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1.
J Sci Food Agric ; 2024 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-38779961

RESUMO

BACKGROUND: Green rooibos (Aspalathus linearis (Burm.f.) R.Dahlgren) herbal tea is popular due to its health-promoting properties. Information on its characteristic sensory profile is scarce and sensory tools to define product variation are needed. The storage conditions and time during its shelf-life are hypothesized to affect the product quality. RESULTS: Production batches from two producers spanning 5 years (n = 57) were analyzed using descriptive sensory analysis. Primary attributes (>30 median intensity; 100% occurrence frequency) included 'hay/dried grass', 'cooked oats', 'tobacco', 'honey' and 'caramel' aromas, and astringent mouthfeel. 'Cooked vegetables', 'green grass', 'stewed fruit', 'rooibos-woody', 'marmalade' and 'cardboard' aromas, sweet taste and bitter taste were secondary attributes (10-20 median intensity; 100% occurrence frequency). The same flavor attributes were present, except for sweet-associated and fruity notes. A sensory lexicon and sensory wheels for aroma and palate attributes were constructed from the data. The shelf-life stability of green rooibos was evaluated in moisture-impermeable (pouches) and moisture-permeable (sachets) packaging at 25 and 40 °C at 60% relative humidity over 24 weeks. Green rooibos samples stored in pouches at 4 °C were also evaluated. Storage in sachets led to moisture uptake (~10 g (100 g)-1 dry basis) and an increase in water activity (>0.6), causing degradation of chlorophyll and dihydrochalcones. Changes in color and sensory profile (decreased vegetal, cereal and cardboard aromas and increased sweet-associated and fruity aromas) were evident and more pronounced at the higher storage temperature. CONCLUSIONS: Storage at ≤25 °C in moisture-impermeable packaging material is recommended for green rooibos herbal tea. © 2024 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

2.
Int J Mol Sci ; 24(4)2023 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-36835279

RESUMO

Previously, we reported that a crude polyphenol-enriched fraction of Cyclopia intermedia (CPEF), a plant consumed as the herbal tea, commonly known as honeybush, reduced lipid content in 3T3-L1 adipocytes and inhibited body weight gain in obese, diabetic female leptin receptor-deficient (db/db) mice. In the current study, the mechanisms underlying decreased body weight gain in db/db mice were further elucidated using western blot analysis and in silico approaches. CPEF induced uncoupling protein 1 (UCP1, 3.4-fold, p < 0.05) and peroxisome proliferator-activated receptor alpha (PPARα, 2.6-fold, p < 0.05) expression in brown adipose tissue. In the liver, CPEF induced PPARα expression (2.2-fold, p < 0.05), which was accompanied by a 31.9% decrease in fat droplets in Hematoxylin and Eosin (H&E)-stained liver sections (p < 0.001). Molecular docking analysis revealed that the CPEF compounds, hesperidin and neoponcirin, had the highest binding affinities for UCP1 and PPARα, respectively. This was validated with stabilising intermolecular interactions within the active sites of UCP1 and PPARα when complexed with these compounds. This study suggests that CPEF may exert its anti-obesity effects by promoting thermogenesis and fatty acid oxidation via inducing UCP1 and PPARα expression, and that hesperidin and neoponcirin may be responsible for these effects. Findings from this study could pave the way for designing target-specific anti-obesity therapeutics from C. intermedia.


Assuntos
Fabaceae , Obesidade , Animais , Camundongos , Hesperidina/farmacologia , Hesperidina/uso terapêutico , Camundongos Obesos , Simulação de Acoplamento Molecular , Obesidade/terapia , PPAR alfa/metabolismo , Proteína Desacopladora 1/metabolismo
3.
J Sci Food Agric ; 103(12): 5697-5708, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37078979

RESUMO

BACKGROUND: The shelf-life of a functional herbal tea-based beverage is important not only for consumer acceptability, but also for the retention of bioactive compounds. The present study aimed to clarify the role of common iced tea beverage ingredients (citric and ascorbic acids) on the shelf-life stability of an herbal tea-based beverage. A hot water extract of green Cyclopia subternata, also used as honeybush tea, was selected as the main ingredient because it provides different types of phenolic compounds associated with bioactive properties (i.e. xanthones, benzophenones, flavanones, flavones and dihydrochalcones). RESULTS: The model solutions were stored for 180 and 90 days at 25 and 40 °C, respectively. Changes in their volatile profiles and color were also quantified as they contribute to product quality. 3',5'-Di-ß-d-glucopyranosyl-3-hydroxyphloretin (HPDG; dihydrochalcone) and, to a lesser extent, mangiferin (xanthone), were the most labile compounds. Both compounds were thus identified as critical quality indicators to determine shelf-life. The stability-enhancing activity of the acids depended on the compound; ascorbic acid and citric acid enhanced the stability of HPDG and mangiferin, respectively. However, when considering all the major phenolic compounds, the base solution without acids was the most stable. This was also observed for the color and major volatile aroma-active compounds [α-terpineol, (E)-ß-damascenone, 1-p-menthen-9-al and trans-ocimenol]. CONCLUSION: The addition of acids, added for stability and taste in ready-to-drink iced tea beverages, could thus have unwanted consequences in that they could accelerate compositional changes and shorten the shelf-life of polyphenol-rich herbal tea beverages. © 2023 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.


