Enhancing transmucosal delivery of CBD through nanoemulsion: in vitro and in vivo studies.

Cannabidiol (CBD) has gained significant attention as a complementary and alternative medicine due to its promising therapeutic properties. However, CBD faces obstacles when administered orally due to its poor solubility in water, leading to limited absorption into the bloodstream and low and variable bioavailability. Therefore, the development of innovative delivery approaches that can enhance CBD's bioavailability, facilitate administration, and promote patient adherence is crucial. We propose a new approach for buccal delivery of CBD based on a self-assembling nanoemulsion (NE) made of a mixture of surfactants (Tween 80 and Labrasol) and medium chain triglycerides (MCTs). The NE formulation showed properties suitable for buccal administration, including appropriate size, CBD content, and surface properties, and, if compared to a CBD-MCT solution, it exhibited better control of administered doses, faster dissolution in buccal medium, and enhanced stability. The CBD-NE effectively released its active load within 5 h, remained stable even when diluted in simulated buccal fluids, and could be easily administered through a commercially available spray, providing consistent and reproducible doses of NE with optimized properties. In vitro permeation studies demonstrated that the CBD-NE facilitated swift and consistent permeation through the buccal mucosa, resulting in a higher concentration in the acceptor compartment compared to CBD-MCT. Furthermore, the in vivo study in mice showed that a single buccal administration of CBD-NE led to a quicker onset of action than a CBD solution in MCT, while maintaining the same plasma levels over time and leading to typically higher plasma concentrations compared to those usually achieved through oral administration. In conclusion, our CBD-NE represents a promising alternative formulation strategy for buccal CBD administration, overcoming the challenges associated with conventional formulations such as variable bioavailability and low control of administered doses.

Effect of Dewaxed Coffee on Gastroesophageal Symptoms in Patients with GERD: A Randomized Pilot Study.

Gastroesophageal Reflux Disease (GERD) is multifactorial pathogenesis characterized by the abnormal reflux of stomach contents into the esophagus. Symptoms are worse after the ingestion of certain foods, such as coffee. Hence, a randomized pilot study conducted on 40 Italian subjects was assessed to verify the effect of standard (SC) and dewaxed coffee (DC) consumption on gastroesophageal reflux symptoms and quality of life in patients with gastrointestinal diseases. The assessment of patient diaries highlighted a significant percentage reduction of symptoms frequency when consuming DC and a significant increase in both heartburn-free and regurgitation-free days. Consequentially, patients had a significant increase of antacid-free days during the DC assumption. Moreover, the polyphenolic profile of coffee pods was ascertained through UHPLC-Q-Orbitrap HRMS analysis. Chlorogenic acids (CGAs) were the most abundant investigated compounds with a concentration level ranging between 7.316 (DC) and 6.721 mg/g (SC). Apart from CGAs, caffeine was quantified at a concentration level of 5.691 mg/g and 11.091 for DC and SC, respectively. While still preliminary, data obtained from the present pilot study provide promising evidence for the efficacy of DC consumption in patients with GERD. Therefore, this treatment might represent a feasible way to make coffee more digestible and better tolerated.

Bioactive Compounds and Antioxidant Activity of Lettuce Grown in Different Mixtures of Monogastric-Based Manure With Lunar and Martian Soils.

