RESUMEN

Background: Monitoring noncommunicable diseases is regarded as a critical concern that has to be managed in order to avoid a wide variety of complications such as increasing blood lipid levels known as dyslipidemia. Statin drugs, mostly, Rosuvastatin (RSV) was investigated for its effectiveness in treating dyslipidemia. However, reaching the most efficient treatment is essential and improving the effect of RSV is crucial. Therefore, a combination therapy was a good approach for achieving significant benefit. Although RSV is hydrophobic, which would affect its absorption and bioavailability following oral administration, overcoming this obstacle was important. Purpose: To that end, the purpose of the present investigation was to incorporate RSV into certain lipid-based nanocarriers, namely, nanostructured lipid carrier (NLC) prepared with virgin coconut oil (CCO). Methods: The optimized RSV-NLC formula was selected, characterized and examined for its in vitro, kinetic, and stability profiles. Eventually, the formula was investigated for its in vivo hypolipidemic action. Results: The optimized NLC formulation showed a suitable particle size (279.3±5.03 nm) with PDI 0.237 and displayed good entrapment efficiency (75.6±1.9%). Regarding in vitro release, it was efficiently prolonged for 24 h providing 93.7±1.47%. The optimized formula was established to be stable after 3 months storage at two different conditions; 4°C and 25°C. Importantly, including CCO in the development of RSV-NLC could impressively enhance lowering total cholesterol level in obese rat models, which endorse the potential synergistic action between RSV and CCO. Conclusion: The study could elucidate the impact of developing NLC using CCO for improving RSV anti-hyperlipidemic activity.

Asunto(s)

Aceite de Coco , Portadores de Fármacos , Hipolipemiantes , Nanoestructuras , Tamaño de la Partícula , Rosuvastatina Cálcica , Animales , Rosuvastatina Cálcica/farmacocinética , Rosuvastatina Cálcica/química , Rosuvastatina Cálcica/farmacología , Rosuvastatina Cálcica/administración & dosificación , Aceite de Coco/química , Aceite de Coco/farmacología , Hipolipemiantes/química , Hipolipemiantes/farmacología , Hipolipemiantes/farmacocinética , Hipolipemiantes/administración & dosificación , Portadores de Fármacos/química , Masculino , Ratas , Nanoestructuras/química , Lípidos/química , Lípidos/sangre , Ratas Wistar , Liberación de Fármacos , Disponibilidad Biológica , Administración Oral

RESUMEN

This study aimed to identify and quantify the primary components in lotus leaf and to explore the hypolipidemic components through spectral-effect relationships and chemometric methods. Utilizing a data-dependent acquisition-diagnostic fragment ion/characteristic neutral loss screening strategy (DFI-NLS), a reliable HPLC-Q-TOF-MS analysis was conducted, identifying 77 compounds, including 36 flavonoids, 21 alkaloids, 3 terpenoids, 11 organic acids, 4 phenols, 1 lignin and 1 unsaturated hydrocarbon. A straightforward HPLC-DAD method was developed for the simultaneous determination of seven major components in lotus leaf, and quercetin-3-O-glucuronide (Q3GA) was identified as the most abundant component. The HPLC fingerprints of 36 lotus leaf sample batches were assessed using chemometric approaches such as principal component analysis and hierarchical cluster analysis. The hypolipidemic effect of these samples was analyzed by measuring total cholesterol (TC) and total triglycerides (TG) levels in palmitic acid (PA) and oleic acid (OA)-induced lipid modeling in HepG-2 cells, employing partial least squares regression and grey relation analysis to investigate the spectral-effect relationship of the lotus leaf. The in vivo hypolipidemic effect of these compounds was assessed using an egg yolk powder-induced high-fat zebrafish model. The findings indicated that peak No.11 (Q3GA) in the chemical fingerprint was significantly associated with hypolipidemic activity, suggesting it as a potential hypolipidemic compound in lotus leaf. In summary, this study facilitates the exploration of the phytochemical compounds and their bioactive properties in the lotus leaf.