Assuntos
Fabaceae , Chás de Ervas , Xantonas , Chás de Ervas/análise , Fabaceae/química , Bebidas/análise , Fenóis/química , Ácido Ascórbico/química , Chá , Extratos Vegetais/química
4.
Crit Rev Food Sci Nutr ; : 1-28, 2022 Jul 14.
Artigo em Inglês | MEDLINE | ID: mdl-35833472

RESUMO

Phenolic compounds are known to degrade and/or undergo changes during food production and storage. Reaction kinetic modeling is generally used to define kinetic parameters of a food system and predict changes during thermal processing and storage. Data for phenolic acids and flavonoids, such as anthocyanins and flavan-3-ols, have been reviewed in detail, but the flavonoid sub-classes, dihydrochalcones and flavanones, have been mostly neglected. Other neglected phenolic classes are xanthones and benzophenones. The stability of these types of compounds is important as they are present in fruits and exposed to heat when processed into juice and jam. Other sources of the compounds are herbal teas, which are also subjected to thermal processing, either during the primary processing of the plant material, or the production of extracts for use as food ingredients. The theoretical background is given to understand the review of literature on these classes/sub-classes. Results of research on kinetic modeling are discussed in detail, while research on compound stability without the application of reaction kinetic modeling is briefly mentioned to provide context. The studies discussed included those focusing on heating during the processing and storage of model solutions, liquid foods, plant material, dried extracts, and extracts formulated with other food ingredients.

5.
Planta Med ; 88(12): 1078-1091, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34662924

RESUMO

Postprandial hyperglycemia is treated with the oral antidiabetic drug acarbose, an intestinal α-glucosidase inhibitor. Side effects of acarbose motivated a growing number of screening studies to identify novel α-glucosidase inhibitors derived from plant extracts and other natural sources. As "gold standard", acarbose is frequently included as the reference standard to assess the potency of these candidate α-glucosidase inhibitors, with many outperforming acarbose by several orders of magnitude. The results are subsequently used to identify suitable compounds/products with strong potential for in vivo efficacy. However, most α-glucosidase inhibitor screening studies use enzyme preparations obtained from nonmammalian sources (typically Saccharomyces cerevisiae), despite strong evidence that inhibition data obtained using nonmammalian α-glucosidase may hold limited value in terms of identifying α-glucosidase inhibitors with actual in vivo hypoglycemic potential. The aim was to critically discuss the screening of novel α-glucosidase inhibitors from plant sources, emphasizing inconsistencies and pitfalls, specifically where acarbose was included as the reference standard. An assessment of the available literature emphasized the cruciality of stating the biological source of α-glucosidase in such screening studies to allow for unambiguous and rational interpretation of the data. The review also highlights the lack of a universally adopted screening assay for novel α-glucosidase inhibitors and the commercial availability of a standardized preparation of mammalian α-glucosidase.


Assuntos
Acarbose , Inibidores de Glicosídeo Hidrolases , Acarbose/farmacologia , Acarbose/uso terapêutico , Animais , Inibidores Enzimáticos/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Mamíferos , Extratos Vegetais/farmacologia , Padrões de Referência , alfa-Glucosidases
6.
J Sci Food Agric ; 102(3): 1047-1055, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-34312869

RESUMO

BACKGROUND: Ultrafiltration of green honeybush (Cyclopia genistoides) extract results in a by-product (retentate). Application of further separation processes for recovery of polyphenols would entail creation of additional waste. Repurposing the retentate as a food flavour ingredient provides an alternative valorization approach. RESULTS: The retentate, suspended in water (270 g L-1 ), was heat-treated at 80 °C for 2, 4, 8 and 16 h, and at 90 °C for 2, 4, 6 and 8 h to change its sensory profile. The heat-treated retentate, diluted to beverage strength (2.15 g L-1 ), had prominent 'grape/Muscat-like' and 'marmalade/citrus' aroma and flavour notes. Overall, heating for ≤ 4 h increased the intensities of positive flavour and aroma notes, while reducing those of 'green/grass', 'hay' and bitterness, whereafter further heating only had a slight effect on the aroma profile at 80 °C (P < 0.05), but not at 90 °C (P ≥ 0.05). The heat treatments, 80 °C/4 h and 90 °C/4 h, were subsequently applied to different batches of retentate (n = 10) to accommodate the effect of natural product variation. Heating at 90 °C produced higher intensities of positive aroma attributes (P < 0.05), but was more detrimental to the phenolic stability, compared to 80 °C. CONCLUSION: After heat treatment, the phenolic content of C. genistoides retentate, reconstituted to beverage strength, still fell within the range of a typical 'fermented' (oxidized) honeybush leaf tea infusion. The change in phenolic composition will not diminish the benefit of an improved sensory profile for the retentate by-product through heating. © 2021 Society of Chemical Industry.


