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1.
Food Res Int ; 184: 114222, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38609214

RESUMO

Anthocyanin (AN) has good antioxidant and anti-inflammatory bioactivities, but its poor biocompatibility and low stability limit the application of AN in the food industry. In this study, core-shell structured carriers were constructed by noncovalent interaction using tannic acid (TA) and poloxamer 188 (F68) to improve the biocompatibility, stability and smart response of AN. Under different treatment conditions, TA-F68 and AN were mainly bound by hydrophobic interaction. The PDI is less than 0.1, and the particle size of nanoparticles (NPs) is uniform and concentrated. The retention of the complex was 15.50 % higher than that of AN alone after 9 d of light treatment. After heat treatment for 180 min, the retention rate after loading was 13.87 % higher than that of AN alone. The carrier reduce the damage of AN by the digestive environment, and intelligently and sustainedly release AN when the esterase is highly expressed. In vitro studies demonstrated that the nanocarriers had good biocompatibility and significantly inhibited the overproduction of reactive oxygen species induced by oxidative stress. In addition, AN-TA-F68 has great potential for free radical scavenging at sites of inflammation. In conclusion, the constructed nano-delivery system provides a potential application for oral ingestion of bioactive substances for intervention in ulcerative colitis.


Assuntos
Antocianinas , Nanopartículas , Antocianinas/farmacologia , Polifenóis/farmacologia , Antioxidantes/farmacologia
2.
Molecules ; 29(7)2024 Mar 27.
Artigo em Inglês | MEDLINE | ID: mdl-38611771

RESUMO

To explore the composition of anthocyanins and expand their biological activities, anthocyanins were systematically isolated and purified from tubers of Solanum tuberosum L., and their tyrosinase inhibitory activity was investigated. In this study, two new anthocyanin degradation compounds, norpetanin (9) and 4-O-(p-coumaryl) rhamnose (10), along with 17 known anthocyanins and their derivatives, were isolated and purified from an acid-ethanolic extract of fresh purple potato tubers. Their structures were elucidated via 1D and 2D NMR and HR-ESI-MS and compared with those reported in the literature. The extracts were evaluated for anthocyanins and their derivatives using a tyrosinase inhibitor screening kit and molecular docking technology, and the results showed that petanin, norpetanin, 4-O-(p-coumaryl) rhamnose, and lyciruthephenylpropanoid D/E possessed tyrosinase inhibitory activity, with 50% inhibiting concentration (IC50) values of 122.37 ± 8.03, 115.53 ± 7.51, 335.03 ± 12.99, and 156.27 ± 11.22 µM (Mean ± SEM, n = 3), respectively. Furthermore, petanin was validated against melanogenesis in zebrafish; it was found that it could significantly inhibit melanin pigmentation (p < 0.001), and the inhibition rate of melanin was 17% compared with the normal group. This finding may provide potential treatments for diseases with abnormal melanin production, and high-quality raw materials for whitening cosmetics.


Assuntos
Antocianinas , Solanum tuberosum , Animais , Antocianinas/farmacologia , Monofenol Mono-Oxigenase , Melaninas , Simulação de Acoplamento Molecular , Ramnose , Peixe-Zebra
3.
Nutr Diabetes ; 14(1): 7, 2024 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-38429305

RESUMO

BACKGROUND: Anthocyanins are a group of natural products widely found in plants. They have been found to alleviate the disorders of glucose metabolism in type 2 diabetes mellitus (T2DM), while the underlying mechanisms remain unclear. METHODS: HepG2 and L02 cells were incubated with 0.2 mM PA and 30 mM glucose for 24 h to induce IR, and cells treated with 5 mM glucose were used as the control. C57BL/6 J male mice and db/db male mice were fed with a chow diet and gavaged with pure water or cyanidin-3-O-glucoside (C3G) solution (150 mg/kg/day) for 6 weeks. RESULTS: In this study, the anthocyanin C3G, extracted from red bayberry, was found to alleviate disorders of glucose metabolism, which resulted in increased insulin sensitivity in hepatocytes, and achieved by enhancing the glucose consumption as well as glycogen synthesis in insulin resistance (IR) hepatpcytes. Subsequently, the expression of key proteins involved in IR was detected by western blotting analysis. Protein tyrosine phosphatase-1B (PTP1B), a negative regulator of insulin signaling, could reduce cellular sensitivity to insulin by inhibiting the phosphorylation of insulin receptor substrate-2 (IRS-2). Results of this study showed that C3G inhibited the increase in PTP1B after high glucose and palmitic acid treatment. And this inhibition was accompanied by increased phosphorylation of IRS proteins. Furthermore, the effect of C3G on improving IR in vivo was validated by using a diabetic db/db mouse model. CONCLUSION: These findings demonstrated that C3G could alleviate IR in vitro and in vivo to increase insulin sensitivity, which may offer a new insight for regulating glucose metabolism during T2DM by using the natural dietary bioactive components. C3G promotes the phosphorylation of IRS-2 proteins by suppressing the expression of PTP1B, and then enhances the sensitivity of hepatocyte to insulin.