Asunto(s)

Hipolipemiantes , Lotus , Fitoquímicos , Hojas de la Planta , Pez Cebra , Cromatografía Líquida de Alta Presión/métodos , Hojas de la Planta/química , Hipolipemiantes/análisis , Hipolipemiantes/farmacología , Hipolipemiantes/química , Animales , Lotus/química , Fitoquímicos/análisis , Fitoquímicos/farmacología , Fitoquímicos/química , Humanos , Células Hep G2 , Extractos Vegetales/farmacología , Extractos Vegetales/química , Triglicéridos/análisis , Flavonoides/análisis , Flavonoides/farmacología , Quercetina/análogos & derivados , Quercetina/análisis , Quercetina/farmacología , Colesterol/análisis , Espectrometría de Masas/métodos , Alcaloides/análisis , Alcaloides/farmacología

RESUMEN

Lipid metabolism dysregulation can lead to dyslipidemia and obesity, which are major causes of cardiovascular disease and associated mortality worldwide. The purpose of the study was to obtain and characterize six plant extracts (ACE-Allii cepae extractum; RSE-Rosmarini extractum; CHE-Cichorii extractum; CE-Cynarae extractum; AGE-Apii graveolentis extractum; CGE-Crataegi extractum) as promising adjuvant therapies for the prevention and treatment of dyslipidemia and its related metabolic diseases. Phytochemical screening revealed that RSE was the richest extract in total polyphenols (39.62 ± 13.16 g tannic acid/100 g dry extract) and phenolcarboxylic acids (22.05 ± 1.31 g chlorogenic acid/100 g dry extract). Moreover, the spectrophotometric chemical profile highlighted a significant concentration of flavones for CGE (5.32 ± 0.26 g rutoside/100 g dry extract), in contrast to the other extracts. UHPLC-MS quantification detected considerable amounts of phenolic constituents, especially chlorogenic acid in CGE (187.435 ± 1.96 mg/g extract) and rosmarinic acid in RSE (317.100 ± 2.70 mg/g extract). Rosemary and hawthorn extracts showed significantly stronger free radical scavenging activity compared to the other plant extracts (p < 0.05). Pearson correlation analysis and the heatmap correlation matrix indicated significant correlations between phytochemical contents and in vitro antioxidant activities. Computational studies were performed to investigate the potential anti-obesity mechanism of the studied extracts using target prediction, homology modeling, molecular docking, and molecular dynamics approaches. Our study revealed that rosmarinic acid (RA) and chlorogenic acid (CGA) can form stable complexes with the active site of carbonic anhydrase 5A by either interacting with the zinc-bound catalytic water molecule or by directly binding Zn2+. Further studies are warranted to experimentally validate the predicted CA5A inhibitory activities of RA and CGA and to investigate the hypolipidemic and antioxidant activities of the proposed plant extracts in animal models of dyslipidemia and obesity.

RESUMEN

Camellia polyodonta flowers are rich sources of phenolics and less attention has been paid to their potential biological activity. This study aims to explore the crude extracts and resulting purified fractions (CPFP-I, II, III, and IV) through compositional analysis and antioxidant and hypolipidemic activities in vitro and in vivo. Among four fractions, CPFP-II contained the highest total phenolic content and flavonoid content, while CPFP-III exhibited the greatest total proanthocyanidin content. Among the 14 phenolic compounds, CPFP-II displayed the highest content of procyanidin B2, B4, and C1, whereas CPFP-III contained the highest amount of 1,2,3,6-tetragalloylglucose. The DPPH, ABTS, and FRAP assessments demonstrated a consistent trend: CPFP-II > CPFP-III > CPFP-I > CPFP-IV. In vivo experiments showed that that all four fractions significantly reduced lipid levels in hyperlipidemic C. elegans (p < 0.05), with CPFP-II exhibiting the most potent effect. Furthermore, CPFP-II effectively bound to bile acids and inhibited the enzymatic activity of pancreatic lipase in vitro. Consequently, CPFP-II should be prioritized as a promising fraction for further exploration and should provide substantial support for the feasibility of the C. polyodonta flower as a natural alternative.