Assuntos
Cyclopia (Planta)/química , Aromatizantes/isolamento & purificação , Manipulação de Alimentos/métodos , Extratos Vegetais/isolamento & purificação , Bebidas/análise , Cyclopia (Planta)/metabolismo , Aromatizantes/química , Aromatizantes/metabolismo , Manipulação de Alimentos/instrumentação , Temperatura Alta , Odorantes , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Polifenóis/química , Polifenóis/isolamento & purificação , Paladar , Ultrafiltração
7.
Nutr Cancer ; 73(10): 2050-2064, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32930006

RESUMO

Differential anti-proliferative and pro-apoptotic effects of aqueous extracts of green rooibos (Rg; Aspalathus linearis) and green tea (GT; Camellia sinensis) and an aspalathin-enriched extract of green rooibos (GRE), were investigated in primary rat hepatocytes (PH) and human liver (HepG2) and colon (HT-29) cancer cells. Rooibos flavonoids, aspalathin and luteolin, and the green tea flavanol, epigallocatechin gallate (EGCG), were included to assess their contribution relative to their extract concentrations. GRE was the most effective in reducing cell growth parameters which was associated with a high total polyphenol content and high ferric reducing potential. Differential cell responses were noticed with HepG2 cells more sensitive than PH toward the induction of apoptosis by GRE. Luteolin induced apoptosis in PH and HepG2 cells while aspalathin lacked any effect. EGCG induced apoptosis in HepG2 cells while PH were resistant. HT-29 cells were resistant to apoptosis induction by the tea and pure flavonoids. Differences existed in the individual effects of the major rooibos and GT flavonoids against cell growth parameters compared to their equivalent concentrations in the extract mixtures. Diversity of the flavonoid constituents, physicochemical properties and cellular redox status governing cell survival are likely to explain the differential cell responses.


Assuntos
Aspalathus , Neoplasias do Colo , Animais , Neoplasias do Colo/tratamento farmacológico , Flavonoides/farmacologia , Hepatócitos , Humanos , Fígado , Extratos Vegetais/farmacologia , Ratos , Chá
8.
Planta Med ; 87(4): 325-335, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33142345

RESUMO

Fractions of an ultrafiltered Cyclopia genistoides extract, respectively enriched in xanthones and benzophenones, were previously shown to inhibit mammalian α-glucosidase in vitro. The present study investigated ex vivo intestinal transport of these fractions, using excised porcine jejunal tissue, to determine whether the gut could be a predominant in vivo site of action. The major bioactive compounds, the xanthones (mangiferin, isomangiferin) and benzophenones (3-ß-D-glucopyranosyliriflophenone, 3-ß-D-glucopyranosyl-4-O-ß-D-glucopyranosyliriflophenone) exhibited poor permeation in the absorptive direction with a relatively high efflux ratio (efflux ratio > 1). The efflux ratio of 3-ß-D-glucopyranosyl-4-O-ß-D-glucopyranosyliriflophenone (3.05) was similar to rhodamine 123 (2.99), a known substrate of intestinal P-glycoprotein 1 efflux transporters. Low epithelial membrane transport rates, coupled with efflux mechanisms, would effectively concentrate these bioactive compounds at the target site (gut lumen). Storage stability testing and moisture sorption assays of the xanthone-enriched fraction, benzophenone-enriched fraction, and ultrafiltered Cyclopia genistoides extract were performed to determine their susceptibility to physical and chemical degradation during storage. Hygroscopicity of the powders, indicated by moisture uptake, decreased in the order: benzophenone-enriched fraction (22.7%) > ultrafiltered Cyclopia genistoides extract (14.0%) > xanthone-enriched fraction (10.7%). 3-ß-D-Glucopyranosylmaclurin, a minor benzophenone, was the least stable of the compounds, degrading faster in the benzophenone-enriched fraction than in ultrafiltered Cyclopia genistoides extract, suggesting that the ultrafiltered extract matrix may provide a degree of protection against chemical degradation. Compound degradation during 12 wk of storage at 40 °C in moisture-impermeable containers was best explained by first order reaction kinetics.


