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1.
Fitoterapia ; 175: 105953, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38588905

RESUMO

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.


Assuntos
Antocianinas , Inflamação , Intestinos , Animais , Humanos , Antocianinas/administração & dosagem , Inflamação/tratamento farmacológico , Mucosa Intestinal/efeitos dos fármacos , Mucosa Intestinal/metabolismo , Intestinos/efeitos dos fármacos , Proteínas de Junções Íntimas/metabolismo , Dieta Baseada em Plantas
2.
Molecules ; 28(6)2023 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-36985768

RESUMO

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.


Assuntos
Acne Vulgar , Cistus , Cistus/química , Antibacterianos , Antioxidantes/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Anti-Inflamatórios/farmacologia , Compostos Fitoquímicos/farmacologia , Acne Vulgar/tratamento farmacológico , Acne Vulgar/microbiologia , Testes de Sensibilidade Microbiana
3.
Molecules ; 27(21)2022 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-36364258

RESUMO

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.


Assuntos
Lamiaceae , Lamiaceae/química , Antioxidantes/farmacologia , Antioxidantes/química , Águas Residuárias , Fenóis/química , Anti-Inflamatórios/farmacologia , Compostos Fitoquímicos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Água
4.
Nat Prod Res ; 36(18): 4768-4775, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34844501

RESUMO

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.


Assuntos
Glycyrrhiza , Resistência à Insulina , Adipócitos , Animais , Humanos , Hipertrofia/metabolismo , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Inositol/análogos & derivados , Insulina/metabolismo , Insulina/farmacologia , Palmitatos , Ácido Palmítico , Extratos Vegetais/metabolismo , Extratos Vegetais/farmacologia , Transdução de Sinais
5.
Arch Physiol Biochem ; 128(5): 1225-1234, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32476488

RESUMO

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.


Assuntos
Glycyrrhiza , Insulina , Células Endoteliais , Ácidos Graxos não Esterificados , Glycyrrhiza/química , Humanos , Inositol/análogos & derivados , Ácido Palmítico/toxicidade , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Resíduos
6.
Molecules ; 26(15)2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-34361819

RESUMO

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.


Assuntos
Produtos Biológicos/uso terapêutico , Curcumina/uso terapêutico , Neoplasias/tratamento farmacológico , Resveratrol/uso terapêutico , Antineoplásicos/química , Antineoplásicos/uso terapêutico , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/uso terapêutico , Produtos Biológicos/química , Curcumina/química , Sistemas de Liberação de Medicamentos , Ouro/química , Humanos , Nanopartículas Metálicas/química , Nanopartículas Metálicas/uso terapêutico , Resveratrol/química , Estilbenos/química
7.
Chem Biodivers ; 18(8): e2100316, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34114723

RESUMO

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.


Assuntos
Anti-Inflamatórios/química , Asteraceae/química , Inibidores Enzimáticos/química , Monofenol Mono-Oxigenase/antagonistas & inibidores , Extratos Vegetais/química , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/metabolismo , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Asteraceae/metabolismo , Células CACO-2 , Diferenciação Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Ácidos Cumáricos/química , Ácidos Cumáricos/isolamento & purificação , Ácidos Cumáricos/metabolismo , Ácidos Cumáricos/farmacologia , Embrião não Mamífero/citologia , Embrião não Mamífero/efeitos dos fármacos , Embrião não Mamífero/metabolismo , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/metabolismo , Inibidores Enzimáticos/farmacologia , Flavonóis/química , Flavonóis/isolamento & purificação , Flavonóis/metabolismo , Flavonóis/farmacologia , Humanos , Melaninas/metabolismo , Monofenol Mono-Oxigenase/metabolismo , Componentes Aéreos da Planta/química , Componentes Aéreos da Planta/metabolismo , Plantas Medicinais/química , Plantas Medicinais/metabolismo , Espectrometria de Massas por Ionização por Electrospray , Tunísia , Peixe-Zebra/metabolismo
8.
Chem Biodivers ; 18(6): e2100185, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33860977

RESUMO

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.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Antioxidantes/farmacologia , Inflamação/tratamento farmacológico , Metanol/química , Compostos Fitoquímicos/farmacologia , Rumex/química , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/antagonistas & inibidores , Células CACO-2 , Bovinos , Células Cultivadas , Humanos , Camundongos , Células NIH 3T3 , Estresse Oxidativo/efeitos dos fármacos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Picratos/antagonistas & inibidores , Soroalbumina Bovina/antagonistas & inibidores
9.
Chem Biodivers ; 17(8): e2000345, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32501568

RESUMO

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.


