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1.
Int J Mol Sci ; 24(7)2023 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-37047195

RESUMO

E. globulus leaves have been mainly exploited for essential oil recovery or for energy generation in industrial pulp mills, neglecting the abundance of valuable families of extractives, namely, triterpenic acids, that might open new ways for the integrated valorization of this biomass. Therefore, this study highlights the lipophilic characterization of E. globulus leaves before and after hydrodistillation, aiming at the integrated valorization of both essential oils and triterpenic acids. The lipophilic composition of E. globulus leaves after hydrodistillation is reported for the first time. Extracts were obtained by dichloromethane Soxhlet extraction and analyzed by gas chromatography-mass spectrometry. In addition, their cytotoxicity on different cell lines representative of the innate immune system, skin, liver, and intestine were evaluated. Triterpenic acids, such as betulonic, oleanolic, betulinic and ursolic acids, were found to be the main components of these lipophilic extracts, ranging from 30.63-37.14 g kg-1 of dry weight (dw), and representing 87.7-89.0% w/w of the total content of the identified compounds. In particular, ursolic acid was the major constituent of all extracts, representing 46.8-50.7% w/w of the total content of the identified compounds. Other constituents, such as fatty acids, long-chain aliphatic alcohols and ß-sitosterol were also found in smaller amounts in the studied extracts. This study also demonstrates that the hydrodistillation process does not affect the recovery of compounds of greatest interest, namely, triterpenic acids. Therefore, the results establish that this biomass residue can be considered as a promising source of value-added bioactive compounds, opening new strategies for upgrading pulp industry residues within an integrated biorefinery context.


Assuntos
Eucalyptus , Óleos Voláteis , Triterpenos , Eucalyptus/química , Ácidos Graxos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Álcoois , Triterpenos/farmacologia , Triterpenos/química
2.
Int J Mol Sci ; 23(19)2022 Sep 22.
Artigo em Inglês | MEDLINE | ID: mdl-36232458

RESUMO

The chemical composition, investigated by gas chromatography-mass spectrometry, and antibacterial activity of lipophilic extractives of three varieties of Opuntia ficus-indica roots from Algeria are reported in this paper for the first time. The results obtained revealed a total of 55 compounds, including fatty acids, sterols, monoglycerides and long chain aliphatic alcohols that were identified and quantified. ß-Sitosterol was found as the major compound of the roots of the three varieties. Furthermore, considerable amounts of essential fatty acids (ω3, ω6, and ω9) such as oleic, linoleic, and linolenic acids were also identified. The green variety was the richest among the three studied varieties. The antibacterial activity, evaluated with disc diffusion method, revealed that lipophilic extracts were effective mainly against Gram-positive Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA) (19~23 mm). Gram-negative strains mainly Pseudomonas aeruginosa gave an inhibition zone of 18 mm, which is considered high antibacterial activity. The minimal inhibitory concentrations of the tested bacteria revealed interesting values against the majority of bacteria tested: 75-100 µg mL-1 for Bacillus sp., 250-350 µg/mL for the two Staphylococcus strains, 550-600 µg mL-1 for E. coli, and 750-950 µg mL-1 obtained with Pseudomonas sp. This study allows us to conclude that the lipophilic fractions of cactus roots possess interesting phytochemicals such as steroids, some fatty acids and long chain alcohols that acted as antibiotic-like compounds countering pathogenic strains.


Assuntos
Staphylococcus aureus Resistente à Meticilina , Opuntia , Fitosteróis , Álcoois/farmacologia , Argélia , Antibacterianos/química , Antibacterianos/farmacologia , Escherichia coli , Ácidos Linolênicos/farmacologia , Testes de Sensibilidade Microbiana , Monoglicerídeos/farmacologia , Opuntia/química , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Fitosteróis/farmacologia , Extratos Vegetais/química
3.
Molecules ; 27(2)2022 Jan 13.
Artigo em Inglês | MEDLINE | ID: mdl-35056798