Assuntos
Fabaceae , Xantonas , Animais , Benzofenonas , Holoprosencefalia , Permeabilidade , Extratos Vegetais , Suínos
9.
Appetite ; 167: 105606, 2021 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-34298013

RESUMO

Globally, the role of food labels in reducing non-communicable disease remains a point of debate. A particular area of contention is the use of health claims, an approach currently under consideration in South Africa - a developing country with vast socio-economic disparity. In the present study, in-depth interviews were conducted with 49 diverse stakeholders, including consumers and professionals from the food industry and other occupations, who shared their views about the use of health claims in a developing country context. The qualitative approach and inclusion of multiple perspectives that had not been motivated by a single stakeholder group added a novel view. Themes identified based on inductive analysis included: (i) practical barriers to label use; (ii) contextual and personal variables influencing engagement with label information; (iii) messaging preferences (for positively worded claims, compared to more cautionary statements); (iv) stakeholder complexities - mainly related to responsibility and trust; and (v) ambassadors to change. Findings indicate that there are persistent barriers to label use, such as challenges related to literacy and legibility. Furthermore, the socio-economic circumstances prevalent in South Africa drive large volumes of food sales in informal markets where labels are often not present. Unresolved questions about the substantiation and enforcement of health claims, combined with no solution being apparent for reaching consumers in the informal market, would limit the benefits that could be associated with the implementation of health claims at this point in time.


Assuntos
Indústria Alimentícia , Rotulagem de Alimentos , Humanos , Pesquisa Qualitativa , África do Sul , Confiança
10.
Phytochem Anal ; 32(3): 347-361, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-32803806

RESUMO

INTRODUCTION: The minor phenolic constituents of Cyclopia pubescens Eckl. & Zeyh. are unknown and one dimensional (1D) liquid chromatography (LC) is unable to provide sufficient separation. METHODOLOGY: A two-dimensional (2D) LC method incorporating normal-phasehigh performance countercurrent chromatography (NP-HPCCC) in the first dimension (1 D) and reversed-phase ultra-high-performance liquid chromatography (RP-UHPLC) as the second dimension (2 D) was developed. The analytical HPCCC method was subsequently scaled up to semi-preparative mode and fractions pooled based on phenolic sub-groups. The phenolic compounds in selected fractions were subsequently isolated using RP-HPLC on a C18 column. Isolated compounds were identified by nuclear magnetic resonance (NMR) spectroscopy. The absolute configurations of compounds were determined by optical rotation and electronic circular dichroism spectra. Sugars were identified by gas chromatography-mass spectrometry (GC-MS) analysis. RESULTS: The comprehensive off-line 2D CCC × LC method gave a good spread of the phenolic compounds. Orthogonality calculated using both the convex hull and conditional entropy methods were 81%. High-resolution mass spectrometric fragmentation spectra obtained from a quadrupole-time-of-flight instrument and ultraviolet-visible (UV-vis) spectral data were used to (tentatively) identify 32 phenolic compounds from the analytical CCC fractions. Of the seven isolated compounds, (2S)-5-O-[α-l-rhamnopyranosyl-(1 → 2)-ß-d-glucopyranosyl]eriodictyol (3) and (2S)-5-O-[α-l-rhamnopyranosyl-(1 → 2)-ß-d-glucopyranosyl]-5,7,3',4'-tetrahydroxyflavan (4) were newly identified in all plants. The other isolated compounds were identified as (2S)-5-O-[α-l-rhamnopyranosyl-(1 → 2)-ß-d-glucopyranosyl]naringenin (1), R-neo-eriocitrin (2), 3-O-α-l-arabinopyranosyl-3,4-dihydroxybenzoic acid (5), 4-O-ß-d-glucopyranosyl-Z-4-hydroxycinnamic acid (6) and 4-(4'-O-ß-d-glucopyranosyl-4'-hydroxy-3'-methoxyphenyl)-2-butanone (7). CONCLUSIONS: Among the 32 compounds (tentatively) identified, only six were previously identified in Cyclopia pubescens using 1D LC. Most of the isolated compounds were also identified for the first time in Cyclopia spp., improving the knowledge of the minor phenolic compounds of this genus.


