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.

The objective of this work was to characterize exotic fruits (cambuci, araça-boi, camu-camu, jaracatia, araça) and commercial frozen pulps (araça, cambuci, umbu, coquinho, pana, native passion fruit, cagaita) from Brazil in relation to their bioactive compounds contents and antioxidant capacity. Camu-camu (Myrciaria dubia) presented the highest vitamin C and total phenolics contents (397 and 1797 mg/100 gf.w., respectively) and the highest DPPH• scavenging capacity. Coquinho (Butia capitata) also showed a significant vitamin C content (43 mg/100 gf.w.). Among the commercial frozen pulps, cagaita presented the higher DPPH scavenging activity and inhibition of β-carotene bleaching. A good correlation between total phenols and DPPH scavenging activity was found for fruits (r = 0.997) and commercial frozen pulps (r = 0.738). However, no correlation was found for total phenols and inhibition of β-carotene bleaching. Quercetin and kaempferol derivatives were the main flavonoids present in all samples and cyanidin derivatives were detected only in camu-camu. Camu-camu and araça (Psidium guineensis) showed the highest total ellagic acid contents (48 and 63.5 mg/100 gf.w.). All commercial frozen pulps presented lower contents of bioactive compounds and antioxidant capacity than their respective fruits. According to our results, camu-camu and araça might be sources of bioactive compounds.

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Local food diversity and traditional crops are essential for cost-effective management of the global epidemic of type 2 diabetes and associated complications of hypertension. Water and 12% ethanol extracts of native Peruvian fruits such as Lucuma (Pouteria lucuma), Pacae (Inga feuille), Papayita arequipeña (Carica pubescens), Capuli (Prunus capuli), Aguaymanto (Physalis peruviana), and Algarrobo (Prosopis pallida) were evaluated for total phenolics, antioxidant activity based on 2, 2-diphenyl-1-picrylhydrazyl radical scavenging assay, and functionality such as in vitro inhibition of alpha-amylase, alpha-glucosidase, and angiotensin I-converting enzyme (ACE) relevant for potential management of hyperglycemia and hypertension linked to type 2 diabetes. The total phenolic content ranged from 3.2 (Aguaymanto) to 11.4 (Lucuma fruit) mg/g of sample dry weight. A significant positive correlation was found between total phenolic content and antioxidant activity for the ethanolic extracts. No phenolic compound was detected in Lucuma (fruit and powder) and Pacae. Aqueous extracts from Lucuma and Algarrobo had the highest alpha-glucosidase inhibitory activities. Papayita arequipeña and Algarrobo had significant ACE inhibitory activities reflecting antihypertensive potential. These in vitro results point to the excellent potential of Peruvian fruits for food-based strategies for complementing effective antidiabetes and antihypertension solutions based on further animal and clinical studies.

The well-known health benefits of apples have been attributed in part to the presence of polyphenols and related antioxidant capacity. The consumption of apples could provide health benefits by reducing the risk for chronic diseases such as metabolic syndrome disease, including type 2 diabetes. Thus, the objective of this study was to investigate the phenolic-linked antihyperglycemia bioactive factors in aqueous and 12% ethanol extracts of peel and pulp from 10 different freshly harvested apple varieties commonly consumed in the United States. The extracts were analyzed for total soluble phenolics, 2,2-diphenyl-1-picrylhydrazyl-linked antioxidant activity, and their associated in vitro α-glucosidase and α-amylase inhibitory activities. In general, peel extracts had higher total soluble phenolic content and related antioxidant capacity than pulp extracts. Quercetin derivatives, protocatechuic acid, chlorogenic acid, and p-coumaric acid were detected, and the amount varied significantly between aqueous and ethanolic extracts. Honeycrisp and Red Delicious varieties had the highest total phenolic contents and a significant correlation with antioxidant capacity (r = 0.91). In addition, high α-amylase and α-glucosidase inhibitory activities in aqueous pulp extracts were found. However, the peel extracts had the highest α-glucosidase inhibitory activity along with low α-amylase inhibitory activity. No correlation between α-amylase inhibitory activity and total phenolic content was observed. However, positive correlations between α-glucosidase inhibitory activity and total phenolics in aqueous (r = 0.50) and ethanolic (r = 0.70) extracts were observed. This study provides the biochemical rationale for animal and clinical studies to determine the suitable varieties with optimum bioactive factors with antihyperglycemia potential.

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