Bioavailability of bioactive food compounds: a challenging journey to bioefficacy
01 Mar 2013-British Journal of Clinical Pharmacology (Wiley/Blackwell (10.1111))-Vol. 75, Iss: 3, pp 588-602
TL;DR: This review focuses on some of the major factors affecting the bioavailability of the aforementioned bioactive food compounds.
Abstract: Bioavailability is a key step in ensuring bioefficacy of bioactive food compounds or oral drugs. Bioavailability is a complex process involving several different stages: liberation, absorption, distribution, metabolism and elimination phases (LADME). Bioactive food compounds, whether derived from various plant or animal sources, need to be bioavailable in order to exert any beneficial effects. Through a better understanding of the digestive fate of bioactive food compounds we can impact the promotion of health and improvement of performance. Many varying factors affect bioavailability, such as bioaccessibility, food matrix effect, transporters, molecular structures and metabolizing enzymes. Bioefficacy may be improved through enhanced bioavailability. Therefore, several technologies have been developed to improve the bioavailability of xenobiotics, including structural modifications, nanotechnology and colloidal systems. Due to the complex nature of food bioactive compounds and also to the different mechanisms of absorption of hydrophilic and lipophilic bioactive compounds, unravelling the bioavailability of food constituents is challenging. Among the food sources discussed during this review, coffee, tea, citrus fruit and fish oil were included as sources of food bioactive compounds (e.g. (poly)phenols and polyunsaturated fatty acids (PUFAs)) since they are examples of important ingredients for the food industry. Although there are many studies reporting on bioavailability and bioefficacy of these bioactive food components, understanding their interactions, metabolism and mechanism of action still requires extensive work. This review focuses on some of the major factors affecting the bioavailability of the aforementioned bioactive food compounds.
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TL;DR: The theoretical aspects and recent developments in structural properties, biosynthesis and enhancement, processing, methods of analysis, composition in fruits and vegetables, and bioaccessibility and bioavailability of carotenoids are discussed.
492 citations
Cites background from "Bioavailability of bioactive food c..."
...The bioavailability of β-carotene from plant sources is generally low (10- 65 %), due to resistance of carotene–protein complexes, fibres and the plant cell walls to digestion and degradation to achieve adequate release of carotenoids (Rein et al., 2013)....
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TL;DR: Comparison between in vivo and in vitro procedures used to determine bioaccessibility and bioavailability is carried out, taking into account the strengths and limitations of each experimental technique, along with an intensive description of actual approaches applied to assess bio accessibility of bioactive compounds.
Abstract: Determination of bioactive compounds content directly from foodstuff is not enough for the prediction of potential in vivo effects, as metabolites reaching the blood system may be different from the original compounds found in food, as a result of an intensive metabolism that takes place during absorption. Nutritional efficacy of food products may be ensured by the determination of bioaccessibility, which provides valuable information in order to select the appropriate dosage and source of food matrices. However, between all the methods available, there is a need to establish the best approach for the assessment of specific compounds. Comparison between in vivo and in vitro procedures used to determine bioaccessibility and bioavailability is carried out, taking into account the strengths and limitations of each experimental technique, along with an intensive description of actual approaches applied to assess bioaccessibility of bioactive compounds. Applications of these methods for specific bioactive compound's bioaccessibility or bioavailability are also discussed, considering studies regarding the bioavailability of carotenoids, polyphenolic compounds, glucosinolates, vitamin E, and phytosterols.
483 citations
TL;DR: It is possible that a lower dosage from plant sources could be effective due to of its higher bioavailability compared to the aglycone form, and studies are needed to evaluate the potential cardiovascular benefits of plants rich in quercetin and kaempferol glycoside conjugates.