The supplementation of bioactive compounds in astronaut's diets is undeniable, especially in the extreme and inhospitable habitat of future space settlements. This study aims to enhance the Martian and Lunar regolith fertility (testing two commercial simulants) through the provision of organic matter (manure) as established by in situ resource utilization (ISRU) approach. In this perspective, we obtained 8 different substrates after mixing Mojave Mars Simulant (MMS-1) or Lunar Highlands Simulant (LHS-1), with four different rates of manure (0, 10, 30, and 50%, w/w) from monogastric animals. Then, we assessed how these substrates can modulate fresh yield, organic acid, carotenoid content, antioxidant activity, and phenolic profile of lettuce plants (Lactuca sativa L.). Regarding fresh biomass production, MMS-1-amended substrates recorded higher yields than LHS-1-ones; plants grown on a 70:30 MMS-1/manure mixture produced the highest foliar biomass. Moreover, we found an increase in lutein and ß-carotene content by + 181 and + 263%, respectively, when applying the highest percentage of manure (50%) compared with pure simulants or less-amended mixtures. The 50:50 MMS-1/manure treatment also contained the highest amounts of individual and total organic acids, especially malate content. The highest antioxidant activity for the ABTS assay was recorded when no manure was added. The highest content of total hydroxycinnamic acids was observed when no manure was added, whereas ferulic acid content (most abundant compound) was the highest in 70:30 simulant/manure treatment, as well as in pure LHS-1 simulant. The flavonoid content was the highest in pure-simulant treatment (for most of the compounds), resulting in the highest total flavonoid and total phenol content. Our findings indicate that the addition of manure at specific rates (30%) may increase the biomass production of lettuce plants cultivated in MMS-1 simulant, while the phytochemical composition is variably affected by manure addition, depending on the stimulant. Therefore, the agronomic practice of manure amendment showed promising results; however, it must be tested with other species or in combination with other factors, such as fertilization rates and biostimulants application, to verify its applicability in space colonies for food production purposes.

Antioxidant and Anti-Inflammatory Activity of Coffee Brew Evaluated after Simulated Gastrointestinal Digestion.

Coffee contains human health-related molecules, namely polyphenols that possess a wide range of pharmacological functions, and their intake is associated with reduced colon cancer risk. This study aimed to assess the changes in the anti-inflammatory and antioxidant activity of coffee after simulated gastrointestinal digestion. The evaluation of intracellular reactive oxygen species (ROS) levels in the HT-29 human colon cancer cell line and three in vitro spectrophotometric assays were performed to determine the antioxidant activity of the samples. Characterization of coffee composition was also assessed through a Q-Orbitrap high-resolution mass spectrometry analysis. The results highlighted that the levels of polyphenols in the digested coffee brews were higher than those of the non-digested ones. All assayed samples decreased the levels of intracellular ROS when compared to untreated cells, while digested coffee samples exhibited higher antioxidant capacity and total phenolic content than not-digested coffee samples. Digested coffee samples showed a higher reduction in interleukin-6 levels than the not-digested samples in lipopolysaccharide-stimulated HT-29 cells treated for 48 h and fewer cytotoxic effects in the MTT assay. Overall, our findings suggest that coffee may exert antioxidant and anti-inflammatory properties, and the digestion process may be able to release compounds with higher bioactivity.

Chemical Composition, In Vitro Bioaccessibility and Antioxidant Activity of Polyphenolic Compounds from Nutraceutical Fennel Waste Extract.

Fennel (Foeniculum vulgare Mill.) waste contains a broad range of bioactive molecules, including polyphenols, which have poor bioaccessibility during gastrointestinal digestion. This work aimed to investigate the bioaccessibility of total phenolic compounds and the antioxidant capacity during simulated gastrointestinal digestion using two nutraceutical formulations based on non-acid-resistant (NAR) and acid-resistant (AR) capsules containing aqueous-based extracts from fennel waste. Moreover, to obtain a comprehensive investigation of the polyphenolic constituents of the fennel waste extract, a high-resolution mass spectrometry (Q-Orbitrap) analysis was performed. Notably, chlorogenic acids, such as 4-caffeoylquinic acid and 3,4-dicaffeoylquinic acid, were the most detected compounds found in assayed samples (1.949 and 0.490 mg/g, respectively). After in vitro gastrointestinal digestion, the extract contained in AR capsules displayed higher bioaccessibility in both the duodenal and colonic stages (1.96 and 5.19 mg GAE/g, respectively) than NAR capsules (1.72 and 3.50 mg GAE/g, respectively), suggesting that the acidic gastric conditions negatively affected the polyphenol compounds released from the NAR capsules. Therefore, the aqueous extract of fennel waste could be proposed as an innovative and easily available source of dietary polyphenols. Furthermore, the use of an AR capsule could improve the polyphenol bioaccessibility and can be proposed as a nutraceutical formulation.