RESUMEN

Five trichothecenes including a new one, together with two previously undescribed benzene derivatives were isolated from the solid culture of Trichothecium sp. Their structures were established by 1D and 2D NMR data in conjunction with HR-ESI-MS analysis. Compounds 1-5 exhibited cytotoxicity against MCF-7 cell lines at various levels ranging from IC50 of 7.23 to 16.95 µM. Compound 6 decreased the concentration of blood lipids in zebra fish at the concentration of 20 µM.

RESUMEN

The proteins were mainly derived from Protaetia brevitarsis larval extracts obtained using two empty intestine methods (traditional static method: TSM or salt immersion stress method: SISM) and extraction solvents (water: W or 50 % water-ethanol: W:E), and the proteins were used as objects to investigate the effect of emptying intestine methods on hypolipidemic peptides. The results revealed that the F-2 fractions of protein hydrolysate had stronger in vitro hypolipidemic activity, with the peptides obtained by SISM possessing a stronger cholesterol micelle solubility inhibition rate, especially in SISM-W:E-P. Moreover, a total of 106 peptides were tentatively identified, among which SISM identified more peptides with an amino acid number < 8. Meanwhile, five novel peptides (YPPFH, YPGFGK, KYPF, SPLPGPR and VPPP) exhibited good hypolipidemic activity in vitro and in vivo, among which YPPFH, VPPP and KYPF had strong inhibitory activities on pancreatic lipase (PL) and cholesteryl esterase (CE), and KYPF, SPLPGPR and VPPP could significantly reduce the TG content in Caenorhabditis elegans. Thus, P. brevitarsis can be developed as a naturally derived hypolipidemic component for the development and application in functional foods.

Asunto(s)

Escarabajos , Hidrolisados de Proteína , Animales , Larva/química , Hidrolisados de Proteína/farmacología , Hidrolisados de Proteína/metabolismo , Escarabajos/química , Péptidos/farmacología , Péptidos/metabolismo , Agua/metabolismo , Proteínas de Insectos/farmacología , Proteínas de Insectos/metabolismo

RESUMEN

Chlorella oil nanoliposomes (CO-NLP) were synthesized through ultrasonic injection with ethanol, and their physicochemical properties and hypolipidemic efficacy were systematically investigated. The results revealed that the mean particle size of CO-NLP was 86.90 nm and the encapsulation efficiency (EE) was 92.84%. Storage conditions at 4 °C were conducive to the stability of CO-NLP, maintaining an EE of approximately 90% even after 10 days of storage. The release profile of CO-NLP adhered more closely to the first-order kinetic model during in vitro assessments, exhibiting a slower release rate compared to free microalgae oil. In simulated in vitro digestion experiments, lipolytic reactions of CO-NLP were observed during intestinal digestion subsequent to nanoliposome administration. Notably, the inhibitory effect of CO-NLP on cholesterol esterase activity was measured at 85.42%. Additionally, the average fluorescence intensity of nematodes in the CO-NLP group was 52.17% lower than in the control group at a CO-NLP concentration of 500 µg/mL, which suggests a pronounced lipid-lowering effect of CO-NLP. Therefore, the CO-NLP exhibited characteristics of small and uniform particle size, elevated storage stability, gradual release during intestinal digestion, and a noteworthy hypolipidemic effect. These findings designate CO-NLP as a novel lipid-lowering active product, demonstrating potential for the development of functional foods.

RESUMEN

This study investigated the effects of three oil production methods on the physicochemical properties of dietary fiber from rice bran flour, and the hypolipidemic effects of the dietary fibers were investigated in vitro and in vivo. The particle size results showed that the organic-solvent-impregnated rice bran meal dietary fiber (N-RBDF) had the smallest average particle size and the aqueous enzymatic rice bran meal dietary fiber (E-RBDF) had the narrowest particle size distribution. Scanning electron microscopy (SEM) results demonstrated that all three kinds of rice bran meal dietary fibers (RBDFs) were irregularly flaky. Fourier transform infrared spectroscopy (FT-IR) results revealed that the three RBDFs had similar reactive groups, and X-ray diffraction (XRD) results indicated that all three RBDFs were cellulose type I crystals. The results of thermogravimetric analysis showed that the lignin content of N-RBDF was significantly lower than that of the other two. Among the three kinds of RBDFs, E-RBDF had higher water retention capacity, swelling capacity, oil holding capacity, and adsorption capacity for cholesterol and sodium bile salts. The results of experimental studies in hyperlipidemic rats showed that all three kinds of RBDFs significantly reduced triglycerides (TG), total cholesterol (TC), and low-density lipoprotein cholesterol (LDL-C) and elevated high-density lipoprotein cholesterol (HDL-C) in the serum of hyperlipidemic rats; they also significantly lowered malondialdehyde (MDA) and elevated total superoxide dismutase (T-SOD) and glutathione peroxidase (GSH-Px) activities in the livers of rats. In addition, all three kinds of RBDFs decreased aminotransferase (ALT) and aminotransferase (AST) activity in serum and also improved liver steatosis and reduced atherosclerosis index (AI) in rats with hyperlipidemia. Our study provides a reference for the development and utilization of rice bran meal and the application of rice bran meal dietary fiber in food processing.

