Search results for " bioavailability"

Intrinsic Absolute Bioavailability Prediction in Rats Based on In Situ Absorption Rate Constants and/or In Vitro Partition Coefficients: 6‐Fluoroquin…

2000

A preliminary study attempting to predict the intrinsic absolute bioavailability of a group of antibacterial 6-fluoroquinolones-including true and imperfect homologues as well as heterologues-was carried out. The intrinsic absolute bioavailability of the test compounds, F, was assessed on permanently cannulated conscious rats by comparing the trapezoidal normalized areas under the plasma concentration-time curves obtained by intravenous and oral routes (n = 8-12). The high-performance liquid chromatography analytical methods used for plasma samples are described. Prediction of the absolute bioavailability of the compounds was based on their intrinsic rat gut in situ absorption rate constant…

Δ5-Cholenoyl-amino acids as selective and orally available antagonists of the Epheephrin system

2015

The Eph receptor-ephrin system is an emerging target for the development of novel anti-angiogenic therapies. Research programs aimed at developing small-molecule antagonists of the Eph receptors are still in their initial stage as available compounds suffer from pharmacological drawbacks, limiting their application in vitro and in vivo. In the present work, we report the design, synthesis and evaluation of structure-activity relationships of a class of Δ(5)-cholenoyl-amino acid conjugates as Eph-ephrin antagonists. As a major achievement of our exploration, we identified N-(3β-hydroxy-Δ(5)-cholen-24-oyl)-L-tryptophan (UniPR1331) as the first small molecule antagonist of the Eph-ephrin syste…

Impacts of weathered microplastics on bioavailability of pollutants in Paracentrotus lividus and Danio rerio: molecular and ecotoxicological approach…

2022

Plastic materials provide countless applications in every sector of human life, from food and health preservation to textiles and electronics industry (Cole et al., 2011;Thompson et al., 2009) which is resulting in huge amount of plastic waste. Recently, it was estimated that plastics account for the 80-90% of the whole marine litter (Derraik, 2002) and over 5 trillion microscopic plastic fragments are floating on the surface of the World Oceans (Eriksen et al., 2014). The predominant form of marine plastic litter is called “Microplastics (MPs)", terminology by Thompson et al. 2004, used to indicate small plastic fragments, fibers and granules of microscopic size (1 μm to 5 mm in diameter).…

Nanoassemblies Based on Supramolecular Complexes of Nonionic Amphiphilic Cyclodextrin and Sorafenib as Effective Weapons to Kill Human HCC Cells

2015

Sorafenib (Sor), an effective chemiotherapeutic drug utilized against hepatocellular carcinoma (HOC), robustly interacts with nonionic amphiphilic cyclodextrin (aCD, SC6OH), forming, in aqueous solution, supramolecular complexes that behave as building blocks of highly water-dispersible colloidal nanoassemblies. SC6OH/Sor complex has been characterized by complementary spectroscopic techniques, such as UV-vis, steady-state fluorescence and anisotropy, resonance light scattering and H-1 NMR. The spectroscopic evidences and experiments carried out in the presence of an adamantane derivative, which competes with drug for CD cavity, agree with the entrapment of Sor in aCD, pointing out the role…

Milk versus caseinophosphopeptides added to fruit beverage: Resistance and release from simulated gastrointestinal digestion

2010

The influence of simulated gastrointestinal digestion on caseinophosphopeptides (CPPs) formation in milk-based fruit beverage was evaluated, together with resistance of a pool of CPPs added to fruit beverage. In milk-based fruit beverage, four CPPs were identified that can be justified by their presence in raw milk or due to processing. When it was subjected to simulated gastrointestinal digestion, 10 CPPs were identified, and only 1 presented the cluster (SpSpSpEE) (3 phosphoseryl group followed by 2 glutamic acid residues), which corresponded to αs2-CN(1-19)4P. CPPs added to fruit beverage are resistant to simulated gastrointestinal digestion, and 16 CPPs were identified originating from …

Redox Properties, Bioactivity and Health Effects of Indicaxanthin, a Bioavailable Phytochemical from Opuntia ficus indica, L.: A Critical Review of A…

2022

Phytochemicals from plant foods are considered essential to human health. Known for their role in the adaptation of plants to their environment, these compounds can induce adaptive responses in cells, many of which are directed at maintaining the redox tone. Indicaxanthin is a long-known betalain pigment found in the genus Opuntia of cactus pear and highly concentrated in the edible fruits of O. ficus indica, L. whose bioactivity has been overlooked until recently. This review summarizes studies conducted so far in vitro and in vivo, most of which have been performed in our laboratory. The chemical and physicochemical characteristics of Indicaxanthin are reflected in the molecule’s reducing…

Iron intake among Lebanese women: sociodemographic factors, iron-rich dietary patterns, and preparation of hummus, a Mediterranean dish

2021

Background: Plant-based foods such as hummus are alternative to animal protein, and when properly pre-pared, they help to alleviate nutritional iron deficiency that leads to anemia, a global health problem. Objective: The objective was to assess iron intake among Lebanese women and related participant’s charac-teristics, discern iron-rich dietary patterns, evaluate their association with nutrients intake and participant’s sociodemographic characteristics, and identify the women preparing hummus traditionally and properly for an enhanced iron bioavailability. Design: A cross-sectional study of 400 Lebanese women (18–74 years old) was conducted in Lebanon. Data from a questionnaire, including…

Uptake of Betanin and Indicaxanthin by Caco-2 cell monolayer.

2009

In vitro evaluation of glycol chitosan based formulations as oral delivery systems for efflux pump inhibition.

2017

Recently, we have reported that glycol chitosan (GCS) was able to reverse the P- glycoprotein (P-gp) efflux pump. The objective of the present study was to evaluate the potential of two GCS-based dosage forms (aqueous solution or nanoparticle suspension) for oral administration of the P-gp substrate Rho-123. A further aim of the present study was to assess the effect of the glycol chitosan-4-thiobutylamidine thiomer (GCS-TBA) on P-gp activity considering that the corresponding thiomer of chitosan series is a well-known P-gp inhibitor. Pre-treatment of Caco-2 cell monolayer with a GCS solution or GCS-based nanoparticles increased the absorptive transport of Rho-123 across the monolayer of 1.…

In vitrobioaccessibility of iron and zinc in fortified fruit beverages

2009

Summary Iron and zinc bioaccessibility was estimated in the in vitro gastrointestinal digests of six different fortified fruit beverages (Fb) containing iron and/or zinc and/or skimmed milk (M). Solubility values can be used to establish trends in relative bioavailability of iron and zinc, as the first stage towards mineral bioavailability comprises solubility in the intestinal tract. FbFe, FbFeM and FbFeZnM samples showed iron bioaccessibility above 88%, differing (P < 0.05) from those of FbFeZn (53%). In turn, FbZn, FbFeZn and FbZnM samples presented higher zinc bioaccessibility (above 68%), differing (P < 0.05) from those of FbFeZnM (48%). The presence of milk-derived caseinophosphopepti…