Avocado-derived polyhydroxylated fatty alcohols (PFAs), such as avocadene and avocadyne, have been recently identified as potent modulators of mitochondrial metabolism which selectively induce leukemia cell death and reverse pathologies associated with diet-induced obesity. However, avocadene and avocadyne bioaccessibility from avocado pulp is not reported; hence, this study aims to investigate if these PFAs are bioaccessible. Dynamic (TNO dynamic intestinal model-1 (TIM-1)) and static in vitro digestion of lyophilized Hass avocado pulp powder shows lipolytic gastrointestinal enzymes led to appreciable bioaccessibility of avocadene (55%) and avocadyne (50%). Furthermore, TIM-1 digestion of a 1:1 ratio of pure avocadene and avocadyne (avocatin B or AvoB) crystals formulated in an oil-in-water microemulsion has on average 15% higher bioaccessibility than the avocado pulp powder demonstrating both dosage forms as potential dietary sources of avocado PFAs. This research provides the impetus for further research on the nutritional significance of dietary long chain fatty alcohols.
It remains unclear how consuming whole apples, as a food matrix containing pectin and polyphenols, influences lipid digestibility and bioaccessibility from dairy-based meals. Pectin and polyphenols modulate lipid digestion in vitro, but their functionality can be altered by gastric pH, which is buffered by co-consuming dairy products. In the present study, a dairy meal containing 3 wt% protein and 10 wt% fat was digested with and without apples using static (i.e., adapted from INFOGEST standardized static model) and dynamic (TIM-1) in vitro methods to investigate the structure, digestibility, and bioaccessibility of milk fat from emulsion droplets in the presence of consumed apples. Furthermore, in the static digestion, the initial gastric pH was adjusted to 3.0 (i.e., acidic digestion, as INFOGEST protocol suggested) or remained unadjusted (pH = 6.5, i.e., neutral digestion, buffered by the dairy meal) to explore the effects of gastric acidity. Emulsion droplet structure and lipid digestibility in the static digestion were primarily influenced by gastric pH [mean lipolysis rate = 99.32 % and 83.95 % (p < 0.05) for the digestions with neutral and acidic pH in the gastric phase, respectively], but not the presence of apple. However, co-consumption of apples reduced the lipid bioaccessibility measured by TIM-1 [mean bioaccessibility = 65.44 % and 98.92 % (p < 0.05) for the digestions with and without apples, respectively]. Discrepancies in the bioaccessibility of individual fatty acids between the static and TIM-1 models were observed, which may be attributed to variations in the experimental parameters, e.g., chyme transit and enzyme concentration. Overall, this study shows the potential to preferentially modify lipid digestibility and bioaccessibility in high-fat meals by co-consuming apples. It also cautions attention to the digestive conditions of in vitro simulation studies when making comparisons to in vivo conditions.
The objective of this study was to evaluate the feasibility of using fluorescence-based techniques to assess the miscibility and physical stability of a drug–lipid complex pharmaceutical dosage form under a solvent-free condition. An indomethacin–phospholipid complex (IDM–DPC) was used as model complex for this study. The miscibility of indomethacin within the phospholipid was assessed by fluorescence spectroscopy, fluorescence microscopy, and infrared spectroscopy. The miscibility limit of the complex system was determined by fluorescence to be 20%–30% drug loading content, showing good correlation with infrared spectroscopy. The physical stability of the IDM–DPC stored at 40 °C was evaluated by fluorescence microscopy. Indomethacin formulated in the lipid complex with an indomethacin loading not more than 30% remained in an amorphous state within a period of 21 days, whereas the samples with a drug loading over 30% started to crystallize earlier with increasing drug content. IDM–DPC having higher miscibilities were found to be more resistant to recrystallization under heating, thus having better physical stability. Fluorescence-based techniques showed convenience and promise in characterizing drug–lipid miscibility and predicting storage stability under a solvent-free condition.
Living systems require water, proteins, carbohydrates, lipids, nucleic acids, vitamins and minerals. Typically, living systems are comprised of anywhere from 50% to 90% water, making water, arguably, the most important constituent of all living systems. It has an essential role as a reactant and solvent in biochemical pathways, transport of nutrients and waste products. Not only is water essential for life, but it is also essential for food chemistry, microbiology and processing. It influences stability of foods, textural properties, microbial stability and consumer acceptance.
