Exploiting the beneficial effects of Salvia officinalis L. extracts in human health and assessing their activity as potent functional regulators of food microbiota.

Salvia officinalis L. has attracted scientific and industrial interest due to its pharmacological properties. However, its detailed phytochemical profile and its correlation with beneficial effects in the human microbiome and oxidative stress remained elusive. To unveil this, S. officinalis was collected from the region of Epirus and its molecular identity was verified with DNA barcoding. Phytochemical profile for both aqueous and ethanol-based extracts was determined by high-pressure liquid chromatography-tandem mass spectrometry and 103 phytochemicals were determined. The effect of S. officinalis extracts as functional regulators of food microbiota by stimulating the growth of Lacticaseibacillus rhamnosus strains and by suppressing evolution of pathogenic bacteria was verified. Furthermore, we recorded that both extracts exhibited a significant cellular protection against H2O2-induced DNA damage. Finally, both extracts exhibited strong inhibitory effect towards LDL oxidation. This study provides a comprehensive characterization of S. officinalis on its phytochemical components as also its potential impact in human microbiome and oxidative stress.

Development of Dairy Products Fortified with Plant Extracts: Antioxidant and Phenolic Content Characterization.

In recent decades, there has been growing interest in the fortification of dairy products with antioxidants and phenolics derived from plant byproducts and herbs. The present study focused on the analysis of dairy products, including kefir, cream cheese, yogurt, and vegan yogurt, enhanced with aqueous extracts of plant byproducts (Citrus aurantium peel, Citrus limon peel and Rosa canina seed) and herbs (Sideritis spp., Hypericum perforatum, Origanum dictamnus, Mentha pulegium L., Melissa oficinallis, Mentha spicata L. and Lavandula angustifolia) to characterize their antioxidant content, phenolic profile, and organoleptic characteristics. Antioxidant and phenolic content were determined by Folin-Ciocalteu and ferric reducing antioxidant power (FRAP) assays and presented values up to 46.61 ± 7.22 mmol Fe2+/L and 82.97 ± 4.29 mg gallic acid (GAE)/g, respectively for the aqueous extracts, as well as up to 0.68 ± 0.06 mmol Fe2+/L and 2.82 ± 0.36 mg GAE/g for the fortified dairy products. The bioavailability of antioxidants and phenolics in fortified foods was determined after in vitro digestion and ranged between 4 and 68%. The phytochemical profile of the aqueous extracts was determined by mass spectrometry, and 162 phytochemicals were determined, from which 128 belong to the polyphenol family including flavonoids and phenolic acids. Furthermore, most of the identified compounds have been recorded to possess enhanced antioxidant capacity in correlation to the in vitro findings. Finally, organoleptic evaluation showed an overall acceptability around 3.0 ± 1.0 on a 5-point scale. In conclusion, the studied plants and herbal extracts can be used for the fortification of a variety of dairy products with potential positive effects on human health.

Phenethyl Ester of Gallic Acid Ameliorates Experimental Autoimmune Encephalomyelitis.

Gallic acid is a phenolic acid present in various plants, nuts, and fruits. It is well known for its anti-oxidative and anti-inflammatory properties. The phenethyl ester of gallic acid (PEGA) was synthesized with the aim of increasing the bioavailability of gallic acid, and thus its pharmacological potential. Here, the effects of PEGA on encephalitogenic cells were examined, and PEGA was found to modulate the inflammatory activities of T cells and macrophages/microglia. Specifically, PEGA reduced the release of interleukin (IL)-17 and interferon (IFN)-γ from T cells, as well as NO, and IL-6 from macrophages/microglia. Importantly, PEGA ameliorated experimental autoimmune encephalomyelitis, an animal model of chronic inflammatory disease of the central nervous system (CNS)-multiple sclerosis. Thus, PEGA is a potent anti-inflammatory compound with a perspective to be further explored in the context of CNS autoimmunity and other chronic inflammatory disorders.

NMR and computational studies reveal novel aspects in molecular recognition of unsaturated fatty acids with non-labelled serum albumin.

An approach based on the combined use of saturation transfer difference (STD), Tr-NOESY and Inter-ligand NOEs for PHArmacophore Mapping (INPHARMA) NMR techniques and docking calculations is reported, for the first time, for mapping interactions and specific binding sites of caproleic acid (10 : 1 cis-9), oleic acid (18 : 1 cis-9), linoleic acid (18 : 2 cis-9,12) and linolenic (18 : 3, cis-9,12,15) free fatty acids (FFAs) with non-labelled serum albumin (BSA/HSA). Significant negative inter-ligand NOEs between the FFAs and the drugs ibuprofen and warfarin, through competition experiments, were observed. The inter-ligand NOEs and docking calculations were interpreted in terms of competitive binding mode, the significant folding of the bis allylic region and the presence of two orientations of the FFAs in the warfarin binding site (FA7), due to two potential distinctive anchoring polar groups of amino acids. This conformational flexibility is the reason that, the location and conformational states of the FFAs in the binding site of warfarin could not be determined accurately, despite numerous available X-ray structural studies. α-Linolenic acid competes favourably with warfarin at the binding site FA7. Isothermal titration calorimetry experiments of the preformed HSA/α-linolenic acid complex upon titration with warfarin show a significant reduction in the binding constant of warfarin, in very good agreement with NMR and computational data. The combined use, therefore, of STD, Tr-NOESY and INPHARMA NMR, ITC and docking calculations may find promising applications in the field of protein-lipid recognition research.

Rational Design and Synthesis of AT1R Antagonists.

Hypertension is one of the most common diseases nowadays and is still the major cause of premature death despite of the continuous discovery of novel therapeutics. The discovery of the Renin Angiotensin System (RAS) unveiled a path to develop efficient drugs to fruitfully combat hypertension. Several compounds that prevent the Angiotensin II hormone from binding and activating the AT1R, named sartans, have been developed. Herein, we report a comprehensive review of the synthetic paths followed for the development of different sartans since the discovery of the first sartan, Losartan.