Anthocyanins have powerful antioxidant characteristics in vitro.24-26 However, there is much that is not currently understood about their function within biological systems. In fact, there is much that is currently not understood about oxidation within biological systems in general. Studying oxidation in vivo is challenging as a result of the complexities involved in biological systems. Complications arise as a consequence of compartmentalization, variations in substrate and catalyst concentrations, surface properties of membranes, binding properties of macro-molecules, electrical charges on molecules, and intracellular and extracellular environments, which consist of both aqueous-soluble and lipid-soluble phases. These complexities make it difficult to comprehend how anthocyanins and other flavonoids may reduce or prevent oxidation within the body. Therefore, it will likely be many years before a more thorough understanding of the exact contribution of anthocyanins to the body's antioxidant defense system is realized. If anthocyanins are indeed associated with cancer prevention, their mechanisms of action likely go beyond the prevention of oxidation and lesion formation.
The proposed biological activity of anthocyanins relating to their anticancer properties include direct antimutagenic activity, hormonal activity, inhibition of the metabolic activation of carcinogens, and anti-inflammatory activity. Much of these activities are related to the ability of anthocyanins to influence the activity and function of selected mammalian enzymes. Although anthocyanins have demonstrated a vast array of in vitro enzymatic activities, these have not been definitively established in humans (in vivo). Important questions still remain unanswered regarding the biological activity of anthocyanins and other flavonoids. For example, how do these compounds cross cellular membranes and partition intracellularly; and how are these compounds metabolized and distributed within tissues? Although anthocyanins have shown promise in many in vitro antioxidant and anticancer models, it has yet to be established if these compounds can reach their target of suspected action and if their concentrations are high enough to elicit an efficient response. Further dose-dependent studies on their bioavailability, pharmacokinetics, and in vivo bioactivity in controlled human trials are needed following their ingestion as nutraceuticals (supplements) or components of functional foods in varied food matrices. Even though our understanding of phy-tochemical interactions within human biology is still in its infancy, anthocyanins have demonstrated initial promise as anticancer compounds. Their inhibitory influence on cancer (initiation, progression/incidence) may be the result of direct or indirect antioxidant activity, hormonal activity, or the interaction with enzymes important in cancer initiation and/or progression. It is quite probable that their activity is the combined result of all of these reported effects. Regardless of their mechanism of action, the above evidence indicates the potential use of antho-cyanins as a strategy for cancer prevention and perhaps the retardation of cancer progression and/or metastases in future interventions.
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