SAM POSSEMIERS*, LEONIE JT BALTER, SIMON FALLAIS
*Corresponding Author
BioActor BV
Oxfordlaan 70, 6229EV, Maastricht, The Netherlands

Abstract

Polyphenolic compounds from citrus fruits, specifically hesperetin-7-O-rutinoside from orange peels, have gained increasing attention for their positive effects on cardiovascular and metabolic parameters. However, low solubility and complex microbial metabolism in the gut typically limit both applicability in foods and its bioavailability and resulting biological activity in humans. First, we elaborate on the influence of the gut microbiota on polyphenol bioavailability. Second, and as primary focus of this review, we describe results obtained with a novel formulation of hesperetin-7-O-rutinoside 2S. This novel formulation of hesperetin-7-O-rutinoside 2S, compared to a standard hesperetin-7-O-rutinoside (hesperidin) extract, showed superior bioavailability of the active polyphenols in a human cross-over pharmacokinetic study. The bioavailability is over 50% higher for the novel formulation. This increased bioavailability creates a great opportunity to induce stronger beneficial health effects as were found up to now with standard hesperidin extracts.

INTRODUCTION
Polyphenols are a group of chemical substances found in plants characterised by the presence of an aromatic ring structure bearing one or more hydroxyl groups (1-2). Interestingly, evidence for their role in the prevention of degenerative human diseases such as cardiovascular diseases (CVD) and cancer is emerging which is reflected by an increasing amount of botanical extracts available for the use in food supplements (4-5). Their beneficial health effects are mostly being attributed to their antioxidant capacity. However, reality is more complex as polyphenols have also been shown to modulate the activity of a wide range of enzymes and cell receptors (3,6). Adding to the complexity, polyphenols are typically susceptible to interindividual variation in ADME (absorption-distribution-metabolism-excretion)-characteristics. Intensive host and especially microbial metabolism therefore results in often low circulat ... ... ...