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1.
Molecules ; 29(10)2024 May 19.
Artículo en Inglés | MEDLINE | ID: mdl-38792254

RESUMEN

In recent years, there has been a growing interest in the use of medicinal plants and phytochemicals as potential treatments for acne vulgaris. This condition, characterized by chronic inflammation, predominantly affects adolescents and young adults. Conventional treatment typically targets the key factors contributing to its development: the proliferation of Cutibacterium acnes and the associated inflammation. However, these treatments often involve the use of potent drugs. As a result, the exploration of herbal medicine as a complementary approach has emerged as a promising strategy. By harnessing the therapeutic properties of medicinal plants and phytochemicals, it may be possible to address acne vulgaris while minimizing the reliance on strong drugs. This approach not only offers potential benefits for individuals seeking alternative treatments but also underscores the importance of natural remedies of plant origin in dermatological care. The primary aim of this study was to assess the antimicrobial, antioxidant, and anti-inflammatory properties of plants and their phytochemical constituents in the management of mild acne vulgaris. A comprehensive search of scientific databases was conducted from 2018 to September 2023. The findings of this review suggest that medicinal plants and their phytochemical components hold promise as treatments for mild acne vulgaris. However, it is crucial to note that further research employing high-quality evidence and standardized methodologies is essential to substantiate their efficacy and safety profiles.


Asunto(s)
Acné Vulgar , Fitoquímicos , Plantas Medicinales , Acné Vulgar/tratamiento farmacológico , Plantas Medicinales/química , Humanos , Fitoquímicos/farmacología , Fitoquímicos/química , Fitoquímicos/uso terapéutico , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Antiinflamatorios/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Antioxidantes/farmacología , Antioxidantes/química , Antioxidantes/uso terapéutico
2.
Fitoterapia ; 175: 105953, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38588905

RESUMEN

Structural and functional changes of the intestinal barrier, as a consequence of a number of (epi)genetic and environmental causes, have a main role in penetrations of pathogens and toxic agents, and lead to the development of inflammation-related pathological conditions, not only at the level of the GI tract but also in other extra-digestive tissues and organs. Anthocyanins (ACNs), a subclass of polyphenols belonging to the flavonoid group, are well known for their health-promoting properties and are widely distributed in the human diet. There is large evidence about the correlation between the human intake of ACN-rich products and a reduction of intestinal inflammation and dysfunction. Our review describes the more recent advances in the knowledge of cellular and molecular mechanisms through which ACNs can modulate the main mechanisms involved in intestinal dysfunction and inflammation, in particular the inhibition of the NF-κB, JNK, MAPK, STAT3, and TLR4 proinflammatory pathways, the upregulation of the Nrf2 transcription factor and the expression of tight junction proteins and mucins.


Asunto(s)
Antocianinas , Inflamación , Intestinos , Animales , Humanos , Antocianinas/administración & dosificación , Inflamación/tratamiento farmacológico , Mucosa Intestinal/efectos de los fármacos , Mucosa Intestinal/metabolismo , Intestinos/efectos de los fármacos , Proteínas de Uniones Estrechas/metabolismo , Dieta a Base de Plantas
3.
Molecules ; 28(6)2023 Mar 20.
Artículo en Inglés | MEDLINE | ID: mdl-36985768

RESUMEN

BACKGROUND: The genus Cistus L. (Cistaceae) includes several medicinal plants growing wild in the Moroccan area. Acne vulgaris (AV) is a chronic skin disorder treated with topical and systemic therapies that often lead to several side effects in addition to the development of antimicrobial resistance. Our study aimed to investigate the bioactivity of extracts of two Moroccan Cistus species, Cistus laurifolius L. and Cistus salviifolius L., in view of their use as potential coadjuvants in the treatment of mild acne vulgaris. METHODS: Targeted phytochemical profiles obtained by HPLC-DAD and HPLC-ESI/MS analyses and biological activities ascertained by several antioxidants in vitro chemical and cell-based assays of the leaf extracts. Moreover, antimicrobial activity against Gram-positive and Gram-negative bacteria, and Candida albicans was evaluated. RESULTS: Analyses revealed the presence of several polyphenols in the studied extracts, mainly flavonoids and tannins. Cistus laurifolius L. and Cistus salviifolius L. possessed good biological properties and all extracts showed antibacterial activity, particularly against Staphylococcus aureus, S. epidermidis, and Propionibacterium acnes, identified as the main acne-causing bacteria. CONCLUSION: The results suggest that examined extracts are promising agents worthy of further studies to develop coadjuvants/natural remedies for mild acne treatment.


