scholarly journals Oleacein Intestinal Permeation and Metabolism in Rats Using an In Situ Perfusion Technique

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 719
Author(s):  
Anallely López-Yerena ◽  
Maria Pérez ◽  
Anna Vallverdú-Queralt ◽  
Eleftherios Miliarakis ◽  
Rosa M. Lamuela-Raventós ◽  
...  

Oleacein (OLEA) is one of the most important phenolic compounds in extra virgin olive oil in terms of concentration and health-promoting properties, yet there are insufficient data on its absorption and metabolism. Several non-human models have been developed to assess the intestinal permeability of drugs, among them, single-pass intestinal perfusion (SPIP), which is commonly used to investigate the trans-membrane transport of drugs in situ. In this study, the SPIP model and simultaneous luminal blood sampling were used to study the absorption and metabolism of OLEA in rats. Samples of intestinal fluid and mesenteric blood were taken at different times and the ileum segment was excised at the end of the experiment for analysis by LC–ESI–LTQ–Orbitrap–MS. OLEA was mostly metabolized by phase I reactions, undergoing hydrolysis and oxidation, and metabolite levels were much higher in the plasma than in the lumen. The large number of metabolites identified and their relatively high abundance indicates an important intestinal first-pass effect during absorption. According to the results, OLEA is well absorbed in the intestine, with an intestinal permeability similar to that of the highly permeable model compound naproxen. No significant differences were found in the percentage of absorbed OLEA and naproxen (48.98 ± 12.27% and 43.96 ± 7.58%, respectively).

Proceedings ◽  
2020 ◽  
Vol 70 (1) ◽  
pp. 107
Author(s):  
Maria Antoniadou ◽  
Theodoros Varzakas

Olive fruit exerts great socioeconomic impact. Many studies have shown the multiple benefits of healthy olive oil for the human body. The increase in consumption of extra virgin olive oil is mainly due to its unique sensory, nutritive qualities, biological properties, and health-promoting effects. In this review paper recent advances in quality, safety, authenticity, processing, nutrition, health, and oral health of extra virgin olive oil (EVOO) have been discussed and outlined. Regarding safety, the effect of food safety management systems in EVOO has been reported along with the use of different tools such as FMEA and Ishikawa.


Antioxidants ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1016
Author(s):  
Stefania De Santis ◽  
Marina Liso ◽  
Giulio Verna ◽  
Francesca Curci ◽  
Gualtiero Milani ◽  
...  

Extra virgin olive oil (EVOO) represents one of the most important health-promoting foods whose antioxidant and anti-inflammatory activities are mainly associated to its polyphenols content. To date, studies exploring the effect of EVOO polyphenols on dendritic cells (DCs), acting as a crosstalk between the innate and the adaptive immune response, are scanty. Therefore, we studied the ability of three EVOO extracts (cv. Coratina, Cima di Mola/Coratina, and Casaliva), characterized by different polyphenols amount, to regulate DCs maturation in resting conditions or after an inflammatory stimulus. Cima di Mola/Coratina and Casaliva extracts were demonstrated to be the most effective in modulating DCs toward an anti-inflammatory profile by reduction of TNF and IL-6 secretion and CD86 expression, along with a down-modulation of Il-1β and iNOS expression. From factorial analysis results, 9 polyphenols were tentatively established to play a synergistic role in modulating DCs inflammatory ability, thus reducing the risk of chronic inflammation.


Separations ◽  
2021 ◽  
Vol 8 (10) ◽  
pp. 173
Author(s):  
Veronica Termopoli ◽  
Maurizio Piergiovanni ◽  
Achille Cappiello ◽  
Pierangela Palma ◽  
Giorgio Famiglini

Extra virgin olive oil (EVOO) is one of the main ingredients of the Mediterranean diet. It is claimed as a functional food for its unique content of health-promoting compounds. Tyrosol (Tyr), Hydroxytyrosol (Htyr), and their phenolic derivatives present in EVOO show beneficial properties, and their identification and quantification, both in their free form and after the hydrolysis of more complex precursors, are important to certify its quality. An alternative method for quantifying free and total Tyr and Htyr in EVOO is presented using an LC–MS interface based on electron ionization (EI), called liquid electron ionization (LEI). This method requires neither sample preparation nor chromatography; the sample is diluted and injected. The selectivity and sensitivity were assessed in multiple reaction monitoring mode (MRM), obtaining confirmation and quantification in actual samples ranging from 5 to 11 mg/Kg for the free forms and from 32 to 80 mg/Kg for their total amount after hydrolysis. Two MS/MS transitions were acquired for both compounds using the Q/q ratios as confirmatory parameters. Standard addition calibration curves demonstrated optimal linearity and negligible matrix effects, allowing a correct quantification even without expensive and difficult to find labeled internal standards. After several weeks of operation, the system’s repeatability was excellent, with an intraday RSD (%) spanning from five to nine and an interday RSD (%) spanning from 9 to 11.


2018 ◽  
Vol 551 (1-2) ◽  
pp. 148-157 ◽  
Author(s):  
Tamires Guedes Caldeira ◽  
Alejandro Ruiz-Picazo ◽  
Isabel Lozoya-Agullo ◽  
Dênia Antunes Saúde-Guimarães ◽  
Marta González-Álvarez ◽  
...  

2014 ◽  
Vol 55 (5) ◽  
pp. 905-918 ◽  
Author(s):  
Satoshi Yamaguchi ◽  
Bo Zhang ◽  
Takeshi Tomonaga ◽  
Utako Seino ◽  
Akiko Kanagawa ◽  
...  