RESUMO

Zizyphus lotus L. is a perennial shrub particularly used in Algerian folk medicine, but little is known concerning the lipophilic compounds in the most frequently used parts, namely, root bark, pulp, leaves and seeds, which are associated with health benefits. In this vein, the lipophilic fractions of these morphological parts of Z. lotus from Morocco were studied by gas chromatography-mass spectrometry (GC-MS), and their antiproliferative and antimicrobial activities were evaluated. GC-MS analysis allowed the identification and quantification of 99 lipophilic compounds, including fatty acids, long-chain aliphatic alcohols, pentacyclic triterpenic compounds, sterols, monoglycerides, aromatic compounds and other minor components. Lipophilic extracts of pulp, leaves and seeds were revealed to be mainly composed of fatty acids, representing 54.3-88.6% of the total compounds detected. The leaves and seeds were particularly rich in unsaturated fatty acids, namely, (9Z,12Z)-octadeca-9,12-dienoic acid (2431 mg kg-1 of dry weight) and (9Z)-octadec-9-enoic acid (6255 mg kg-1 of dry weight). In contrast, root bark contained a high content of pentacyclic triterpenic compounds, particularly betulinic acid, accounting for 9838 mg kg-1 of dry weight. Root bark extract showed promising antiproliferative activity against a triple-negative breast cancer cell line, MDA-MB-231, with a half-maximal inhibitory concentration (IC50) = 4.23 ± 0.18 µg mL-1 of extract. Leaf extract displayed interesting antimicrobial activity against Escherichia coli, methicillin-sensitive Staphylococcus aureus and Staphylococcus epidermis, presenting minimum inhibitory concentration (MIC) values from 1024 to 2048 µg mL-1 of extract. Our results demonstrate that Zizyphus lotus L. is a source of promising bioactive components, which can be exploited as natural ingredients in pharmaceutical formulations.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ziziphus/química , Álcoois/análise , Antibacterianos/análise , Antineoplásicos Fitogênicos/análise , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Ácidos Graxos/análise , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Testes de Sensibilidade Microbiana , Monoglicerídeos/análise , Marrocos , Extratos Vegetais/análise , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus epidermidis/efeitos dos fármacos , Esteróis/análise , Triterpenos/análise
4.
Molecules ; 27(1)2021 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-35011475

RESUMO

The extraction of proanthocyanidins (PACs), despite being an important and limiting aspect of their industrial application, is still largely unexplored. Herein, the possibility of combining eutectic solvents (ESs) with microwave assisted extraction (MAE) in the extraction of PACs from grape pomace (GP) is explored, aiming to improve not only the extraction yield but also the mean degree of polymerization (mDP). The combination of choline chloride with lactic acid was shown to be the most effective combination for PACs extraction yield (135 mgPAC/gGP) and, despite the occurrence of some depolymerization, also enabled us to achieve the highest mDP (7.13). Additionally, the combination with MAE enabled the process to be completed in 3.56 min, resulting in a considerably reduced extraction time.


Assuntos
Fracionamento Químico/métodos , Micro-Ondas , Proantocianidinas/química , Proantocianidinas/isolamento & purificação , Solventes/química , Vitis/química , Algoritmos , Análise de Variância , Modelos Teóricos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Análise Espectral , Temperatura
5.
Int J Mol Sci ; 21(5)2020 Mar 06.
Artigo em Inglês | MEDLINE | ID: mdl-32155742

RESUMO

Acacia dealbata biomass, either from forest exploitation or from the management of invasive species, can be a strategic topic, namely as a source of high-value compounds. In this sense, the present study aimed at the detailed characterization of the lipophilic components of different morphological parts of A. dealbata and the evaluation of their cytotoxicity in cells representative of different mammals' tissues. The chemical composition of lipophilic extracts from A. dealbata bark, wood and leaves was evaluated using gas chromatography-mass spectrometry (GC-MS). Terpenic compounds (representing 50.2%-68.4% of the total bark and leaves extracts, respectively) and sterols (60.5% of the total wood extract) were the main components of these extracts. Other constituents, such as fatty acids, long-chain aliphatic alcohols, monoglycerides, and aromatic compounds were also detected in the studied extracts. All the extracts showed low or no cytotoxicity in the different cells tested, demonstrating their safety profile and highlighting their potential to be used in nutraceutical or pharmaceutical applications. This study is therefore an important contribution to the valorization of A. dealbata, demonstrating the potential of this species as a source of high value lipophilic compounds.