Assuntos
Diabetes Mellitus Tipo 2 , Resistência à Insulina , Camundongos , Animais , Insulina/metabolismo , Antocianinas/farmacologia , Antocianinas/uso terapêutico , Antocianinas/metabolismo , Resistência à Insulina/fisiologia , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/metabolismo , Glucosídeos/farmacologia , Glucosídeos/uso terapêutico , Camundongos Endogâmicos C57BL , Hepatócitos/metabolismo , Glucose/metabolismo
4.
Nutrients ; 16(5)2024 Feb 29.
Artigo em Inglês | MEDLINE | ID: mdl-38474822

RESUMO

Alcoholic liver disease (ALD) is primarily caused by long-term excessive alcohol consumption. Cyanidin-3-O-glucoside (C3G) is a widely occurring natural anthocyanin with multiple biological activities. This study aims to investigate the effects of C3G isolated from black rice on ALD and explore the potential mechanism. C57BL/6J mice (male) were fed with standard diet (CON) and Lieber-DeCarli liquid-fed (Eth) or supplemented with a 100 mg/kg/d C3G Diet (Eth-C3G), respectively. Our results showed that C3G could effectively ameliorate the pathological structure and liver function, and also inhibited the accumulation of liver lipids. C3G supplementation could partially alleviate the injury of intestinal barrier in the alcohol-induced mice. C3G supplementation could increase the abundance of Norank_f_Muribaculaceae, meanwhile, the abundances of Bacteroides, Blautia, Collinsella, Escherichia-Shigella, Enterococcus, Prevotella, [Ruminococcus]_gnavus_group, Methylobacterium-Methylorubrum, Romboutsia, Streptococcus, Bilophila, were decreased. Spearman's correlation analysis showed that 12 distinct genera were correlated with blood lipid levels. Non-targeted metabolic analyses of cecal contents showed that C3G supplementation could affect the composition of intestinal metabolites, particularly bile acids. In conclusion, C3G can attenuate alcohol-induced liver injury by modulating the gut microbiota and metabolites, suggesting its potential as a functional food ingredient against alcoholic liver disease.


Assuntos
Microbioma Gastrointestinal , Hepatopatias Alcoólicas , Camundongos , Masculino , Animais , Antocianinas/farmacologia , Camundongos Endogâmicos C57BL , Fígado/metabolismo , Hepatopatias Alcoólicas/metabolismo , Glucosídeos/farmacologia
5.
Int J Biol Macromol ; 264(Pt 1): 130595, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38437939

RESUMO

The digestive instability of anthocyanins (ACNs) limits their application in food nutrition, especially precision nutrition. Blueberry ACNs-loaded nanoparticles (Lipo/GA-ACNs NPs) were prepared using gum arabic (GA) as the delivery carrier and liposomal vesicles (Lipo) prepared from soy lecithin as the targeting scaffold. The average particle size of the NPs was 99.4 nm, and the polydispersion index (PDI) was 0.46. The results showed that the presence of the Lipo-GA matrix enhanced the NPs' in vitro stability and antioxidant activity. In addition, the in vitro biocompatibility, uptake ability, lipid-lowering activity, and free-radical scavenging ability were improved to a certain extent. In a high-fat diet (HFD)-induced obese mouse model, oral administration of ACNs-LNP (LNP, liver-targeted nanoparticle) showed better effects on body weight, liver injury, and lipid droplet accumulation in the liver than ACNs. In addition, ACNs-LNP also played a role in regulating HFD-induced gut microbiota imbalance. These results provide a promising ACNs delivery strategy with the potential to be developed into a functional food that targets the liver to prevent fatty liver.


Assuntos
Mirtilos Azuis (Planta) , Microbioma Gastrointestinal , Nanopartículas , Animais , Camundongos , Dieta Hiperlipídica/efeitos adversos , Antocianinas/farmacologia , Camundongos Obesos , Lecitinas , Goma Arábica/farmacologia , Gotículas Lipídicas , Camundongos Endogâmicos C57BL
6.
Biomolecules ; 14(3)2024 Mar 12.
Artigo em Inglês | MEDLINE | ID: mdl-38540758

RESUMO

Pigmented corn is a gramineae food of great biological, cultural and nutritional importance for many Latin American countries, with more than 250 breeds on the American continent. It confers a large number of health benefits due to its diverse and abundant bioactive compounds. In this narrative review we decided to organize the information on the nutrients, bioactive compounds and phytochemicals present in pigmented corn, as well as their effects on human health. Phenolic compounds and anthocyanins are some of the most studied and representative compounds in these grasses, with a wide range of health properties, mainly the reduction of pro-oxidant molecules. Carotenoids are a group of molecules belonging to the terpenic compounds, present in a large number of pigmented corn breeds, mainly the yellow ones, whose biological activity incorporates a wide spectrum. Bioactive peptides can be found in abundance in corn, having very diverse biological effects that include analgesic, opioid and antihypertensive activities. Other compounds with biological activity found in pigmented corn are resistant starches, some fatty acids, phytosterols, policosanols, phospholipids, ferulic acid and phlobaphenes, as well as a great variety of vitamins, elements and fibers. This review aims to disseminate and integrate the existing knowledge on compounds with biological activity in pigmented corn in order to promote their research, interest and use by scientists, nutrition professionals, physicians, industries and the general population.