Chemical Analysis of Minor Bioactive Components and Cannabidiolic Acid in Commercial Hemp Seed Oil.

Although hemp seed (HS) oil is characterized by more than 80% polyunsaturated fatty acids (PUFAs), a very high ω-6-to-ω-3 ratio is not a popular commodity. The aim of this work was to provide useful data about the bioactive components and cannabidiolic acid content in thirteen different commercial hemp seed oils. The investigated HS oils showed a good ω-6/ω-3 ratio, ranging from 1.71 to 2.27, massively differed in their chlorophylls (0.041-2.64 µg/g) and carotenoids contents (0.29-1.73 µg/g), as well as in total phenols (22.1-160.8 mg Gallic Acid Equivalents (GAE)/g) and tocopherols (3.47-13.25 mg/100 g). Since the high content of PUFAs in HS oils, photo-oxidative stability was investigated by determining the Thiobarbituric Acid Reactive Substances (TBARS) assay and extinction coefficient K232 and K270 after the photo-oxidative test. The percentage of increase in K232 and K270 ranged from 1.2 to 8.5% and from 3.7 to 26.0%, respectively, indicating good oxidative stability, but TBARS showed a 1.5- to 2.5-fold increase in oxidative behavior when compared to the initial values. Therefore, the diversity in bioactive compounds in HS oils, and their high nutritional value, suggest the need for a disciplinary booklet that well defines agronomic and post-harvest management conditions for achieving a good food objective.

New Strategies in the Cultivation of Olive Trees and Repercussions on the Nutritional Value of the Extra Virgin Olive Oil.

The health advantages of extra-virgin olive oil (EVOO) are ascribed mainly to the antioxidant ability of the phenolic compounds. Secoiridoids, hydroxytyrosol, tyrosol, phenolic acid, and flavones, are the main nutraceutical substances of EVOO. Applications of beneficial microbes and/or their metabolites impact the plant metabolome. In this study the effects of application of selected Trichoderma strains or their effectors (secondary metabolites) on the phenolic compounds content and antioxidant potential of the EVOOs have been evaluated. For this purpose, Trichoderma virens (strain GV41) and Trichoderma harzianum (strain T22), well-known biocontrol agents, and two their metabolites harzianic acid (HA) and 6-pentyl-α-pyrone (6PP) were been used to treat plants of Olea europaea var. Leccino and var. Carolea. Then the nutraceutical potential of EVOO was evaluated. Total phenolic content was estimated by Folin-Ciocalteau's assay, metabolic profile by High-Resolution Mass spectroscopy (HRMS-Orbitrap), and antioxidant activity by DPPH and ABTS assays. Our results showed that in the cultivation of the olive tree, T22 and its metabolites improve the nutraceutical value of the EVOOs modulating the phenolic profile and improving antioxidants activity.

In Vitro Bioaccessibility and Antioxidant Activity of Coffee Silverskin Polyphenolic Extract and Characterization of Bioactive Compounds Using UHPLC-Q-Orbitrap HRMS.

Coffee silverskin (CS), the main by-product in the coffee industry, contains a vast number of human health-related compounds, which may justify its exploitation as a functional food ingredient. This study aimed to provide a comprehensive analysis of the polyphenolic and alkaloid profile through UHPLC-Q-Orbitrap HRMS analysis. The bioaccessibility of total phenolic compounds and changes in the antioxidant activity during an in vitro gastrointestinal digestion were also evaluated through spectrophotometric tests (TPC by Folin-Ciocalteu, ABTS, DPPH, and FRAP), to elucidate their efficacy for future applications in the nutraceutical industry. Caffeoylquinic and feruloylquinic acids were the most representative polyphenols, with a mean concentration of 5.93 and 4.25 mg/g, respectively. Results showed a high content of caffeine in the analyzed CS extracts, with a mean value of 31.2 mg/g, meaning a two-fold increase when compared to coffee brews. Our findings highlighted that both the bioaccessibility and antioxidant activity of CS polyphenols significantly increased in each in vitro gastrointestinal digestion stage. In addition, the colon stage might constitute the main biological site of action of these antioxidant compounds. These results suggest that in vivo, the dietary polyphenols from CS might be metabolized by human colonic microflora, generating metabolites with a greater antioxidant activity, increasing their well-known beneficial effects.