Assuntos
Acacia/química , Ácidos Graxos/isolamento & purificação , Ácidos Graxos/farmacologia , Neoplasias/patologia , Fitosteróis/farmacologia , Extratos Vegetais/farmacologia , Animais , Sobrevivência Celular , Humanos , Camundongos , Neoplasias/tratamento farmacológico , Folhas de Planta/química , Células Tumorais Cultivadas
6.
Mar Drugs ; 17(10)2019 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-31569367

RESUMO

Marine resources are considered as a very promising source of bioactive molecules, and macroalgae in particular have gained special attention, due to their structurally diverse composition. Particular interest has been devoted to the brown macroalga Bifurcaria bifurcata, due to their abundance in bioactive linear diterpenes. In this appraisal, a thorough review concerning the methodologies used in the extraction, fractionation, and identification of diterpenes from B. bifurcata is provided and discussed in detail. An exhaustive compilation of the mass spectra and nuclear magnetic resonance (NMR) data are also provided. The in vitro and in chemico assays already performed to assess different biological activities attributed to B. bifurcata diterpenes are also reviewed, emphasizing the use of isolated components, enriched fractions, or crude extracts. The associated major strengths and challenges for the exploitation of B. bifurcata diterpenes for high-value applications are critically discussed.


Assuntos
Diterpenos/farmacologia , Phaeophyceae/química , Extratos Vegetais/isolamento & purificação , Alga Marinha/química , Anti-Infecciosos/isolamento & purificação , Antioxidantes/isolamento & purificação , Diterpenos/isolamento & purificação , Química Verde/métodos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Estrutura Molecular
7.
Int J Mol Sci ; 20(4)2019 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-30795544

RESUMO

Worldwide, foodborne diseases are a growing public health problem. Among the infectious bacteria, non-typhoidal Salmonella enterica serovars (NTS) are the major cause of hospitalization and death, and the emergence and spread of their antibiotic-resistance is becoming a worldwide health issue. This, coupled with the restrictions of antibiotics use in agriculture and animal production, calls for alternative approaches to solve this problem. Plant-derived aqueous extracts compounds could provide novel straightforward approaches to control pathogenic bacteria. This review discusses the antimicrobial activity of aqueous plant extracts against Salmonella serovars, the possible mechanisms of action involved, which components/structures might be responsible for such activity, and the current challenges for the use of these extracts/components in Salmonella infection management and their application perspectives.


Assuntos
Antibacterianos/uso terapêutico , Extratos Vegetais/uso terapêutico , Infecções por Salmonella/tratamento farmacológico , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Humanos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Salmonella enterica/efeitos dos fármacos
8.
Int J Mol Sci ; 20(1)2019 Jan 08.
Artigo em Inglês | MEDLINE | ID: mdl-30625994

RESUMO

Three different high performance liquid chromatography columns were accessed for phenolic compounds (PC) separation in the hydrophilic fraction of extra virgin olive oil (EVOO). Two fully porous C18 bonded silica phases and one partially porous biphenyl column were used. Biphenyl column allowed for an increase of more than 30% in peak capacity (nc), higher selectivity (α) (1.045), and improved retention (k), with a reduction of 22.1% in the retention time. The higher resolution (Rs) was obtained by using the biphenyl column, with a fair separation of oleuropein aglycone isomers (OAI) and a good identification of caffeic acid (CA). Tyrosol (T), hydroxytyrosol (HT), and dihydroxyphenyl glycol (DHPG) were also well separated and identified. Moreover, the method using a biphenyl column was fully validated according to the requirements for new methods. For all parameters, the method applying the biphenyl column proved to be a reliable, accurate, and robust tool for separation, identification, and quantification of the main PCs in EVOOs.


