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Capsaicin ameliorates diet-induced disturbances of glucose homeostasis and gut microbiota in mice associating with the circadian clock.

The unique role of the spatial distribution of crystallizable emulsifiers in regulating the structure and properties of double emulsions has been gradually recognized. Herein, we utilized crystallizable monoglycerides of different carbon chain length (GMS/GMP/GML) to "structuring" the intermediate oil phase of double emulsions during a two-stage emulsification process followed by a cooling treatment. A ternary eigenvector (I, M, E) based on the numerical processing of polarization images was invented to quantitatively characterize the distribution pattern of monoglycerides. Crystallization kinetics analysis and dissipative particle dynamic simulation were then employed to reveal the regulatory mechanism for the site-specific interface distribution behavior. Results suggested that the distribution pattern of monoglycerides could be pricesly tuned as the internal interface-, external interface- or oil-phase dominated one in double emulsions. The surface activity as well as crystallization rates of monoglycerides dominated the interfacial distribution kinetics, and the cooling gradient along the interface region further regulated their interfacial distribution potential. Specificly, shorter crystallization time (t

Double emulsions (DEs) are promising delivery vehicles for the protective and programmed release of bioactive compounds. Herein, DEs with monoglycerides crystallized at the internal- or external interface or oil phase were fabricated. The results suggested that the crystallization site of monoglycerides exerts a significant role in retarding the structural degradation and lipid digestion of DEs by affecting the available contact area of lipase. At the initial stage of intestinal digestion, compared with noncrystalline DEs (82.1%, 3.7 min), the burst release of internal markers in the internal interface crystallized emulsions was decreased by 42.4% and the lag time of free fatty acid (FFA) release was delayed by 5.8 min in the external interface crystallized emulsions. The structural integrity and digestion kinetics of the external interface crystallized DEs were synchronized with the retention time of the interfacial crystals. Therefore, crystallizable emulsifiers exhibit unique and fine regulatory effects on the digestive properties of emulsions.

BACKGROUND The development of lipid-lowering products has become the focus of food industry due to increasing consumer awareness of the relationship between diet and health. Recently, edible oleofoams have drew attention due to their enormous potential in reformulating food products with reduced fat content and unique mouth feel. RESULTS We have developed an edible oleofoam system by whipping oleogel composed of fatty acids mixtures in sunflower oil. The crystal morphology, gelation properties, and foaming properties of these oleogels could be tailored by changing the ratio of stearic acid (SA) and myristic acid (MA). Specifically, SA:MA = 2:8 (2S8M) was demonstrated to have superior foaming capability and foam stability, likely due to the densely packed and uniformly distributed crystals formed at this fatty acid ratio. Small lipid crystals in 2S8M absorbed to the A/O interface more efficiently, and together with the strengthened network established in the bulk phase, helped stabilize the foam structure. As a result, the 2S8M oleofoam showed excellent foaming properties: strong plasticity, significantly increased overrun (up to 63.56 ± 2.58%), and significantly improved foam stability. The XRD results indicated that the diffraction pattern observed for 2S8M samples at d-spacing of 4.20 a and 3.79 a was related to the characteristic peak of β' type crystals, which were responsible for the enhanced foaming capability of 2S8M oleogels. Oleophobic property of 2S8M increased, as indicated by wettability in oil phase, which could possibly drive crystals to the air/oil interface. CONCLUSIONS These results highlighted the importance of lipid crystal morphology in determining the whippability of oleogels. This article is protected by copyright. All rights reserved.

There is increasing interest in the development of oleogel-based emulsions. However, they usually contained surfactants for stabilization, especially small-molecular weight surfactants, which may have adverse health impacts.Herein, a surfactant-free oleogel-based emulsion stabilized by co-assembled ceramide/lecithin (CER/LEC) crystals was developed. The formation and stabilization mechanisms were explored. The different molar ratios of gelator (LEC and CER) in emulsions resulted in different crystal morphology, crystallinity as well as different emulsion properties. This suggested that appropriate crystallinity, crystal size, and interfacial distribution of these crystals provided higher surface coverage against droplets coalescence, thus better emulsion stabilization. Both X-ray diffractograms and contact angle results confirmed that the crystals which were primarily responsible for emulsion stabilization, are co-assembled crystals consisted of both gelators (CER and LEC). Furthermore, the percentage of free fatty acids (FFAs%) results revealed a negative relationship between lipid digestibility and crystal concentration.This strategy greatly enriched surfactant-free oleogel-based emulsion formulations, as well as their potential applications in healthy lipid-based products and novel food delivery systems with controlled lipid digestibility. © 2022 Society of Chemical Industry.