Selenium Biofortification Impacts the Nutritive Value, Polyphenolic Content, and Bioactive Constitution of Variable Microgreens Genotypes.

Selenium (Se) is considered essential for human nutrition as it is involved in the metabolic pathway of selenoproteins and relevant biological functions. Microgreens, defined as tender immature greens, constitute an emerging functional food characterized by overall higher levels of phytonutrients than their mature counterparts. The nutraceutical value of microgreens can be further improved through Se biofortification, delivering Se-enriched foods and potentially an enhanced content of bioactive compounds. The current study defined the effect of sodium selenate applications at three concentrations (0, 8, and 16 µM Se) on the bioactive compounds and mineral content of coriander, green basil, purple basil, and tatsoi microgreens grown in soilless cultivation. Analytical emphasis was dedicated to the identification and quantification of polyphenols by UHPLC-Q-Orbitrap-HRMS, major carotenoids by HPLC-DAD, and macro micro-minerals by ICP-OES. Twenty-seven phenolic compounds were quantified, of which the most abundant were: Chlorogenic acid and rutin in coriander, caffeic acid hexoside and kaempferol-3-O(caffeoyl) sophoroside-7-O-glucoside in tatsoi, and cichoric acid and rosmarinic acid in both green and purple basil. In coriander and tatsoi microgreens, the application of 16 µM Se increased the total phenols content by 21% and 95%, respectively; moreover, it improved the yield by 44% and 18%, respectively. At the same Se dose, the bioactive value of coriander and tatsoi was enhanced by a significant increase in rutin (33%) and kaempferol-3-O(feruloyl)sophoroside-7-O-glucoside (157%), respectively, compared to the control. In green and purple basil microgreens, the 8 µM Se application enhanced the lutein concentration by 7% and 19%, respectively. The same application rate also increased the overall macroelements content by 35% and total polyphenols concentration by 32% but only in the green cultivar. The latter actually had a tripled chicoric acid content compared to the untreated control. All microgreen genotypes exhibited an increase in the Se content in response to the biofortification treatments, thereby satisfying the recommended daily allowance for Se (RDA-Se) from 20% to 133%. The optimal Se dose that guarantees the effectiveness of Se biofortification and improves the content of bioactive compounds was 16 µM in coriander and tatsoi, and 8 µM in green and purple basil.

Analysis of Phenolic Compounds in Commercial Cannabis sativa L. Inflorescences Using UHPLC-Q-Orbitrap HRMS.

Industrial hemp (Cannabis sativa L. Family Cannabaceae) contains a vast number of bioactive relevant compounds, namely polyphenols including flavonoids, phenolic acids, phenol amides, and lignanamides, well known for their therapeutic properties. Nowadays, many polyphenols-containing products made of herbal extracts are marketed, claiming to exert health-promoting effects. In this context, industrial hemp inflorescence may represent an innovative source of bioactive compounds to be used in nutraceutical formulations. The aim of this work was to provide a comprehensive analysis of the polyphenolic fraction contained in polar extracts of four different commercial cultivars (Kompoti, Tiborszallasi, Antal, and Carmagnola Cs) of hemp inflorescences through spectrophotometric (TPC, DPPH tests) and spectrometry measurement (UHPLC-Q-Orbitrap HRMS). Results highlighted a high content of cannflavin A and B in inflorescence analyzed samples, which appear to be cannabis-specific, with a mean value of 61.8 and 84.5 mg/kg, meaning a ten-to-hundred times increase compared to other parts of the plant. Among flavonols, quercetin-3-glucoside reached up to 285.9 mg/kg in the Carmagnola CS cultivar. Catechin and epicatechin were the most representative flavanols, with a mean concentration of 53.3 and 66.2 mg/kg, respectively, for all cultivars. Total polyphenolic content in inflorescence samples was quantified in the range of 10.51 to 52.58 mg GAE/g and free radical-scavenging included in the range from 27.5 to 77.6 mmol trolox/kg. Therefore, C. sativa inflorescence could be considered as a potential novel source of polyphenols intended for nutraceutical formulations.

