Red Wine High-Molecular-Weight Polyphenolic Complex Ameliorates High-Fat Diet-Induced Metabolic Dysregulation and Perturbation in Gut Microbiota in Mice.

Red wine polyphenolic complexes have attracted increasing attention as potential modulators of human metabolic disease risk. Our previous study discovered that red wine high-molecular-weight polymeric polyphenolic complexes (HPPCs) could inhibit key metabolic syndrome-associated enzymes and favorably modulate human gut microbiota (GM) in simulated colonic fermentation assay in vitro. In this work, the efficacy of HPPC supplementation (150 and 300 mg/kg/day, respectively) against high-fat diet (HFD)-induced metabolic disturbance in mice was investigated. HPPCs effectively attenuated HFD-induced obesity, insulin resistance, and lipid and glucose metabolic dysregulation and ameliorated inflammatory response and hepatic and colonic damage. It also improved the relative abundance of Bacteroidetes and Firmicutes, consistent with an anti-obesity phenotype. The favorable modulation of GM was further supported by improvement in the profile of fecal short-chain fatty acids. The higher dosage generally had a better performance in these effects than the low dosage. Moreover, serum metabolite profiling and pathway enrichment analysis revealed that HPPCs significantly modulated vitamin B metabolism-associated pathways and identified N-acetylneuraminic acid and 2-methylbutyroylcarnitine as potential biomarkers of the favorable effect on HFD-induced metabolic dysregulation. These findings highlight that dietary supplementation with red wine HPPCs is a promising strategy for the management of weight gain and metabolic dysregulation associated with HFD.

Suppression of palmitic acid-induced hepatic oxidative injury by neohesperidin-loaded pectin-chitosan decorated nanoliposomes.

The biological activity of neohesperidin (NH, a flavanone glycoside) is limited due to instability in the physiological environment. Thus, the current study aimed to explore the protective effect of NH-loaded pectin-chitosan decorated liposomes (P-CH-NH-NL) against palmitic acid (PA)-induced hepatic oxidative injury in L02 cells. The particles were characterized using DLS, TEM, HPLC, DSC, and cellular uptake study. Then, the protective effect of NH-loaded liposomal systems (NH-NLs) against PA-induced oxidative injury was evaluated in terms of cell viability study, intracellular ROS, superoxide ions (O2-), MMP, and cellular GSH determination. Our results exhibited that NH-NLs significantly lessened the PA-induced hepatic oxidative injury in L02 cells via decreasing ROS and O2- generation, reducing MMP collapse, and attenuating GSH reduction, whereas the free NH samples were ineffective. Furthermore, the coated NH-NLs were more effective than that of uncoated nanoliposome. Overall, our study confirmed that P-CH-NH-NL was capable of reducing PA-induced hepatic oxidative injury. Therefore, the pectin-chitosan decorated nanoliposome can be considered as an efficient delivery system for enhancing cellular uptake of lipophilic compound with controlled release and greater biological activity.

Improving the physicochemical stability and functionality of nanoliposome using green polymer for the delivery of pelargonidin-3-O-glucoside.

This study aimed to improve the physicochemical stability of nanoliposome (NL) with enhanced functionality for the delivery of Pelargonidin-3-O-glucoside (P3G) using biopolymers, i.e. chitosan (CH) and pectin (P). In this study, we successfully developed stabilized liposomal carriers, i.e. CH-conjugated NL (CH-NL) and P-conjugated CH-NL (P-CH-NL) using an optimum concentration of CH (0.6 wt%) and P (0.5 wt%). Results revealed that P-CH-NL had better physical stability to salt and pH with maximum P3G retention (>97%) under oxidative, thermal, and UV conditions. Nanoliposomes were more stable under refrigerated-storage and ensured high P3G retention (>96%). In vitro mucoadhesion study revealed that CH-NL had better mucin adsorption efficiency (59.72%) followed by P-CH-NL and NL. Furthermore, CH-NL and P-CH-NL alternatively had better stability to serum than NL. Taken together, the stabilization of nanoliposome using chitosan and pectin can be a promising approach for the delivery of hydrophilic compounds in association with enhanced stability and functionality.

Surface decoration of neohesperidin-loaded nanoliposome using chitosan and pectin for improving stability and controlled release.