Abstract: Fruit and vegetable intake has been associated with a reduced risk of cardiovascular disease. Quercetin and kaempferol are among the most ubiquitous polyphenols in fruit and vegetables. Most of the quercetin and kaempferol in plants is attached to sugar moieties rather than in the free form. The types and attachments of sugars impact bioavailability, and thus bioactivity. This article aims to review the current literature on the bioavailability of quercetin and kaempferol from food sources and evaluate the potential cardiovascular effects in humans. Foods with the highest concentrations of quercetin and kaempferol in plants are not necessarily the most bioavailable sources. Glucoside conjugates which are found in onions appear to have the highest bioavailability in humans. The absorbed quercetin and kaempferol are rapidly metabolized in the liver and circulate as methyl, glucuronide, and sulfate metabolites. These metabolites can be measured in the blood and urine to assess bioactivity in human trials. The optimal effective dose of quercetin reported to have beneficial effect of lowering blood pressure and inflammation is 500 mg of the aglycone form. Few clinical studies have examined the potential cardiovascular effects of high intakes of quercetin- and kaempferol-rich plants. However, it is possible that a lower dosage from plant sources could be effective due to of its higher bioavailability compared to the aglycone form. Studies are needed to evaluate the potential cardiovascular benefits of plants rich in quercetin and kaempferol glycoside conjugates.
347 citations
Cites background from "Bioavailability of bioactive food c..."
...One of the important factors of bioavailability is the fat solubility of the ingested flavonols [10]....
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...Bioavailability from a nutritional perspective is defined as the extent of digestion, absorption, metabolism, and excretion of a compound after the ingestion of food [10]....
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...bioavailability of bioactive compounds is an essential step in determining the potential mechanisms of action of flavonols [10]....
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TL;DR: Beetroot’s biological activity is discussed and evidence from studies that specifically investigated the effect of beetroot supplementation on inflammation, oxidative stress, cognition and endothelial function are evaluated.
Abstract: In recent years there has been a growing interest in the biological activity of red beetroot (Beta vulgaris rubra) and its potential utility as a health promoting and disease preventing functional food. As a source of nitrate, beetroot ingestion provides a natural means of increasing in vivo nitric oxide (NO) availability and has emerged as a potential strategy to prevent and manage pathologies associated with diminished NO bioavailability, notably hypertension and endothelial function. Beetroot is also being considered as a promising therapeutic treatment in a range of clinical pathologies associated with oxidative stress and inflammation. Its constituents, most notably the betalain pigments, display potent antioxidant, anti-inflammatory and chemo-preventive activity in vitro and in vivo. The purpose of this review is to discuss beetroot’s biological activity and to evaluate evidence from studies that specifically investigated the effect of beetroot supplementation on inflammation, oxidative stress, cognition and endothelial function.
344 citations
Cites background from "Bioavailability of bioactive food c..."
...molecule and affect its eventual rate and extent of absorption [33,34]....
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...These studies might be interpreted to suggest only small level of bioavailability; however, it is important to realise that betacyanins are unlikely to be exclusively eliminated via the renal pathway [36] Indeed, the use of urinary excretion as a sole indicator of bioavailability has received criticism because it does not account for the biliary and circulatory clearance of compounds, thus underestimating true bioavailability [33]....
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..., first pass metabolism, interactions with gut microflora and protease enzyme degradation) have a significant influence on the concentration of the nutrient that eventually reaches the circulation [33,34]....
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TL;DR: Interactions between ingested fermented food, intestinal microbiota and their correlations to metabolomics profiles and health represent an important perspective deserving to be further explored.
337 citations
Cites background from "Bioavailability of bioactive food c..."
...Interactions with other food components, such as proteins, play also a role (Bohn et al., 2015; Aedín Cassidy &Minihane, 2017; Rein et al., 2013)....
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References
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TL;DR: The nature and contents of the various polyphenols present in food sources and the influence of agricultural practices and industrial processes are reviewed, and bioavailability appears to differ greatly between the variousPolyphenols, and the most abundantpolyphenols in the authors' diet are not necessarily those that have the best bioavailability profile.
