Biological fate, functional properties, and design strategies for oral delivery systems for cinnamaldehyde.

Cinnamaldehyde (CA) is the main bioactive component extracted from the internal bark of cinnamon trees with many health benefits. In this paper, the bioavailability and biological activities of cinnamaldehyde, and the underlying molecular mechanism are reviewed and discussed, including antioxidant, cardioprotective, anti-inflammatory, anti-obesity, anticancer, and antibacterial properties. Common delivery systems that could improve the stability and bioavailability of CA are also summarized and evaluated, such as micelles, microcapsules, liposomes, nanoparticles, and nanoemulsions. This work provides a comprehensive understanding of the beneficial functions and delivery strategies of CA, which is useful for the future application of CA in the functional food industry.

Interfacial crystallized oleogel emulsion with improved freeze-thaw stability and tribological properties: Influence of cooling rate.

In this study, the influence of cooling rate on the freeze-thaw stability, rheological and tribological properties of interfacial crystalized oleogel emulsion was investigated. Results showed that slower cooling rate could promote formation of larger crystals and stronger network in oleogels. Additionally, oleogel emulsions showed higher freeze-thaw stability than those stabilized solely by emulsifiers. The slower cooling rate resulted in larger crystals adsorbed at the droplet surface. This led to greater steric hindrance that prevented the migration of oil droplets with higher resistance to disruption by ice crystals. The rheological and tribological measurements suggested that with appropriate amount of crystals, the tribological properties were better maintained for emulsions prepared at slow cooling rate after freeze-thaw treatment. This strategy greatly enriched oleogel emulsion formulations and provided important clues for potential applications in food products involved with freeze-thaw treatment.

Piperine Attenuates Bmal1-Mediated Glucose Metabolism Disorder in a Trpv1-Dependent Manner in HepG2 Cells.

Piperine (PIP), a pungent alkaloid found in black pepper, has various pharmacological effects by activating the transient receptor potential vanilloid 1 (TRPV1) receptor. In this study, the regulating effect of PIP on glucose metabolism and the underlying mechanism were examined using an insulin-resistant cell model. Results showed that PIP alleviated glucosamine (GlcN)-induced glucose metabolism disorder (from 59.19 ± 1.90 to 88.36 ± 6.57%), restored cellular redox balance (from 148.43 ± 3.52 to 110.47 ± 3.52%), improved mitochondrial function (from 63.76 ± 4.87 to 85.98 ± 5.12%), and mitigated circadian disruption in HepG2 cells via the mediation of circadian clock gene Bmal1. After the knockdown of the Trpv1 gene, the modulating effect of PIP on Bmal1-mediated glucose metabolism was weakened, indicating that PIP alleviated Bmal1-involved insulin resistance and circadian misalignment in a Trpv1-dependent manner in HepG2 cells.

Bioavailability, Health Benefits, and Delivery Systems of Allicin: A Review.

Garlic has been used worldwide as a spice due to its pungent taste and flavor-enhancing properties. As a main biologically active component of the freshly crushed garlic extracts, allicin (diallyl thiosulfinate) is converted from alliin by alliinase upon damaging the garlic clove, which has been reported to have many potent beneficial biological functions. In this work, allicin formation, stability, bioavailability, and metabolism process are examined and summarized. The biological functions of allicin and potential underlying mechanisms are reviewed and discussed, including antioxidation, anti-inflammation, antidiabetic, cardioprotective, antineurodegenerative, antitumor, and antiobesity effects. Novel delivery systems of allicin with enhanced stability, encapsulation efficiency, and bioavailability are also evaluated, such as nanoparticles, gels, liposomes, and micelles. This study could provide a comprehensive understanding of the physiochemical properties and health benefits of allicin, with great potential for further applications in the food and nutraceutical industries.

A novel strategy for preparation of rice bran protein oleogels based on high internal phase emulsion template.