RESUMEN

Kiwifruit pomace is abundant in polysaccharides that exhibit diverse biological activities and prebiotic potential. This study delves into the digestive behavior and fermentation characteristics of kiwifruit pomace polysaccharides (KFP) through an in vitro simulated saliva-gastrointestinal digestion and fecal fermentation. The results reveal that following simulated digestion of KFP, its molecular weight reduced by 4.7%, and the reducing sugar (CR) increased by 9.5%. However, the monosaccharide composition and Fourier transform infrared spectroscopy characteristics showed no significant changes, suggesting that KFP remained undigested. Furthermore, even after saliva-gastrointestinal digestion, KFP retained in vitro hypolipidemic and hypoglycemic activities. Subsequently, fecal fermentation significantly altered the physicochemical properties of indigestible KFP (KFPI), particularly leading to an 89.71% reduction in CR. This indicates that gut microbiota could decompose KFPI and metabolize it into SCFAs. Moreover, after 48 h of KFPI fecal fermentation, it was observed that KFPI contributed to maintaining the balance of gut microbiota by promoting the proliferation of beneficial bacteria like Bacteroides, Lactobacillus, and Bifidobacterium, while inhibiting the unfavorable bacteria like Bilophila. In summary, this study offers a comprehensive exploration of in vitro digestion and fecal fermentation characteristics of KFP, providing valuable insights for potential development of KFP as a prebiotic for promoting intestinal health.

Asunto(s)

Actinidia , Microbioma Gastrointestinal , Humanos , Fermentación , Digestión , Polisacáridos/farmacología , Polisacáridos/metabolismo , Heces/microbiología , Prebióticos , Actinidia/metabolismo , Ácidos Grasos Volátiles/metabolismo

RESUMEN

Bioactive polysaccharides known as the biological response modifiers, can directly interact with intestinal epithelium cells (IEC) and regulate key metabolic processes such as lipid metabolism. Here, the coculture of Caco-2/HT29 monolayer (>400 Ω × cm2) and HepG2 cells was developed to mimic the gut-liver interactions. This system was used to investigate the effects of raw and fermented barley ß-glucans (RBG and FBG) on lipid metabolism by directly interacting with IEC. Both RBG and FBG significantly and consistently reduced the lipid droplets and triacylglycerol levels in monoculture and coculture of HepG2 overloaded with oleic acid. Notably, FBG significantly and distinctly elevated PPARα (p < 0.05) and PPARα-responsive ACOX-1 (p < 0.01) gene expressions, promoting lipid degradation in cocultured HepG2. Moreover, the metabolomics analyses revealed that FBG had a unique impact on extracellular metabolites, among them, the differential metabolite thiomorpholine 3-carboxylate was significantly and strongly correlated with PPARα (r = -0.68, p < 0.01) and ACOX-1 (r = -0.76, p < 0.01) expression levels. Taken together, our findings suggest that FBG-mediated gut-liver interactions play a key role in its lipid-lowering effects that are superior to those of RBG. These results support the application of Lactiplantibacillus fermentation for improving hypolipidemic outcomes.