Assuntos
Extratos Vegetais/química , Extratos Vegetais/farmacologia , Rumex/química , Anti-Inflamatórios/farmacologia , Células CACO-2 , Cromatografia Líquida de Alta Pressão/métodos , Humanos , Metanol/química , Estresse Oxidativo/efeitos dos fármacos , Rumex/classificação , Especificidade da Espécie , Espectrometria de Massas por Ionização por Electrospray/métodos
11.
Phytother Res ; 33(7): 1888-1897, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31155812

RESUMO

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.


Assuntos
Adipócitos/efeitos dos fármacos , Antocianinas/farmacologia , Anti-Inflamatórios/farmacologia , Resistência à Insulina , Células 3T3-L1 , Adipócitos/metabolismo , Animais , Hipertrofia , Camundongos , Ácido Palmítico
12.
Phytochemistry ; 152: 162-173, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29775867

RESUMO

Hypericum is one out of the nine genera belonging to the botanical family Clusiaceae Lindl (syn. Hypericaceae Juss.; APG III, 2009). The genus contains 484 species spread worldwide, one of which, Hypericum perforatum, is largely used in folk medicine. The aim of this study was to evaluate the chemical composition, along with the antioxidant and phototoxic activity, of 11 Hypericum species grown in Sicily (H. perforatum L., H. aegypticum L., H. androsaemum L., H. calycinum L., H. hircinum L., H. hirsutum L., H. montanum L., H. patulum Thunb., H. perfoliatum L., H. pubescens Boiss., H. tetrapterum Fr.). Samples of flowering tops collected from these Hypericum species were extracted and analysed by high performance liquid chromatography with diode-array detection and mass spectrometry (HPLC-DAD-MS) to determine their content of main polyphenols, acylphloroglucinols, and naphthodianthrones. The extracts were also subjected to a photocytotoxic assay using murine fibroblast (NIH/3T3), and their antioxidant activity evaluated by means of Folin-Ciocalteau, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, and oxygen radical antioxidant capacity assays. Phytochemical analysis allowed us to identify and quantify 20 metabolites, each of them possessing a well-known biological activity. Furthermore, all examined species showed a good cytotoxic and antioxidant/radical scavenging activity. These results indicate that in addition to the well-known H. perforatum, at least other three species (H. tetrapterum, H. pubescens, and H. montanum) represent potential sources of biologically active compounds, and at least other two species (H. perfoliatum and H. tetrapterum), due to their phototoxicity are candidates for application in photodynamic therapy.


Assuntos
Antioxidantes/farmacologia , Compostos de Bifenilo/antagonistas & inibidores , Fibroblastos/efeitos dos fármacos , Hypericum/química , Compostos Fitoquímicos/farmacologia , Picratos/antagonistas & inibidores , Espécies Reativas de Oxigênio/antagonistas & inibidores , Animais , Antioxidantes/química , Antioxidantes/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Dermatite Fototóxica , Flores/química , Espectrometria de Massas , Camundongos , Células NIH 3T3 , Fotoquimioterapia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Especificidade da Espécie
13.
Iran J Pharm Res ; 16(1): 315-327, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28496485