Asunto(s)
Acné Vulgar , Cistus , Cistus/química , Antibacterianos , Antioxidantes/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/química , Bacterias Gramnegativas , Bacterias Grampositivas , Antiinflamatorios/farmacología , Fitoquímicos/farmacología , Acné Vulgar/tratamiento farmacológico , Acné Vulgar/microbiología , Pruebas de Sensibilidad Microbiana
4.
Molecules ; 27(21)2022 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-36364258

RESUMEN

Distillation is the most widely used method to obtain an essential oil from plant material. The biomass used in the process is returned as a solid residue together with variable amounts of water rich in water-soluble compounds, which currently are not addressed to any further application. The scope of this work was to evaluate the phytochemical composition of wastewaters coming from hydrodistillation (DWWs) of five aromatic plants belonging to the Lamiaceae family, and to assess their in vitro antioxidant and anti-inflammatory activities. The phenolic profiles of the DWWs were determined by HPLC-DAD and HPLC-ESI/MS. Free radical scavenging ability, oxygen radical antioxidant capacity and superoxide dismutase mimetic activity of the samples under study were measured. Moreover, to investigate the anti-inflammatory activity of the DWWs, an in vitro experimental model of intestinal inflammation was used. The DWW samples' phytochemical analysis allowed the identification of 37 phenolic compounds, all exhibiting good antioxidant and anti-inflammatory activity. Our study contributes to the knowledge on the polyphenolic composition of the DWWs of five aromatic plants of the Lamiaceae family. The results highlight the presence of compounds with proven biological activity, and therefore of great interest in the pharmaceutical and nutraceutical fields.


Asunto(s)
Lamiaceae , Lamiaceae/química , Antioxidantes/farmacología , Antioxidantes/química , Aguas Residuales , Fenoles/química , Antiinflamatorios/farmacología , Fitoquímicos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Agua
5.
Org Biomol Chem ; 20(42): 8293-8304, 2022 Nov 02.
Artículo en Inglés | MEDLINE | ID: mdl-36227250

RESUMEN

α,α-Difluoromethyl ketones (DFMKs) have emerged as currently investigated agents benefiting from the merging of chemico-physical features conferred by the constitutive elements (-CHF2 and carbonyl moietites). With a view to biological applications, the additional incorporation of heterocycles is a desirable property enabling the tuning of critical factors encompassing the pharmaco-dynamic and kinetic profiles. The underexplored assembling of α,α-difluoromethyl-heteroaromatic ketones is herein implemented via a conceptually intuitive Weinreb amide acylative transfer of a putative difluoromethyl-carbanion. To make the strategy productive, we adopted the commercially available TMSCHF2 pronucleophile - characterized by robust chemical stability and manipulability (bp 65 °C) - which upon Lewis-base mediated activation delivers the competent CHF2-nucleophile. The synthetic protocol was carried out on pyrazole- and isoxazole-based scaffolds, and a panel of heteroaryl-DFMKs was consequently developed as potential COX-inhibitors. In this sense, the bioisosterism deducted through docking studies between the widely expressed carboxylic group (in several clinically used COX inhibitors) and the -COCHF2 motif introduced herein supports this rationale. To confirm the docking results, all compounds were tested against both COX-1 and COX-2 enzyme isoforms showing activity in the micromolar range and a good selectivity index (SI). They were also evaluated for their biocompatibility using NIH/3T3 cells to which they did not show any significant toxicity.


Asunto(s)
Isoxazoles , Cetonas , Ratones , Animales , Cetonas/química , Inhibidores de la Ciclooxigenasa/química , Pirazoles/química , Ciclooxigenasa 2/metabolismo , Inhibidores de la Ciclooxigenasa 2 , Relación Estructura-Actividad
6.
Psychiatry Res ; 311: 114527, 2022 05.
Artículo en Inglés | MEDLINE | ID: mdl-35344686

RESUMEN

Schizophrenia pathophysiology is still not well understood. Genetic factors involving biochemical systems are key players and oxidative stress takes part to the development and worsening of SZ. Oxidative stress led to the permanent production of oxidation products such as advanced glycation end products (AGEs) and advanced oxidation protein products (AOPPs). These proteins interact with their receptor amplifying ROS production and pro-inflammatory cytokines sustaining a permanent loop. We tested plasma levels of AGEs and AOPPs in 30 SZ patients. Their levels were statistically higher than controls confirming their involvement in mental disorders. Antioxidant nutraceuticals and a healthy lifestyle could diminish oxidative stress and ameliorate SZ symptoms.