BACKGROUND: Oleogels have been extensively explored as fat substitutes with no trans fatty acids and low saturated fatty acids in recent years as a result of increased health problems found to be related to the intake of trans and saturated fatty acids. RESULTS: Herein, high internal phase emulsion (HIPE) stabilized by rice bran protein (RBP) was prepared and further utilized as a template for preparation of RBP oleogels. RBP HIPE with the strongest rheological properties was obtained at pH 5.0 as a result of appropriate structural deformation, surface charge and a high three-phase contact angle at this pH. However, RBP oleogels prepared at pH 9.0 exhibited the highest yield stress after drying process. At this pH, RBP showed higher resistance to deformation caused by water evaporation. This highlighted the importance of structural stability of protein network on rheological properties of the resultant oleogels. Furthermore, with an increase in drying temperature, RBP oleogels exhibited higher yield stress and gel strength because water was better removed as a result of an enhanced capability to overcome the capillary pressure of emulsion. CONCLUSION: The present study further revealed the structure-activity relationship between protein, HIPE and oleogel, and also provided theoretical support for the development of protein-based oleogel. © 2023 Society of Chemical Industry.

Construction of interfacial crystallized oleogel emulsion with improved thermal stability.

In this study, we reported a facile strategy to produce an interfacial crystallized oleogel emulsion for improved thermal stability. The interfacial crystallization of ceramide (non-interfacial active oleogelator) was achieved by addition of a surface active compound, which was demonstrated by interfacial rheology tests and polarized light microscopy. For successfully prepared interfacial crystallized emulsions, smaller particle size was observed when the gelator concentration was lower. However, better thermal stability was achieved when oleogelator concentration was higher than 1 wt%. Results from differential scanning calorimetry, X-ray diffraction and Fourier transform infrared spectroscopy suggested that the interfacial adsorption of ceramide was due to its co-crystallization with the emulsifier driven by hydrogen bonds formed by multiple sites. It provided appropriate crystallinity and steric repulsion for oleogel emulsions against oil droplet coalescence during heating process. This strategy greatly enriches oleogel emulsion formulations and their potential applications in food products involved with thermal treatment.

Piperine Improves Lipid Dysregulation by Modulating Circadian Genes Bmal1 and Clock in HepG2 Cells.

Metabolic disorders are closely associated with the dysregulation of circadian rhythms. Many bioactive components with lipid metabolism-regulating effects have been reported to function through circadian clock-related mechanisms. As the main pungent principle of black pepper, piperine (PIP) has been demonstrated to possess anti-obesity bioactivity by affecting hepatic lipid metabolism-related factors. However, whether the circadian clock genes Bmal1 and Clock are involved in the protective effect of PIP against lipid metabolism disorders remains unknown. In this work, oleic acid (OA) induced lipid accumulation in HepG2 cells. The effect of PIP on redox status, mitochondrial functions, and circadian rhythms of core clock genes were evaluated. Results revealed that PIP alleviated circadian desynchrony, ROS overproduction, and mitochondrial dysfunction. A mechanism study showed that PIP could activate the SREBP-1c/PPARγ and AMPK/AKT-mTOR signaling pathways in a Bmal1/Clock-dependent manner in HepG2 cells. These results indicated that Bmal1 and Clock played important roles in the regulating effect of PIP on hepatic lipid homeostasis.

Capsaicin Attenuates Oleic Acid-Induced Lipid Accumulation via the Regulation of Circadian Clock Genes in HepG2 Cells.

As the major component in red chili peppers, capsaicin is useful in the prevention of lipid metabolism disorders. In this study, the attenuation effect of capsaicin on oleic acid (OA)-induced lipid accumulation in HepG2 cells was evaluated with respect to circadian clock gene expressions. Lipid profiles, including triacylglycerols, total cholesterols, high-density lipoproteins, low-density lipoproteins, and aspartate aminotransferase content, were measured using enzymatic assay kits. The mitochondrial membrane potential, cellular redox status, and lipid droplet morphology were also determined using different assay kits and staining methods. The mRNA and protein expressions of core circadian clock genes and major lipometabolism-related factors were assessed using RT-qPCR and western blotting. Results showed that 50 µM capsaicin alleviated the circadian desynchrony and inhibited OA-induced ROS overproduction (from 166.44 ± 12.63% to 119.90 ± 5.43%) and mitochondrial dysfunction (from 0.60 ± 0.08 to 0.83 ± 0.09, represented by the red/green fluorescence ratio) in HepG2 cells. The amelioration effect of capsaicin on OA-induced lipid accumulation was weakened after Bmal1-knockdown, demonstrating that the rhythmic expression of the circadian clock gene is involved in the regulation process of capsaicin in lipid metabolism.

Health benefits of dietary chronobiotics: beyond resynchronizing internal clocks.