Assuntos
Cromatografia de Fase Reversa , Distribuição Contracorrente , Cromatografia Líquida , Cromatografia Gasosa-Espectrometria de Massas , Holoprosencefalia
11.
Int J Mol Sci ; 23(1)2021 Dec 29.
Artigo em Inglês | MEDLINE | ID: mdl-35008779

RESUMO

In the pursuit of bioactive phytochemicals as a therapeutic strategy to manage metabolic risk factors for type 2 diabetes (T2D), aspalathin, C-glucosyl dihydrochalcone from rooibos (Aspalathus linearis), has received much attention, along with its C-glucosyl flavone derivatives and phlorizin, the apple O-glucosyl dihydrochalcone well-known for its antidiabetic properties. We provided context for dietary exposure by highlighting dietary sources, compound stability during processing, bioavailability and microbial biotransformation. The review covered the role of these compounds in attenuating insulin resistance and enhancing glucose metabolism, alleviating gut dysbiosis and associated oxidative stress and inflammation, and hyperuricemia associated with T2D, focusing largely on the literature of the past 5 years. A key focus of this review was on emerging targets in the management of T2D, as highlighted in the recent literature, including enhancing of the insulin receptor and insulin receptor substrate 1 signaling via protein tyrosine phosphatase inhibition, increasing glycolysis with suppression of gluconeogenesis by sirtuin modulation, and reducing renal glucose reabsorption via sodium-glucose co-transporter 2. We conclude that biotransformation in the gut is most likely responsible for enhancing therapeutic effects observed for the C-glycosyl parent compounds, including aspalathin, and that these compounds and their derivatives have the potential to regulate multiple factors associated with the development and progression of T2D.


Assuntos
Chalconas/uso terapêutico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Compostos Fitoquímicos/uso terapêutico , Animais , Disponibilidade Biológica , Biotransformação , Chalconas/química , Chalconas/farmacologia , Microbioma Gastrointestinal/efeitos dos fármacos , Humanos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Resultado do Tratamento
12.
Molecules ; 26(17)2021 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-34500693

RESUMO

Green rooibos extract (GRE), shown to improve hyperglycemia and HDL/LDL blood cholesterol, has potential as a nutraceutical beverage ingredient. The main bioactive compound of the extract is aspalathin, a C-glucosyl dihydrochalcone. The study aimed to determine the effect of common iced tea ingredients (citric acid, ascorbic acid, and xylitol) on the stability of GRE, microencapsulated with inulin for production of a powdered beverage. The stability of the powder mixtures stored in semi-permeable (5 months) and impermeable (12 months) single-serve packaging at 30 °C and 40 °C/65% relative humidity was assessed. More pronounced clumping and darkening of the powders, in combination with higher first order reaction rate constants for dihydrochalcone degradation, indicated the negative effect of higher storage temperature and an increase in moisture content when stored in the semi-permeable packaging. These changes were further increased by the addition of crystalline ingredients, especially citric acid monohydrate. The sensory profile of the powders (reconstituted to beverage strength iced tea solutions) changed with storage from a predominant green-vegetal aroma to a fruity-sweet aroma, especially when stored at 40 °C/65% RH in the semi-permeable packaging. The change in the sensory profile of the powder mixtures could be attributed to a decrease in volatile compounds such as 2-hexenal, (Z)-2-heptenal, (E)-2-octenal, (E)-2-nonenal, (E,Z)-2,6-nonadienal and (E)-2-decenal associated with "green-like" aromas, rather than an increase in fruity and sweet aroma-impact compounds. Green rooibos extract powders would require storage at temperatures ≤ 30 °C and protection against moisture uptake to be chemically and physically shelf-stable and maintain their sensory profiles.


Assuntos
Aspalathus/química , Bebidas/análise , Chá/química , Compostos Orgânicos Voláteis/química
13.
Pharmacol Res ; 158: 104867, 2020 08.
Artigo em Inglês | MEDLINE | ID: mdl-32407953

RESUMO

Isoorientin is a natural C-glucosyl flavone that is generating a lot of interest due to its multiple pharmacological activities. Increasing experimental data have shown that the robust antioxidant and anti-inflammatory properties of isoorientin remain important in ameliorating a number of metabolic complications. In fact, plants rich in isoorientin have demonstrated strong ameliorative properties against complications such as hyperglycemia, hyperlipidemia, and insulin resistance. However, while such evidence is accumulating, it has not been reviewed to better inform on the therapeutic potential of this flavone in improving human health. This review examines and extrapolates available literature on the potential beneficial or detrimental effects associated with the use of isoorientin in mitigating metabolic diseases, with a specific focus on diabetes, obesity, and insulin resistance, including associated complications. The discussion includes effective doses in various experimental settings and proposed molecular mechanisms by which isoorientin may exert its therapeutic effects. In addition, the protective effects of extracts of a number of isoorientin-rich plants against metabolic complications will be highlighted.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Antioxidantes/uso terapêutico , Luteolina/uso terapêutico , Doenças Metabólicas/tratamento farmacológico , Animais , Diabetes Mellitus/dietoterapia , Diabetes Mellitus/tratamento farmacológico , Dieta , Humanos , Resistência à Insulina , Doenças Metabólicas/dietoterapia , Estresse Oxidativo/efeitos dos fármacos
14.
Bioorg Chem ; 101: 103966, 2020 08.
Artigo em Inglês | MEDLINE | ID: mdl-32506016

RESUMO

A phytochemical survey to obtain bioactive natural products from Ajuga pantantha afforded five new neo-clerodane diterpenoids (1-5). The structures were established by analysis of their NMR spectroscopic data, and electronic circular dichroism calculations were applied to define their absolute configurations. Compounds 2 and 5 were found to have the property of inhibiting NO production (IC50 values < 40 µM). Molecular docking and Western blotting were used to study the mechanism of anti-inflammatory action. Furthermore, compound 5 with the highest activity was tested for its in vivo anti-inflammatory effects using a zebrafish model.