Asunto(s)
Productos Avanzados de Oxidación de Proteínas , Esquizofrenia , Biomarcadores , Productos Finales de Glicación Avanzada/metabolismo , Humanos , Estrés Oxidativo
7.
Molecules ; 27(6)2022 Mar 08.
Artículo en Inglés | MEDLINE | ID: mdl-35335138

RESUMEN

Liver cancer is one of the most common causes of cancer mortality worldwide. Chemotherapy and radiotherapy are the conventional therapies generally employed in patients with liver tumors. The major issue associated with the administration of chemotherapeutics is their high toxicity and lack of selectivity, leading to systemic toxicity that can be detrimental to the patient's quality of life. An important approach to the development of original liver-targeted therapeutic products takes advantage of the employment of biologically active ligands able to bind specific receptors on the cytoplasmatic membranes of liver cells. In this perspective, glycyrrhetinic acid (GA), a pentacyclic triterpenoid present in roots and rhizomes of licorice, has been used as a ligand for targeting the liver due to the expression of GA receptors on the sinusoidal surface of mammalian hepatocytes, so it may be employed to modify drug delivery systems (DDSs) and obtain better liver or hepatocyte drug uptake and efficacy. In the current review, we focus on the most recent and interesting research advances in the development of GA-based hybrid compounds and DDSs developed for potential employment as efficacious therapeutic options for the treatment of hepatic cancer.


Asunto(s)
Ácido Glicirretínico , Neoplasias Hepáticas , Animales , Materiales Biocompatibles/uso terapéutico , Humanos , Neoplasias Hepáticas/tratamiento farmacológico , Neoplasias Hepáticas/metabolismo , Mamíferos , Calidad de Vida
8.
Nat Prod Res ; 36(18): 4768-4775, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-34844501

RESUMEN

Glycyrrhiza glabra roots have been well studied for their pharmacological activities, whereas less research has been conducted on liquorice aerial parts. Leaves represent a good source of D-pinitol, useful in the treatment of insulin resistance-related pathologies. Herein, we analyzed the in vitro effects of a D-pinitol-rich methanolic extract from Glycyrrhiza glabra leaves (GGLME) against lipotoxicity-related hypertrophy, inflammation, and insulin resistance in 3T3-L1 adipocytes exposed to palmitic acid (PA), comparing its activity with D-pinitol. GGLME pretreatment decreased lipid deposition, PPAR-γ, and NF-κB pathway induced by PA, similarly to D-pinitol, and improved insulin sensitivity, in presence or not of PA, increasing PI3K, pAkt, and GLUT1 levels. This study confirms that liquorice leaves, considered a waste of resource, could potentially be reused, and support further in vivo studies on animal and human models. In conclusion, liquorice leaves extract represents a potential candidate for prevention of metabolically induced inflammation, frequently leading to metabolic disorders.


Asunto(s)
Glycyrrhiza , Resistencia a la Insulina , Adipocitos , Animales , Humanos , Hipertrofia/metabolismo , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Inositol/análogos & derivados , Insulina/metabolismo , Insulina/farmacología , Palmitatos , Ácido Palmítico , Extractos Vegetales/metabolismo , Extractos Vegetales/farmacología , Transducción de Señal
9.
Arch Physiol Biochem ; 128(5): 1225-1234, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-32476488

RESUMEN

Background: Glycyrrhyza glabra L. is one of the most popular medicinal plant in the world, its roots having been used since ancient times in many traditional medicines. On the contrary, scarce attention has been dedicated to liquorice aerial parts. Previous studies showed the presence of a large group of polyphenols and a consistent amount of d-pinitol in the leaf extract.Methods: The methanolic extract from G. glabra leaves was profiled for its content in polyphenols; the amount of d-pinitol was also measured with two independent methods (HPLC-ELSD and NMR). The extract was tested for its in vitro protective effects against insulin resistance-related endothelial dysfunction in human umbilical vein endothelial cells exposed to palmitic acid, which is the most prevalent saturated free fatty acid in circulation.Results: Methanolic extract from liquorice leaves has a protective effect against the lipotoxicity-associated alterations of insulin pathway in human endothelial cells, similarly to what observed with pure d-pinitol.Conclusions: Liquorice leaves are to be considered a waste product which gives a phytocomplex endowed with interesting potential therapeutic properties, moreover the use of a liquorice leaves phytocomplex rather than a pure compound allows avoiding a series of isolation/purification procedures and can be easily scaled up for industrial applications.