BACKGROUND As an edible and medicinal herb in Chinese folk medicine, Cyclocarya paliurus (Batal.) Iljinskaja leaves are traditionally widely used in the treatment of metabolic disorders. The vegetable Momordica charantia L. has been consumed worldwide for thousands of years as a traditional drug due to its activities against obesity and diabetes. In view of the therapeutic value of Momordica saponins (MSs) and C. paliurus polysaccharides (CPPs), an independently developed MSs- and CPPs-containing beverage (MC) was evaluated for its efficacy in controlling oxidative stress and obesity in Caenorhabditis elegans. RESULTS First, we found that MC could promote the nuclear localization of DAF-16 and the translation of SOD-3. Further exploring its antioxidant properties, the oxidative stress by-products reactive oxygen species, malondialdehyde, and nonesterified fatty acids were significantly inhibited in C. elegans. Moreover, damage due to diseases related to oxidative stress (age pigments and neurodegenerative diseases) was alleviated. Furthermore, fat accumulation was significantly reduced in normal and high-fat models. Finally, the lipid-lowering effects of MC might involve reductions in the size and number of lipid droplets without impairing basic physiological functions in C. elegans. CONCLUSION These results provide promising data indicating MC as an innovative health beverage for the pharmacological management of oxidative stress and obesity. © 2020 Society of Chemical Industry.

The present study investigates the effect of oil type on the formation, morphology and mechanical properties of phytosterol-based organogels. The formation of organogels can be satisfactorily predicted with a criterion based on Hansen Solubility Parameters (HSPs), provided that the sterol and sterol ester in these systems assemble as tubules. When structures other than tubules are formed, the predictability of the HSP-based criterion becomes void. In cases where organogelling occurred, the morphology and mechanical properties of the tubular network of the gels and water-in-oil emulsions were investigated. The findings revealed that the structure of the tubular network formed in oils with different compositions, could be grouped based on the dielectric constants of the oils. Curly and bundled tubules which formed networks, were observed in gels prepared with low dielectric constant oils (i.e. decane and limonene). For oils with a moderate dielectric constant (i.e. castor oil and sunflower oil), the tubules became less curly and straighter. Upon increasing the dielectric constant of the oil (eugenol), individual tubules were observed next to the bundled tubules. The results showed that straighter, bundled tubules are associated with firmer gels, whereas less straight (i.e. curly) tubules rendered weaker gels. The tubular network of the water-in-oil emulsions obtained for oils with a low dielectric constant appeared more open with straighter tubules. For oils with relatively high dielectric constant, the water-in-oil emulsions lost most of their tubular structure and only a few tubules could be observed. In the presence of emulsion droplets fewer tubules are formed, resulting in weaker networks.

5-Demethylnobiletin (5DN) is a unique flavonoid mainly found in citrus fruits. In this study, we determined the chemopreventive effects of 5DN and its major colonic metabolites on both a colitis-driven colon carcinogenesis mouse model and a human colon cancer cell model. In azoxymethane/dextran sulfate sodium-treated mice, dietary 5DN (0.05% w/w in the diet) significantly decreased the tumor incidence, multiplicity and burden, and showed potent anti-proliferative, proapoptotic, and anti-inflammatory activities in mouse colon tissue. Three major metabolites of 5DN, named 5,3'-didemethylnobiletin (M1), 5,4'-didemethylnobiletin (M2) and 5,3',4'-tridemethylnobiletin (M3), were found in the colonic mucosa of 5DN-treated mice, and the combined level of these metabolites in mouse colonic mucosa was 1.56-fold higher than that of 5DN. Cell culture studies revealed that 5DN and its colonic metabolites profoundly inhibited the growth of human colon cancer cells by inducing cell cycle arrest, triggering apoptosis and modulating key signaling proteins related to cell proliferation and apoptosis. Importantly, the colonic metabolites, especially M1, showed much stronger effects than those produced by 5DN itself. Overall, our results demonstrated that dietary 5DN significantly inhibited colitis-driven colon carcinogenesis in mice, and this chemopreventive effect was associated with its metabolites in the colon.

A mixture of ceramide (CER) and lecithin (LEC) at specific ratios was capable of forming oleogels in sunflower oil triggered by adding a trace amount of water. It was noted that the addition of water at different temperatures (TW) resulted in different gelation behaviors and microstructures. To better illuminate the assembly mechanism at different TW, samples with water added at different TW (20 °C, 45 °C, 70 °C and 95 °C) were prepared. The viscoelastic properties, microstructures, and the crystal packing of these samples were investigated. It was observed that all samples prepared at TW of 20 °C and 95 °C formed gels, while most samples prepared at TW of 45 °C and 70 °C were too weak to form gels. Gels prepared at 95 °C were stronger but more fragile in texture compared to gels produced at 20 °C. The crystal morphology of gels drastically changed with TW. Spindle-shaped crystals were observed in gels prepared at low TW (20 °C), while gels prepared at high TW (95 °C) exhibited a network with packed oil droplets stabilized by lamellar shells together with fibrillar crystals in the bulk phase. X-ray diffractograms showed a different reflection peak (d-spacing of 14.5 Å) in gel prepared at 20 °C, compared to the d-spacing in oleogels with a single gelator (13.14 Å and 15.33 Å, respectively, for CER and LEC). Gel prepared at 95 °C showed two long-spacing characteristic peaks, which correspond to the characteristic peaks of CER gel (∼13 Å) and LEC gel (∼12 Å). Fourier transform infrared spectroscopy results indicated that the different gelation behaviors at different TW were mainly caused by vibrational changes in the amide bond of CER. Our hypothesized assembly mechanism can be concluded as: increasing TW resulted in the conversion of CER and LEC crystallization from co-assembly (TW = 20 °C) to self-sorting by individual gelators (TW = 95 °C). In this study, novel water-induced oleogels were produced by manipulating TW, and such information further assists the rational design of lipid-based healthy fat products.