Assuntos
Ajuga/química , Anti-Inflamatórios/química , Diterpenos Clerodânicos/uso terapêutico , Simulação de Acoplamento Molecular/métodos , Animais , Modelos Animais de Doenças , Diterpenos Clerodânicos/farmacologia , Estrutura Molecular , Compostos Fitoquímicos , Peixe-Zebra
15.
Planta Med ; 85(1): 6-13, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30016826

RESUMO

Modulation of the expression of hepatic and renal genes encoding xenobiotic metabolizing enzymes by an aspalathin-enriched green rooibos (Aspalathus linearis) extract (GRE) was investigated in the liver and kidneys of F344 rats following dietary exposure of 28 d, as well as selected xenobiotic metabolizing genes in rat primary hepatocytes. In the liver, GRE upregulated genes (p < 0.05) encoding aldehyde dehydrogenase, glucose phosphate isomerase, and cytochrome P450 while 17ß-hydroxysteroid dehydrogenase 2 (Hsd17ß2) was downregulated. In primary hepatocytes, GRE lacked any effect, while aspalathin downregulated Hsd17ß2, mimicking the effect of GRE in vivo, and upregulated catechol-O-methyl transferase and marginally (p < 0.1) cytochrome P450 2e1. In the kidneys, GRE upregulated (p < 0.05) genes encoding the phase II xenobiotic metabolism enzymes, glutathione-S-transferase mµ and microsomal glutathione-S-transferase, while downregulating genes encoding the ATP binding cassette transporter, cytochrome P450, gamma glutamyltransferase 1, and N-acetyltransferase 1. Differential modulation of the expression of xenobiotic metabolizing genes in vivo and in vitro by GRE is dose-related, duration of exposure, the tissue type, and interactions between specific polyphenol and/or combinations thereof. Aspalathin is likely to be responsible for the downregulation of estradiol and testosterone catabolism by GRE in the liver. The differential gene expression by GRE in the liver and kidneys could, depending on the duration exposure and dose utilized, determine the safe use of such an extract in humans for specific health and/or disease outcomes.


Assuntos
Aspalathus/química , Chalconas/farmacologia , Regulação Enzimológica da Expressão Gênica/efeitos dos fármacos , Rim/enzimologia , Fígado/enzimologia , Extratos Vegetais/farmacologia , Animais , Células Cultivadas , Masculino , Extratos Vegetais/isolamento & purificação , Ratos , Xenobióticos/metabolismo
16.
Int J Mol Sci ; 20(3)2019 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-30717198

RESUMO

We previously demonstrated that an aspalathin-enriched green rooibos extract (GRE) reversed palmitate-induced insulin resistance in C2C12 skeletal muscle and 3T3-L1 fat cells by modulating key effectors of insulin signalling such as phosphatidylinositol-4,5-bisphosphate 3-kinase/protein kinase B (PI3K/AKT) and AMP-activated protein kinase (AMPK). However, the effect of GRE on hepatic insulin resistance is unknown. The effects of GRE on lipid-induced hepatic insulin resistance using palmitate-exposed C3A liver cells and obese insulin resistant (OBIR) rats were explored. GRE attenuated the palmitate-induced impairment of glucose and lipid metabolism in treated C3A cells and improved insulin sensitivity in OBIR rats. Mechanistically, GRE treatment significantly increased PI3K/AKT and AMPK phosphorylation while concurrently enhancing glucose transporter 2 expression. These findings were further supported by marked stimulation of genes involved in glucose metabolism, such as insulin receptor (Insr) and insulin receptor substrate 1 and 2 (Irs1 and Irs2), as well as those involved in lipid metabolism, including Forkhead box protein O1 (FOXO1) and carnitine palmitoyl transferase 1 (CPT1) following GRE treatment. GRE showed a strong potential to ameliorate hepatic insulin resistance by improving insulin sensitivity through the regulation of PI3K/AKT, FOXO1 and AMPK-mediated pathways.