Asunto(s)
Glycyrrhiza , Insulina , Células Endoteliales , Ácidos Grasos no Esterificados , Glycyrrhiza/química , Humanos , Inositol/análogos & derivados , Ácido Palmítico/toxicidad , Extractos Vegetales/química , Extractos Vegetales/farmacología , Polifenoles/farmacología , Residuos
10.
Molecules ; 26(15)2021 Jul 31.
Artículo en Inglés | MEDLINE | ID: mdl-34361819

RESUMEN

One of the main current strategies for cancer treatment is represented by combination chemotherapy. More recently, this strategy shifted to the "hybrid strategy", namely the designing of a new molecular entity containing two or more biologically active molecules and having superior features compared with the individual components. Moreover, the term "hybrid" has further extended to innovative drug delivery systems based on biocompatible nanomaterials and able to deliver one or more drugs to specific tissues or cells. At the same time, there is an increased interest in plant-derived polyphenols used as antitumoral drugs. The present review reports the most recent and intriguing research advances in the development of hybrids based on the polyphenols curcumin and resveratrol, which are known to act as multifunctional agents. We focused on two issues that are particularly interesting for the innovative chemical strategy involved in their development. On one hand, the pharmacophoric groups of these compounds have been used for the synthesis of new hybrid molecules. On the other hand, these polyphenols have been introduced into hybrid nanomaterials based on gold nanoparticles, which have many potential applications for both drug delivery and theranostics in chemotherapy.


Asunto(s)
Productos Biológicos/uso terapéutico , Curcumina/uso terapéutico , Neoplasias/tratamiento farmacológico , Resveratrol/uso terapéutico , Antineoplásicos/química , Antineoplásicos/uso terapéutico , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/uso terapéutico , Productos Biológicos/química , Curcumina/química , Sistemas de Liberación de Medicamentos , Oro/química , Humanos , Nanopartículas del Metal/química , Nanopartículas del Metal/uso terapéutico , Resveratrol/química , Estilbenos/química
11.
Chem Biodivers ; 18(8): e2100316, 2021 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-34114723

RESUMEN

The genus Rhanterium (Asteraceae) is a widely distributed medicinal plant throughout western North Africa and some Rhanterium species are used in folk medicine. The aim of research was to investigate methanolic extracts from different parts (flowers, leaves, and stems) of Tunisian Rhanterium suaveolens as potential sources of bioactive products useful for healthy purposes. In particular, were analyzed the phenolic composition of these extracts and their antioxidant, anti-inflammatory, and anti-tyrosinase properties. The phytochemical analyses were performed using standard colorimetric procedures, HPLC-DAD and HPLC-DAD-ESI-MS. Then, several in vitro cell-free assays have been used to estimate the antioxidant/free radical scavenging capability of the extracts. Moreover, in vitro, and in vivo anti-melanogenesis activities of these extracts were tested, respectively, with the tyrosinase inhibition assay and the Zebrafish embryo model. Finally, the anti-inflammatory potential of these extracts in an in vitro model of acute intestinal inflammation in differentiated Caco-2 cells was evaluated. The R. suaveolens extracts under study appeared particularly rich in flavonols and hydroxycinnamic acids and all extracts appeared endowed with good antioxidant/free radical scavenging properties, being the flower extracts slightly more active than the others. Moreover, R. suaveolens flowers extract was able to inhibit in vitro tyrosinase activity and exhibited bleaching effects on the pigmentation of zebrafish embryos. Furthermore, all extracts showed good anti-inflammatory activity in intestinal epithelial cells as demonstrated by the inhibition of TNF-α-induced gene expression of IL-6 and IL-8. R. suaveolens aerial parts may be considered as a potential source of whitening agents, as well as of agents for the treatment of disorders related to oxidative stress and inflammation.