The aim of this study was to improve the physicochemical stability of neohesperidin (NH) using nanoliposomal encapsulation in association with surface decoration strategy employing chitosan (CH) and pectin (P). Different nanoliposomal systems, i.e. NH-loaded nanoliposome (NH-NL), CH-coated NH-NL (CH-NH-NL), and P-coated CH-NH-NL (P-CH-NH-NL) were characterized through DLS, HPLC, TEM, and FTIR. The results confirmed good encapsulation efficiency (>90%) and successful layer formation with nano-sized and spherical carrier. Both CH-NL and P-CH-NL exhibited better physicochemical stability than NL under storage, thermal, pH, ionic, UV, oxidative, and serum conditions. In vitro mucin adsorption study revealed that CH-NL (60%) was more effective in mucoadhesion followed by P-CH-NL (46%) and NL (41%). Furthermore, P-CH-NL showed better performance in NH retention under different food simulants compared to CH-NH-NL and NH-NL, in which the release was mainly governed by the diffusion process. Thus, the P-CH conjugated nanoliposome could be a promising nano-carrier for neohesperidin.

Colonic delivery of pelargonidin-3-O-glucoside using pectin-chitosan-nanoliposome: Transport mechanism and bioactivity retention.

Colon-targeted delivery is an active area of research as it can improve drug stability, bioactivity, and lessen the systematic toxicity. In this study, the colon-specific delivery of pelargonidin-3-O-glucoside (P3G) was investigated using pectin (P)/chitosan (CH)-functionalized nanoliposome (NL). The food simulant stability, transport mechanism, and bioactivity retention potential of carrier systems were studied. Results showed that polymer-coated nanoliposomes (P-CH-NL and CH-NL) improved the thermal and food simulant stability as well as enhanced the P3G retention during the in vitro digestion. The maximum P3G retention after enzymatic and non-enzymatic digestion was observed by P-CH-NL and the values were 47.5% and 57.5%, respectively. However, all nanoliposomal carriers followed Fickian diffusion mechanism both in in vitro food simulants and in vitro digestion models. Digested functionalized nanoliposomes revealed higher antioxidant properties after gastric digestion. Following by simulated intestinal fluid digestion, ABTS antioxidant activity of P-CH-P3G-NL was 12.52% and 6.31% higher than that of P3G-NL and CH-P3G-NL, respectively, while DPPH scavenging capacity of P-CH-P3G-NL was 5.57% and 1.86% greater than that of P3G-NL and CH-P3G-NL, respectively. Therefore, the developed functionalized nanoliposome can be useful for colon-targeted delivery and applicable in functional foods and/or beverages.

In vitro study of bioaccessibility, antioxidant, and α-glucosidase inhibitory effect of pelargonidin-3-O-glucoside after interacting with beta-lactoglobulin and chitosan/pectin.

Polysaccharides and fruit extracts are applied in dairy products to enhance their nutritional property, but the effects of such formulations on the functions and biological activities are yet to be explored. Therefore, this study was aimed at evaluating the effect of interactions among milk protein (beta-lactoglobulin; BLG), polysaccharides (pectin, P; chitosan, CH), and anthocyanin (pelargonidin-3-O-glucoside; P3G) in improving the bioavailability and biological activity of P3G. After gastrointestinal digestion (GID), the content of free P3G in different model solutions were as follows: P3G-alone (73.59 µg/mL), P3G-P (66.59 µg/mL), P3G-CH (36.72 µg/mL), P3G-BLG (64.92 µg/mL), P3G-P-BLG (64.92 µg/mL), and P3G-CH-BLG (39.61 µg/mL). Less amount of free P3G in model solutions indicated increased complex formation of P3G with protein and/or polysaccharides during GID. These complexes resulted in protection and progressive release of P3G in the gastrointestinal tract. Chitosan exhibited more protection to P3G compared with P and BLG. In addition, α-glucosidase inhibitory activity and ROS scavenging activities of conjugated-P3G samples were potentially augmented after GID. However, the presence of polysaccharides and protein in the model solutions did not show any negative effect on the biological activity of P3G. Thus, pure P3G can be used as a nutritional ingredient in dairy industries.