RESUMO

Rosmarinus officinalis L., a medicinal herb from the labiates family, has been reported to have potential benefit in the treatment and prevention of several diseases. In particular its phenolics have demonstrated protective effects on various types of cancer through several mechanisms. The present study aimed to determine the effects of rosemary phenolic extracts on human cell functions, with particular regard to their anti-proliferative properties in three cell types U937, CaCo-2 and the peripheral blood mononuclear cells (PBMCs). The radical scavenging and Ferric reducing abilities of the extracts have been assessed as well as their cyto-toxicity and effects on cell cycle distribution and apoptosis. About 13 compounds were identified with dominance of rosmarinic acid in the methanolic extract and phenolic diterpens in the ethyl acetate fraction (Carnosol, Carnosic acid and methyl Carnosate). The total polyphenolic content was important in the first extract with 2.589 ± 0.005 g/100 g in gallic acid equivalent compared to 0.763 ± 0.005 g/100 g. The methanolic fraction displayed higher antioxidant activity (DPPHIC50: 0.510 mg/mL and FRAP: 1.714 ± 0.068 mmol Fe2+/g) while ethyl acetate showed pronounced antiproliferative effects (IC50: 14.85 ± 0.20µg/mL and 14.95 ± 2.32 µg/mL respectively for U937 and CaCo-2 cells). The anti-proliferative effect was associated with a cell cycle arrest in S phase for U937 (62% of the population at 5 µg/mL) with a concomitant decrease in G1 and G2/M phases. Tested extracts displayed in addition early apoptotic effects in U937 and late apoptosis in CaCo-2 cells. The obtained data indicate that the identified phenolics are at least partially responsible for the observed cytotoxicity.

14.
Pharmacogn Mag ; 12(47): 203-10, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27601851

RESUMO

BACKGROUND: Thymelaea microphylla Coss. et Dur. (Thymelaeaceae) (TM) is a rare medicinal plant endemic to Algeria. Leaves decoction is used in folk medicine for anticancer, anti-inflammatory, and antidiabetic properties. OBJECTIVE: Herein, the antioxidant and anti-inflammatory properties of different extracts from leaves and flowers of Algerian TM were evaluated. MATERIALS AND METHODS: The study was carried out by in vitro cell-free assays (antioxidant/radical properties), ex vivo experiments (inhibition of prostaglandin E2 and thromboxane B2 release in human whole blood) and in vitro experiments on cell systems (cytotoxicity on peripheral blood mononuclear cells, and protective effects on human vein endothelial cells exposed to TNF-α). RESULTS: The acetone TM extract showed significant antioxidant properties and excellent anti-inflammatory and cyclooxygenase-inhibitory activity, together with lack of toxicity on normal human blood cells; furthermore, it was able to protect endothelial cells against dysfunction induced by TNF-α, as shown by decrease in cell death, e-selectin expression and leukocyte adhesion. CONCLUSION: On these bases, TM leaves and flowers appear to be a good source of bioactive compounds with significant antioxidant and antiinflammatory capability, and potentially effective in prevention and treatment of pathological conditions related to oxidative stress and inflammation, such as endothelial dysfunction. SUMMARY: Thymelaea microphylla leaves and flowers are a good source of bioactive compounds with significant antioxidant/free radical scavenger and antiinflammatory activity.The acetone extract from leaves and flowers of Algerian Thymelaea microphylla possesses excellent cyclooxygenase-inhibitory activity.This extract is able to protect against endothelial dysfunction, an early event in development of atherosclerosis and vascular diseases. Abbreviations used: TM: Thymelaea microphylla; BCB: Beta-carotene bleaching; AcE: Acetone extract; PGE2: Prostaglandin E2; TxB2: Thromboxane B2; FL: Fluorescein; Cat: Catechin; DPPH: 2,2-diphenyl-1-picrylhydrazyl; ABTS: 2,2'-azinobis-(3-ethyl-benzothiazolin-6-sulfonic acid)+; Que: Quercetin; ORAC: Oxygen radical absorbance capacity; AAPH: 2,2'-azobis (2-methylpropionamidine)dihydrochloride; PMS/NADH: Phenazine methosulfate/nicotinamide adenine dinucleotide; HUVECs: Human umbilical vein endothelial cells.