Asunto(s)
Antiinflamatorios/química , Asteraceae/química , Inhibidores Enzimáticos/química , Monofenol Monooxigenasa/antagonistas & inhibidores , Extractos Vegetales/química , Animales , Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/metabolismo , Antiinflamatorios/farmacología , Antioxidantes/química , Asteraceae/metabolismo , Células CACO-2 , Diferenciación Celular/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Ácidos Cumáricos/química , Ácidos Cumáricos/aislamiento & purificación , Ácidos Cumáricos/metabolismo , Ácidos Cumáricos/farmacología , Embrión no Mamífero/citología , Embrión no Mamífero/efectos de los fármacos , Embrión no Mamífero/metabolismo , Inhibidores Enzimáticos/aislamiento & purificación , Inhibidores Enzimáticos/metabolismo , Inhibidores Enzimáticos/farmacología , Flavonoles/química , Flavonoles/aislamiento & purificación , Flavonoles/metabolismo , Flavonoles/farmacología , Humanos , Melaninas/metabolismo , Monofenol Monooxigenasa/metabolismo , Componentes Aéreos de las Plantas/química , Componentes Aéreos de las Plantas/metabolismo , Plantas Medicinales/química , Plantas Medicinales/metabolismo , Espectrometría de Masa por Ionización de Electrospray , Túnez , Pez Cebra/metabolismo
12.
Chem Biodivers ; 18(6): e2100185, 2021 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-33860977

RESUMEN

The genus Rumex (Polygonaceae) is distributed worldwide and the different species belonging to it are used in traditional medicine. The present study aimed at the evaluation of the phytochemical profile and the biochemical properties of methanolic extracts from different parts (roots, stems, and leaves) of Rumex roseus, a wild local Tunisian plant traditionally used as food. The phytochemical analysis on the extracts was performed using standard colorimetric procedures, HPLC-DAD, and HPLC-DAD-ESI-MS; then, several in vitro cell-free assays have been used to estimate their antioxidant/free radical scavenging capability (TAC-PM, DPPH, TEAC, FRAP, ORAC, SOD-like activity, and HOCl-induced albumin degradation). Additionally, anti-inflammatory effect of these extracts was evaluated in an in vitro model of acute intestinal inflammation in differentiated Caco-2 cells. The results showed that the methanolic extracts from stems and, especially, leaves contain substantial amounts of flavones (apigenin and luteolin, together with their derivatives), while the extract from roots is characterized by the presence of tannins and quinic acid derivatives. All the extracts appeared endowed with excellent antioxidant/free radical scavenging properties. In particular, the extract from roots was characterized by a remarkable activity, probably due to its different and peculiar polyphenolic composition. Furthermore, both Rumex roseus roots and stems extracts demonstrated an anti-inflammatory effect in intestinal epithelial cells, reducing TNF-α-induced gene expression of IL-6 and IL-8. In conclusion, R. roseus methanolic extracts have shown to be potential sources of bioactive compounds to be used in the prevention and treatment of pathologies related to oxidative stress and inflammation.


Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Antioxidantes/farmacología , Inflamación/tratamiento farmacológico , Metanol/química , Fitoquímicos/farmacología , Rumex/química , Animales , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Compuestos de Bifenilo/antagonistas & inhibidores , Células CACO-2 , Bovinos , Células Cultivadas , Humanos , Ratones , Células 3T3 NIH , Estrés Oxidativo/efectos de los fármacos , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Picratos/antagonistas & inhibidores , Albúmina Sérica Bovina/antagonistas & inhibidores
13.
Thyroid ; 31(1): 96-105, 2021 01.
Artículo en Inglés | MEDLINE | ID: mdl-32729374

RESUMEN

Background: There is a growing awareness that nutritional habits may influence risk of several inflammatory and immune-mediated disorders, including autoimmune diseases, through various mechanisms. The aim of the present study was to investigate dietary habits and their relationship with redox homeostasis in the setting of thyroid autoimmunity. Materials and Methods: Two hundred subjects (173 females and 27 males; median age, 37 years) were enrolled. None were under any pharmacological treatment. Exclusion criteria were any infectious/inflammatory/autoimmune comorbidity, kidney failure, diabetes, and cancer. In each subject, serum thyrotropin (TSH), free thyroxine, antithyroid antibodies, and circulating oxidative stress markers were measured. A questionnaire on dietary habits, evaluating the intake frequencies of food groups and adherence to the Mediterranean diet, was submitted to each participant. Results: Among the 200 recruited subjects, 81 (71 females and 10 males) were diagnosed with euthyroid Hashimoto's thyroiditis (HT); the remaining 119 (102 females and 17 males) served as controls. In questionnaires, HT subjects reported higher intake frequencies of animal foods (meat, p = 0.0001; fish, p = 0.0001; dairy products, p = 0.004) compared with controls, who reported higher intake frequencies of plant foods (legumes, p = 0.001; fruits and vegetables, p = 0.030; nuts, p = 0.0005). The number of subjects who preferentially consumed poultry instead of red/processed meat was lower in HT subjects than in controls (p = 0.0141). In logistic regression analysis, meat consumption was associated with increased odds ratio of developing thyroid autoimmunity, while the Mediterranean diet traits were protective. In HT subjects, serum advanced glycation end products (markers of oxidative stress) were significantly higher (p = 0.0001) than in controls, while the activity of glutathione peroxidase and thioredoxin reductase, as well as total plasma antioxidant activity, were lower (p = 0.020, p = 0.023, and p = 0.002, respectively), indicating a condition of oxidative stress. Stepwise regression models demonstrated a significant dependence of oxidative stress parameters on consumption of animal foods, mainly meat. Conclusions: The present study suggests a protective effect of low intake of animal foods toward thyroid autoimmunity and a positive influence of such nutritional patterns on redox balance and potentially on oxidative stress-related disorders.