Assuntos
Compostos de Bifenilo/química , Cromatografia Líquida de Alta Pressão/métodos , Azeite de Oliva/química , Fenóis/isolamento & purificação , Interações Hidrofóbicas e Hidrofílicas , Limite de Detecção , Espectrometria de Massas , Fenóis/química , Álcool Feniletílico/análogos & derivados , Álcool Feniletílico/análise
9.
Int J Mol Sci ; 20(17)2019 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-31480214

RESUMO

Substantial amounts of vine wastes are produced during vineyard management, and the chemical profiling of high-value lipophilic phytochemicals is becoming crucial in order to find a complementary route towards their integrated valorisation. The prospection of bioactive phytochemicals from unripe grape, vine shoot, vine cane, stalk and leaf dichloromethane extracts was carried out by gas chromatography-mass spectrometry (GC-MS), analysing samples from a mixture of four red Vitis vinifera L. varieties (Baga, Aragonez, Água Santa and Shiraz), collected at Bairrada Appellation, as a representative case study of typical multi-variety Portuguese vineyards. Vine wastes showed distinct amounts of lipophilic extract, ranging from 0.68% (vine canes) to 13.35% (vine leaves) at dry weight (dw). Thirty-three components were identified, including fatty acids and alcohols, sterols and triterpenoids accounting for amounts from 118.9 mg/100 g dw to 1512.0 mg/100 g dw. The integrated study revealed that unripe grape, stalk and leaf dichloromethane extracts stood out as possible sources of triterpenic compounds (103.2 to 653.5 mg/100 g dw), with lupeol, ursolic and oleanolic acids prevailing. Leaf extract is also reported as an undervalued source of α-tocopherol, as the major component detected in this matrix (300.5 mg/100 g dw). These exploratory results are a relevant contribution for the exploitation of undervalued vine residues as a source of health-promoting components with the potential to be used as supplements or nutraceutical ingredients.


Assuntos
Lipídeos/química , Compostos Fitoquímicos/farmacologia , Vitis/química , Resíduos/análise , Álcoois/análise , Ácidos Graxos/análise , Extratos Vegetais/química , Esteróis/análise , Triterpenos/análise
10.
Molecules ; 23(10)2018 Oct 20.
Artigo em Inglês | MEDLINE | ID: mdl-30347848

RESUMO

The long-term effect of thermal pasteurization (TP) and high-pressure processing (HPP) of orange juices stored under refrigeration, on the bioactive components and antioxidant activity, was compared. Total phenolic content (TPC), flavonoid, anthocyanin, and carotenoid contents, the individual content of major phenolic components, and the antioxidant activity, were evaluated in TP- and HPP-treated juices over a 36-day period. At day 0, no significant differences in TPC, and a decrease in carotenoid content after both treatments, were observed. TP caused a decrease of flavonoid and anthocyanin contents, while HPP increased flavonoid content. Three major phenolic components were identified: apigenin-6,8-di-C-glucoside, naringenin-7-O-rutinoside, and hesperetin-7-O-rutinoside, the latter increasing ca. 45% immediately after HPP. During storage, a decrease in TPC, and in the anthocyanin and carotenoid contents of both treated juices was observed, with higher anthocyanin and phenolic contents in HPP juices. A significant increase of hesperetin-7-O-rutinoside content was observed in HPP juice. Both treatments caused a decrease (26% and 13%, respectively) of antioxidant activity. Most of the kinetic profiles followed zero-order patterns, with HPP juices showing a considerably higher half-life than TP ones. These results clearly demonstrate the advantages of HPP for orange juice preservation allowing, also, their nutritional benefits to be enhanced by increasing the content of some bioactive components.