15.
Pharmacogn Mag ; 11(Suppl 1): S102-9, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-26109754

RESUMO

BACKGROUND: Rhamnus alaternus (Rhamnaceae) L. has been traditionally used for treatment of many diseases. OBJECTIVE: In this study, we determined the antioxidant/free radical scavenger properties, the flavonoid profile and the cytotoxicity of aqueous and methanolic extracts obtained by maceration from Algerian R. alaternus bark, like also of aqueous extract prepared by decoction according to the traditional method. This to estimate the usefulness of the drug traditional preparation and compare it with those made in the laboratory. MATERIALS AND METHODS: The antioxidant activity of the extracts was evaluated using five different redox-based assays, all involving one redox reaction with the oxidant. High-performance liquid chromatography/diode array detection/electrospray ionization mass spectrometry analysis was used to identify and quantify the flavonoids content. Cytotoxicity on human monocytic leukemia cells (U937) was also carried out. RESULTS: All the extracts tested showed a good antioxidant/free radical scavenger activity and a similar flavonoid fingerprint. However, the methanolic one presented the best antioxidant activity that can be due to the highest flavonoid amount and significantly reduced the proliferation of leukemia cells. The results confirm that the extract prepared by decoction contains efficient antioxidant compounds and this justifies in part the therapeutic and preventive usefulness. Moreover, the methanolic extract exerted excellent cytotoxicity on U937 that could be attributed to kaempferol and rhamnocitrin glycosides.

16.
Nat Prod Commun ; 9(12): 1761-4, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25632479

RESUMO

Three dihydrostilbenes belonging to the polyphenol pool characterized in the leaves of Sicilian liquorice (Glycyrrhiza glabra L.) have been tested for their antioxidant and anti-inflammatory activity. The three dihydrostilbenes (PA-82, GA-23, DO-07) were in vitro tested to evaluate their capability to scavenge the stable radical 1,1-diphenyl-2-picrylhydrazyl (DPPH), and to decrease thromboxane B2 (TxB2) and prostaglandin E2 (PGE2) release in human whole blood samples. On the basis of the observed capability of these compounds to affect the cell COX-1/COX-2 pathway, a molecular docking study was carried out in order to understand in detail the ability of these compounds to bind to COX-1 and COX-2. The results show that the liquorice dihydrostilbenes are preferred ligands for COX-2 rather than for COX-1, providing a good rational for the observed selectivity in ex vivo experiments. Therefore, they appear to be good candidates for employment in human therapy against inflammation-related pathological conditions.


Assuntos
Inibidores de Ciclo-Oxigenase 2/farmacologia , Glycyrrhiza/química , Estilbenos/farmacologia , Humanos , Técnicas In Vitro , Simulação de Acoplamento Molecular , Folhas de Planta/química , Relação Estrutura-Atividade
17.
Fitoterapia ; 85: 41-8, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-23313777

RESUMO

Pistachio (Pistacia vera L.) nuts are a rich source of phenolic compounds, known for their high antioxidant activity, and contained not only in the seeds but also in the skin. A pistachio cultivar of high quality is typical of Bronte, Sicily, Italy. The purpose of our study was to investigate the chemical composition and antioxidant properties of two polyphenol-rich extracts from skins (TP) and decorticated seeds (SP) of Bronte pistachios, and to verify the potential use of these extracts for topical photoprotective products. Chemical analysis showed that the TP and SP extracts contain high levels of phenolic compounds, but the TP extract is about ten times richer in phenols than the SP extract, being anthocyanins the most abundant compounds found in the TP extract. Both these extracts, and especially the TP extract, possess good radical scavenger/antioxidant properties, as shown in a series of in vitro assays carried out using homogenous and non-homogenous chemical environment. Furthermore both the TP extract and, although at a lower degree, the SP extract reduce, when topically applied, UV-B-induced skin erythema in human volunteers. These findings suggest that extracts from Bronte TP and SP could be successfully employed as photoprotective ingredients in topical cosmetic and pharmaceutical formulations.