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.

In this study, the influence of non-isothermal conditions on multi-component oleogel (lecithin, LEC and ceramide, CER) was systematically investigated by rheological characterization, polarized light microscopy, and differential scanning calorimetry. Jeziorny and Mo models were applied to reveal the crystallization behavior. When the cooling rate increased, the LEC/CER oleogel exhibited lower G' and larger crystal size. The crystallization kinetics showed that at lower cooling rate, the LEC/CER co-assembled crystals grew at 2-3 dimensions by one step crystallization process. While at high cooling rate, the crystals first grew at 1-2 dimensions through self-assembly of CER. Then, the primary CER crystals served as nuclei for further co-assembly of CER/LEC growing in 2-3 dimensions. Our findings indicated that the cooling rate not only modulated the crystal structure and physical properties, but also the assembly mechanism of multi-component oleogels. Such information is useful for engineering the functional properties of oleogel-based lipidic materials.

Abnormal glucose homeostasis is linked to a variety of metabolic syndromes, such as insulin resistance, obesity, type-2 diabetes mellitus, hypertension and cardiovascular diseases. Maintenance of normal glucose homeostasis is important for the body to keep normal biological functions. As the major bioactive ingredient in chili peppers responsible for the pungent flavor, capsaicin has been reported to effectively improve glucose homeostasis with low cytotoxicity. In this review, the modulating effects of capsaicin on glucose homeostasis in cell models, animal models and human trials are summarized through both TRPV1 dependent and TRPV1 independent pathways. The relevant molecular mechanisms underlying its regulatory effects are also evaluated. Understanding the effects and mechanisms of capsaicin on glucose metabolism could provide theoretical evidence for its application in the food and pharmaceutical industries.

Simple Summary For the first time, this study investigated the extraction of bioactive substances with different polarities from immature honey pomelo fruit (IPF), a by-product of pomelo planting processing that causes resource waste and environmental pollution, using novel continuous phase transition extraction technology (CPTE). The results showed that CPTE was suitable for extracting essential oil, naringin, and pectin in sequence according to their polarities. The naringin extraction process was optimized by the response surface methodology, resulting in an extract ratio up to 99.47%. Moreover, the pectin extracted from IPF by CPTE showed better quality compared to commercial counterparts, as evidenced by lower protein and ash contents and higher white value. Together, these results suggested that CPTE could be a promising technology to improve the application value of IPF. For instance, the extracted bioactive components can be utilized as nutraceutical food ingredients. The scientific insights from this study will contribute to the development of functional food ingredients and comprehensive utilization of farming by-products. Abstract The immature honey pomelo fruit (IPF) is a huge agro-industrial by-product generated during pomelo planting. Although IPF is rich in nutrients, more than 95% of IPF is discarded annually, which causes resource waste and a serious environmental problem. Here, we report a novel continuous phase transition extraction technology (CPTE) to improve the comprehensive utilization of IPF by sequentially generating high value products and solve pollution problems related to their disposal. First, essential oil was successively extracted by CPTE at a yield of 1.12 ± 0.36%, in which 43 species were identified. Second, naringin extraction parameters were optimized using the response surface methodology (RSM), resulting in a maximum extraction rate of 99.47 ± 0.15%. Finally, pectin was extracted at a yield of 20.23 ± 0.66%, which is similar to the contents of commercial pectin. In conclusion, this study suggested that IPF was an excellent potential substrate for the production of value-added components by CPTE.

Ceramide (CER) is a highly effective organogelator with numerous health implications. Lecithin (LEC) is often used as a crystal modifier to improve gel properties. It was found in this study that in the presence of a small amount of water, CER and LEC self-assembled at specific ratios and form oleogels in sunflower oil (SFO), and the structure of which differed from any of the mono-component gel structures. To the best of our knowledge, this is the first water-induced multi-component oleogelation reported to date. To clarify when gelation occurs, a phase diagram of the four-component system SFO/CER/LEC/water was established and characterized. In the gel region, confocal laser scanning microscopy revealed that water was evenly distributed in the self-assembled microstructure. To clarify the vital role of water in formation of stable gel, a series of samples with varying ratios in CER and LEC with and without water were explored. The thermal properties, viscoelastic properties, microstructures, as well as crystal packing were investigated. With water added, the microscopic structures of CER/LEC gels changed from three-dimensional dendritic crystals to two-dimensional rod-like or platelet-like crystals, which are more effective at structuring liquid oil. A different reflection was observed (d-spacing of 14.9 Å), suggesting the rearrangement in crystal packing of ceramide and lecithin molecules, compared to the d-spacing in oleogels with single gelator (13.1 Å and 15.3 Å, respectively for ceramide and lecithin). Fourier transform infrared spectroscopy results indicated the presence of interaction between water and gelators, which confirmed the importance of water in self-assembly of this mixed-gelator system. Water-induced conversion of oleogelation provides alternatives in producing hard-stock fat replacers as well as possibilities to incorporate water-soluble nutrients into oil-based products.