Asunto(s)

Hordeum , beta-Glucanos , Humanos , Hordeum/metabolismo , PPAR alfa/metabolismo , Fermentación , beta-Glucanos/farmacología , beta-Glucanos/metabolismo , Células CACO-2 , Hígado/metabolismo , Triglicéridos/metabolismo

RESUMEN

κ-Carrageenase can degrade κ-carrageenan to produce bioactive κ-carrageenan oligosaccharides (KCOs) that have potential applications in pharmaceutical, food, agricultural, and cosmetics industries. Immobilized enzymes gain their popularity due to their good reusability, enhanced stability, and tunability. In this study, the previously characterized catalytic domain of Pseudoalteromonas purpurea κ-carrageenase was covalently immobilized on the synthesized amine-modified zeolitic imidazolate framework-8 nanoparticles with the formation of cross-linked enzyme aggregates, and the immobilized κ-carrageenase was further characterized. The immobilized κ-carrageenase demonstrated excellent pH stability and good reusability, and exhibited higher optimal reaction temperature, better thermostability, and extended storage stability compared with the free enzyme. The KCOs produced by the immobilized κ-carrageenase could significantly decrease the TC, TG, and LDL-C levels in HepG2 cells, increase the HDL-C level in HepG2 cells, and reduce the free fatty acids level in Caco-2 cells. Biochemical assays showed that the KCOs could activate AMPK activity, increase the ratios of p-AMPK/AMPK and p-ACC/ACC, and downregulate the expression of the lipid metabolism related proteins including SREBP1 and HMGCR in the hyperlipidemic HepG2 cells. This study provides a novel and effective method for immobilization of κ-carrageenase, and the KCOs produced by the immobilized enzyme could be a potential therapeutic agent to prevent hyperlipidemia.

Asunto(s)

Proteínas Quinasas Activadas por AMP , Proteínas Bacterianas , Humanos , Carragenina/química , Células CACO-2 , Células Hep G2 , Proteínas Bacterianas/química , Glicósido Hidrolasas/química , Oligosacáridos/química , Enzimas Inmovilizadas

RESUMEN

There are approximately 250 species of Eryngium L. distributed throughout the world, with North America and South America being centers of diversity on this continent. In the central-western region of Mexico there may be around 28 species of this genus. Some Eryngium species are cultivated as leafy vegetables, ornamental, and medicinal plants. In traditional medicine they are used to treat respiratory and gastrointestinal conditions, diabetes, and dyslipidemia, among others. This review addresses the phytochemistry and biological activities, as well as traditional uses, distribution, and characteristics of the eight species of Eryngium reported as medicinal in the central-western region of Mexico: E. cymosum, E. longifolium, E. fluitans (or mexicanum), E. beecheyanum, E. carlinae, E. comosum, E. heterophyllum, and E. nasturtiifolium. The extracts of the different Eryngium spp. have shown biological activities such as hypoglycemic, hypocholesterolemic, renoprotective, anti-inflammatory, antibacterial, and antioxidant, among others. E. carlinae is the most studied species, and phytochemical analyses, performed mainly by high-performance liquid chromatography (HPLC) and gas chromatography coupled with mass spectrometry (GC-MS), have shown its content of terpenoids, fatty acids, organic acids, phenolic acids, flavonoids, sterols, saccharides, polyalcohols, and aromatic and aliphatic aldehydes. According to the results of this review on Eryngium spp., they constitute a relevant alternative as a source of bioactive compounds for pharmaceutical, food, and other industries. However, there is a lot of research to be conducted regarding phytochemistry, biological activities, cultivation, and propagation, in those species with few or no reports.

Asunto(s)

Apiaceae , Eryngium , Etnobotánica , Eryngium/química , México , Extractos Vegetales/farmacología , Extractos Vegetales/química , Fitoquímicos/farmacología , Fitoquímicos/química , Etnofarmacología

RESUMEN

A soybean protein isolate (SPI)-apricot polysaccharide gel with hypolipidemic activity that can be used for 3D printing was prepared and the mechanism of its gel formation was studied in this work. The results demonstrated that adding apricot polysaccharide to SPI could effectively improve the bound water content, viscoelastic properties and rheological properties of the gels. Low-field NMR, FT-IR spectroscopy and surface hydrophobicity confirmed that the interactions between SPI and apricot polysaccharide were mainly realized by electrostatic interactions, hydrophobic and hydrogen bonding. Furthermore, adding modified polysaccharide treated by ultrasonic-assisted Fenton method to SPI on the basis of low-concentration apricot polysaccharide contributed to improving the 3D printing accuracy and stability of the gel. Consequently, the gel formed by adding apricot polysaccharide (0.5 %, m/v) and modified polysaccharide (0.1 %, m/v) to SPI had the best hypolipidemic activity (the binding rate of sodium taurocholate and sodium glycocholate were 75.33 % and 72.86 %, respectively) and 3D printing characteristics.