Ultra-High-Performance Liquid Chromatography Coupled with Quadrupole Orbitrap High-Resolution Mass Spectrometry for Multi-Residue Analysis of Mycotoxins and Pesticides in Botanical Nutraceuticals.

Cannabidiol (CBD) food supplements made of Cannabis sativa L. extracts have quickly become popular products due to their health-promoting effects. However, potential contaminants, such as mycotoxins and pesticides, can be coextracted during the manufacturing process and placed into the final product. Accordingly, a novel methodology using ultra-high-performance liquid chromatography coupled with quadrupole Orbitrap high-resolution mass spectrometry (UHPLC-Q-Orbitrap HRMS) was developed to quantify 16 mycotoxins produced by major C. sativa fungi, followed by a post-target screening of 283 pesticides based on a comprehensive spectral library. The validated procedure was applied to ten CBD-based products. Up to six different Fusarium mycotoxins were found in seven samples, the most prevalent being zearalenone (60%) and enniatin B1 (30%), both found at a maximum level of 11.6 ng/g. Co-occurrence was observed in four samples, including one with enniatin B1, enniatin A and enniatin A1. On the other hand, 46 different pesticides were detected after retrospective analysis. Ethoxyquin (50%), piperonyl butoxide (40%), simazine (30%) and cyanazine (30%) were the major residues found. These results highlight the necessity of monitoring contaminants in food supplements in order to ensure a safe consumption, even more considering the increase trend in their use. Furthermore, the developed procedure is proposed as a powerful analytical tool to evaluate the potential mycotoxin profile of these particular products.

Use of greenhouse-covering films with tailored UV-B transmission dose for growing 'medicines' through plants: rocket salad case.

BACKGROUND: The effects of ultraviolet B (UV-B) radiation on plants are well known and have recently attracted a great deal of attention due to the production of large quantities of secondary metabolites, which are very beneficial for human health. Recent studies have demonstrated the possibility of exploiting UV-B radiation to induce metabolic changes in fruit, vegetables, and herbs. The role of UV-B rays in inducing secondary plant metabolites is enhanced by new plastic films, which, as a result of their optical properties, permit the necessary dosage of UV-B to be transmitted into the greenhouse to stimulate such metabolites without altering the harvest. RESULTS: The main goal of the present paper is to demonstrate that, by using a greenhouse plastic film with appropriate transmittance of UV-B for rocket salad cultivation, it is possible to increase the nutraceutical elements in comparison with the same species grown in absence of such radiation. Tests compared nutritional elements extracted from rocket salad grown under greenhouses covered with several plastic films differing in UV-B transmittance. We found that rocket salad grown under plastic with 27% UV-B transmittance exhibited very high luteolin and quercetin content in comparison with rocket salad cultivated under film blocking UV-B radiation. CONCLUSIONS: Our experimental results confirm the possibility of exploiting UV-B radiation in the correct amounts by appropriate greenhouse plastic covers, to produce natural 'medicines' using the plants and to satisfy increasing consumer demand for natural health-promoting food products. © 2019 Society of Chemical Industry.

Effect of Dietary Incorporation of Linseed Alone or Together with Tomato-Red Pepper Mix on Laying Hens' Egg Yolk Fatty Acids Profile and Health Lipid Indexes.

This study evaluated the effect of linseed incorporation in laying hens' feed (alone or along with a tomato-red pepper mix) on laying hens' egg yolk fatty acids profile, as well as on their atherogenic (IA) and thrombogenic (IT) health lipid indexes, and the ratio between the hypocholesterolemic and hypercholesterolemic fatty acids (HH). Sixty 27 weeks-old Novogen White laying hens were divided into three groups and given 100 g/hen/day of a standard diet (Control, C) containing 4.5% of ground linseed (Linseed diet, L), containing 1% of dried tomato paste and 1% sweet red pepper (Lineseeds-Tomato-Pepper, LTP). The linseed dietary inclusion significantly reduced the egg yolk content of palmitic acid from 25.41% (C) to 23.43% (L) and that of stearic acid from 14.75% (C) to 12.52% (L). Feeding 4.5% ground linseed did not affect the egg yolk content of α-Linolenic acid but significantly increased the egg yolk concentration of eicosapentaenoic acid (EPA) from 0.011% (C) to 0.047% (L) and that of docosahexaenoic acid (DHA) from 1.94% (C) to 2.73% (L). The IA and the HH were not affected (p > 0.05) by the dietary addition of linseed, whereas the IT decreased (p < 0.05) from 1.16 (C) to 0.86 (L). Adding tomato-sweet red pepper mix to the linseed-supplemented feed did not affect the measured parameters as compared to the linseed dietary treatment.