Assuntos
Antioxidantes/química , Citrus sinensis/química , Armazenamento de Alimentos/métodos , Pasteurização/métodos , Antocianinas/química , Apigenina/química , Bebidas/análise , Carotenoides/química , Sucos de Frutas e Vegetais/análise , Glucosídeos/química , Hesperidina/química , Polifenóis/química , Pressão
11.
Mar Drugs ; 15(11)2017 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-29104253

RESUMO

Macroalgae have been seen as an alternative source of molecules with promising bioactivities to use in the prevention and treatment of current lifestyle diseases. In this vein, the lipophilic fraction of short-term (three weeks) cultivated Bifurcaria bifurcata was characterized in detail by gas chromatography-mass spectrometry (GC-MS). B. bifurcata dichloromethane extract was composed mainly by diterpenes (1892.78 ± 133.97 mg kg-1 dry weight (DW)), followed by fatty acids, both saturated (550.35 ± 15.67 mg kg-1 DW) and unsaturated (397.06 ± 18.44 mg kg-1 DW). Considerable amounts of sterols, namely fucosterol (317.68 ± 26.11 mg kg-1 DW) were also found. In vitro tests demonstrated that the B. bifurcata lipophilic extract show antioxidant, anti-inflammatory and antibacterial activities (against both Gram-positive and Gram-negative bacteria), using low extract concentrations (in the order of µg mL-1). Enhancement of antibiotic activity of drug families of major clinical importance was observed by the use of B. bifurcata extract. This enhancement of antibiotic activity depends on the microbial strain and on the antibiotic. This work represents the first detailed phytochemical study of the lipophilic extract of B. bifurcata and is, therefore, an important contribution for the valorization of B. bifurcata macroalgae, with promising applications in functional foods, nutraceutical, cosmetic and biomedical fields.


Assuntos
Antibacterianos/farmacologia , Organismos Aquáticos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Extratos Vegetais/farmacologia , Alga Marinha , Animais , Antibacterianos/química , Lipídeos/química , Testes de Sensibilidade Microbiana , Extratos Vegetais/química
12.
Int J Mol Sci ; 18(1)2016 Dec 29.
Artigo em Inglês | MEDLINE | ID: mdl-28036090

RESUMO

Besides being traditionally used to relieve hepatobiliary disorders, Cynara cardunculus L. has evidenced anticancer potential on triple-negative breast cancer (TNBC). This study highlights the antiproliferative effects of lipophilic extracts from C. cardunculus L. var. altilis (DC) leaves and florets, and of their major compounds, namely cynaropicrin and taraxasteryl acetate, against MDA-MB-231 cells. Our results demonstrated that MDA-MB-231 cells were much less resistant to leaves extract (IC50 10.39 µg/mL) than to florets extract (IC50 315.22 µg/mL), during 48 h. Moreover, leaves extract and cynaropicrin (IC50 6.19 µg/mL) suppressed MDA-MB-231 cells colonies formation, via an anchorage-independent growth assay. Leaves extract and cynaropicrin were also assessed regarding their regulation on caspase-3 activity, by using a spectrophotometric assay, and expression levels of G2/mitosis checkpoint and Akt signaling pathway proteins, by Western blotting. Leaves extract increased caspase-3 activity, while cynaropicrin did not affect it. Additionally, they caused p21Waf1/Cip1 upregulation, as well as cyclin B1 and phospho(Tyr15)-CDK1 accumulation, which may be related to G2 cell cycle arrest. They also downregulated phospho(Ser473)-Akt, without changing total Akt1 level. Cynaropicrin probably contributed to leaves extract antiproliferative action. These promising insights suggest that cultivated cardoon leaves lipophilic extract and cynaropicrin may be considered toward a natural-based therapeutic approach on TNBC.