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TL;DR: Enhanced bioavailability of curcumin in the near future is likely to bring this promising natural product to the forefront of therapeutic agents for treatment of human disease.
Abstract: Curcumin, a polyphenolic compound derived from dietary spice turmeric, possesses diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Phase I clinical trials have shown that curcumin is safe even at high doses (12 g/day) in humans but exhibit poor bioavailability. Major reasons contributing to the low plasma and tissue levels of curcumin appear to be due to poor absorption, rapid metabolism, and rapid systemic elimination. To improve the bioavailability of curcumin, numerous approaches have been undertaken. These approaches involve, first, the use of adjuvant like piperine that interferes with glucuronidation; second, the use of liposomal curcumin; third, curcumin nanoparticles; fourth, the use of curcumin phospholipid complex; and fifth, the use of structural analogues of curcumin (e.g., EF-24). The latter has been reported to have a rapid absorption with a peak plasma half-life. Despite the lower bioavailability, therapeutic efficacy of...
4,275 citations
TL;DR: An overview of the nutritional effects of the main groups of polyphenolic compounds, including their metabolism, effects on nutrient bioavailability, and antioxidant activity, is offered, as well as a brief description of the chemistry ofpolyphenols and their occurrence in plant foods.
Abstract: Polyphenols constitute one of the most numerous and ubiquitous groups of plant metabolites and are an integral part of both human and animal diets. Ranging from simple phenolic molecules to highly polymerized compounds with molecular weights of greater than 30,000 Da, the occurrence of this complex group of substances in plant foods is extremely variable. Polyphenols traditionally have been considered antinutrients by animal nutritionists, because of the adverse effect of tannins, one type of polyphenol, on protein digestibility. However, recent interest in food phenolics has increased greatly, owing to their antioxidant capacity (free radical scavenging and metal chelating activities) and their possible beneficial implications in human health, such as in the treatment and prevention of cancer, cardiovascular disease, and other pathologies. Much of the literature refers to a single group of plant phenolics, the flavonoids. This review offers an overview of the nutritional effects of the main groups of polyphenolic compounds, including their metabolism, effects on nutrient bioavailability, and antioxidant activity, as well as a brief description of the chemistry of polyphenols and their occurrence in plant foods.
3,821 citations
TL;DR: Gallic acid and isoflavones are the most well-absorbed polyphenols, followed by catechins, flavanones, and quercetin glucosides, but with different kinetics, and the least well- absorption polyphenol are the proanthocyanidins, the galloylated tea catech ins, andThe anthocyanins.
3,534 citations
TL;DR: Both chemical and biochemical factors that affect the absorption and metabolism of polyphenols are reviewed, with particular emphasis on flavonoid glycosides.
Abstract: The main dietary sources of polyphenols are reviewed, and the daily intake is calculated for a given diet containing some common fruits, vegetables and beverages. Phenolic acids account for about one third of the total intake and flavonoids account for the remaining two thirds. The most abundant flavonoids in the diet are flavanols (catechins plus proanthocyanidins), anthocyanins and their oxidation products. The main polyphenol dietary sources are fruit and beverages (fruit juice, wine, tea, coffee, chocolate and beer) and, to a lesser extent vegetables, dry legumes and cereals. The total intake is approximately 1 g/d. Large uncertainties remain due to the lack of comprehensive data on the content of some of the main polyphenol classes in food. Bioavailability studies in humans are discussed. The maximum concentration in plasma rarely exceeds 1 microM after the consumption of 10-100 mg of a single phenolic compound. However, the total plasma phenol concentration is probably higher due to the presence of metabolites formed in the body's tissues or by the colonic microflora. These metabolites are still largely unknown and not accounted for. Both chemical and biochemical factors that affect the absorption and metabolism of polyphenols are reviewed, with particular emphasis on flavonoid glycosides. A better understanding of these factors is essential to explain the large variations in bioavailability observed among polyphenols and among individuals.
3,394 citations