The internal circadian clock in mammals drives whole-body biological activity rhythms. The clock reflects changes in external signals by controlling enzyme functions and the release of hormones involved in metabolic processes. Thus, misalignments between the circadian clock and an individual's daily schedule are recognized to be related to various metabolic diseases, such as obesity and diabetes. Although evidence has shown the existence of a complex relationship between circadian clock regulation and daily food intake, the regulatory effects of phytochemicals on the circadian clock remain unclarified. To better elucidate these relationships/effects, the circadian system components in mammals, circadian misalignment-related metabolic diseases, circadian rhythm-adjusting phytochemicals (including the heterocycles, acids, flavonoids and others) and the potential mechanisms (including the regulation of clock genes/proteins, metabolites of gut microbiota and secondary metabolites) are reviewed here. The bioactive components of functional foods discussed in this review could be considered potentially effective factors for the prevention and treatment of metabolic disorders related to circadian misalignment.

Modified citrus pectins by UV/H2O2 oxidation at acidic and basic conditions: Structures and in vitro anti-inflammatory, anti-proliferative activities.

Two modified citrus pectins, MCP4 and MCP10, were prepared by UV/H2O2 treatment at pH 4 and pH 10, respectively, and their structures were characterized. MCP10 had a rhamnogalacturonan-I (RG-I) enriched backbone with a high degree of branching (DB ∼61 %) and a low methoxylation degree (24 %). MCP4 had a homogalacturonan enriched backbone with a high degree (46 %) of methoxylation and a low DB (∼41 %) of RG-I branches. MCP10 exhibited a higher anti-inflammatory activity than MCP4 in suppressing the NF-κB expression and the production of pro-inflammatory factors TNF-α and IL-1ß of THP-1 cells stimulated by lipopolysaccharide. MCP10 also showed a stronger inhibitory effect on Caco-2 cell proliferation. The stronger bioactivities of MCP10 may be attributable to the abundant branches and the proper length of terminal galactan residues attached to the RG-I domain.

Capsaicin-the major bioactive ingredient of chili peppers: bio-efficacy and delivery systems.

Capsaicin is the primary bioactive substance in red chili peppers, which produces the pungent flavor. During the past few decades, pharmacological benefits of capsaicin and its underlying mechanisms have been examined extensively. In this paper, major biological efficacies of capsaicin are reviewed, including analgesic, antioxidant, anti-inflammatory, anti-cancer, anti-obesity, cardio-protective, and metabolic modulation effects. Novel delivery systems, such as liposomes, micelles, micro/nano-emulsions, colloidal capsules and solid nanoparticles, for enhancing the oral bioavailability of capsaicin are also evaluated depending on the stability, encapsulation efficiency and biological properties. This review provides a theoretical basis for capsaicin to be further developed into a multi-functional ingredient with health-promoting functions in the nutraceutical industry.

Capsaicin Ameliorates the Redox Imbalance and Glucose Metabolism Disorder in an Insulin-Resistance Model via Circadian Clock-Related Mechanisms.

Circadian rhythms are closely associated with metabolic homeostasis. Metabolic disorders can be alleviated by many bioactive components through controlling of clock gene expressions. Capsaicin has been demonstrated with many beneficial effects including anti-obesity and anti-insulin resistance activities, yet whether the rhythmic expression of circadian clock genes are involved in the regulation of redox imbalance and glucose metabolism disorder by capsaicin remains unclear. In this work, the insulin resistance was induced in HepG2 cells by treatment of glucosamine. Glucose uptake levels, reactive oxygen species, H2O2 production, and mitochondrial membrane potential (MMP) were measured with/without capsaicin cotreatment. The mRNA and protein expressions of core circadian clock genes were evaluated by RT-qPCR and western blot analysis. Our study revealed that circadian misalignment could be ameliorated by capsaicin. The glucosamine-induced cellular redox imbalance and glucose metabolism disorder were ameliorated by capsaicin in a Bmal1-dependent manner.

Extraction, bioavailability, and bioefficacy of capsaicinoids.

Capsaicinoids are active constituents responsible for the pungent and spicy flavor in chili peppers. During the past few decades, various extraction methods of capsaicinoids from peppers have been developed with high yields. Through biological studies, pharmacological benefits have been reported such as pain relief, antiinflammation, anticancer, cardio-protection, as well as weight loss. In this paper, the extraction methods and bioavailability of capsaicinoids are reviewed and discussed. In addition, the pharmacological effects and their underlying mechanisms are also studied.