Assuntos
Antioxidantes , Zea mays , Humanos , Antioxidantes/química , Zea mays/química , Antocianinas/farmacologia , Melhoramento Vegetal , Carotenoides/farmacologia
7.
Molecules ; 29(6)2024 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-38543024

RESUMO

Aronia melanocarpa fruit contains a variety of active ingredients, such as phenolic acids, anthocyanins, proanthocyanidins, etc. Relevant in vivo and in vitro studies have concluded that it has beneficial effects in terms of treating dyslipidemia, hypertension, glucose metabolism disorders, etc. This article discusses the nutritional value and food processing of Aronia melanocarpa and reviews the chemical components of Aronia melanocarpa and the pharmacological activities of related substances in order to summarize the chemical characteristics of the fruit and its development prospects. The process optimization of juice production, the impact of antioxidant capacity, and the comprehensive utilization of pomace in feed are discussed. This article provides a reference for future comprehensive application research and product development of Aronia melanocarpa.


Assuntos
Photinia , Proantocianidinas , Antocianinas/farmacologia , Photinia/química , Antioxidantes/farmacologia , Antioxidantes/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química
8.
Food Funct ; 15(7): 3274-3299, 2024 Apr 02.
Artigo em Inglês | MEDLINE | ID: mdl-38482946

RESUMO

Cardiovascular diseases (CVDs) are a group of chronic health disorders prevalent worldwide that claim millions of lives yearly. Inflammation and oxidative stress are intricately associated with myocardial tissue damage, endothelial dysfunction, and increased odds of heart failure. Thus, dietary strategies aimed at decreasing the odds of CVDs are paramount. In this regard, the consumption of anthocyanins, natural pigments found in edible flowers, fruits, and vegetables, has attracted attention due to their potential to promote cardiovascular health. The main mechanisms of action linked with their protective effects on antioxidant and anti-inflammatory activities, serum lipid profile modulation, and other cardiovascular health parameters are explained and exemplified. However, little is known about the dose-dependency nature of the effects, which anthocyanin has better efficiency, and whether anthocyanin-containing foods display better in vivo efficacy than nutraceuticals (i.e., concentrated extracts containing higher levels of anthocyanins than foods). Thus, this systematic review focused on determining the effects of anthocyanin-containing foods and nutraceuticals on biomarkers associated with CVDs using animal studies and human interventions supported by in vitro mechanistic insights. Overall, the results showed that the regular consumption of anthocyanin-containing foods and nutraceuticals improved vascular function, lipid profile, and antioxidant and anti-inflammatory effects. The daily dosage, the participants' health status, and the duration of the intervention also significantly influenced the results.


Assuntos
Antioxidantes , Doenças Cardiovasculares , Animais , Humanos , Antioxidantes/farmacologia , Antocianinas/farmacologia , Suplementos Nutricionais , Estresse Oxidativo , Inflamação , Doenças Cardiovasculares/prevenção & controle , Doenças Cardiovasculares/tratamento farmacológico , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Biomarcadores , Lipídeos/farmacologia
9.
Arch Toxicol ; 98(5): 1323-1367, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38483584

RESUMO

Reactive oxygen species (ROS) and reactive nitrogen species (RNS) are well recognized for playing a dual role, since they can be either deleterious or beneficial to biological systems. An imbalance between ROS production and elimination is termed oxidative stress, a critical factor and common denominator of many chronic diseases such as cancer, cardiovascular diseases, metabolic diseases, neurological disorders (Alzheimer's and Parkinson's diseases), and other disorders. To counteract the harmful effects of ROS, organisms have evolved a complex, three-line antioxidant defense system. The first-line defense mechanism is the most efficient and involves antioxidant enzymes such as superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx). This line of defense plays an irreplaceable role in the dismutation of superoxide radicals (O2•-) and hydrogen peroxide (H2O2). The removal of superoxide radicals by SOD prevents the formation of the much more damaging peroxynitrite ONOO- (O2•- + NO• → ONOO-) and maintains the physiologically relevant level of nitric oxide (NO•), an important molecule in neurotransmission, inflammation, and vasodilation. The second-line antioxidant defense pathway involves exogenous diet-derived small-molecule antioxidants. The third-line antioxidant defense is ensured by the repair or removal of oxidized proteins and other biomolecules by a variety of enzyme systems. This review briefly discusses the endogenous (mitochondria, NADPH, xanthine oxidase (XO), Fenton reaction) and exogenous (e.g., smoking, radiation, drugs, pollution) sources of ROS (superoxide radical, hydrogen peroxide, hydroxyl radical, peroxyl radical, hypochlorous acid, peroxynitrite). Attention has been given to the first-line antioxidant defense system provided by SOD, CAT, and GPx. The chemical and molecular mechanisms of antioxidant enzymes, enzyme-related diseases (cancer, cardiovascular, lung, metabolic, and neurological diseases), and the role of enzymes (e.g., GPx4) in cellular processes such as ferroptosis are discussed. Potential therapeutic applications of enzyme mimics and recent progress in metal-based (copper, iron, cobalt, molybdenum, cerium) and nonmetal (carbon)-based nanomaterials with enzyme-like activities (nanozymes) are also discussed. Moreover, attention has been given to the mechanisms of action of low-molecular-weight antioxidants (vitamin C (ascorbate), vitamin E (alpha-tocopherol), carotenoids (e.g., ß-carotene, lycopene, lutein), flavonoids (e.g., quercetin, anthocyanins, epicatechin), and glutathione (GSH)), the activation of transcription factors such as Nrf2, and the protection against chronic diseases. Given that there is a discrepancy between preclinical and clinical studies, approaches that may result in greater pharmacological and clinical success of low-molecular-weight antioxidant therapies are also subject to discussion.