Asunto(s)

Prunus armeniaca , Proteínas de Soja , Proteínas de Soja/química , Espectroscopía Infrarroja por Transformada de Fourier , Tinta , Polisacáridos/química , Geles/química

RESUMEN

In this study, hypolipidemic peptides were obtained from tea protein by enzymatic hydrolysis, ultrafiltration and high-performance liquid chromatography. Subsequently, the hypolipidemic peptides were identified by mass spectrometry and screened through molecular docking technology, and the hypolipidemic activities and mechanisms of the active peptides were explored. The results showed that the hydrolysate of hypolipidemic peptides obtained by pepsin hydrolysis for 3 h had good bile salt binding ability. After purification, identification and molecular docking screening, three novel hypolipidemic peptides FLF, IYF and QIF were obtained. FLF, IYF and QIF can interact with the receptor proteins 1LPB and 1F6W through hydrogen bonds, π-π bonds, hydrophobic interactions and van der Waals forces, thus exerting hypolipidemic activities. Activity studies showed that, compared with the positive controls, FLF, IYF and QIF had excellent sodium taurocholate binding abilities, pancreatic lipase inhibitory activities and cholesterol esterase inhibitory activities. Moreover, FLF, IYF and QIF can effectively inhibit lipogenic differentiation of 3T3-L1 preadipocytes, reduce intracellular lipid and low-density lipoprotein content and increase high-density lipoprotein content. These results indicated that the three novel hypolipidemic peptides screened in this study had excellent hypolipidemic activities and were expected to be used as natural-derived hypolipidemic active ingredients for the development and application in functional foods.

Asunto(s)

Lipasa , Péptidos , Ratones , Animales , Simulación del Acoplamiento Molecular , Células 3T3-L1 , Té

RESUMEN

Teas based on nutraceutical herbs are an effective tool against hyperlipidemia. However, the adulteration with chemical drugs is frequently detected. By coupling bioluminescent bioautography with high performance thin-layer chromatography (HPTLC), we developed a facile method suitable for screening hypolipidemic drugs (ciprofibrate and bezafibrate) adulteration in five different herbal teas (lotus leaf, Apocynum, Ginkgo biloba, Gynostemia and chrysanthemum). First, the sensitivity of a bioluminescent bacteria to the analyte was evaluated on different HPTLC layer materials, revealing that the best performance was achieved on the silica gel layer. On this basis, sample extracts were separated on silica gel plates via a standardized HPTLC procedure, forming a selective detection window for the targeted compound. Then, the separation results were rapidly visualized by the bioluminescence inhibition of bacteria cells within 6 min after dipping. The observed inhibition displayed an acceptable limit of detection (<20 ng/zone or 2 mg/kg) and linearity (R2 ≥ 0.9279) within a wide concentration range (50-1000 ng/zone). Furthermore, the optimized method was performed with artificially adulterated samples and the recovery rates were determined to be within the range of 71% to 91%, bracing its practical reliability. Showing superiorly high simplicity, throughput and specificity, this work demonstrated that the analytical method jointly based on HPTLC and bioautography was an ideal tool for screening bioactive compounds in complex biological matrix.