Asunto(s)
Dieta Saludable , Dieta Mediterránea , Conducta Alimentaria , Enfermedad de Hashimoto/metabolismo , Estrés Oxidativo , Adolescente , Adulto , Anciano , Biomarcadores/sangre , Estudios de Casos y Controles , Femenino , Enfermedad de Hashimoto/sangre , Enfermedad de Hashimoto/diagnóstico , Enfermedad de Hashimoto/prevención & control , Humanos , Masculino , Persona de Mediana Edad , Estado Nutricional , Valor Nutritivo , Oxidación-Reducción , Factores Protectores , Medición de Riesgo , Factores de Riesgo , Adulto Joven
14.
Molecules ; 25(14)2020 Jul 16.
Artículo en Inglés | MEDLINE | ID: mdl-32708833

RESUMEN

This review deals with hydrogels as soft and biocompatible vehicles for the delivery of plant-derived (poly)phenols, compounds with low general toxicity and an extraordinary and partially unexplored wide range of biological properties, whose use presents some major issues due to their poor bioavailability and water solubility. Hydrogels are composed of polymeric networks which are able to absorb large amounts of water or biological fluids while retaining their three-dimensional structure. Apart from this primary swelling capacity, hydrogels may be easily tailored in their properties according to the chemical structure of the polymeric component in order to obtain smart delivery systems that can be responsive to various internal/external stimuli. The functionalization of the polymeric component of hydrogels may also be widely exploited to facilitate the incorporation of bioactive compounds with different physicochemical properties into the system. Several prototype hydrogel systems have been designed for effective polyphenol delivery and potential employment in the treatment of human diseases. Therefore, the inherent features of hydrogels have been the focus of considerable research efforts over the past few decades. Herein, we review the most recent advances in (poly)phenol-loaded hydrogels by analyzing them primarily from the therapeutic perspective and highlighting the innovative aspects in terms of design and chemistry.


Asunto(s)
Sistemas de Liberación de Medicamentos , Hidrogeles/química , Polifenoles/química , Materiales Biocompatibles/química , Materiales Biocompatibles/farmacología , Disponibilidad Biológica , Humanos , Hidrogeles/farmacología , Polímeros/química , Polímeros/farmacología , Polifenoles/uso terapéutico
15.
Arch Biochem Biophys ; 691: 108488, 2020 09 30.
Artículo en Inglés | MEDLINE | ID: mdl-32692982

RESUMEN

Obesity is a metabolic disorder characterized by excess adipose tissue, macrophages infiltration, and inflammation which in turn lead to insulin-resistance. Epidemiological evidences reported that anthocyanins possess not only high antioxidant and antiinflammatory activities, but also improve metabolic complications associated with obesity. The aim of this work was to evaluate the in vitro beneficial effects of cyanidin-3-O-glucoside (C3G) in counteracting inflammation and insulin-resistance in 3T3-L1 hypertrophic adipocytes exposed to palmitic acid (PA). In the present study murine 3T3-L1 adipocytes were pretreated with C3G for 24 h and then exposed to palmitic acid (PA) for 24 h. Real-time PCR, western blotting analysis and Oil Red O staining were applied for investigating the mechanism involved in adipocytes dysfunction. C3G pretreatment reduced lipid accumulation, PPARγ pathway and NF-κB pathway induced by PA in murine adipocytes. In addition, our data demonstrated that PA reduced insulin signaling via IRS-1 Ser307phosphorylation while C3G dose-dependently improved insulin sensitivity restoring IRS-1/PI3K/Akt pathway. Furthermore, C3G improved adiponectin mRNA levels altered by PA in 3T3-L1 murine and SGBS human adipocytes. Herein reported data demonstrate that C3G ameliorated adipose tissue dysfunction, thus suggesting new potential roles for this compound of nutritional interest in the prevention of pathological conditions linked to obesity.