Assuntos
Antineoplásicos/farmacologia , Proliferação de Células/efeitos dos fármacos , Cynara/química , Lactonas/farmacologia , Extratos Vegetais/farmacologia , Sesquiterpenos/farmacologia , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Proteína Quinase CDC2 , Linhagem Celular Tumoral , Ciclina B1/genética , Ciclina B1/metabolismo , Inibidor de Quinase Dependente de Ciclina p21/genética , Inibidor de Quinase Dependente de Ciclina p21/metabolismo , Quinases Ciclina-Dependentes/genética , Quinases Ciclina-Dependentes/metabolismo , Humanos , Lactonas/química , Extratos Vegetais/química , Proteínas Proto-Oncogênicas c-akt/genética , Proteínas Proto-Oncogênicas c-akt/metabolismo , Sesquiterpenos/química
13.
Int J Mol Sci ; 18(1)2016 Dec 22.
Artigo em Inglês | MEDLINE | ID: mdl-28025494

RESUMO

Elderberry (Sambucus nigra L.) lipophilic and polar extract dietary supplementation effects were evaluated according to diabetes management indices, using an in vivo model. A research pipeline was constructed, that ranged from extract preparation, partial chemical characterization and toxicity evaluation, to examining the elderberry extract dietary supplementation effects on biofluid and tissues. Extracts toxicity was screened using an Aliivibrio fischeri bioluminescence model. A concentration of up to 60 mg/L was selected, and rat doses for oral supplementation were computed applying the interspecies correlation between A. fischeri and rats. Wistar type 2 diabetic rats, induced by streptozotocin (STZ), were fed a high-fat diet and supplemented for 4 weeks at doses of 190 and 350 mg/kg body weight/day of lipophilic and polar extract, respectively. As far as we know, lipophilic elderberry extract supplementation was assessed for the first time, while polar extract was administrated at higher doses and for a shorter period compared to previous studies, aiming to evaluate subacute supplementation effects. The polar extract modulated glucose metabolism by correcting hyperglycemia, while the lipophilic extract lowered insulin secretion. Both extracts lowered insulin resistance, without remarkable alterations to hematological indices, sera lipids and sera and tissular trace element homeostasis. In conclusion, elderberries are a potential source of bioactive compounds for formulations to be used as co-adjuvants in diabetes management.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Extratos Vegetais/uso terapêutico , Sambucus nigra/química , Animais , Glicemia/metabolismo , Diabetes Mellitus Experimental/etiologia , Dieta Hiperlipídica/efeitos adversos , Suplementos Nutricionais , Hipoglicemiantes/administração & dosagem , Hipoglicemiantes/química , Resistência à Insulina , Masculino , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Ratos , Ratos Wistar , Estreptozocina/toxicidade
14.
Int J Mol Sci ; 16(6): 14194-209, 2015 Jun 23.
Artigo em Inglês | MEDLINE | ID: mdl-26110390

RESUMO

The lipophilic composition of wild Arbutus unedo L. berries, collected from six locations in Penacova (center of Portugal), as well as some general chemical parameters, namely total soluble solids, pH, titratable acidity, total phenolic content and antioxidant activity was studied in detail to better understand its potential as a source of bioactive compounds. The chemical composition of the lipophilic extracts, focused on the fatty acids, triterpenoids, sterols, long chain aliphatic alcohols and tocopherols, was investigated by gas chromatography-mass spectrometry (GC-MS) analysis of the dichloromethane extracts. The lipophilic extractives of the ripe A. unedo berries ranged from 0.72% to 1.66% (w/w of dry weight), and consisted mainly of triterpenoids, fatty acids and sterols. Minor amounts of long chain aliphatic alcohols and tocopherols were also identified. Forty-one compounds were identified and among these, ursolic acid, lupeol, α-amyrin, linoleic and α-linolenic acids, and ß-sitosterol were highlighted as the major components. To the best of our knowledge the current research study provides the most detailed phytochemical repository for the lipophilic composition of A. unedo, and offers valuable information for future valuation and exploitation of these berries.