The legalization of cannabis in Canada and in other jurisdictions around the World, will lead to increased demand for alternative forms of consumption including edible cannabis products. Cannabis research from a food science perspective has largely been absent. Existing processing methods commonly used in the pharmaceutical and food and beverage industries such as homogenization, ultrasonic cavitation and microfluidization can be applied in the production of cannabis edibles but special considerations must be taken in order to preserve the bioactive cannabinoids. The use of different surfactants must also be taken into account in order to improve cannabinoid solubility and enhance oral bioavailability. This review aims to summarize the latest information about technologies used to obtain cannabis products for oral consumption.
Altering sn-fatty acid position of glycerol mono-oleate (GMO) from sn-1 to sn-2 decreases fatty acid bioaccessibility by 25.9% providing possible strategies to tailor lipemic responses of food emulsions. Lipid digestion kinetics and fatty acid bioaccessibility of monomodal O/W emulsions stabilized at their minimum surfactant concentration (0.5 < MSC > 0.7 (w/w)) were studied in the TNO Intestinal Model (TIM-1) gastrointestinal (GI) tract. No significant differences were observed between induction times nor rate constants when using 1-GMO and 1-GMS, Span 60, Tween 60 and Tween 80 as surfactants in O/W emulsions, as determined by fitting a three-parameter shifted logistic model to the cumulative bioaccessibility. Comparable trends were observed between area under the curve (AUC) of the absolute bioaccessibility and total overall bioaccessibility.
Phyto-phospholipid complexes have been developed as a common way of improving the oral bioavailability of poorly absorbable phyto-pharmaceuticals; however, the complexation with phospholipids can induce positive or negative effects on the bioaccessibility of such plant-derived active ingredients in different parts of the gastrointestinal tract (GIT). The purpose of this study was to investigate the effects of phospholipid complexation on the bioaccessibility of a rosmarinic acid-phospholipid complex (RA-PLC) using the TNO dynamic intestinal model-1 (TIM-1). Preparation of RA-PLC was confirmed using X-ray diffraction, Fourier-transform infrared spectroscopy, partition coefficient measurement, and Caco-2 monolayer permeation test. Bioaccessibility parameters in different GIT compartments were investigated. Complexation by phospholipids reduced the bioaccessibility of RA in jejunum compartment, while maintaining the ileum bioaccessibility. The overall bioaccessibility of RA-PLC was lower than the unformulated drug, suggesting that the improved oral absorption from a previous animal study could be considered as a net result of decreased bioaccessibility overwhelmed by enhanced intestinal permeability. This study provides insights into the effects of phospholipid on the bioaccessibility of hydrophilic compounds, and analyzes them based on the relationship between bioaccessibility, membrane permeability, and bioavailability. Additionally, TIM-1 shows promise in the evaluation of dosage forms containing materials with complicated effects on bioaccessibility.
The bioaccessibility, antioxidant and anti-inflammatory activities of phenolics in a cooked green lentil (Lens culinaris) (cultivar Greenland) was studied using a simulated upper gastrointestinal (UGI) digestion model combined with chemical- and cell- based antioxidant assays. The amount of released soluble phenolics increased stepwise from gastric to intestinal digestion phase. The bioaccessibility of phenolics ranged from 27 to 67% after UGI digestion. Flavonols were the main phenolic group and were found to remain relatively stable during UGI digestion. Flavanols were mainly released after intestinal digestion as opposed to phenolic acids which were mainly released from food matrix in the gastric phase (21–45%) but not detected following intestinal digestion. Phenolics of the nondigested lentil showed dose dependent anti-inflammatory activity as seen in significant inhibition of the pro-inflammatory cytokines COX-2, IL-1β and IL-6 in TNF-α-induced inflammation in Caco-2 cells. The Antioxidant and anti-inflammatory activities were positively correlated with the total and individual phenolic contents.