In this study, it was discovered for the first time that oleogel can be prepared via a facile, low temperature process through rice bran protein (RBP) foam-templates. The RBP foams were freeze-dried to create a highly porous cryogel, which could physically absorb liquid oil and form an oleogel with strong mechanical strength. It was observed that both the foamability and foam stability of RBP were significantly enhanced when the pH was far from the isoelectric point (pH 4.6), which was mostly determined by change in the secondary structure and surface hydrophobicity of RBP. The foams prepared at higher pH (7.0, 9.0 and 11.0) showed excellent foaming capability. Scanning electric microscopy results showed that the corresponding cryogels exhibited dense and uniform porous networks with superior oil absorption ability (up to 18.39 g rice bran oil/g RBP cryogel). The foam prepared at pH 3.0 showed a particularly high foam stability, due to formation of a strong interfacial film filled with tiny bubbles. However, the corresponding cryogel was less efficient in oil absorption due to less porous structure after freeze dried. The resulting oleogels showed high G′ (up to 1.5 × 105 Pa) and yield stress (up to about 1000 Pa), indicating a strong interaction between the cryogel and rice bran oil. The gel strength of oleogel was inversely correlated to oil absorption rate of the corresponding cryogels. This work provides a novel route for fabrication of foam-templated oleogels with RBP as the sole structurant, which were great candidates for hard-stock fat replacement with zero trans fatty acid and low saturated fatty acids.

Ceramide (CER) is a novel food-grade organogelator with beneficial health effects. Lecithin (LEC) is not an effective gelator; however, it may alter the crystal morphology of the host gelator in a multicomponent system. In this paper, LEC and CER were mixed at various molar ratios in sunflower oil leading to different gelation behaviors. It was interesting since in this multicomponent system, gels formed when there was more less-effective gelator (LEC), while gels hardly formed when there was more effective gelator (CER). This drew our attention since there might not be only one kind of assembly mode between the LEC and the CER. A comprehensive rheological investigation was conducted. It was found that at specific ratios (6L4C and 5L5C), strong gels (G' > 1.0 × 105 Pa) formed with superior oil binding capacity (up to 99.84%). Meanwhile, these gels exhibited higher tolerance level to permanent deformation than the monocomponent gel. However, weak gels were observed off the optimal ratio (8L2C, 7L3C, 4L6C and 3L7C). The crystal morphology of gels drastically changed with change in gelator proportion. Short needle-like crystals and small rosette crystals were observed in 6L4C and 5L5C, respectively, while other samples exhibited spherulite-shaped crystals (8L2C, 7L3C, 4L6C, and 3L7C), which differed from any of the monocomponent gel structures (10L0C and 0L10C). Results from differential scanning calorimetry and polarized light microscopy suggested that the macroscopic properties are determined by the morphology and distribution of crystals rather than the crystallinity of the matrix. Fourier transform infrared spectroscopy results indicated the presence of van der Waals forces and the formation of hydrogen bonding between the phosphate of the LEC and the amide group of the CER. The above results indicated that the LEC and CER co-assembled at approximately equal molar ratio, and the redundant LEC or CER at other ratios self-sorted to combine with the co-assembled fibers by lateral association, leading to potentially different underlying microstructures. These multicomponent supramolecular oleogels with high tunability may further broaden their applicability in various healthy lipid-based product formats.

Obesity and overweight have become serious health problems in the world and are linked to a variety of metabolic disorders. Phytochemicals with a weight-loss effect have been widely studied for the past few decades. Capsaicin is the major bioactive component in red chili peppers with many beneficial functions. Its anti-obesity effects have been evaluated extensively using different model systems, including cell models, animal models and human subjects. In this paper, anti-obesity effects of capsaicin are reviewed and the underlying mechanisms are characterized.