Assuntos
Ericaceae/química , Frutas/química , Cromatografia Gasosa-Espectrometria de Massas/métodos , Lipídeos/análise , Compostos Fitoquímicos/análise , Extratos Vegetais/análise , Fitosteróis/análise
15.
Biochim Biophys Acta ; 1832(1): 39-45, 2013 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-23069388

RESUMO

The transthyretin amyloidoses (ATTR) are devastating diseases characterized by progressive neuropathy and/or cardiomyopathy for which novel therapeutic strategies are needed. We have recently shown that curcumin (diferuloylmethane), the major bioactive polyphenol of turmeric, strongly suppresses TTR fibril formation in vitro, either by stabilization of TTR tetramer or by generating nonfibrillar small intermediates that are innocuous to cultured neuronal cells. In the present study, we aim to assess the effect of curcumin on TTR amyloidogenesis in vivo, using a well characterized mouse model for familial amyloidotic polyneuropathy (FAP). Mice were given 2% (w/w) dietary curcumin or control diet for a six week period. Curcumin supplementation resulted in micromolar steady-state levels in plasma as determined by LC/MS/MS. We show that curcumin binds selectively to the TTR thyroxine-binding sites of the tetramer over all the other plasma proteins. The effect on plasma TTR stability was determined by isoelectric focusing (IEF) and curcumin was found to significantly increase TTR tetramer resistance to dissociation. Most importantly, immunohistochemistry (IHC) analysis of mice tissues demonstrated that curcumin reduced TTR load in as much as 70% and lowered cytotoxicity associated with TTR aggregation by decreasing activation of death receptor Fas/CD95, endoplasmic reticulum (ER) chaperone BiP and 3-nitrotyrosine in tissues. Taken together, our results highlight the potential use of curcumin as a lead molecule for the prevention and treatment of TTR amyloidosis.


Assuntos
Neuropatias Amiloides Familiares/tratamento farmacológico , Neuropatias Amiloides Familiares/metabolismo , Amiloide/metabolismo , Curcumina/administração & dosagem , Pré-Albumina/metabolismo , Animais , Humanos , Camundongos , Camundongos Transgênicos
16.
Chem Bio Eng ; 1(1): 44-52, 2024 Feb 22.
Artigo em Inglês | MEDLINE | ID: mdl-38434799

RESUMO

Artemisinin, a drug used to treat malaria, can be chemically synthesized or extracted from Artemisia annua L. However, the extraction method for artemisinin from biomass needs to be more sustainable while maintaining or enhancing its bioactivity. This work investigates the use of aqueous solutions of salts and ionic liquids with hydrotropic properties as alternative solvents for artemisinin extraction from Artemisia annua L. Among the investigated solvents, aqueous solutions of cholinium salicylate and sodium salicylate were found to be the most promising. To optimize the extraction process, a response surface method was further applied, in which the extraction time, hydrotrope concentration, and temperature were optimized. The optimized conditions resulted in extraction yields of up to 6.50 and 6.44 mg·g-1, obtained with aqueous solutions of sodium salicylate and cholinium salicylate, respectively. The extracts obtained were tested for their antimalarial activity, showing a higher efficacy against the Plasmodium falciparum strain compared with pure (synthetic) artemisinin or extracts obtained with conventional organic solvents. Characterization of the extracts revealed the presence of artemisinin together with other compounds, such as artemitin, chrysosplenol D, arteannuin B, and arteannuin J. These compounds act synergistically with artemisinin and enhance the antimalarial activity of the obtained extracts. Given the growing concern about artemisinin resistance, the results here obtained pave the way for the development of sustainable and biobased antimalarial drugs.

17.
Heliyon ; 10(7): e28894, 2024 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-38623258

RESUMO

The bioaccessibility and bioavailability of phenolic compounds (PC) influence directly their role in disease prevention/control. Studies have evaluated this ability through complex plant and food matrices, which may reflect more a synergistic effect of the matrix than the ability of the PCs, hindering their individual exploitation in nutraceutical or pharmaceutical applications. In the present study ten pure PCs representing major classes were evaluated for their bioaccessibility and intestinal absorption in an in vitro simulated gastrointestinal digestion (SGD). This is the first study concerning the bioaccessibility evaluation of pure phloretin, phloroglucinol, naringin, naringenin and daidzein, while no in vitro SGD has been performed before for the other compounds considered here. PCs were analyzed through ultra-high-performance liquid chromatography coupled with diode-array detection and tandem mass spectrometry (UHPLC-DAD-MSn). Most of the compounds remained present along the gastrointestinal tract, and the bioaccessibility was in general higher than 50%, except for quercetin, epigallocatechin gallate, and ellagic acid. All compounds were highly absorbed in the intestine, with phloretin showing the lowest percentage at about 82%. The study findings provide new knowledge on the bioaccessibility and intestinal absorption of different PCs classes.