Purified phenolic extracts of cooked regular-darkening (RR) and non-darkening (CND) cranberry beans were evaluated for their phenolic content, antioxidant and anti-inflammatory activity and bioavailability using a human colonic carcinoma (Caco-2) cell model. Major compounds included flavanols such as catechin, epicatechin and proanthocyanidins which were predominant to RR extract. RR and CND both contained p-coumaric acid, ferulic acid and tryptophan. Our results showed strong cellular antioxidant activity in RR and dose-dependent attenuation of TNF-α-induced pro-inflammatory cytokine Interleukin-8 (IL-8) secretion. In addition, the extracts displayed protective benefit to endogenous antioxidant enzymes such as SOD, CAT, GPx and GR as well as GSH. Flavanols displayed poor bioavailability suggesting the beneficial effects occur via adsorption on the cell surface leading to cell signalling and localized radical scavenging activity. Our results support the beneficial effects of cranberry bean phenolics in their ability to ameliorate oxidative stress conditions notably in intestinal inflammatory responses.
Various fatty acids, tocopherols, carotenoids, and their respective antioxidant contributions in 7 amaranth seed and 11 quinoa seed samples along with a new evaluation method are reported. The lipid yield was 6.98-7.22% in amaranth seeds and 6.03-6.74% in quinoa seeds, with unsaturated fatty acids (UFAs) being the predominant fatty acids, 71.58-72.44% in amaranth seeds and 81.44-84.49% in quinoa seeds, respectively. Carotenoids, mainly lutein and zeaxanthin, are confirmed for the first time in amaranth seeds, while β-carotene is reported first in quinoa seeds. The predominant tocopherols in amaranth seeds are δ- and α-tocopherol, whereas γ- and α-tocopherol are the primary tocopherols in quinoa seeds. UFAs, carotenoids, and tocopherols showed good correlation with antioxidant activity. All of the amaranth seeds demonstrated lower overall lipophilic quality than quinoa seeds, with the AS1 and QS10 cultivars providing the highest scores for amaranth and quinoa seeds, respectively. Results from this study will contribute to developing quinoa seeds and related functional foods with increased benefits.
Unextractable phenolics from plant foods and their role in health benefits have become increasingly important. Meal residues of three quinoa seeds free of fat and extractable phenolics were subjected to acid, alkaline, and enzymatic hydrolyses. The total and individual phenolic compounds released were analyzed, and 19 phenolics, predominantly phenolic acids and several flavonoids, were identified. The concentration of bound phenolics was highest in black quinoa followed by red and white, regardless of the hydrolysis method. Higher phenolic contents also showed stronger antioxidant activities and inhibition of α-glucosidase and pancreatic lipase activities. Carbohydrases, that is, pectinase, xylanase and feruloyl esterase, which effectively liberated bound phenolics are known to be secreted by colonic bacteria, suggesting potential antioxidant and anti-inflammatory effects by these compounds in the large intestine during colonic fermentation. These results can also be applied to treat foods high in bound phenolics to enhance bioaccessibility.
Cranberry beans (Phaseolus vulgaris L.) from 7 different cultivars were characterized for phytochemicals and assessed for antioxidant activities. In vitro colorimetric methods were used to measure total phenolic (TPC) and total proanthocyanidin (PAC) contents. Free, conjugated and bound phenolic acids and flavonoids were also identified and quantified using HPLC-DAD/ESI-MS(n). Regular-darkening (RD) seeds contained higher TPC, PAC and flavonoids which were absent in the non-darkening (ND) seeds. Bound and conjugated phenolics in RD and ND mainly included cinnamic and benzoic acids. DPPH, FRAP and ORAC showed strong positive correlation with TPC, PAC, and with specific phenolics such as free catechin and bound p-hydroxybenzoic acid. Lipophilic extracts were rich in polyunsaturated fatty acids (69.20-76.89%). Carotenoid and tocopherol were limited to γ-tocopherol and β-carotene. Results from this study can contribute to the development of cranberry bean cultivars with increased health benefits and addresses specific phenolic contributors to antioxidant activity.
Postharvest darkening in dry bean (Phaseolus vulgaris L.) negatively impacts consumer preference. Regular-darkening (RD) and non-darkening (ND) cranberry beans were profiled for seed coat phenolics using HPLC–DAD/LC–ESI–MSn and assessed for antioxidant activity using oxygen radical absorbing capacity (ORAC) and ferric-reducing antioxidant power (FRAP) assays. Flavonoids were exclusive to free phenolic extracts of RD beans. Total phenolic content (TPC) was significantly higher (p < 0.05) in RD seed coats (52.41–56.43 mg GAE/g) compared to ND seed coats (2.00–2.06 mg GAE/g). Alkaline hydrolysis revealed the presence of phenolic acids and flavonoid conjugates in RD beans. Only p-coumaric and ferulic acids were found in ND beans. Overall antioxidant activity was stronger in RD seed coats (125.28–287.87 µmole TE/g and 20.71–54.01 µmole AAE/g) compared to ND seed coats (2.11–10.09 µmole TE/g and 0.73–1.88 µmole AAE/g). This is the first report of specific flavonoids in cranberry beans.