Tangeretin (TAN) exhibited antilipogenic, antidiabetic, and lipid-lowering effects. However, the lipid biomarkers and the underlying mechanisms for antiobesity and cholesterol-lowering effects of TAN have not been sufficiently investigated. Herein, we integrated biochemical analysis with lipidomics to elucidate its efficacy and mechanisms in high-fat diet-fed rats. TAN at supplementation levels of 0.04 and 0.08% not only significantly decreased body weight gain, serum total cholesterol, and low-density lipoprotein cholesterol levels but also ameliorated hepatic steatosis. These beneficial effects were associated with the declining levels of fatty acids, diacylglycerols (DGs), triacylglycerols, ceramides, and cholesteryl esters by hepatic lipidomics analysis, which were attributed to downregulating lipogenesis-related genes and upregulating lipid oxidation- and bile acid biosynthesis-related genes. Additionally, 21 lipids were identified as potential lipid biomarkers, such as DGs and phosphatidylethanolamines. These findings indicated that the modulation of lipid homeostasis might be the key pathways for the mechanisms of TAN in the antiobesity and cholesterol-lowering effects.

In vivo studies measuring true fractional calcium (Ca) absorption have shown that dietary fat is a significant predictor of absorption and is influenced by luminal pH levels. However, whether changes in Ca bioaccessibility (CaB) can explain the effects on absorption has not been examined. In the current study, we examined two high fat diets enriched in either monounsaturated fatty acids or saturated fatty acids (SFA), and a low-fat diet (LFD), each with 50 mg Ca, and measured CaB at different intestinal regions during normal acidic or higher (pH = 7) gastrointestinal conditions using an in vitro gastrointestinal model. During normal pH conditions in the jejunum, there was an interaction between diet and time for CaB (P < 0.02), and CaB during the SFA diet was higher than LFD (P = 0.05). CaB was reduced by 90 ± 3% during higher compared with normal pH under all dietary conditions (P < 0.001). These findings indicate that fat intake, especially SFA enriched, is associated with a greater CaB in the jejunum, and may explain the higher Ca absorption in previous studies. In addition, the marked reduction in CaB under higher pH conditions could have implications in persons taking medications to reduce gastric acid.

The optimal conditions for preparation of egg white peptides-calcium chelate (EWPs-Ca) were determined by response surface methodology (RSM). Under the optimal condition (mass ratio of peptide: calcium of 4:1 at 53 °C and pH 8.2 for 30 min), the calcium content of EWPs-Ca was 44.1 mg/kg. The results of Ultraviolet–Visible absorption spectroscopy (UV) and Fourier transform infrared spectroscopy (FTIR) indicated that the carboxyl oxygen and amino nitrogen atoms of the egg white peptides (EWPs) may chelate with calcium during the chelation. Amino acid analysis suggested that glutamate, aspartic acid, cysteine, threonine, glycine and lysine played important roles during the chelation. The scanning electron microscopy showed that due to EWPs combined with calcium, the structure of EWPs-Ca became loose porous sponge. Moreover, the amount of transferred calcium of EWPs-Ca was 46.18 ± 2.12, 63.86 ± 0.36, 106.91 ± 0.44, 123.61 ± 1.59 μg/mL at 30, 60, 120, 180 min in Caco-2 cell monolayers, respectively. Compared with the blank control, the proliferation rate of Human fetal osteoblast (HFOB) cells reached the maximum value of 119.55 ± 1.36%, 110.20 ± 1.56% and 112.58 ± 1.62% at 24, 48 and 72 h, respectively and EWPs-Ca also improved the activity of alkaline phosphatase (ALP).

Jackfruit (Artocarpus heterophyllus Lam.) is an underutilized edible fruit in the tropics and subtropics. The aim of this study was to explore the chemical composition, antioxidant capacity and cytoprotective effects of jackfruit extracts. Based on DPPH assay, it was found that jackfruit axis extract showed the strongest antioxidant activity, and 53 main compounds were identified by the HPLC-MS/MS. The extract showed excellent antioxidant activities in DPPH (IC50 = 2.871 mg/mL), ABTS (IC50 = 0.259 mg/mL), ferrous ion chelation (IC50 = 2.164 mg/mL) and ORAC (48.19 μmol of TE) assays. The CAA assay showed that the extract possesses a potent antioxidant activity (EC50 = 2.074 μg/mL) in HepG2 cells. Additionally, 70 μg/mL jackfruit axis extract protected cells against alcohol-induced cytotoxicity and its protection was even more efficacious than that of vitamin C. Overall, these results indicated that the jackfruit axis extract has great potential for use as functional foods.

The ability of casein phosphopeptides (CPPs) to bind and transport minerals has been previously studied. However, the single bioactive peptides responsible for the effects of CPPs have not been identified. This study was to purify calcium-binding peptides from CPPs and to determine their effects on calcium and magnesium uptake by Caco-2 cell monolayers. Five monomer peptides designated P1 to P5 were isolated and the amino acid sequences were determined using LC-MS/MS. Compared with the CPP-free control, all five monomeric peptides exhibited significant enhancing effects on the uptake of calcium and magnesium (P0.05). Interestingly, when calcium and magnesium were presented simultaneously with P5, magnesium was taken up with priority over calcium in the Caco-2 cell monolayers. For example, at 180 min, the amount of transferred magnesium and calcium was 78.4 ± 0.95 μg/well and 2.56 ± 0.64 μg/well, respectively, showing a more than 30-fold difference in the amount of transport caused by P5. These results provide novel insight into the mineral transport activity of phosphopeptides obtained from casein.