Assuntos
Antioxidantes , Neoplasias , Humanos , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Peróxido de Hidrogênio , Superóxidos , Ácido Peroxinitroso/farmacologia , Antocianinas/metabolismo , Antocianinas/farmacologia , Estresse Oxidativo , Óxido Nítrico , Superóxido Dismutase/metabolismo , Doença Crônica
10.
J Agric Food Chem ; 72(13): 7140-7154, 2024 Apr 03.
Artigo em Inglês | MEDLINE | ID: mdl-38518253

RESUMO

Microplastics derived from plastic waste have emerged as a pervasive environmental pollutant with potential transfer and accumulation through the food chain, thus posing risks to both ecosystems and human health. The gut microbiota, tightly intertwined with metabolic processes, exert substantial influences on host physiology by utilizing dietary compounds and generating bacterial metabolites such as tryptophan and bile acid. Our previous studies have demonstrated that exposure to microplastic polystyrene (PS) disrupts the gut microbiota and induces colonic inflammation. Meanwhile, intervention with cyanidin-3-O-glucoside (C3G), a natural anthocyanin derived from red bayberry, could mitigate colonic inflammation by reshaping the gut bacterial composition. Despite these findings, the specific influence of gut bacteria and their metabolites on alleviating colonic inflammation through C3G intervention remains incompletely elucidated. Therefore, employing a C57BL/6 mouse model, this study aims to investigate the mechanisms underlying how C3G modulates gut bacteria and their metabolites to alleviate colonic inflammation. Notably, our findings demonstrated the efficacy of C3G in reversing the elevated levels of pro-inflammatory cytokines (IL-6, IL-1ß, and TNF-α) and the upregulation of mRNA expression (Il-6, Il-1ß, and Tnf-α) induced by PS exposure. Meanwhile, C3G effectively inhibited the reduction in levels (IL-22, IL-10, and IL-4) and the downregulation of mRNA expression (Il-22, Il-10, and Il-4) of anti-inflammatory cytokines induced by PS exposure. Moreover, PS-induced phosphorylation of the transcription factor NF-κB in the nucleus, as well as the increased level of protein expression of iNOS and COX-2 in the colon, were inhibited by C3G. Metabolisms of gut bacterial tryptophan and bile acids have been extensively implicated in the regulation of inflammatory processes. The 16S rRNA high-throughput sequencing disclosed that PS treatment significantly increased the abundance of pro-inflammatory bacteria (Desulfovibrio, norank_f_Oscillospiraceae, Helicobacter, and Lachnoclostridium) while decreasing the abundance of anti-inflammatory bacteria (Dubosiella, Akkermansia, and Alistipes). Intriguingly, C3G intervention reversed these pro-inflammatory changes in bacterial abundances and augmented the enrichment of bacterial genes involved in tryptophan and bile acid metabolism pathways. Furthermore, untargeted metabolomic analysis revealed the notable upregulation of metabolites associated with tryptophan metabolism (shikimate, l-tryptophan, indole-3-lactic acid, and N-acetylserotonin) and bile acid metabolism (3b-hydroxy-5-cholenoic acid, chenodeoxycholate, taurine, and lithocholic acid) following C3G administration. Collectively, these findings shed new light on the protective effects of dietary C3G against PS exposure and underscore the involvement of specific gut bacterial metabolites in the amelioration of colonic inflammation.


