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1.
J Physiol Biochem ; 79(2): 427-440, 2023 May.
Artículo en Inglés | MEDLINE | ID: mdl-36961724

RESUMEN

Diabetes mellitus (DM) is a metabolic disease characterized by a high blood sugar level that can cause severe complications to the organism or even death when not treated. However, certain dietary habits and foods may have beneficial effects on this condition. A polyphenolic-rich extract (containing hyperoside, isoquercitrin, quercetin, ellagic acid, and vanillic acid) of Tageres erecta L. (T. erecta) was obtained from yellow and orange flowers using an ethanolic Soxhlet extraction. These extracts were screened for antidiabetic and anti-obesity properties using in vitro and in vivo procedures. The capacity to inhibit the enzymes lipase and α-glucosidase, as well as the inhibition of advance glycation end-products (AGEs) was tested in vitro. Caenorhabditis elegans (C. elegans) was used as an obesity in vivo model to assess extracts effects on fat accumulation using the wild-type strain N2 and a mutant with no N3 fatty acid desaturase activity BX24. Extracts from both cultivars (yellow and orange) T. erecta presented in vitro inhibitory activity against the enzymes lipase and α-glucosidase, showing lower IC50 values than acarbose (control). They also showed important activity in preventing AGEs formation. The polyphenol-rich matrices reduced the fat content of obese worms in the wild-type strain (N2) down to levels of untreated C. elegans, with no significant differences found between negative control (100% reduction) and both tested samples (p < 0.05). Meanwhile, the fat reduction was considerably lower in the BX24 mutants (fat-1(wa-9)), suggesting that N3 fatty acid desaturase activity could be partially involved in the T. erecta flower effect. Our findings suggested that polyphenols from T. erecta can be considered candidate bioactive compounds in the prevention and improvement of metabolic chronic diseases such as obesity and diabetes.


Asunto(s)
Polifenoles , Tagetes , Animales , Polifenoles/farmacología , Polifenoles/metabolismo , Caenorhabditis elegans/metabolismo , Hipoglucemiantes/farmacología , Hipoglucemiantes/uso terapéutico , alfa-Glucosidasas/metabolismo , alfa-Glucosidasas/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/metabolismo , Flores , Obesidad/tratamiento farmacológico , Lipasa/metabolismo , Productos Finales de Glicación Avanzada/metabolismo , Productos Finales de Glicación Avanzada/farmacología , Ácido Graso Desaturasas/metabolismo , Ácido Graso Desaturasas/farmacología
2.
Pharm Biol ; 60(1): 1994-2001, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36219451

RESUMEN

CONTEXT: Brassica incana Ten. (Brassicaceae) is an edible plant with very limited available information. Previous studies have demonstrated the polyphenolic profile and the antioxidant and cytotoxic properties of the leaf and flowering top hydroalcoholic extracts. OBJECTIVE: The volatile composition and the antidiabetic and anti-obesity potential of B. incana leaf and flowering top extracts have been investigated. MATERIAL AND METHODS: The volatile characterization of the extracts was attained by HS-SPME-GC/MS analysis. The antidiabetic and anti-obesity potential was investigated spectrophotometrically in vitro by the ability to modulate pancreatic lipase and α-glucosidase at different concentrations using orlistat and acarbose as reference drugs. The inhibition of advanced glycation end-products (AGEs) was measured with aminoguanidine as reference and the antioxidant activity with the xanthine/xanthine oxidase system and Trolox for comparative purposes. RESULTS: Several volatiles belonging to different chemical classes were identified, being sulphur compounds the most abundant in both leaf and flowering top extracts (56.33% and 64.40% of all volatiles). Although the leaf extract showed lower IC50 values in most of the assays (0.968 and 1.921 mg/mL for α-glucosidase; 0.192 and 0.262 mg/mL for AGEs; 0.022 and 0.038 mg/mL for superoxide scavenging), there were no statistically significant differences between both samples. These extracts showed a similar behaviour to Trolox in the xanthine oxidase assay (IC50 values of 0.022 mg/mL for leaf extract; 0.038 mg/mL for flowering top and 0.028 for Trolox). CONCLUSIONS: Leaves and flowering tops from B. incana can be used as sources of functional compounds that could act as antidiabetic and anti-obesogenic agents.


Asunto(s)
Brassica , Hipoglucemiantes , Acarbosa , Antioxidantes/química , Antioxidantes/farmacología , Copas de Floración , Hipoglucemiantes/química , Hipoglucemiantes/farmacología , Lipasa , Orlistat , Extractos Vegetales/química , Extractos Vegetales/farmacología , Compuestos de Azufre , Superóxidos , Xantina Oxidasa , Xantinas , alfa-Glucosidasas
3.
Antioxidants (Basel) ; 11(6)2022 May 31.
Artículo en Inglés | MEDLINE | ID: mdl-35739989

RESUMEN

Helichrysum stoechas (L.) Moench (H. stoechas) is a medicinal plant traditionally used in the Iberian Peninsula to treat different disorders such as arterial hypertension. The aim of this study was to investigate the vascular effects of a polyphenolic methanolic extract of H. stoechas, which has high antioxidant activity, and its mechanism of action. Isometric myography studies were performed in an organ bath with rat aortic rings with intact endothelium. The H. stoechas extract produced vasorelaxation in the aortic rings that were precontracted by phenylephrine or KCl. L-NAME and Rp-8-Br-PET-cGMPS but not indomethacin or H-89; it also reduced the relaxant response evoked by H. stoechas extract on the phenylephrine-induced contractions. H. stoechas extract reduced the response to CaCl2 similar to verapamil and reduced the phenylephrine-induced contractions comparable with heparin. TRAM-34, apamin and glibenclamide reduced relaxation induced by the H. stoechas extract. The combination of L-NAME+TRAM-34+apamin almost completely inhibited the H. stoechas-induced effect. In conclusion, the relaxant effect of the H. stoechas extract is partially mediated by endothelium through the activation of the NO/PKG/cGMP pathway and the opening of Ca2+-activated K+ channels. Furthermore, the decrease in the cytosolic Ca2+ by the inhibition of Ca2+ influx through the L-type Ca2+ channels and by the reduction of Ca2+ release from the sarcoplasmic reticulum via the IP3 pathway is also involved.

4.
Pharmaceuticals (Basel) ; 15(1)2022 Jan 14.
Artículo en Inglés | MEDLINE | ID: mdl-35056156

RESUMEN

Black mulberry, Morus nigra L. (family: Moraceae), is a healthy food and medicinal plant. Microwave hydrodiffusion and gravity (MHG) is one of the most innovative applications of solvent-free microwave extraction. The aim of this study was to optimize for the first time the MHG solvent-free extraction of polyphenols and sugars from M. nigra fruits. Optimization was carried out using a central composite design (CCD) with selected responses such as extraction yield, total polyphenol (TPC), flavonoid (TFC), anthocyanin (TAC), and sugar (TSC) contents, in addition to DPPH radical scavenging, and α-glucosidase (AGHi), lipase (Li), and xanthine oxidase (XOi) inhibition as tools to evaluate the best parameters for efficient and rapid extraction of black mulberry. The optimized extract was characterized in terms of the aforementioned parameters to validate the models, and was further analyzed for 36 individual polyphenols using HPLC-MS/MS. The optimized MHG extract was finally compared with traditional extracts, and demonstrated much better performance in terms of TPC, TAC, and Li, while the traditional extracts showed better XOi and AGHi. In conclusion, MHG is a valuable green technique for the production of non-degraded black mulberry polyphenol-rich extract and we suggest its larger use in the pharmaceutical and food industries.

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