Oenothein B (OeB), a dimeric macrocyclic ellagitannin isolated from eucalyptus leaves has been demonstrated as a promising natural bioactive compound for its remarkable antitumor, antioxidant, anti-inflammatory and immunomodulating effects. Unfortunately, early study indicates that OeB has quite low bioaccessibility for oral consumption due to their susceptibility to decomposition both in vitro and in vivo. Herein, we report the design and synthesis of food-grade polyelectrolyte complex coacervate using caseinophosphopeptides (CPPs) and chitosan (CS) to encapsulate OeB for enhanced protection through gastrointestinal (GI) tract. Turbidimetric titration, dynamic light scattering (DLS), ζ-potential and scanning electric microscopy (SEM), as well as theoretical calculations based on principle of charge neutralization, were conducted to provide tentative and quantitative description for phase behavior in formation and disassociation of the complex. The optimum fabrication conditions were found to be at pH 5.5, with CPP : CS at 1 : 1, using CS of high molecular weight (980 kDa). The genipin cross-linking protected the system from disassembling in harsh acidic environments. The best cross-linking conditions were found to be 0.6 mg ml−1 genipin addition at 4 h cross-linking reaction time. The particle size and zeta potential of the nanoparticles varied from 200 to 300 nm and +20 to +24.2 mV, respectively. Scanning electron microscopy (SEM) revealed a spherical coacervate phase. Results from in vitro release study proved that controlled release of OeB through GI tract using CPP–CS nanoparticles cross-linked with genipin was achievable.

Peptides are a promising class of gelators, due to their structural simplicity, biocompatibility and versatility. Peptides were synthesized based on four amino acids: leucine, phenylalanine, tyrosine and tryptophan. These peptide gelators, with systematic structural variances in side chain structure and chain length, were investigated using Hansen solubility parameters to clarify molecular features that promote gelation in a wide array of solvents. It is of utmost importance to combine both changes to structural motifs and solvent in simultaneous studies to obtain a global perspective of molecular gelation. It was found that cyclization of symmetric dipeptides, into 2,5-diketopiperazines, drastically altered the gelation ability of the dipeptides. C-L-LL and C-L-YY, which are among the smallest peptide LMOGs reported to date, are robust gelators with a large radius of gelation (13.44 MPa1/2 and 13.90 MPa1/2, respectively), and even outperformed L-FF (5.61 MPa1/2). Interestingly, both linear dipeptides (L-FF and L-LL) gelled similar solvents, yet when cyclized only cyclo-dityrosine was a robust gelator, while cyclo-diphenylalanine was not. Changes in the side chains drastically affected the crystal morphology of the resultant gels. Symmetric cyclo dipeptides of leucine and tyrosine were capable of forming extremely high aspect ratio fibers in numerous solvents, which represent new molecular motifs capable of driving self-assembly.

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.

In this study, the influence of crystal morphology and cooling temperature on the oxidative stability of oleogel-structured perilla oil emulsion was explored. The formation and distribution of the internal crystals were confirmed by differential scanning calorimetry and polarized light microscopy. All beeswax (BW) crystals existed in the internal phase while stearic acid (SA) crystals appeared in the aqueous phase as well. As the crystal grew, the HPMC/SDS emulsified layers were pierced, leading to release of the SA crystals into the aqueous phase with partial droplet flocculation. As a result, the physical and oxidative stability of the BW-structured emulsion was significantly better than that of SA-structured emulsion. The crystallinity of the emulsion increased with higher gelator concentration. The denser crystal network were more effective preventing the penetration of pro-oxidants into the internal phase, resulting in the stronger the oxidation stability. Processing methods with different cooling temperature affected more of the properties of bulk oleogels rather than the oleogel-structured emulsion for long-term storage. Overall, choosing a gelling agent that forms relatively small crystals and preparing an oleogel-structured emulsion with appropriate crystallinity can effectively improve the oxidative stability of structured emulsion with longer shelf life.

Guava leaf flavonoids were obtained using a simple extraction method to evaluate their anti-hyperglycemic and liver protective effects with a high-fat diet and a low-dose streptozotocin induced diabetic mouse model. Flavonoids supplementation significantly decreased fasting plasma glucose, glucose tolerance, and the insulin resistance index in diabetic mice, lowered the serum total cholesterol, triacylglycerol, and low-density lipoprotein cholesterol compared to the diabetic control group (p

