Abstract
Although there are many studies reporting the potential health benefits of the diverse bioactive compounds present in our diet, many aspects related to their bioavailability and bioaccessibility, and particularly their metabolism, have been poorly investigated. In order to exert an effect in the body, a compound should be able to reach the target site of action at concentrations that will trigger the expected response. When considering the potential beneficial effects of bioactive food compounds, it is important to take into account the many factors that can have a significant effect on their bioavailability, and consequently can alter the amount of these compounds that will be absorbed and that will ultimately reach the site of action. This chapter focuses on the several means of improving bioavailability that are described in the literature, including bioaccessibility, food matrix, biological transporters, metabolizing enzymes, and molecular interactions.
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References
Appeldoorn MM, Vincken J-P, Aura A-M, Hollman PCH, Gruppen H (2009) Procyanidin dimers are metabolized by human microbiota with 2-(3,4-dihydroxyphenyl)acetic acid and 5-(3,4-dihydroxyphenyl)-gamma-valerolactone as the major metabolites. J Agric Food Chem 57:1084–1092
Benito P, Miller D (1998) Iron absorption and bioavailability: An updated review. Nutrition Research 18:581–603
Benzie IFF, Chung WY, Wang J, Richelle M, Bucheli P (2006) Enhanced bioavailability of zeaxanthin in a milk-based formulation of wolfberry (Gou Qi Zi; Fructus barbarum L.). Br J Nutr 96:154–160
Boileau TW-M, Boileau AC, Erdman JW Jr (2002) Bioavailability of all-trans and cis-isomers of lycopene. Exp. Biol. Med. (Maywood) 227:914–919
Brand W, van der Wel PAI, Rein MJ, Barron D, Williamson G, van Bladeren PJ, Rietjens IMCM (2008) Metabolism and transport of the citrus flavonoid hesperetin in Caco-2 cell monolayers. Drug Metab Dispos 36:1794–1802
Brett GM, Hollands W, Needs PW, Teucher B, Dainty JR, Davis BD, Brodbelt JS, Kroon PA (2009) Absorption, metabolism and excretion of flavanones from single portions of orange fruit and juice and effects of anthropometric variables and contraceptive pill use on flavanone excretion. Br J Nutr 101:664–675
Chow S-C, Liu J-p (eds.) (2009) Introduction. In: Design and analysis of bioavailability and bioequivalence studies, 3rd edn. CRC, Chapman & Hall, p 3–11
Cilla A, AlegrÃa A, de Ancos B, Sánchez-Moreno C, Cano MP, Plaza L, Clemente G, Lagarda MJ, Barberá R (2012) Bioaccessibility of tocopherols, carotenoids, and ascorbic acid from milk- and soy-based fruit beverages: influence of food matrix and processing. J Agric Food Chem 60:7282–7290
Colle IJP, Lemmens L, Van Buggenhout S, Met K, Van Loey AM, Hendrickx ME (2013) Processing tomato pulp in the presence of lipids: The impact on lycopene bioaccessibility. Food Res Int 51:32–38
Cruz-Hernandez C, Thakkar SK, Moulin J, Oliveira M, Masserey-Elmelegy I, Dionisi F, Destaillats F (2012) Benefits of structured and free monoacylglycerols to deliver eicosapentaenoic (EPA) in a model of lipid malabsorption. Nutrients 4:1781–1793
Da Silva Pinto M (2013) Tea: A new perspective on health benefits. Food Res Int 53:558–567
Déprez S, Brezillon C, Rabot S, Philippe C, Mila I, Lapierre C, Scalbert A (2000) Polymeric Proanthocyanidins Are Catabolized by Human Colonic Microflora into Low-Molecular-Weight Phenolic Acids. J Nutr 130:2733–2738
Dresser GK, Bailey DG (2003) The effects of fruit juices on drug disposition: a new model for drug interactions. Eur J Clin Invest 33(Suppl 2):10–16
Dupas CJ, Marsset-Baglieri AC, Ordonaud CS, Ducept FMG, Maillard M-N (2006) Coffee Antioxidant Properties: Effects of Milk Addition and Processing Conditions. J Food Sci 71:S253–S258
Erlund I, Kosonen T, Alfthan G, Mäenpää J, Perttunen K, Kenraali J, Parantainen J, Aro A (2000) Pharmacokinetics of quercetin from quercetin aglycone and rutin in healthy volunteers. Eur J Clin Pharmacol 56:545–553
European Food Safety Authority (EFSA). Scientific opinion: Guidence to the risk assessment of the application of nanoscience and nanotechnologies in the food and feed chain. 2011