Assuntos
Microbioma Gastrointestinal , Interleucina-10 , Camundongos , Animais , Humanos , Antocianinas/farmacologia , RNA Ribossômico 16S , Fator de Necrose Tumoral alfa/farmacologia , Plásticos/farmacologia , Poliestirenos/farmacologia , Interleucina-6/farmacologia , Interleucina-4 , Ecossistema , Triptofano/farmacologia , Camundongos Endogâmicos C57BL , Citocinas/genética , Citocinas/metabolismo , Inflamação/tratamento farmacológico , Inflamação/genética , Anti-Inflamatórios/farmacologia , Glucosídeos/farmacologia , Ácidos e Sais Biliares/farmacologia , RNA Mensageiro
11.
Int J Biol Macromol ; 263(Pt 2): 130523, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38428771

RESUMO

As a natural pH-sensing colorant, purple sweet potato anthocyanins (PSPAs) have demonstrated great potential in colorimetric film for freshness monitoring. However, the photothermal instability of PSPAs is still a challengeable issue. Herein, γ-cyclodextrin metal-organic framework (CD-MOF) loaded with PSPAs (PSPAs@CD-MOF, i.e., PM) and eugenol (EUG) were incorporated in cellulose acetate (CA) matrix for developing a smart active colorimetric film of CA/PM/EUG, where PM and EUG were hydrogen-bonded with CA. Attentions were focused on the photothermal colorimetric stability, colorimetric response, and antibacterial activity of the films. The presence of PM and EUG endowed the film outstanding UV-blocking performance and enhanced the barrier against water vapor and oxygen. Target film of CA/PM15/EUG10 had good photothermal colorimetric stability due to the protection of CD-MOF on PSPAs and the color changes with pH-stimuli were sensitive and reversible. In addition to antioxidant activity, CA/PM15/EUG10 had antibacterial activity against Escherichia coli and Staphylococcus aureus. The application trial results indicated that the CA/PM15/EUG10 was valid to indicate pork freshness and extended the shelf-life by 100 % at 25 °C, which has demonstrated a good perspective on smart active packaging for freshness monitoring and shelf-life extension.


Assuntos
Celulose/análogos & derivados , Ciclodextrinas , Ipomoea batatas , Estruturas Metalorgânicas , Carne de Porco , Carne Vermelha , Suínos , Animais , Antocianinas/farmacologia , Colorimetria , Eugenol , Antibacterianos/farmacologia , Escherichia coli , Embalagem de Alimentos , Concentração de Íons de Hidrogênio
12.
Ann Pharm Fr ; 82(3): 373-391, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38354975

RESUMO

Nonalcoholic fatty liver disease (NAFLD) is described by too much hepatic fat deposition causing steatosis, which further develops into nonalcoholic steatohepatitis (NASH), defined by necroinflammation and fibrosis, progressing further to hepatic cirrhosis, hepatocellular carcinoma, and liver failure. NAFLD is linked to different aspects of the metabolic syndrome like obesity, insulin resistance, hypertension, and dyslipidemia, and its pathogenesis involves several elements including diet, obesity, disruption of lipid homeostasis, and a high buildup of triglycerides and other lipids in liver cells. It is therefore linked to an increase in the susceptibility to developing diabetes mellitus and cardiovascular diseases. Several interventions exist regarding its management, but the availability of natural sources through diet will be a benefit in dealing with the disorder due to the immensely growing dependence of the population worldwide on natural sources owing to their ability to treat the root cause of the disease. Anthocyanins (ACNs) are naturally occurring polyphenolic pigments that exist in the form of glycosides, which are the glucosides of anthocyanidins and are produced from flavonoids via the phenyl propanoid pathway. To understand their mode of action in NAFLD and their therapeutic potential, the literature on in vitro, in vivo, and clinical trials on naturally occurring ACN-rich sources was exhaustively reviewed. It was concluded that ACNs show their potential in the treatment of NAFLD through their antioxidant properties and their efficacy to control lipid metabolism, glucose homeostasis, transcription factors, and inflammation. This led to the conclusion that ACNs possess efficacy in the amelioration of NAFLD and the various features associated with it. However, additional clinical trials are required to justify the potential of ACNs in NAFLD.


Assuntos
Resistência à Insulina , Hepatopatia Gordurosa não Alcoólica , Humanos , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Hepatopatia Gordurosa não Alcoólica/epidemiologia , Hepatopatia Gordurosa não Alcoólica/metabolismo , Antocianinas/farmacologia , Antocianinas/uso terapêutico , Antocianinas/metabolismo , Obesidade/complicações , Obesidade/metabolismo , Obesidade/patologia , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/metabolismo , Fígado/metabolismo , Fígado/patologia
13.
PLoS One ; 19(2): e0293115, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38346085