Asunto(s)

Tés de Hierbas , Cromatografía en Capa Delgada/métodos , Tés de Hierbas/análisis , Hipolipemiantes/análisis , Gel de Sílice , Reproducibilidad de los Resultados

RESUMEN

Dyslipidemia is a lipid metabolism disorder associated with the loss of the physiological homeostasis that ensures safe levels of lipids in the organism. This metabolic disorder can trigger pathological conditions such as atherosclerosis and cardiovascular diseases. In this regard, statins currently represent the main pharmacological therapy, but their contraindications and side effects limit their use. This is stimulating the search for new therapeutic strategies. In this work, we investigated in HepG2 cells the hypolipidemic potential of a picrocrocin-enriched fraction, analyzed by high-resolution 1H NMR and obtained from a saffron extract, the stigmas of Crocus sativus L., a precious spice that has already displayed interesting biological properties. Spectrophotometric assays, as well as expression level of the main enzymes involved in lipid metabolism, have highlighted the interesting hypolipidemic effects of this natural compound; they seem to be exerted through a non-statin-like mechanism. Overall, this work provides new insights into the metabolic effects of picrocrocin, thus confirming the biological potential of saffron and paving the way for in vivo studies that could validate this spice or its phytocomplexes as useful adjuvants in balancing blood lipid homeostasis.

Asunto(s)

Crocus , Humanos , Crocus/química , Células Hep G2 , Extractos Vegetales/farmacología , Terpenos/farmacología , Ciclohexenos/farmacología

RESUMEN

Passiflora cincinnata Mast. is described as a native Caatinga species, used by nutritional and medicinal purposes, although there are still few studies and pharmacological data related to this species. This paper aims to evaluate the safety profile and hypolipidemic potential of the fruit peel of this species in mice. It was analyzed the chemical composition of ethanolic extract (EtOH-Pc) by HPLC-DAD-MS/MS, and the organic and inorganic composition of flour (MF-Pc). Also were evaluated the acute toxicity, the lipid-lowering potential of these samples, through of a pretreatment (oral: 100 and 200 mg/kg), and a single treatment with the same doses, after hyperlipidemic induction with triton WR-1339, using as animal model Swiss Mus musculus mice, besides histopathological analysis. The presence of flavonoids in the extract was confirmed, mainly C-glycosides, and antioxidant minerals and pectin, in flour. No clinical signs of toxicity or death were reported in the study. In the hyperlipidemia study model used, the analyzed substances, at all doses, notably decreased the lipid levels of TC, TG, LDL-c and VLDL-c and increase the HDL-c levels in the induced hyperlipidemic mice (p < 0.05). The results of the histopathological analysis showed that in the group only induced was identified the discrete presence of hepatic steatosis, in 2 animals at the analysis of 24 h, not being visualized in the groups treated with the substances evaluated. The results obtained in the present study suggest a hypolipidemic potential of the extract and flour, obtained from the fruit peel of Passiflora cincinnata Mast.

Asunto(s)

Passiflora , Passifloraceae , Ratones , Animales , Passiflora/química , Harina , Espectrometría de Masas en Tándem , Extractos Vegetales/farmacología , Etanol , Pectinas , Lípidos

RESUMEN

The disease of type 2 diabetes mellitus (T2DM) is principally induced by insufficient insulin secretion and insulin resistance. In the current study, Sanghuangporus vaninii fruit body polysaccharide (SVP) was prepared and structurally characterized. It was shown that the yield of SVP was 1.91%, and SVP mainly contains small molecular weight polysaccharides. Afterward, the hypoglycemic and hypolipidemic effects and the potential mechanism of SVP in T2DM mice were investigated. The results exhibited oral SVP could reverse the body weight loss, high levels of blood glucose, insulin resistance, hyperlipidemia, and inflammation in T2DM mice. Oral SVP increased fecal short-chain fatty acids (SCFAs) concentrations of T2DM mice. Additionally, 16S rRNA sequencing analysis illustrated that SVP can modulate the structure and function of intestinal microflora in T2DM mice, indicating as decreasing the levels of Firmicutes/Bacteroidetes, Flavonifractor, Odoribacter, and increasing the levels of Weissella, Alloprevotella, and Dubosiella. Additionally, the levels of predicted metabolic functions of Citrate cycle, GABAergic synapse, Insulin signaling pathway were increased, and those of Purine metabolism, Taurine and hypotaurine metabolism, and Starch and sucrose metabolism were decreased in intestinal microflora after SVP treatment. These findings demonstrate that SVP could potentially play hypoglycemic and hypolipidemic effects by regulating gut microflora and be a promising nutraceutical for ameliorating T2DM.