Assuntos
Proteínas Quinases Ativadas por AMP/genética , Chalconas/farmacologia , Hiperglicemia/tratamento farmacológico , Hipoglicemiantes/farmacologia , Resistência à Insulina , Fosfatidilinositol 3-Quinases/genética , Proteínas Proto-Oncogênicas c-akt/genética , Células 3T3 , Proteínas Quinases Ativadas por AMP/metabolismo , Animais , Aspalathus/química , Carnitina O-Palmitoiltransferase/genética , Carnitina O-Palmitoiltransferase/metabolismo , Linhagem Celular , Chalconas/isolamento & purificação , Dieta Hiperlipídica/efeitos adversos , Açúcares da Dieta/efeitos adversos , Regulação da Expressão Gênica , Hepatócitos/citologia , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Hiperglicemia/etiologia , Hiperglicemia/genética , Hiperglicemia/metabolismo , Hipoglicemiantes/isolamento & purificação , Proteínas Substratos do Receptor de Insulina/genética , Proteínas Substratos do Receptor de Insulina/metabolismo , Masculino , Camundongos , Fibras Musculares Esqueléticas/citologia , Fibras Musculares Esqueléticas/efeitos dos fármacos , Fibras Musculares Esqueléticas/metabolismo , Proteínas do Tecido Nervoso/genética , Proteínas do Tecido Nervoso/metabolismo , Ácido Palmítico/farmacologia , Fosfatidilinositol 3-Quinases/metabolismo , Fosforilação/efeitos dos fármacos , Extratos Vegetais/química , Proteínas Proto-Oncogênicas c-akt/metabolismo , Ratos , Ratos Wistar , Receptor de Insulina/genética , Receptor de Insulina/metabolismo , Transdução de Sinais
17.
Molecules ; 24(9)2019 May 02.
Artigo em Inglês | MEDLINE | ID: mdl-31052590

RESUMO

Type 2 diabetic patients possess a two to four fold-increased risk for Cardiovascular Diseases (CVD). Hyperglycemia, oxidative stress associated with endothelial dysfunction and dyslipidemia are regarded as pro-atherogenic mechanisms of CVD. In this study, high-fat diet-induced diabetic and non-diabetic vervet monkeys were treated with 90 mg/kg of aspalathin-rich green rooibos extract (Afriplex GRT) for 28 days, followed by a 1-month wash-out period. Supplementation showed improvements in both the intravenous glucose tolerance test (IVGTT) glycemic area under curve (AUC) and total cholesterol (due to a decrease of the low-density lipoprotein [LDL]) values in diabetics, while non-diabetic monkeys benefited from an increase in high-density lipoprotein (HDL) levels. No variation of plasma coenzyme Q10 (CoQ10) were found, suggesting that the LDL-lowering effect of Afriplex GRT could be related to its ability to modulate the mevalonate pathway differently from statins. Concerning the plasma oxidative status, a decrease in percentage of oxidized CoQ10 and circulating oxidized LDL (ox-LDL) levels after supplementation was observed in diabetics. Finally, the direct correlation between the amount of oxidized LDL and total LDL concentration, and the inverse correlation between ox-LDL and plasma CoQ10 levels, detected in the diabetic monkeys highlighted the potential cardiovascular protective role of green rooibos extract. Taken together, these findings suggest that Afriplex GRT could counteract hyperglycemia, oxidative stress and dyslipidemia, thereby lowering fundamental cardiovascular risk factors associated with diabetes.


Assuntos
Chalconas/farmacologia , LDL-Colesterol/sangue , Diabetes Mellitus Experimental/etiologia , Diabetes Mellitus Experimental/metabolismo , Dieta Hiperlipídica/efeitos adversos , Oxirredução/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Animais , Biomarcadores , Glicemia/efeitos dos fármacos , Chlorocebus aethiops , Diabetes Mellitus Experimental/tratamento farmacológico , Modelos Animais de Doenças , Feminino , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Lipídeos/sangue , Lipoproteínas LDL/sangue , Masculino , Extratos Vegetais/farmacologia , Ubiquinona/análogos & derivados , Ubiquinona/sangue
18.
J Sci Food Agric ; 99(3): 1334-1341, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30094845

RESUMO

BACKGROUND: Steam treatment of shredded, fresh C. maculata (honeybush) plant material improves the aroma of this green herbal tea with a slight impact on color and phenolic content, but the effect on storage stability is not known. RESULTS: Steam-treated (60 s before drying) and untreated (control) dried plant material was stored under normal storage conditions in semi-permeable sachets at 25 °C and 60% relative humidity. Reference samples of treated (steamed) and untreated (control) material were stored at 0 °C in impermeable pouches for maximum retention of quality. The stability of the herbal tea was assessed in terms of sensory profile, phenolic composition and color over a storage period of 6 months. Normal storage conditions resulted in a significant (P < 0.05) decrease in green color, especially in steamed samples. Intensities of fruity and sweet-associated aroma attributes increased progressively during storage, while the opposite was observed for vegetal and cereal-like attributes. These changes in the aroma profile were more pronounced in untreated (control) samples. Individual phenolic content remained stable during storage. CONCLUSIONS: Storage of 3 to 6 months may result in a more appealing aroma profile and enhanced product quality, despite loss of green color. © 2018 Society of Chemical Industry.