RESUMO

AIM: Formulation of Pomegranate Extracts (PE)-loaded sphingosomes as an antitumor therapy for the intravenous and passive targeted delivery to various tumor types, especially that of the breast, colon, and uterus; to increase the therapeutic activity and decrease the adverse effects profile. METHODS: The pericarp and seeds' juice of Punica granatum were each extracted using D.W. and ethanol. Phytochemical investigation of all extracts was carried out including total phenolics, flavonoids, and anthocyanins contents, the antioxidant activity, as well as HPLC analysis of phenolics and flavonoids. The antitumor potential of all extracts was also tested utilizing three cell lines: MCF-7, HeLa, and HCT116. The candidate extract was chosen for the formulation phase and was entrapped into the sphingosomes using the thin-film hydration method and employing three different PE: lipids weight ratios. The synthesized formulations were characterized for their size, morphological features, zeta potential, entrapment efficiency, and in vitro drug release and kinetics modeling studies. The optimized formula was further analyzed by FTIR spectroscopy and electron microscopy. The antitumor activity of F2 was also investigated using the same cancer cell lines compared to the plant extract. RESULTS: The highest phenolics, flavonoids, and anthocyanins contents were observed in the ethanolic pericarps extract (EPE), followed by the ethanolic seeds extract (ESE). Consequently, EPE showed a higher antitumor activity hence it was selected for the formulation phase. PE-loaded sphingosomes formula (F2) was selected for having the highest EE% (71.64%), and a sustained release profile with the highest in vitro release (42.5±9.44%). By employing the DDSolver, the Weibull model was found the most suitable to describe the PE release kinetics compared to other models. The release mechanism was found to follow Fickian diffusion. Simulated pharmacokinetic parameters have portrayed F2 as the candidate formula, with the highest AUC (536.095) and slowest MDT (0.642 h). In addition, F2 exhibited a significant (p>0.05) stronger and prolonged anticancer effect against MCF-7, HeLa, and HCT116 cell lines at all concentrations tested compared to the free extract. CONCLUSION: The results proved that sphingosomes are an effective delivery system, improving pharmacological efficacy and reducing serious side effects of anticancer medications and natural products.


Assuntos
Neoplasias , Punica granatum , Feminino , Humanos , Antocianinas/farmacologia , Extratos Vegetais/química , Neoplasias/tratamento farmacológico , Compostos Fitoquímicos , Fenóis , Flavonoides/farmacologia
14.
J Mol Graph Model ; 129: 108732, 2024 06.
Artigo em Inglês | MEDLINE | ID: mdl-38412813

RESUMO

Recent evidence from in vitro and in vivo studies has shown that anthocyanins and anthocyanidins can reduce and inhibit the amyloid beta (Aß) species, one of the hallmarks of Alzheimer's disease (AD). However, their inhibition mechanisms on Aß species at molecular details remain elusive. Therefore, in the present study, molecular modelling methods were employed to investigate their inhibitory mechanisms on Aß(1-42) peptide. The results highlighted that anthocyanidins effectively inhibited the conformational transitions of helices into beta-sheet (ß-sheet) conformation within Aß(1-42) peptide by two different mechanisms: 1) the obstruction of two terminals from coming into contact due to the binding of anthocyanidins with residues of N- and second hydrophobic core (SHC)-C-terminals, and 2) the prevention of the folding process due to the binding of anthocyanidin with the central polar (Asp23 and Lys28) and native helix (Asp23, Lys28, and Leu34) residues. These new findings on the inhibition of ß-sheet formation by targeting both N- and SHC-C-terminals, and the long-established target, D23-K28 salt bridge residues, not with the conventional central hydrophobic core (CHC) as reported in the literature, might aid in designing more potent inhibitors for AD treatment.


Assuntos
Doença de Alzheimer , Peptídeos beta-Amiloides , Humanos , Peptídeos beta-Amiloides/química , Antocianinas/farmacologia , Simulação de Dinâmica Molecular , Simulação de Acoplamento Molecular , Fragmentos de Peptídeos/química , Doença de Alzheimer/metabolismo
15.
Biochem Pharmacol ; 222: 116069, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38387526

RESUMO

High-fat diet (HFD) consumption and excess nutrient availability can cause alterations in mitochondrial function and dynamics. We previously showed that anthocyanins (AC) decreased HFD-induced body weight gain and fat deposition. This study investigated: i) the capacity of AC to mitigate HFD-induced alterations in mitochondrial dynamics, biogenesis, and thermogenesis in mouse subcutaneous white adipose tissue (sWAT), and ii) the underlying mechanisms of action of cyanidin-3-O-glucoside (C3G), delphinidin-3-O-glucoside (D3G), and their gut metabolites on mitochondria function/dynamics in 3T3-L1 adipocytes treated with palmitate. Mice were fed control or HFD diets, added or not with 40 mg AC/kg body weight (BW). Compared to control and AC-supplemented mice, HFD-fed mice had fewer sWAT mitochondria that presented alterations of their architecture. AC supplementation prevented HFD-induced decrease of proteins involved in mitochondria biogenesis (PPARγ, PRDM16 and PGC-1α), and thermogenesis (UCP-1), and decreased AMPK phosphorylation. AC supplementation also restored the alterations in sWAT mitochondrial dynamics (Drp-1, OPA1, MNF-2, and Fis-1) and mitophagy (BNIP3L/NIX) caused by HFD consumption. In mature 3T3-L1, C3G, D3G, and their metabolites protocatechuic acid (PCA), 4-hydroxybenzaldehyde (HB), and gallic acid (GA) differentially affected palmitate-mediated decreased cAMP, PKA, AMPK, and SIRT-1 signaling pathways. C3G, D3G, and metabolites also prevented palmitate-mediated decreased expression of PPARγ, PRDM16, PGC-1α, and UCP1. Results suggest that consumption of select AC, i.e. cyanidin and delphinidin, could promote sWAT mitochondriogenesis and improve mitochondria dynamics in the context of HFD/obesity-induced dysmetabolism in part by regulating PKA, AMPK, and SIRT-1 signaling pathways.