Fernández-GarcÃa E, Carvajal-Lérida I, Pérez-Gálvez A (2009) In vitro bioaccessibility assessment as a prediction tool of nutritional efficiency. Nutr Res 29:751–760
Fernández-GarcÃa E, Rincón F, Pérez-Gálvez A (2008) Developing an emulsifier system to improve the bioaccessibility of carotenoids. J Agric Food Chem 56:10384–10390
Hollman PC, Bijsman MN, van Gameren Y, Cnossen EP, de Vries JH, Katan MB (1999) The sugar moiety is a major determinant of the absorption of dietary flavonoid glycosides in man. Free Radic. Res. 31:569–573
Hong J, Lambert JD, Lee SH, Sinko PJ, Yang CS (2003) Involvement of multidrug resistance-associated proteins in regulating cellular levels of (−)-epigallocatechin-3-gallate and its methyl metabolites. Biochem. Biophys. Res. Commun. 310:222–227
Jensen SK, Nørgaard JV, Lauridsen C (2006) Bioavailability of alpha-tocopherol stereoisomers in rats depends on dietary doses of all-rac- or RRR-alpha-tocopheryl acetate. Br J Nutr 95:477–487
Keck A-S, Qiao Q, Jeffery EH (2003) Food matrix effects on bioactivity of broccoli-derived sulforaphane in liver and colon of F344 rats. J Agric Food Chem 51:3320–3327
Keogh JB, McInerney J, Clifton PM (2007) The effect of milk protein on the bioavailability of cocoa polyphenols. J Food Sci 72:S230–S233
Kerns EH, Di L (2008) Transporters. In: Drug-like properties: concepts, structure design and methods, from ADME to toxicity optimization, 1st edn. Elsevier, New York, pp 103–122
Kimura Y, Ito H, Ohnishi R, Hatano T (2010) Inhibitory effects of polyphenols on human cytochrome P450 3A4 and 2C9 activity. Food Chem Toxicol 48:429–435
Kussmann M, Affolter M, Nagy K, Holst B, Fay LB (2007) Mass spectrometry in nutrition: understanding dietary health effects at the molecular level. Mass Spectrom Rev 26:727–750
Lee H-R, Cho S-D, Lee WK, Kim G-H, Shim S-M (2014) Digestive recovery of sulfur-methyl-L-methionine and its bioaccessibility in Kimchi cabbages using a simulated in vitro digestion model system. J Sci Food Agric 94:109–112
Leucuta SE (2014) Selecting oral bioavailability enhancing formulations during drug discovery and development. Expert Opin Drug Discov 9(2) 139-150
Lévèques A, Actis-Goretta L, Rein MJ, Williamson G, Dionisi F, Giuffrida F (2012) UPLC-MS/MS quantification of total hesperetin and hesperetin enantiomers in biological matrices. J Pharm Biomed Anal 57:1–6
Li S-D, Huang L (2008) Pharmacokinetics and Biodistribution of Nanoparticles. Mol. Pharmaceutics 5:496–504
Livny O, Reifen R, Levy I, Madar Z, Faulks R, Southon S, Schwartz B (2003) Beta-carotene bioavailability from differently processed carrot meals in human ileostomy volunteers. Eur J Nutr 42:338–345
Mateo Anson N, van den Berg R, Havenaar R, Bast A, Haenen GRMM (2009) Bioavailability of ferulic acid is determined by its bioaccessibility. J Cereal Sci 49:296–300
McClements DJ (2013) Utilizing food effects to overcome challenges in delivery of lipophilic bioactives: structural design of medical and functional foods. Expert Opin Drug Deliv 10:1621–1632
Moelants KRN, Lemmens L, Vandebroeck M, Van Buggenhout S, Van Loey AM, Hendrickx ME (2012) Relation between particle size and carotenoid bioaccessibility in carrot- and tomato-derived suspensions. J Agric Food Chem 60:11995–12003
Moran NE, Clinton SK, Erdman JW Jr (2013) Differential bioavailability, clearance, and tissue distribution of the acyclic tomato carotenoids lycopene and phytoene in mongolian gerbils. J Nutr 143:1920–1926
Mullen W, Edwards CA, Serafini M, Crozier A (2008a) Bioavailability of pelargonidin-3-O-glucoside and its metabolites in humans following the ingestion of strawberries with and without cream. J Agric Food Chem 56:713–719
Mullen W, Archeveque M-A, Edwards CA, Matsumoto H, Crozier A (2008b) Bioavailability and metabolism of orange juice flavanones in humans: impact of a full-fat yogurt. J Agric Food Chem 56:11157–11164
Mullen W, Borges G, Donovan JL, Edwards CA, Serafini M, Lean MEJ, Crozier A (2009) Milk decreases urinary excretion but not plasma pharmacokinetics of cocoa flavan-3-ol metabolites in humans. Am J Clin Nutr 89:1784–1791
