Background and Perspectives on the Utilization of Canes' and Bunch Stems' Residues from Wine Industry as Sources of Bioactive Phenolic Compounds.

Viticulture activity produces a significant amount of grapevine woody byproducts, such as bunch stems and canes, which constitute potential sources of a wide range of phenolic compounds (PCs) with purported applications. Recently, the study of these byproducts has been increased as a source of health-promoting phytochemicals. Antioxidant, antimicrobial, antifungal, and antiaging properties have been reported, with most of these effects being linked to the high content of PCs with antioxidant properties. This Review summarizes the data related to the qualitative and quantitative composition of PCs recovered from canes and bunch stems side streams of the wine industry, the influence that the different environmental and storage conditions have on the final concentration of PCs, and the current reported applications in specific technological fields. The objective is to give a complete valuation of the key factors to consider, starting from the field to the final extracts, to attain the most suitable and stable characterized product.

Metabolic Profiling of Inga Species with Antitumor Activity.

This work evaluated the metabolic profiling of Inga species with antitumor potential. In addition, we described the antigenotoxicity of polyphenols isolated from I. laurina and a proteomic approach using HepG2 cells after treatment with these metabolites. The in vitro cytotoxic activity against HepG2, HT-29 and T98G cancer cell lines was investigated. The assessment of genotoxic damage was carried out through the comet assay. The ethanolic extract from I. laurina seeds was subjected to bioassay-guided fractionation and the most active fractions were characterized. One bioactive fraction with high cytotoxicity against HT-29 human colon cancer cells (IC50 = 4.0 µg mL-1) was found, and it was characterized as a mixture of p-hydroxybenzoic acid and 4-vinyl-phenol. The I. edulis fruit peel (IC50 = 18.6 µg mL-1) and I. laurina seed (IC50 = 15.2 µg mL-1) extracts had cytotoxic activity against the cell line T98G, and its chemical composition showed a variety of phenolic acids. The chemical composition of this species indicated a wide variety of aromatic acids, flavonoids, tannins, and carotenoids. The high concentration (ranging from 5% to 30%) of these polyphenols in the bioactive extract may be responsible for the antitumor potential. Regarding the proteomic approach, we detected proteins directly related to the elimination of ROS, DNA repair, expression of tumor proteins, and apoptosis.

Hydroxycinnamic acids loaded in lipid-core nanocapsules.

Ferulic, caffeic, sinapic, and coumaric acids, belonging to the class of hydroxycinnamic acids (HAs), are bioactive polyphenols widespread in the plant kingdom and present in the human diet. Due to their biological properties and effects in the prevention of various diseases associated with oxidative stress, HAs can be exploited for attractive nutraceutical applications. Starting from this and in order to increase bioaccessibility, we encapsulated HAs in lipid-core nanocapsules (NCs) based on a biodegradable and biocompatible poly(ε-caprolactone) polymer. The results showed that nanoparticles loaded with hydroxycinnamic acids (HA-NCs) have diameter of 224-253 nm, encapsulation efficiency of 53-78%, and are stable over time (30 days). In vitro tests evidenced that NCs are able to preserve HAs in the gastric simulated fluid and release them in the intestinal simulated fluid. The delivery system developed could be employed to create novel functional foods.

Affinity Crystallography Reveals the Bioactive Compounds of Industrial Juicing Byproducts of Punica granatum for Glycogen Phosphorylase.

BACKGROUND: Glycogen phosphorylase (GP) is a pharmaceutical target for the discovery of new antihyperglycaemic agents. Punica granatum is a well-known plant for its potent antioxidant and antimicrobial activities but so far has not been examined for antihyperglycaemic activity. OBJECTIVE: The aim was to examine the inhibitory potency of eighteen polyphenolic extracts obtained from Punica granatum fruits and industrial juicing byproducts against GP and discover their most bioactive ingredients. METHOD: Kinetic experiments were conducted to measure the IC50 values of the extracts while affinity crystallography was used to identify the most bioactive ingredient. The inhibitory effect of one of the polyphenolic extracts was also verified ex vivo, in HepG2 cells. RESULTS: All extracts exhibited significant in vitro inhibitory potency (IC50 values in the range of low µg/mL). Affinity crystallography revealed that the most bioactive ingredients of the extracts were chlorogenic and ellagic acids, found bound in the active and the inhibitor site of GP, respectively.While ellagic acid is an established GP inhibitor, the inhibition of chlorogenic acid is reported for the first time. Kinetic analysis indicated that chlorogenic acid is an inhibitor with Ki=2.5 x 10-3Mthat acts synergistically with ellagic acid. CONCLUSION: Our study provides the first evidence for a potential antidiabetic usage of Punica granatum extracts as antidiabetic food supplements. Although, more in vivo studies have to be performed before these extracts reach the stage of antidiabetic food supplements, our study provides a first positive step towards this process.

Biochemical and biological assessment of the inhibitory potency of extracts from vinification byproducts of Vitis vinifera extracts against glycogen phosphorylase.

The inhibitory potency of thirteen polyphenolic extracts obtained from vinification byproducts of Greek varieties of Vitis vinifera against glycogen phosphorylase (GP) has been studied by kinetic experiments. GP is an enzyme involved in glucose homeostasis and a molecular target for the discovery of new hypoglycemic agents. Studies have shown that all extracts display significant inhibitory potency for GP in vitro with IC50 values in the range of low µg/mL. X-ray crystallographic analysis of GP crystals soaked with two of these extracts revealed that the most active ingredient is quercetin which binds at novel binding site, distinct from the other known sites of the enzyme. One of the most potent of the studied extracts had also a moderate effect on glycogenolysis in the cellular lever with an IC50 value of 17.35 µg/mL. These results highlight the importance of natural resources in the quest for the discovery of new hypoglycemic agents, while at the same time they can serve as the starting point for their exploitation for antidiabetic usage and the development of novel biofunctional foods.