Asunto(s)
Adipocitos/efectos de los fármacos , Antocianinas/farmacología , Glucósidos/farmacología , Inflamación/prevención & control , Transducción de Señal/efectos de los fármacos , Células 3T3-L1 , Adipogénesis/efectos de los fármacos , Adiponectina/metabolismo , Animales , Proteínas de Unión a Ácidos Grasos/metabolismo , Transportador de Glucosa de Tipo 1/metabolismo , Humanos , Resistencia a la Insulina/fisiología , Ratones , FN-kappa B/metabolismo , PPAR gamma/metabolismo , Ácido Palmítico/farmacología
16.
Chem Biodivers ; 17(8): e2000345, 2020 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-32501568

RESUMEN

The present study is aimed at the evaluation of the phytochemical profile and the biochemical properties of methanolic extracts obtained from different parts of Rumex algeriensis and Rumex tunetanus, two relict species limited to the North Africa. Phytochemical analyses of these extracts were performed using standard colorimetric procedures, HPLC-DAD, and HPLC-DAD-ESI/MS, and their antioxidant/free radical scavenging capability was estimated through several in vitro cell-free assays. Moreover, the anti-inflammatory potential of these extracts was demonstrated in an in vitro model of acute intestinal inflammation using differentiated Caco-2 cells. The results showed that all the extracts appeared endowed with excellent antioxidant/free radical scavenging properties. In particular, the extracts from both R. algeriensis and R. tunetanus flowers, and that from R. algeriensis stems were characterized by a remarkable SOD-like and NO-scavenging activity, as well as by the capability to protect albumin against HClO-induced degradation. Furthermore, the extracts from flowers of both Rumex species, as well as R. algeriensis stems, showed an anti-inflammatory effect in intestinal epithelial cells, as demonstrated by the inhibition of TNF-α-induced gene expression of IL-6 and IL-8. In conclusion, R. algeriensis and R. tunetanus have shown to be potential sources of bioactive products to be used in the prevention and treatment of pathologies related to oxidative stress and inflammation.


Asunto(s)
Extractos Vegetales/química , Extractos Vegetales/farmacología , Rumex/química , Antiinflamatorios/farmacología , Células CACO-2 , Cromatografía Líquida de Alta Presión/métodos , Humanos , Metanol/química , Estrés Oxidativo/efectos de los fármacos , Rumex/clasificación , Especificidad de la Especie , Espectrometría de Masa por Ionización de Electrospray/métodos
17.
Curr Med Chem ; 27(12): 1955-1996, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-30417771

RESUMEN

Chronic Noncommunicable Diseases (NCDs), mostly represented by cardiovascular diseases, diabetes, chronic pulmonary diseases, cancers, and several chronic pathologies, are one of the main causes of morbidity and mortality, and are mainly related to the occurrence of metabolic risk factors. Anthocyanins (ACNs) possess a wide spectrum of biological activities, such as anti-inflammatory, antioxidant, cardioprotective and chemopreventive properties, which are able to promote human health. Although ACNs present an apparent low bioavailability, their metabolites may play an important role in the in vivo protective effects observed. This article directly addresses the scientific evidences supporting that ACNs could be useful to protect human population against several NCDs not only acting as antioxidant but through their capability to modulate cell redox-dependent signaling. In particular, ACNs interact with the NF-κB and AP-1 signal transduction pathways, which respond to oxidative signals and mediate a proinflammatory effect, and the Nrf2/ARE pathway and its regulated cytoprotective proteins (GST, NQO, HO-1, etc.), involved in both cellular antioxidant defenses and elimination/inactivation of toxic compounds, so countering the alterations caused by conditions of chemical/oxidative stress. In addition, supposed crosstalks could contribute to explain the protective effects of ACNs in different pathological conditions characterized by an altered balance among these pathways. Thus, this review underlines the importance of specific nutritional molecules for human health and focuses on the molecular targets and the underlying mechanisms of ACNs against various diseases.