Muthyala RS, Ju YH, Sheng S, Williams LD, Doerge DR, Katzenellenbogen BS, Helferich WG, Katzenellenbogen JA (2004) Equol, a natural estrogenic metabolite from soy isoflavones: convenient preparation and resolution of R- and S-equols and their differing binding and biological activity through estrogen receptors alpha and beta. Bioorg. Med. Chem. 12:1559–1567
Neilson AP, Ferruzzi MG (2011) Influence of formulation and processing on absorption and metabolism of flavan-3-ols from tea and cocoa. Annu Rev Food Sci Technol 2:125–151
Neilson AP, George JC, Janle EM, Mattes RD, Rudolph R, Matusheski NV, Ferruzzi MG (2009) Influence of chocolate matrix composition on cocoa flavan-3-ol bioaccessibility in vitro and bioavailability in humans. J Agric Food Chem 57:9418–9426
Netzel M, Netzel G, Zabaras D, Lundin L, Day L, Addepalli R, Osborne SA, Seymour R (2011) Release and absorption of carotenes from processed carrots (Daucus carota) using in vitro digestion coupled with a Caco-2 cell trans-well culture model. Food Res Int 44:868–874
Neves AR, Lúcio M, Martins S, Lima JLC, Reis S (2013) Novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability. Int J Nanomedicine 8:177–187
Nielsen ILF, Chee WSS, Poulsen L, Offord-Cavin E, Rasmussen SE, Frederiksen H, Enslen M, Barron D, Horcajada M-N, Williamson G (2006a) Bioavailability is improved by enzymatic modification of the citrus flavonoid hesperidin in humans: a randomized, double-blind, crossover trial. J Nutr 136:404–408
Nielsen ILF, Chee WSS, Poulsen L, Offord-Cavin E, Rasmussen SE, Frederiksen H, Enslen M, Barron D, Horcajada M-N, Williamson G (2006b) Bioavailability is improved by enzymatic modification of the citrus flavonoid hesperidin in humans: a randomized, double-blind, crossover trial. J Nutr 136:404–408
Ottaviani JI, Momma TY, Heiss C, Kwik-Uribe C, Schroeter H, Keen CL (2011) The stereochemical configuration of flavanols influences the level and metabolism of flavanols in humans and their biological activity in vivo. Free Radic Biol Med 50:237–244
Patil BS, Jayaprakasha GK, Chidambara Murthy KN, Vikram A (2009) Bioactive compounds: historical perspectives, opportunities, and challenges. J Agric Food Chem 57:8142–8160
Ramprasath VR, Eyal I, Zchut S, Jones PJH (2013) Enhanced increase of omega-3 index in healthy individuals with response to 4-week n-3 fatty acid supplementation from krill oil versus fish oil. Lipids Health Dis 12:178
Reddy VC, Vidya Sagar GV, Sreeramulu D, Venu L, Raghunath M (2005) Addition of milk does not alter the antioxidant activity of black tea. Ann Nutr Metab 49:189–195
Rein MJ, Renouf M, Cruz-Hernandez C, Actis-Goretta L, Thakkar SK, da Silva Pinto M (2013) Bioavailability of bioactive food compounds: a challenging journey to bioefficacy. Br J Clin Pharmacol 75:588–602
Renouf M, Marmet C, Guy P, Fraering A-L, Longet K, Moulin J, Enslen M, Barron D, Cavin C, Dionisi F, Rezzi S, Kochhar S, Steiling H, Williamson G (2010) Nondairy creamer, but not milk, delays the appearance of coffee phenolic acid equivalents in human plasma. J Nutr 140:259–263
Ribnicky DM, Roopchand DE, Oren A, Grace M, Poulev A, Lila MA, Havenaar R, Raskin I (2014) Effects of a high fat meal matrix and protein complexation on the bioaccessibility of blueberry anthocyanins using the TNO gastrointestinal model (TIM-1). Food Chem 142:349–357
Rocha RA, de la Fuente B, Clemente MJ, Ruiz A, Vélez D, Devesa V (2013) Factors affecting the bioaccessibility of fluoride from seafood products. Food Chem Toxicol 59:104–110
Rossi L, ten Hoorn JWMS, Melnikov SM, Velikov KP (2010) Colloidal phytosterols: synthesis, characterization and bioaccessibility. Soft Matter 6:928–936
Roura E, Andrés-Lacueva C, Estruch R, Lourdes Mata Bilbao M, Izquierdo-Pulido M, Lamuela-Raventós RM (2008) The effects of milk as a food matrix for polyphenols on the excretion profile of cocoa (−)-epicatechin metabolites in healthy human subjects. Br J Nutr 100:846–851