1987 ◽  
Vol 63 (5) ◽  
pp. 2084-2092 ◽  
Author(s):  
M. Shirahata ◽  
S. Andronikou ◽  
S. Lahiri

Effects of oligomycin on carotid chemoreceptor responses to O2 and CO2 were investigated using an in situ perfusion technique. Cats were anesthetized, paralyzed, and artificially ventilated. To avoid a possible reaction between an oligomycin-ethanol mixture and blood, we administered oligomycin to the carotid body via cell- and protein-free perfusate. Except for the perfusion periods, the carotid body received its own natural blood supply. Responses to O2, CO2, sodium cyanide, and nicotine of the same carotid chemoreceptor afferents were studied before and after each perfusion. An appropriate low dose of oligomycin completely blocked carotid chemoreceptor response to O2 while preserving the CO2 response. At the same time cyanide response was attenuated leaving nicotine response intact. Additional doses of oligomycin attenuated carotid chemoreceptor response to CO2 as well. Perfusion with a blank solution containing ethanol did not change the carotid body chemoreceptor responses. These effects of oligomycin on carotid chemoreceptor responses to O2 and CO2 were reversible, and restoration of the response to CO2 preceded that to O2. In addition, oligomycin administered into the blood with close intra-arterial injection produced similar differential blockade of O2 and CO2 chemoreception, preserving the nicotine and dopamine effects. This study confirmed the previous findings and provided new evidence showing that 1) the responses of carotid chemoreceptor to O2 and CO2 were separable by oligomycin due to the inhibition of oxidative phosphorylation and 2) the responses to nicotine and dopamine were intact even after blockade of O2 response.


Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 182
Author(s):  
Claudia Miranda ◽  
Alejandro Ruiz-Picazo ◽  
Paula Pomares ◽  
Isabel Gonzalez-Alvarez ◽  
Marival Bermejo ◽  
...  

The main aim of this work is the biopharmaceutical characterization of a new hybrid benzodiazepine-dihydropyridine derivative, JM-20, derived with potent anti-ischemic and neuroprotective effects. In this study, the pKa and the pH-solubility profile were experimentally determined. Additionally, effective intestinal permeability was measured using three in vitro epithelial cell lines (MDCK, MDCK-MDR1 and Caco-2) and an in situ closed-loop intestinal perfusion technique. The results indicate that JM-20 is more soluble at acidic pH (9.18 ± 0.16); however, the Dose number (Do) was greater than 1, suggesting that it is a low-solubility compound. The permeability values obtained with in vitro cell lines as well as with the in situ perfusion method show that JM-20 is a highly permeable compound (Caco-2 value 3.8 × 10−5). The presence of an absorption carrier-mediated transport mechanism was also demonstrated, as well as the efflux effect of P-glycoprotein on the permeability values. Finally, JM-20 was provisionally classified as class 2 according to the biopharmaceutical classification system (BCS) due to its high intestinal permeability and low solubility. The potential good oral absorption of this compound could be limited by its solubility.


Sensors ◽  
2021 ◽  
Vol 21 (16) ◽  
pp. 5432
Author(s):  
Donato Calabria ◽  
Massimo Guardigli ◽  
Paolo Severi ◽  
Ilaria Trozzi ◽  
Andrea Pace ◽  
...  

In recent years, there has been a continuously growing interest in antioxidants by both customers and food industry. The beneficial health effects of antioxidants led to their widespread use in fortified functional foods, as dietary supplements and as preservatives. A variety of analytical methods are available to evaluate the total antioxidant capacity (TAC) of food extracts and beverages. However, most of them are expensive, time-consuming, and require laboratory instrumentation. Therefore, simple, cheap, and fast portable sensors for point-of-need measurement of antioxidants in food samples are needed. Here, we describe a smartphone-based chemosensor for on-site assessment of TAC of aqueous matrices, relying on the antioxidant-induced formation of gold nanoparticles. The reaction takes place in ready-to-use analytical cartridges containing an hydrogel reaction medium preloaded with Au(III) and is monitored by using the smartphone’s CMOS camera. An analytical device including an LED-based lighting system was developed to ensure uniform and reproducible illumination of the analytical cartridge. The chemosensor permitted rapid TAC measurements of aqueous samples, including teas, herbal infusions, beverages, and extra virgin olive oil extracts, providing results that correlated with those of the reference methods for TAC assessment, e.g., oxygen radical absorbance capacity (ORAC).


Antioxidants ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 1819
Author(s):  
Alexandra Olmo-Cunillera ◽  
Julián Lozano-Castellón ◽  
Maria Pérez ◽  
Eleftherios Miliarakis ◽  
Anna Tresserra-Rimbau ◽  
...  

To meet the growing demand for high-quality extra-virgin olive oil (EVOO) with health-promoting properties and pleasant sensory properties, studies are needed to establish optimal production parameters. Bioactive components of EVOO, including phenolic compounds, carotenoids, chlorophylls, tocopherols, and squalene, contribute to its organoleptic properties and beneficial health effects. The aim of this study was to develop an Arbequina EVOO with high phenol content, particularly oleocanthal and oleacein, on a laboratory scale by analyzing the effects of different temperatures (20, 25, and 30 °C) and times (30 and 45 min) of malaxation. Higher temperatures decreased the levels of the phenolic compounds, secoiridoids, tocopherols, and squalene, but increased the pigments. EVOO with the highest quality was produced using malaxation parameters of 20 °C and 30 min, although oleocanthal and oleacein were higher at 30 and 25 °C, respectively. Overall, 20 °C and 30 min were the processing conditions that most favored the physiological and chemical processes that contribute to higher levels of bioactive compounds in the oil and diminished their degradation and oxidation processes.


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