whose photothermal conversion efficiency was 40.9 %. Moreover, the phenolic hydroxyl groups can reduce Ag+ in situ to prepare Ag nanoparticles loaded MMPNs composites, which have excellent inhibition performance of drug-resistant bacteria biofilm.


Asunto(s)
Antibacterianos , Antioxidantes , Nanosferas , Tamaño de la Partícula , Antibacterianos/farmacología , Antibacterianos/química , Antioxidantes/farmacología , Antioxidantes/química , Nanosferas/química , Porosidad , Animales , Pruebas de Sensibilidad Microbiana , Bivalvos/química , Fenoles/química , Fenoles/farmacología , Propiedades de Superficie , Escherichia coli/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos
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