Roura E, Andrés-Lacueva C, Estruch R, Mata-Bilbao ML, Izquierdo-Pulido M, Waterhouse AL, Lamuela-Raventós RM (2007) Milk does not affect the bioavailability of cocoa powder flavonoid in healthy human. Ann Nutr Metab 51:493–498
Scheepens A, Tan K, Paxton JW (2010) Improving the oral bioavailability of beneficial polyphenols through designed synergies. Genes Nutr 5:75–87
Scholz S, Williamson G (2007) Interactions affecting the bioavailability of dietary polyphenols in vivo. Int J Vitam Nutr Res 77:224–235
Schroeter H, Holt RR, Orozco TJ, Schmitz HH, Keen CL (2003) Nutrition: milk and absorption of dietary flavanols. Nature 426, 787–788 (discussion 788)
Schweiggert RM, Kopec RE, Villalobos-Gutierrez MG, Högel J, Quesada S, Esquivel P, Schwartz SJ, Carle R (2013) Carotenoids are more bioavailable from papaya than from tomato and carrot in humans: a randomised cross-over study. Br J Nutr 1–9
Serafini M, Bugianesi R, Maiani G, Valtuena S, De Santis S, Crozier A (2003) Plasma antioxidants from chocolate. Nature 424:1013
Serra A, Macià A, Rubió L, Anglès N, Ortega N, Morelló JR, Romero M-P, Motilva M-J (2013) Distribution of procyanidins and their metabolites in rat plasma and tissues in relation to ingestion of procyanidin-enriched or procyanidin-rich cocoa creams. Eur J Nutr 52:1029–1038
Shen Z, Apriani C, Weerakkody R, Sanguansri L, Augustin MA (2011) Food matrix effects on in vitro digestion of microencapsulated tuna oil powder. J Agric Food Chem 59:8442–8449
Tzeng C-W, Yen F-L, Wu T-H, Ko H-H, Lee C-W, Tzeng W-S, Lin C-C (2011) Enhancement of dissolution and antioxidant activity of kaempferol using a nanoparticle engineering process. J Agric Food Chem 59:5073–5080
Van der Burg-Koorevaar MCD, Miret S, Duchateau GSMJE (2011) Effect of milk and brewing method on black tea catechin bioaccessibility. J Agric Food Chem 59:7752–7758
Victoria-Campos CI, de Ornelas-Paz J, Yahia EM, Failla ML (2013) Effect of the interaction of heat-processing style and fat type on the micellarization of lipid-soluble pigments from green and red pungent peppers (Capsicum annuum). J Agric Food Chem 61:3642–3653
Walde CM, Drotleff AM, Ternes W (2013) Comparison of dietary tocotrienols from barley and palm oils in hen’s egg yolk: transfer efficiency, influence of emulsification, and effect on egg cholesterol. J. Sci, Food Agric
Walsh KR, Zhang YC, Vodovotz Y, Schwartz SJ, Failla ML (2003) Stability and bioaccessibility of isoflavones from soy bread during in vitro digestion. J Agric Food Chem 51:4603–4609
Welch IM, Cunningham KM, Read NW (1988a) Regulation of gastric emptying by ileal nutrients in humans. Gastroenterology 94:401–404
Welch IM, Davison PA, Worlding J, Read NW (1988b) Effect of ileal infusion of lipid on jejunal motor patterns after a nutrient and nonnutrient meal. Am J Physiol 255:G800–806
Whitley AC, Sweet DH, Walle T (2005) The dietary polyphenol ellagic acid is a potent inhibitor of hOAT1. Drug Metab Dispos 33:1097–1100
Wu S, Sun K, Wang X, Wang D, Wan X, Zhang J (2013) Protonation of epigallocatechin-3-gallate (EGCG) results in massive aggregation and reduced oral bioavailability of EGCG-dispersed selenium nanoparticles. J Agric Food Chem 61:7268–7275
Xie X, Tao Q, Zou Y, Zhang F, Guo M, Wang Y, Wang H, Zhou Q, Yu S (2011) PLGA nanoparticles improve the oral bioavailability of curcumin in rats: characterizations and mechanisms. J Agric Food Chem 59:9280–9289
Yliperttula M, Urtti A (2009) Nanotechnology for improved drug bioavailability. In: Van de Waterbeemd H. Testa B. (eds) Drug bioavailability: estimation of solubility, permeability, absorption and bioavailability, 2nd edn. Wiley-VCH, p 597–604
Yu H, Shi K, Liu D, Huang Q (2012) Development of a food-grade organogel with high bioaccessibility and loading of curcuminoids. Food Chem 131:48–54
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Rein, M.J., da Silva Pinto, M. (2017). Improvement of Bioaccessibility and Bioavailability: From Molecular Interactions to Delivery Systems. In: Roos, Y., Livney, Y. (eds) Engineering Foods for Bioactives Stability and Delivery. Food Engineering Series. Springer, New York, NY. https://doi.org/10.1007/978-1-4939-6595-3_15
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