Assuntos
Antioxidantes/análise , Eritema/tratamento farmacológico , Fitoterapia , Pistacia/química , Extratos Vegetais/uso terapêutico , Administração Cutânea , Adulto , Antioxidantes/uso terapêutico , Humanos , Sementes/química , Pele/efeitos da radiação , Tocoferóis , Raios Ultravioleta
18.
Fitoterapia ; 82(4): 546-56, 2011 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-21281704

RESUMO

Three extracts of different polarities of Glycyrrhiza glabra L. leaves were characterized and evaluated for their antioxidant, anti-genotoxic and anti-inflammatory activity. In total, thirty components have been identified and quantified through the use of liquid chromatography (LC) with ultraviolet-visible diode-array-detector (UV-vis-DAD) and mass spectrometry (MS). The main components belong to the polyphenols family, being flavonoid and dihydrostilbene derivatives. The extracts have been investigated for their antioxidant, anti-genotoxic and anti-inflammatory activities, which are fundamental requirements of efficacious chemo-preventive agents. The ethyl acetate extract proved to be the most valuable, evidently for the conspicuous presence of several polyphenols, namely flavonoids and dihydrostilbenes.


Assuntos
Anti-Inflamatórios/análise , Antioxidantes/análise , Glycyrrhiza/química , Extratos Vegetais/química , Acetatos , Compostos de Bifenilo , Colorimetria , Avaliação Pré-Clínica de Medicamentos , Medicamentos de Ervas Chinesas/química , Hexanos , Metanol , Molibdênio , Testes de Mutagenicidade , Picratos , Folhas de Planta/química , Compostos de Tungstênio
19.
J Agric Food Chem ; 58(14): 8430-6, 2010 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-20578719

RESUMO

Bergamot ( Citrus bergamia Risso) is a less commercialized Citrus fruit, mainly used for its essential oil extracted from the peel. Bergamot peel (BP) represents about 60% of the processed fruits and is regarded as primary waste. However, it contains good amounts of useful compounds, such as pectins and flavonoids. Many of the bioactivities of Citrus flavonoids appear to impact vascular endothelial cells. Herein, we report the protective effect of two flavonoid-rich extracts from BP (endowed with radical-scavenging properties and lacking genotoxic activity) against alterations in cell modifications induced by the pleiotropic inflammatory cytokine tumor necrosis factor-alpha (TNF-alpha) on human umbilical vein endothelial cells (HUVECs), as demonstrated by monitoring intracellular levels of malondialdehyde/4-hydroxynonenal, reduced and oxidized glutathione and superoxide dismutase activity, and the activation status of nuclear factor-kappaB (NF-kappaB). Thus, BP appears to be a potential source of natural antioxidant/anti-inflammatory phytocomplexes to be employed as ingredients of nutraceutical products or functional foods.


Assuntos
Citrus/química , Células Endoteliais/efeitos dos fármacos , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Fator de Necrose Tumoral alfa/farmacologia , Linhagem Celular , Células Endoteliais/metabolismo , Frutas/química , Humanos
20.
Biofactors ; 30(2): 129-38, 2007.
Artigo em Inglês | MEDLINE | ID: mdl-18356584

RESUMO

UV light is considered one of the major etiological factor in skin aging, cancer and also to systemic impairment such as immunosuppression. Increased production of reactive oxygen species (ROS) and oxidative stress condition are known to play a central role in initiating and driving the signalling events that lead to cellular response following UV irradiation. In the present study we have investigated the photoprotective activity of a standardized extract from red orange (ROE), obtained from three red orange varieties and containing as main active principles phenolic compounds (anthocyanins, flavanones and hydroxycinnamic acids) and ascorbic acid. The aim of this study was to evaluate the efficacy of ROE in modulating cellular responses to UVB in human keratinocytes (HaCaT). Our data indicate that ROE is potentially able to efficiently counteract UVB-induced response, and in particular some events associated to inflammation and apoptosis, such as NF-kB and AP-1 translocation and procaspase-3 cleavage. This activity is probably due to a block of cellular oxidative stress-related events. Thus we can propose ROE as a useful natural standardised extract in skin photoprotection with promising applications in the field of dermatology.


Assuntos
Citrus sinensis/química , Frutas/química , Queratinócitos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Raios Ultravioleta/efeitos adversos , Antocianinas/análise , Apoptose/efeitos dos fármacos , Ácido Ascórbico/análise , Western Blotting , Linhagem Celular Transformada , Ácidos Cumáricos/análise , Ensaio de Desvio de Mobilidade Eletroforética , Flavanonas/análise , Humanos , Inflamação/prevenção & controle , Queratinócitos/efeitos da radiação , Fitoterapia , Extratos Vegetais/química
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