Assuntos
Tecido Adiposo Marrom , Antocianinas , Camundongos , Animais , Antocianinas/farmacologia , Tecido Adiposo Marrom/metabolismo , PPAR gama/metabolismo , Proteínas Quinases Ativadas por AMP/metabolismo , Tecido Adiposo Branco/metabolismo , Obesidade/metabolismo , Dieta Hiperlipídica/efeitos adversos , Fatores de Transcrição/metabolismo , Termogênese , Mitocôndrias/metabolismo , Glucosídeos/metabolismo , Palmitatos/metabolismo , Camundongos Endogâmicos C57BL
16.
Int J Biol Macromol ; 263(Pt 2): 130362, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38395287

RESUMO

In this study, anthocyanin from Garcinia mangostana shell extract (Mse) was used as pH indicator to prepare intelligent carboxymethyl cellulose (CMC) based composite films. The structure and properties of the CMC-based composite films were characterized and discussed in detail. Results showed that the CMC-based composite films with Mse had excellent mechanical, antibacterial and antioxidant abilities. Especially, the carboxymethyl cellulose/corn starch/Garcinia mangostana shell extract (CMC/Cst/Mse) composite film had best mechanical properties (20.62 MPa, 4.06 % EB), lowest water vapor permeability (1.80 × 10-12 g·cm/(cm2·s·Pa)), excellent ultraviolet (UV) blocking performance, and the best antibacterial and antioxidant abilities. The pH sensitivity of composite films which had Mse obviously changed with time when the fish freshness was monitored at 25 °C. Given the good pH sensitivity of the composite films, it had significant potential for application of intelligent packaging film as a food packaging material to indicate the freshness of fish.


Assuntos
Antioxidantes , Garcinia mangostana , Animais , Antioxidantes/química , Antocianinas/farmacologia , Carboximetilcelulose Sódica/química , Antibacterianos/farmacologia , Antibacterianos/química , Embalagem de Alimentos/métodos , Extratos Vegetais/farmacologia
17.
Mol Nutr Food Res ; 68(5): e2300611, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38319040

RESUMO

SCOPE: Rose petal extract (RPE) shows a significant antioxidant effect through its anthocyanin content. However, the mechanism underlying the anti-aging effects of orally administered RPE remains unclear. This study aims to describe the anti-aging effect and mechanism of action of orally administered RPE in ultraviolet (UV)B-induced skin aging. METHODS AND RESULTS: This study evaluates the protein expression of collagen type I alpha 1 (COL1A1) and matrix metalloproteinase 1 (MMP-1) and the mRNA expression of hyaluronic synthase 2 (HAS2) in human dermal fibroblasts. In addition, the hyaluronidase and collagenase inhibitory activities of RPE are confirmed. To evaluate the anti-aging effects of RPE, SKH-1 hairless mice are administered RPE daily for 12 weeks. Wrinkle formation, transepidermal water loss (TEWL), and skin moisture loss induced by UVB irradiation are suppressed in the dorsal skin of SKH-1 hairless mice orally administered RPE. Oral administration of RPE suppresses UVB irradiation-induced collagen disruption and reduction of hyaluronic acid. To find the bioactive compound in the RPE, serum protocatechuic acid (PCA), an anthocyanin metabolite, is analyzed using liquid chromatography-tandem mass spectrometry (LC-MS/MS). CONCLUSION: Anthocyanins in RPE are metabolized to PCA in the body and circulated through the bloodstream to exhibit anti-aging effects on the skin.


Assuntos
Antocianinas , Envelhecimento da Pele , Animais , Camundongos , Humanos , Antocianinas/farmacologia , Camundongos Pelados , Cromatografia Líquida , Espectrometria de Massas em Tandem , Pele , Raios Ultravioleta/efeitos adversos , Extratos Vegetais/farmacologia
18.
Phytomedicine ; 126: 155029, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38417241