RESUMEN

Angelica keiskei contains a variety of bioactive compounds including chalcone, coumarin, and phytochemicals, endowing it with pharmacological effects such as lipid-lowering activity, antitumor activity, liver protection, and nerve protection. This study aims to study the hypoglycemic and hypolipidemic effects of the flavonoid-rich extract from Angelica keiskei (FEAK) in an effort to exploit new applications of FEAK and increase its commercial value. In this paper, flavonoid compounds in Angelica keiskei were extracted using 50% ethanol, and the contents of the flavonoid compounds were analyzed by UPLC-MS/MS. Then, the hypoglycemic and hypolipidemic activities of the FEAK were investigated through in vitro enzyme activity and cell experiments as well as establishing in vivo zebrafish and Caenorhabditis elegans (C. elegans) models. The UPLC-MS/MS results show that the major flavonoid compounds in the FEAK were aureusidin, xanthoangelol, kaempferol, luteolin, and quercetin. The inhibitory rates of the FEAK on the activity of α-amylase and cholesterol esterase were 57.13% and 72.11%, respectively. In cell lipid-lowering experiments, the FEAK significantly reduced the total cholesterol (TC) and total triglyceride (TG) levels in a dose-dependent manner, with 150 µg/mL of FEAK decreasing the intracellular levels of TC and TG by 33.86% and 27.89%, respectively. The fluorescence intensity of the FEAK group was 68.12% higher than that of the control group, indicating that the FEAK exhibited hypoglycemic effects. When the concentration of the FEAK reached 500 µg/mL, the hypoglycemic effect on zebrafish reached up to 57.7%, and the average fluorescence intensity of C. elegans in the FEAK group was 17% lower than that of the control group. The results indicate that the FEAK had hypoglycemic and hypolipidemic activities. The findings of this study provide theoretical references for the high-value utilization of Angelica keiskei and the development of natural functional food with hypoglycemic and hypolipidemic activities.

Asunto(s)

Angelica , Chalconas , Angelica/química , Animales , Caenorhabditis elegans , Chalconas/química , Colesterol , Cromatografía Liquida , Cumarinas , Etanol/química , Flavonoides/farmacología , Hipoglucemiantes/farmacología , Quempferoles , Lípidos , Luteolina , Extractos Vegetales/farmacología , Quercetina , Esterol Esterasa , Espectrometría de Masas en Tándem , Triglicéridos , Pez Cebra , alfa-Amilasas

RESUMEN

Lingonberry (Vaccinium vitis-idaea L.) fruits are important Ericaceous berries to include in a healthy diet of the Northern Hemisphere as a source of bioactive phenolics. The waste generated by the V. vitis-idaea processing industry is hard-skinned press cake that can be a potential source of dietary fiber and has not been studied thus far. In this study, water-soluble polysaccharides of V. vitis-idaea press cake were isolated, separated, and purified by ion-exchange and size-exclusion chromatography. The results of elemental composition, monosaccharide analysis, ultraviolet-visible and Fourier-transform infrared spectroscopy, molecular weight determination, linkage analysis, and alkaline destruction allowed us to characterize two polyphenol-polysaccharide conjugates (PPC) as neutral arabinogalactans cross-linked with monomeric and dimeric hydroxycinnamate residues with molecular weights of 108 and 157 kDa and two non-esterified galacturonans with molecular weights of 258 and 318 kDa. A combination of in vitro and in vivo assays confirmed that expressed antioxidant activity of PPC was due to phenolic-scavenged free radicals, nitrogen oxide, hydrogen peroxide, and chelate ferrous ions. Additionally, marked hypolipidemic potential of both PPC and acidic polymers bind bile acids, cholesterol, and fat, inhibit pancreatic lipase in the in vitro study, reduce body weight, serum level of cholesterol, triglycerides, low/high-density lipoprotein-cholesterol, and malondialdehyde, and increase the enzymatic activity of superoxide dismutase, glutathione peroxidase, and catalase in the livers of hamsters with a 1% cholesterol diet. Polysaccharides and PPC of V. vitis-idaea fruit press cake can be regarded as new antioxidants and hypolipidemic agents that can be potentially used to cure hyperlipidemic metabolic disorders.