Raisins and Currants as Conventional Nutraceuticals in Italian Market: Natural Occurrence of Ochratoxin A.

The healthy consumers make a strong pressure to natural products that can prevent the chronic diseases and improve the general health status, and therefore an important aspect that have to be considered is the safe level of the nutraceuticals. This study reports the occurrence of Ochratoxin A (OTA) and associated fungal contamination in 35 samples of dried vine fruits imported in the European community potentially used for the development of new nutraceutical supplements. High pressure liquid chromatography analysis identified 18 samples as contaminated by OTA with an average level of 2.6 µg/kg. OTA was measured in 4 samples of currants (mean value of 6.6 µg/kg) and 13 samples of raisins (mean value of 1.4 µg/kg). In one sample of currants and one of raisins from Turkey OTA exceeded the limits set by European Commission of 10 µg/kg, being contaminated with 12.61 and 15.99 µg/kg, respectively. All the positive samples were confirmed by Orbitrap Q Exactive through their molecular weight and the corresponding fragmentation. The worldwide consumption of dried vine fruits contributed to OTA exposure in several group of consumers. In particular, considering the potential nutraceutical approach, this consumption may be represent a severe risk for healthy consumers that consider these products like healthy and salutistic for their contents in antioxidants, flavonoids, and polyphenols. Data reported in this study confirmed the need to regularly monitor mycotoxin levels in these food products and optimize the process of fruits drying in order to reduce the development of toxigenic molds.

Direct determination of 3-chloropropanol esters in edible vegetable oils using high resolution mass spectrometry (HRMS-Orbitrap).

A series of refined edible oils derived from mixed seeds, peanuts, corn, sunflower and palm obtained from the local supermarket were analyzed for their content of 3-MCPD esters. A direct analytical method for the determination of 3-monochloropropane-1,2-diol esters (3-MCPD esters) was applied to investigate the major MCPD esters found in common edible oils; in particular seven types of monoesters and eleven types of diesters were detected. The limits of detection (LODs) for monoesters and diesters of 3-MCPD were in the range of 0.079-12.678 µg kg-1 and 0.033-18.610 µg kg-1 in edible oils, and the ranges of limits of quantitation (LOQs) were 0.979-38.035 µg kg-1 and 0.100-55 µg kg-1, respectively. The recoveries of 3-MCPD esters from oil samples were in the range of 80-100%, with RSD ranging between 1.9 and 11.8%. The concentration levels of total 3-MCPD diesters in vegetable oil samples were in the range from 0.106 up to 3.444 µg g-1 whereas total monoesters ranged from 0.005 up to 1.606 µg g-1.

Characterization of autochthonous sweet cherry cultivars (Prunus avium L.) of southern Italy for fruit quality, bioactive compounds and antioxidant activity.