RESUMO

BACKGROUND: Cancer ranks as the second leading cause of death globally, imposing a significant public health burden. The rise in cancer resistance to current therapeutic agents underscores the potential role of phytotherapy. Black raspberry (BRB, Rubus Occidentalis) is a fruit rich in anthocyanins, ellagic acid, and ellagitannins. Accumulating evidence suggests that BRB exhibits promising anticancer effects, positioning it as a viable candidate for phytotherapy. PURPOSE: This article aims to review the existing research on BRB regarding its role in cancer prevention and treatment. It further analyzes the effective components of BRB, their metabolic pathways, and the potential mechanisms underlying the fruit's anticancer effects. METHODS: Ovid MEDLINE, EMBASE, Web of Science, and CENTRAL were searched through the terms of Black Raspberry, Raspberry, and Rubus Occidentali up to January 2023. Two reviewers performed the study selection by screening the title and abstract. Full texts of potentially eligible studies were retrieved to access the details. RESULTS: Out of the 767 articles assessed, 73 papers met the inclusion criteria. Among them, 63 papers investigated the anticancer mechanisms, while 10 conducted clinical trials focusing on cancer treatment or prevention. BRB was found to influence multiple cancer hallmarks by targeting various pathways. Decomposition of free radicals and regulation of estrogen metabolism, BRB can reduce DNA damage caused by reactive oxygen species. BRB can also enhance the function of nucleotide excision repair to repair DNA lesions. Through regulation of epigenetics, BRB can enhance the expression of tumor suppressor genes, inducing cell cycle arrest, and promoting apoptosis and pyroptosis. BRB can reduce the energy and nutrients supply to the cancer nest by inhibiting glycolysis and reducing angiogenesis. The immune and inflammatory microenvironment surrounding cancer cells can also be ameliorated by BRB, inhibiting cancer initiation and progression. However, the limited bioavailability of BRB diminishes its anticancer efficacy. Notably, topical applications of BRB, such as gels and suppositories, have demonstrated significant clinical benefits. CONCLUSION: BRB inhibits cancer initiation, progression, and metastasis through diverse anticancer mechanisms while exhibiting minimal side effects. Given its potential, BRB emerges as a promising phototherapeutic agent for cancer treatment.


Assuntos
Neoplasias , Rubus , Humanos , Antocianinas/farmacologia , Frutas , Neoplasias/prevenção & controle , Fitoterapia , Rubus/metabolismo , Microambiente Tumoral
19.
J Nutr Sci ; 13: e1, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38282655

RESUMO

Ulcerative Colitis (UC), a type of Inflammatory Bowel Disease (IBD), is a chronic, relapsing gastrointestinal condition with increasing global prevalence. The gut microbiome profile of people living with UC differs from healthy controls and this may play a role in the pathogenesis and clinical management of UC. Probiotics have been shown to induce remission in UC; however, their impact on the gut microbiome and inflammation is less clear. Anthocyanins, a flavonoid subclass, have shown anti-inflammatory and microbiota-modulating properties; however, this evidence is largely preclinical. To explore the combined effect and clinical significance of anthocyanins and a multi-strain probiotic, a 3-month randomised controlled trial will be conducted in 100 adults with UC. Participants will be randomly assigned to one of four groups: anthocyanins (blackcurrant powder) + placebo probiotic, probiotic + placebo fruit powder, anthocyanin + probiotic, or double placebo. The primary outcome is a clinically significant change in the health-related quality-of-life measured with the Inflammatory Bowel Disease Questionnaire-32. Secondary outcomes include shotgun metagenomic sequencing of the faecal microbiota, faecal calprotectin, symptom severity, and mood and cognitive tests. This research will identify the role of adjuvant anti-inflammatory dietary treatments in adults with UC and elucidate the relationship between the gut microbiome and inflammatory biomarkers in this disease, to help identify targeted individualised microbial therapies. ANZCTR registration ACTRN12623000630617.


Assuntos
Colite Ulcerativa , Doenças Inflamatórias Intestinais , Probióticos , Adulto , Humanos , Antocianinas/farmacologia , Anti-Inflamatórios , Colite Ulcerativa/terapia , Doenças Inflamatórias Intestinais/terapia , Pós , Probióticos/farmacologia , Ensaios Clínicos Controlados Aleatórios como Assunto
20.
Compr Rev Food Sci Food Saf ; 23(1): e13259, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38284614

RESUMO

Foodborne contaminants refer to substances that are present in food and threaten food safety. Due to the progress in detection technology and the rising concerns regarding public health, there has been a surge in research focusing on the dangers posed by foodborne contaminants. These studies aim to explore and implement strategies that are both safe and efficient in mitigating the associated risks. Anthocyanins, a class of flavonoids, are abundantly present in various plant species, such as blueberries, grapes, purple sweet potatoes, cherries, mulberries, and others. Numerous epidemiological and nutritional intervention studies have provided evidence indicating that the consumption of anthocyanins through dietary intake offers a range of protective effects against the detrimental impact of foodborne contaminants. The present study aims to differentiate between two distinct subclasses of foodborne contaminants: those that are generated during the processing of food and those that originate from the surrounding environment. Furthermore, the impact of anthocyanins on foodborne contaminants was also summarized based on a review of articles published within the last 10 years. However, further investigation is warranted regarding the mechanism by which anthocyanins target foodborne contaminants, as well as the potential impact of individual variations in response. Additionally, it is important to note that there is currently a dearth of clinical research examining the efficacy of anthocyanins as an intervention for mitigating the effects of foodborne pollutants. Thus, by exploring the detoxification effect and mechanism of anthocyanins on foodborne pollutants, this review thereby provides evidence, supporting the utilization of anthocyanin-rich diets as a means to mitigate the detrimental effects of foodborne contaminants.


Assuntos
Antocianinas , Poluentes Ambientais , Antocianinas/farmacologia , Dieta , Inocuidade dos Alimentos , Frutas
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