Ethnopharmacological relevance Phyllanthus emblica L. (P. emblica) as a medical plant has been used to treat diseases in Asia. It is famous for a wide range of biological activities, especially for its antioxidant and anti-inflammatory activity. However, quality control underlying the bioactivity of P. emblica fruits remains to be studied. Materials and methods In this study, we evaluated the HPLC fingerprint and bioactivity of polyphenols extracted from P. emblica fruits grown in different habitats. Results P. emblica fruits collected from 10 different habitats in Guangdong, Fujian, Yunnan, and Guangxi provinces in China were used to establish a simple and reliable HPLC fingerprint assay. Simultaneous quantification of three monophenols was also performed to determine assay quality and consistency. Additionally, chemical assessment of the different ethanolic extract (PEEE) from 10 P. emblica fruits demonstrated that they exhibited antioxidant activity by enhancing reducing power and total antioxidant capacity, scavenging hydroxyl radical and superoxide anion. PEEE protected RAW264.7 cells from oxidative damage by increasing glutathione content and total superoxide dismutase activity, suppressing MDA content. PEPE also alleviated lipopolysaccharide-induced inflammation in RAW 264.7 cells by decreasing release of pro-inflammatory mediators. Notably, the PEEE samples from Yunnan province showed the optimal antioxidant and anti-inflammatory effects among all the PEEE samples. Conclusion In conclusion, The PEEE HPLC fingerprint may help improve P. emblica quality control, and P. emblica with antioxidant and anti-inflammatory activities may be potentially applied in functional foods or in adjuvant therapy for medicinal development.

Deacidification of high-acid soy sauce residue (SSR) oil is crucial to utilization of SSR oil. Aspergillus niger lipase (ANL) has been widely applied for such purpose while its immobilization still has large room for improvement. ANL was immobilized onto six different macroporous acrylic resins, accounting the effect of the different textural properties of resins on stability and their potential for application in enzymatic deacidification. The resin MARE with lower porosity, higher bulk density, and medium hydrophobicity, was chosen as the best carrier for the best thermostability and reusability. ANL-MARE is a promising catalyst than Novozym 40086, which not only exhibited higher deacidification activity and good thermostability, but also was continuously reused for 15 cycles and efficiently catalyzed from high-acid SSR oil into diacylglycerol-enriched oil. Therefore, immobilized ANL was a novel, low-cost and recyclable biocatalyst that could be used as a good alternative to higher-cost commercial lipases in industrial applications.

12-Hydroxystearic acid (12-HSA), a structurally simple and cost-effective low molecular weight organogelator, has been studied extensively. It is established that the primary intermolecular interaction for self-assembly of 12-HSA molecular gels is hydrogen bonding and to a lesser extent van der Waals interactions. Due to the solvent-gelator interplay, it is expected that more polar solvents, especially hydrogen-bonding rich solvents are more likely to dissolve 12-HSA preventing gelation or crystallization. Surprisingly, it is found that 12-HSA is able to gelate a series of diols, but not their mono functional alcohols. A potential gelation mechanism is proposed that the diol co-crystallizes between 12-HSA molecules promoting 1-dimensional growth. The gelation behavior, fiber morphology, thermal properties as well as viscolastic properties of the resultant gels are drastically affected by the structure of diol solvents. Solvents shorter in chain length, with –OH groups at each terminal end, tend to form fibrous aggregates with higher gelation capacity, higher melting points and mechanically are stronger. Both increasing the diol chain length and the position of the hydroxyl groups from the primary positions lead to reduced gelation ability. The resultant gels comprised of highly branched, ‘spherulitic-like’ crystals are mechanically weaker with lower melting point.

Physico-chemical properties of human breast milk were compared to four Similac™ infant formulas, and correlated with in vitro free fatty acid bioaccessibility using a simulated gastrointestinal system (TIM-1). Viscoelastic measurements, as a function of pH (pH 6.5 to 3.0) and shear rate, showed lower viscosities in breast milk compared to infant formulas. Droplet size and distribution measurements showed distinct differences between the tested formulas and breast milk. During lipid digestion, a lag period was observed for only breast milk. The rate of lipolysis was found to be higher in breast milk compared to Similac™ formulas. The total bioaccessible free fatty acids for Advance infant formula and breast milk were not statistically different for the in vitro TIM-1 model and the shifted-logistical model using one-way ANOVA (p

Hansen solubility parameters (HSP) aid in the a priori prediction of which low molecular weight molecules have the potential to act as low molecular weight organogelators (LMOGs) and can immobilize certain liquids. The hydrogen-bonding HSP parameter individually has some predictive capacity on whether a molecule will form a gel, solution, or precipitate in a known liquid; in the case of benzene, gelators with δh > 5 MPa0.5 form gels, while molecules with δh < 10 MPa0.5 gel ethanol. Small molecules, which gel or remain in a solution state tend to cluster in specific regions of Hansen space. Excellent confinement of solutions was observed within a solubility sphere of benzene, ethanol, and acetonitrile. On the basis of the LMOGs selected, both the magnitude and directionality of the vector in Hansen space are important in predicting the gelation capacity (i.e., a gelator tends to gel toluene Δδp < −4 MPa0.5 when combining the role of Δ2δd and Δδp and ignoring Δδh).