BACKGROUND: Characterizing germplasm collections of autochthonous cultivars for fruit quality traits could be a successful approach for selection, improvement of organoleptic quality and levels of antioxidants of crop produce, and development of new market opportunities and coherent strategies for conservation and valorization. The aim of the study was the evaluation of fruit physicochemical traits as well as the content of bioactive compounds and the antioxidant capacity in 25 sweet cherry autochthonous cultivars. RESULTS: Cultivars were a source of statistically significant variation for all evaluated traits. Notably, average fruit ascorbate levels ranged from 34.45 to 244.68 µg g-1 fresh weight (FW) , total flavonoids from 1396.40 to 4694.75 µg quercetin equiv. g-1 FW, monomeric anthocyanins from 4.80 to 360.90 µg g-1 FW, and total antioxidant capacity from 1.53 to 2.58 nmol Trolox equiv. mg-1 FW. Fruit profiling of eight cultivars by high-resolution mass spectrometry identified a total of eight different anthocyanins and twenty-five non-anthocyanin polyphenolic compounds - mostly coumaroylquinic acid and neochlorogenic acid. CONCLUSION: Among the better-performing cultivars for fruit quality traits, Mulegnana Nera and Pagliarella shared high fruit levels of phenolics, flavonoids and antioxidant capacity. This is a forerunner work on the characterization of genetic resources, which is critical to researchers and breeders for exploitation of the genetic potential of cultivars and for their conservation. © 2016 Society of Chemical Industry.

In vitro bioaccessibility, bioavailability and plasma protein interaction of polyphenols from Annurca apple (M. pumila Miller cv Annurca).

The in vitro bioaccessibility, bioavailability and plasma protein interaction of polyphenols from Annurca apple and other conventional cultivars were evaluated. Salivary digestion concentrated into the medium 27-35% of native apple polyphenols, suggesting the potential bioavailability through the oral mucosal epithelium of significant amounts of bioactive compounds that could be gastric sensitive and/or poorly absorbed in the intestine. Annurca flesh revealed the highest content and provided the best intestinal bioaccessibility and bioavailability of oligomeric procyanidins among all of the apple peel and flesh tested. Since 49.4% of native procyanidins were not absorbed, they are expected to accumulate in the intestinal lumen where a potential inhibition capacity of cellular cholesterol uptake could be assumed. The permeated procyanidins (6.7% of their native pattern, 12.0% of intestinal procyanidins) significantly bound (58.7%) to plasma HDLs, suggesting a major role in cholesterol metabolism. Our results would indicate Annurca apple and its potential nutraceuticals as effective in the regulation of plasma cholesterol levels.

Nutraceutical potential of polyphenolic fractions from Annurca apple (M. pumila Miller cv Annurca).

The capacities of polyphenolic extracts from Annurca apple peel and flesh to inhibit the glucose and cholesterol uptake by HepG2 cells were evaluated, and compared with those of other conventional cultivars, such as Red Delicious (RD), Pink Lady (PL), Fuji (F) and Golden Delicious (GD). RD peels exhibited the best hypoglycaemic effects, while Annurca flesh appeared the most active in reducing cell cholesterol uptake among the cultivars tested. The influence of the apple polyphenolic extracts on the cell proliferation and oxidative stress was also evaluated. Particularly, RD, Annurca and PL peels decreased proliferation by a 62.5%, 48.0% and 37.5%, respectively, probably due to their prooxidant capacity. Conversely, flesh extracts appeared more protective of cells than peels: Annurca and RD, particularly, proved to be able of increasing proliferation by a 32.2% and 11.1%, respectively, probably due to their capacity of reducing cell physiological radical levels of a 33.3% and 19.9%, respectively.

Polyphenolic pattern and in vitro cardioprotective properties of typical red wines from vineyards cultivated in Scafati (Salerno, Italy).

Wines are the subject of increasing numbers of investigations owing to the pharmaceutical usefulness of grape phytochemicals. The aim of the present work was to hypothesize the use of lyophilised red wines for the formulation of food supplements potentially useful against both physiological and induced cardiac oxidative stress. Cardiac derived H9C2 myocytes were incubated with increasing doses (0.01-1µg) of lyophilised Aglianico wine (lioAW). Experiments showed an appreciable direct radical scavenging activity at a maximum lioAW dose of 0.03µg that made the caspase-3 activity decrease by about 41%. Cardiac cells were exposed to 1µM doxorubicin and its combination with different doses of lioAW. Maximum lioAW aliquot of 0.03µg seemed to effectively contrast the induced oxidant injury decreasing the reactive oxygen species (ROSs) levels by about 38%and depressing the caspase-3 activity by about 63%. In both assays, pro-oxidant effects at higher lioAW concentrations were detected.