Asunto(s)
Enfermedades no Transmisibles , Antocianinas , Antioxidantes , Humanos , Factor 2 Relacionado con NF-E2 , FN-kappa B , Oxidación-Reducción , Estrés Oxidativo
19.
Artículo en Inglés | MEDLINE | ID: mdl-31316471

RESUMEN

Background: Advanced glycation end-products (AGEs) and their cell receptor (RAGE) are involved in the pathophysiology of cardio-metabolic diseases. Interaction of AGEs with RAGE results in increased generation of oxygen radicals and pro-inflammatory cytokines. Circulating soluble RAGE (sRAGE) interacts with AGEs in order to counterbalance the negative effects of AGEs-RAGE interaction. Objectives: To define factors influencing AGEs, sRAGE, AGEs/sRAGE-ratio, and advanced oxidation-protein products (AOPPs) levels and to investigate changes in oxidative balance among overweight/obese children. Materials and methods: Cross-sectional, one Center, case-control study included 41 overweight and obese children aged between 5 and 16 years and 36 lean matched controls. Inclusion criteria were: BMI ≥ 1 SD; term birth; no genetic or endocrine causes of obesity; no associated chronic diseases neither chronic therapies. All patients underwent clinical and biochemical investigations (lipid and glucose profiles, liver, renal and thyroid function tests, uric acid, C-reactive protein (CRP), AGEs, sRAGE, and AOPPs serum concentrations). Significance was established at 0.050. Results: AOPPs, AGEs/sRAGE-ratio, HOMA-IR, triglycerides, triglycerides/HDL-ratio, total cholesterol (TC)/HDL-ratio, atherogenic-index of plasma (AIP), uric acid, CRP were significantly higher, whereas sRAGE and HDL were significantly lower in overweight/obese children than controls. sRAGE was significantly negatively correlated with BMI SD, TC/HDL-ratio, CRP, AOPPs, and positively with HDL. AGE/sRAGE-ratio and AOPPs were significantly positively correlated with BMI SD, TC/HDL-ratio, AIP, CRP, and negatively with HDL. BMI SD was independently associated with AGEs/sRAGE-ratio (B = 0.06; p = 0.008), AOPPs (B = 0.13; p = 0.02), and sRAGE (B = -73.18; p = 0.000). Conclusions: We demonstrated, for the first time in a pediatric cohort, a significant higher value of AGEs/sRAGE-ratio among overweight/obese children, expression of a relative shift to oxidant from anti-oxidant factors, suggesting an AGE/RAGE-related oxidative homeostasis dysregulation that could enhance susceptibility to oxidative/inflammatory tissues damage. Severity of overweight, influencing the increase of oxidative stress in human organism and even in children, may contribute to the pathogenesis of long-term cardiovascular and metabolic alterations.

20.
Phytother Res ; 33(7): 1888-1897, 2019 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-31155812

RESUMEN

Increased adiposity has been associated with adipose tissue low-grade inflammation leading to insulin resistance. Adipocyte differentiation inhibitors are expected to be effective in preventing obesity and related diseases. Anthocyanins (ACNs) are associated to enhanced adipocyte function and protection from metabolic stress. Herein, we evaluated the in vitro protective effects of an ACN rich extract against palmitic acid (PA)-induced hypertrophy, inflammation, and insulin resistance in 3T3-L1 adipocytes. ACN extract pretreatment reduces lipid accumulation and peroxisome proliferators-activated receptor-γ protein levels induced by PA. In addition, PA induces inflammation with activation of NF-κB pathway, whereas ACN extract pretreatment dose-dependently inhibited this pathway. Furthermore, adipocyte dysfunction associated with hypertrophy induces insulin resistance by affecting phosphatidylinositol 3-kinase-protein kinase B/Akt axis, GLUT-1, and adiponectin mRNA levels. ACN extract pretreatment reverts these effects induced by PA and moreover was able to induce insulin pathway with levels higher than insulin control cells, supporting an insulin sensitizer role for ACNs. This study demonstrates a prevention potential of ACNs against obesity comorbidities, due to their protective effects against inflammation/insulin resistance in adipocytes. In addition, these results contribute to the knowledge and strategies on the evaluation of the mechanism of action of ACNs from a food source under basal and insulin resistance conditions related to obesity.


Asunto(s)
Adipocitos/efectos de los fármacos , Antocianinas/farmacología , Antiinflamatorios/farmacología , Resistencia a la Insulina , Células 3T3-L1 , Adipocitos/metabolismo , Animales , Hipertrofia , Ratones , Ácido Palmítico
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