Solvent properties play a central role in mediating the aggregation and self-assembly of molecular gelators and their growth into fibers. Numerous attempts have been made to correlate the solubility parameters of solvents and gelation abilities of molecular gelators, but a comprehensive comparison of the most important parameters has yet to appear. Here, the degree to which partition coefficients (log P), Henry's law constants (HLC), dipole moments, static relative permittivities (ε(r)), solvatochromic E(T)(30) parameters, Kamlet-Taft parameters (β, α, and π), Catalan's solvatochromic parameters (SPP, SB, and SA), Hildebrand solubility parameters (δ(i)), and Hansen solubility parameters (δ(p), δ(d), δ(h)) and the associated Hansen distance (R(ij)) of 62 solvents (covering a wide range of properties) can be correlated with the self-assembly and gelation of 1,3:2,4-dibenzylidene sorbitol (DBS) gelation, a classic molecular gelator, is assessed systematically. The approach presented describes the basis for each of the parameters and how it can be applied. As such, it is an instructional blueprint for how to assess the appropriate type of solvent parameter for use with other molecular gelators as well as with molecules forming other types of self-assembled materials. The results also reveal several important insights into the factors favoring the gelation of solvents by DBS. The ability of a solvent to accept or donate a hydrogen bond is much more important than solvent polarity in determining whether mixtures with DBS become solutions, clear gels, or opaque gels. Thermodynamically derived parameters could not be correlated to the physical properties of the molecular gels unless they were dissected into their individual HSPs. The DBS solvent phases tend to cluster in regions of Hansen space and are highly influenced by the hydrogen-bonding HSP, δ(h). It is also found that the fate of this molecular gelator, unlike that of polymers, is influenced not only by the magnitude of the distance between the HSPs for DBS and the HSPs of the solvent, R(ij), but also by the directionality of R(ij): if the solvent has a larger hydrogen-bonding HSP (indicating stronger H-bonding) than that of the DBS, then clear gels are formed; opaque gels form when the solvent has a lower δ(h) than does DBS.

Interesterification was previously found to impact stearic acid absorption in a randomized cross-over study, when human volunteers consumed a 70:30 wt% high-oleic sunflower and canola stearin blend (NIE) compared to the same blend which had undergone either chemical (CIE) or enzymatic (EIE) interesterification. In this research, in vitro lipid digestion, bioaccessibility, and changes in undigested lipid composition and melting behavior of these same test fats were investigated using the dynamic, multi-compartmental TIM-1 digestion model and compared with the previous human study. Overall, TIM-1 bioaccessibility was higher with interesterification (p < 0.05). Oleic acid bioaccessibility was higher than stearic acid bioaccessibility for NIE, and vice versa for the interesterified blends (p < 0.05). Stearic acid was more concentrated in the undigested triacylglycerols (TAG) from NIE, corresponding to a relatively higher melting temperature of the undigested lipids. The results confirm the impact of TAG composition, fatty acid position and/or physical properties on lipid digestion. TIM-1 bioaccessibility was linearly correlated (R2 = 0.8640) with postprandial serum TAG concentration in the human study. Therefore, the in vitro digestion model offered predictive insights related to the impacts of lipid interesterificaton on absorption.

The oral bioavailability of hydrophobic compound is usually limited by the poor aqueous solubility in the gastrointestinal (GI) tract. Various oral formulations were developed to enhance the systemic concentration of such molecules. Moreover, compounds with high melting temperature that appear as insoluble crystals imposed a great challenge to the development of oral vehicle. Polymethoxyflavone, an emerging category of bioactive compounds with potent therapeutic efficacies, were characterized as having a hydrophobic and highly crystalline chemical structure. To enhance the oral dosing efficiency of polymethoxyflavone, a viscoelastic emulsion system with a high static viscosity was developed and optimized using tangeretin, one of the most abundant polymethoxyflavones found in natural sources, as a modeling compound. In the present study, different in vitro and in vivo models were used to mechanistically evaluate the effect of emulsification on oral bioavailability of tangeretin. In vitro lipolysis revealed that emulsified tangeretin was digested and became bioaccessible much faster than unprocessed tangeretin oil suspension. By simulating the entire human GI tract, TNO's gastrointestinal model (TIM-1) is a valuable tool to mechanistically study the effect of emulsification on the digestion events that lead to a better oral bioavailability of tangeretin. TIM-1 result indicated that tangeretin was absorbed in the upper GI tract. Thus, a higher oral bioavailability can be expected if the compound becomes bioaccessible in the intestinal lumen soon after dosing. In vivo pharmacokinetics analysis on mice again confirmed that the oral bioavailability of tangeretin increased 2.3 fold when incorporated in the viscoelastic emulsion than unformulated oil suspension. By using the combination of in vitro and in vivo models introduced in this work, the mechanism that underlie the effect of viscoelastic emulsion on the oral bioavailability of tangeretin was well-elucidated.