18.
Food Chem X ; 16: 100468, 2022 Dec 30.
Artigo em Inglês | MEDLINE | ID: mdl-36281231

RESUMO

The accumulation of advanced glycation end-products (AGEs) in the body is implicated in numerous diseases, being methylglyoxal (MGO) one of the main precursors. One of the strategies to reduce AGEs accumulation might be acting in an early stage of glycation by trapping MGO. Thus, this work aimed to evaluate, for the first time, the potential of elderberries polyphenols to trap MGO, access the formation of MGO adducts, and evaluate the cytoprotection effect in HepG2 and Caco-2 cells. The results demonstrated that monoglycosylated anthocyanins (cyanidin-3-glucoside and cyanidin-3-sambubioside) are very efficient in trapping MGO, forming mono- and di-adducts. Quercetin-3-glucoside and quercetin-3-rutinoside reacted slowly, while diglycosylated anthocyanins did not react. The trapping of MGO by elderberry monoglycosylated anthocyanins significantly decreased the MGO cytotoxicity in HepG2 cells (∼70 % of cell viability), while the effect in Caco-2 cells was lower (∼50 %). Thus, elderberry phenolics present antiglycation potential by trapping MGO.

19.
Foods ; 11(1)2021 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-35010230

RESUMO

Improvement of dietary and ecological biodiversity, namely by exploring autochthonous varieties, is a key point to the construction of a more sustainable food system and planetary health. However, the environmental sustainability continues to face huge challenges, reflecting the importance of achieving a better understanding about the functional role of biodiversity in ecosystems. Thus, the main objective of this research is to contribute to the sustainable valorization of Sambucus nigra L. berries through a comprehensive approach to evaluate the effects of elderberry's cultivar, harvest year, and plantation field on the physicochemical berry composition. Moreover, the nutritional value of elderberry juice and respective dried pomace was determined. This complementary information is of huge utility for the rational and, as much as possible, integral use of elderberries. The harvest year, followed by field and the interaction of harvest × field, accounted for the highest impact on the berry's physicochemical parameters, indicating the importance of the combined impact of the macro- and mesoclimate conditions on plant metabolism. Elderberry juice and dried pomace are a good source of carbohydrates (ca. 12 and 82%, respectively) and have low amounts of fat (≤2.5%), making them low-energy foods. Dried pomace may also represent a potential alternative source of vegetal protein (ca. 6%).

20.
Foods ; 10(5)2021 Apr 21.
Artigo em Inglês | MEDLINE | ID: mdl-33919394

RESUMO

Macroalgae of the genus Ulva have long been used as human food. Local environmental conditions, among other factors, can have an impact on their nutrient and phytochemical composition, as well as on the value of the seaweed for food and non-food applications. This study is the first to initiate a comparison between commercial Ulva spp. from different European origins, France (FR, wild-harvested Ulva spp.), and Portugal (PT, farm-raised Ulva rigida), in terms of proximate composition, esterified fatty acids (FA), and polar lipids. The ash content was higher in PT samples, while FR samples had higher levels of proteins, lipids, and carbohydrates and other compounds. The profile of esterified FA, as well as FA-containing polar lipids at the class and species levels were also significantly different. The FR samples showed about three-fold higher amount of n-3 polyunsaturated FA, while PT samples showed two-fold higher content of monounsaturated FA. Quantification of glycolipids and phospholipids revealed, respectively, two-fold and three-fold higher levels in PT samples. Despite the differences found, the polar lipids identified in both batches included some lipid species with recognized bioactivity, valuing Ulva biomass with functional properties, increasing their added value, and promoting new applications, namely in nutraceutical and food markets.

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