Assuntos
Cyclopia (Planta)/química , Conservação de Alimentos/métodos , Chás de Ervas/análise , Xantonas/química , Conservação de Alimentos/instrumentação , Armazenamento de Alimentos , Fenóis/química , Controle de Qualidade , Vapor/análise
19.
J Sci Food Agric ; 99(7): 3653-3661, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30637751

RESUMO

BACKGROUND: Rooibos represents 10% of the global herbal tea market. Shrinking production areas as a result of climate change necessitate the maximum conversion of plant biomass to product. The present study aimed to determine the potential of rooibos tea processing waste (i.e. fine dust and coarse stems) as potential flavour and herbal tea ingredients, respectively. RESULTS: Hot water extraction of soluble solids (SS) from rooibos dust was optimised and extracts from different production batches (n = 20) were prepared. Their sensory profiles were similar, although less intense than that of infusions of commercial rooibos (n = 20) when diluted to the same SS content. The turbidity and flavonoid content of the diluted extracts was mostly lower (P < 0.05) than that of commercial rooibos. An atypical and negative aroma attribute, 'planky/pencil shavings', was predominant in the stem infusions (n = 20), which contained less SS (P < 0.05) than commercial rooibos. Blends of stem infusion and extract could not effectively mask this negative aroma note (P > 0.05). CONCLUSION: Rooibos dust could be used to produce a rooibos flavour extract, whereas the prominent atypical, negative 'planky/pencil shavings' aroma note of the stems would limit their inclusion in commercial rooibos blends. © 2019 Society of Chemical Industry.


Assuntos
Aspalathus/química , Flavonoides/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Caules de Planta/química , Chás de Ervas/análise , Resíduos/análise , Cor , Poeira/análise , Flavonoides/análise , Humanos , Extratos Vegetais/análise , Paladar
20.
Crit Rev Food Sci Nutr ; 58(2): 227-246, 2018 Jan 22.
Artigo em Inglês | MEDLINE | ID: mdl-27305453

RESUMO

Risk factors of type 2 diabetes mellitus (T2D) and cardiovascular disease (CVD) cluster together and are termed the metabolic syndrome. Key factors driving the metabolic syndrome are inflammation, oxidative stress, insulin resistance (IR), and obesity. IR is defined as the impairment of insulin to achieve its physiological effects, resulting in glucose and lipid metabolic dysfunction in tissues such as muscle, fat, kidney, liver, and pancreatic ß-cells. The potential of rooibos extract and its major C-glucosyl flavonoids, in particular aspalathin, a C-glucoside dihydrochalcone, as well as the phenolic precursor, Z-2-(ß-D-glucopyranosyloxy)-3-phenylpropenoic acid, to prevent the metabolic syndrome, will be highlighted. The mechanisms whereby these phenolic compounds elicit positive effects on inflammation, cellular oxidative stress and transcription factors that regulate the expression of genes involved in glucose and lipid metabolism will be discussed in terms of their potential in ameliorating features of the metabolic syndrome and the development of serious metabolic disease. An overview of the phenolic composition of rooibos and the changes during processing will provide relevant background on this herbal tea, while a discussion of the bioavailability of the major rooibos C-glucosyl flavonoids will give insight into a key aspect of the bioefficacy of rooibos.


Assuntos
Antioxidantes/uso terapêutico , Aspalathus/química , Suplementos Nutricionais , Flavonoides/uso terapêutico , Glucosídeos/uso terapêutico , Síndrome Metabólica/prevenção & controle , Fenilpropionatos/uso terapêutico , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios não Esteroides/análise , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/uso terapêutico , Antioxidantes/análise , Antioxidantes/química , Bebidas/análise , Diabetes Mellitus Tipo 2/complicações , Diabetes Mellitus Tipo 2/dietoterapia , Diabetes Mellitus Tipo 2/imunologia , Etnofarmacologia , Flavonoides/análise , Flavonoides/química , Glucosídeos/análise , Glucosídeos/química , Humanos , Isomerismo , Medicinas Tradicionais Africanas , Síndrome Metabólica/complicações , Síndrome Metabólica/etiologia , Obesidade/complicações , Obesidade/dietoterapia , Obesidade/imunologia , Obesidade/fisiopatologia , Fenilpropionatos/análise , Fenilpropionatos/química , Extratos Vegetais/química , Folhas de Planta/química , Caules de Planta/química , África do Sul , Chás de Ervas/análise
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