Quinoa (Chenopodium quinoa Willd.) is known for its exceptional nutritional value and potential health benefits. The present study identified the composition of different forms of extractable phenolics and betacyanins of quinoa cultivars in white, red and black, and how they contribute to antioxidant activities. Results showed that at least 23 phenolic compounds were found in either free or conjugated forms (liberated by alkaline and/or acid hydrolysis); the majority of which were phenolic acids, mainly vanillic acid, ferulic acid and their derivatives as well as main flavonoids quercetin, kaempferol and their glycosides. Betacyanins, mainly betanin and isobetanin, were confirmed for the first time to be the pigments of the red and black quinoa seeds, instead of anthocyanins. Darker quinoa seeds had higher phenolic concentration and antioxidant activity. Findings of these phenolics, along with betacyanins in this study add new knowledge to the functional components of quinoa seeds of different cultivar background.
Cranberry beans from regular (RR) and nondarkening (CND) genotypes were pressure cooked, and free, conjugated, and bound phenolics were analyzed. Simulated in vitro gastrointestinal digestion was used to assess the bioaccessibility of these phenolic fractions. Total phenolic content decreased after cooking and digestion, whereas individual phenolic compounds were affected differently. Cooking significantly increased the release of bound ferulic and sinapic acids and flavanols, whereas digestion released p-coumaric, ferulic, and sinapic acids in both genotypes, and p-hydroxybenzoic acid, epicatechin, and catechin in only RR. Bioaccessibility of phenolics in RR and CND was 8.75 and 14.69%, respectively. Difference in total phenolics was smaller after digestion, and enzymes potentially secreted by colonic bacteria released similar amounts of phenolic acids in both varieties. Resistant and slowly digestible starch contents showed no differences between RR and CND. These results suggest that the lower phenolic content in raw CND may not completely negate its impact on gut health.
Understanding the profile of lipophilic phytochemicals in lentils is necessary to better understand the health benefits of lentils. The fatty acid, carotenoid and tocopherol compositions and antioxidant activities of the lipophilic extracts of 20 lentil cultivars (10 red and 10 green) were therefore examined. Lentils contained 1.52–2.95% lipids, of which 77.5–81.7% were unsaturated essential fatty acids. Total tocopherols ranged from 37 to 64 μg/g DW, predominantly γ-tocopherol (96–98% of the tocopherol content), followed by δ- and α-tocopherol. trans-Lutein was the primary and major carotenoid (64–78%) followed by trans-zeaxanthin (5–13%). Carotenoids and tocopherols showed weak correlation with 2,2-diphenyl-1-picrylhydrazyl (DPPH) activity (r = 0.4893 and 0.3259, respectively), but good correlation when combined (r = 0.6688), suggesting they may act synergistically. Carotenoids were found to contribute the most to the strong antioxidant activity measured by photochemiluminescence (PCL) assay. Results from this study contribute to the development of lentil cultivars and related functional foods with increased health benefits.
Phenolic extracts from 20 Canadian lentil cultivars (Lens culinaris) were evaluated for total phenolic contents and composition, antioxidant activities (DPPH, FRAP, ORAC), and inhibitory properties against α-glucosidase and pancreatic lipase. Twenty one phenolic compounds were identified in the present study, with the majority being flavonoids, including kaempeferol glycosides, catechin/epicatechin glucosides and procyanidins. These phenolic compounds not only contributed significantly to the antioxidant activities, but they were also good inhibitors of α-glucosidase and lipase, two enzymes, respectively, associated with glucose and lipid digestion in the human intestine, thus contributing significantly to the control of blood glucose levels and obesity. More interestingly, it was the flavonols, not the flavanols, which showed the inhibitory activities against α-glucosidase and pancreatic lipase. Our result provides supporting information for developing lentil cultivars and functional foods with improved health benefits and suggests a potential role of lentil consumption in managing weight and control of blood glucose.