Photodynamic therapy (PDT) is a minimally invasive therapeutic approach that has shown promising results in recent years, particularly in the dermatological clinical treatment of several pathologies, including neoplastic skin diseases. In light of the recent discovery of the photosensitizing properties of a water-soluble group of amino-based flavylium dyes, research efforts have led to the development of a novel synthetic dye with two diethylamino moieties in its structure, 7,4'-di(diethylamino)flavylium (7,4'diN(Et)). This dye was tested as a potential photosensitizer for PDT of skin cancer.
View Article and Find Full Text PDFAnthocyanins are phytonutrients with physiological activity belonging to the flavonoid family whose transport and absorption in the human body follow specific pathways. In the upper gastrointestinal tract, anthocyanins are rarely absorbed intact by active transporters, with most reaching the colon, where bacteria convert them into metabolites. There is mounting evidence that anthocyanins can be used for prevention and treatment of intestinal diseases, including inflammatory bowel disease (IBD), irritable bowel syndrome (IBS), and colorectal cancer (CRC), through the protective function on the intestinal epithelial barrier, immunomodulation, antioxidants, and gut microbiota metabolism.
View Article and Find Full Text PDFAnthocyanins are widespread and biologically active water-soluble phenolic pigments responsible for a wide range of vivid colours, from red (acidic conditions) to purplish blue (basic conditions), present in fruits, vegetables, and coloured grains. The pigments' stability and colours are influenced mainly by pH but also by structure, temperature, and light. The colour-stabilizing mechanisms of plants are determined by inter- and intramolecular co-pigmentation and metal complexation, driven by van der Waals, π-π stacking, hydrogen bonding, and metal-ligand interactions.
View Article and Find Full Text PDFFollowing our previous reports on dual-action antibacterial and collagenesis-inducing hybrid peptide constructs based on "pentapeptide-4" (PP4, with amino acid sequence KTTKS), whose -palmitoyl derivative is the well-known cosmeceutical ingredient Matrixyl, herein we disclose novel ionic liquid/PP4 conjugates (IL-KTTKS). These conjugates present potent activity against either antibiotic-susceptible strains or multidrug resistant clinical isolates of both Gram-positive and Gram-negative bacterial species belonging to the so-called "ESKAPE" group of pathogens. Noteworthy, their antibacterial activity is preserved in simulated wound fluid, which anticipates an effective action in the setting of a real wound bed.
View Article and Find Full Text PDFOver the years, anthocyanins have emerged as one of the most enthralling groups of natural phenolic compounds and more than 700 distinct structures have already been identified, illustrating the exceptional variety spread in nature. The interest raised around anthocyanins goes way beyond their visually appealing colors and their acknowledged structural and biological properties have fueled intensive research toward their application in different contexts. However, the high susceptibility of monoglycosylated anthocyanins to degradation under certain external conditions might compromise their application.
View Article and Find Full Text PDFResearch in pharmacological therapy has led to the availability of many antidiabetic agents. New recommendations for precision medicine and particularly precision nutrition may greatly contribute to the control and especially to the prevention of diabetes. This scenario greatly encourages the search for novel non-pharmaceutical molecules.
View Article and Find Full Text PDFType 2 diabetes mellitus (T2DM) is one of the most prevalent chronic metabolic diseases of the 21st century. Nevertheless, its prevalence might be attenuated by taking advantage of bioactive compounds commonly found in fruits and vegetables. This work is focused on the recovery of polyphenols and polysaccharide-polyphenol conjugates from grape pomace for T2DM management and prevention.
View Article and Find Full Text PDFEfficient antibiotics are being exhausted, which compromises the treatment of infections, including complicated skin and skin structure infections (cSSTI) often associated with multidrug resistant (MDR) bacteria, methicillin-resistant (MRSA) being the most prevalent. Antimicrobial peptides (AMP) are being increasingly regarded as the new hope for the post-antibiotic era. Thus, future management of cSSTI may include use of peptides that, on the one hand, behave as AMP and, on the other, are able to promote fast and correct skin rebuilding.
View Article and Find Full Text PDFPhotodynamic therapy (PDT) is a well-established therapeutic for the treatment of different diseases. The growing interest of this technique required the development of new photosensitizers with better photo-features. This work reports the study of the potential of five nature-inspired amino-based flavylium compounds with different structural features as photosensitizers towards topical PDT.
View Article and Find Full Text PDFBacterial quorum sensing (QS) is a cell-cell communication system that regulates several bacterial mechanisms, including the production of virulence factors and biofilm formation. Thus, targeting microbial QS is seen as a plausible alternative strategy to antibiotics, with potentiality to combat multidrug-resistant pathogens. Many phytochemicals with QS interference activity are currently being explored.
View Article and Find Full Text PDFSeaweeds are one of the largest producers of biomass in the marine environment and a source of multiple bioactive metabolites with valuable health benefits. Among these, phlorotannins have been widely recognized for their promising bioactive properties. The potential antitumor capacity of -derived phlorotannins remains, however, poorly explored, especially in gastrointestinal tract-related tumors.
View Article and Find Full Text PDFHuman skin is commonly described as a particularly dynamic and complex environment, with a physiological balance continuously orchestrated by numerous internal and external factors. Intrinsic aging, exposure to UV radiation and skin pathogens are some of the key players that account for dermatological alterations and ailments. In this regard, this study intended to explore the potential skin-health beneficial properties of a group of molecules belonging to the anthocyanin family: cyanidin- and malvidin-3--glucosides and some of their structurally related pigments, resulting in a library of compounds with different structural properties and color hues.
View Article and Find Full Text PDFTyrosinase is the central enzyme involved in the highly complex process of melanin formation, catalyzing the rate-limiting steps of this biosynthetic pathway. Due to such a preponderant role, it has become a major target in the treatment of undesired skin pigmentation conditions and also in the prevention of enzymatic food browning. Numerous phenolic-based structures from natural sources have been pointed out as potential tyrosinase inhibitors, including anthocyanins.
View Article and Find Full Text PDFDuring kiwiberry production, different by-products are generated, including leaves that are removed to increase the fruit's solar exposure. The aim of this work was to extract bioactive compounds from kiwiberry leaf by employing microwave-assisted extraction (MAE). Compatible food solvents (water and ethanol) were employed.
View Article and Find Full Text PDFDihydrochalcones, phlorizin (PZ) and its aglycone phloretin (PT), have evidenced immunomodulatory effects through several mechanisms. However, the differential metabolic signatures that lead to these properties are largely unknown. Since macrophages play an important role in the immune response, our study aimed to characterise human THP-1 macrophages under PZ and PT exposure.
View Article and Find Full Text PDFAntioxidants (Basel)
October 2020
Phenolic compounds are one of the most widespread classes of compounds in nature, with several beneficial biological effects being associated with their anti-oxidant and anti-carcinogenic activities. Their application in the prevention or treatment of numerous chronic diseases have been studied, but a major drawback is still the low bioavailability of these compounds, as well as their instability towards pH, temperature, and light in some cases. Nanotechnology has emerged as an alternative to overcome these limitations, and the use of lipidic encapsulation systems is a promising technique to achieve an efficient drug delivery, protecting molecules from external factors and improving their bioavailability.
View Article and Find Full Text PDFDue to their physical and chemical characteristics, anthocyanins are amongst the most versatile groups of natural compounds. Such unique signature makes these compounds a focus in several different areas of research. Anthocyanins have well been reported as bioactive compounds in a myriad of health disorders such as cardiovascular diseases, cancer, and obesity, among others, due to their anti-inflammatory, antioxidant, anti-diabetic, anti-bacterial, and anti-proliferative capacities.
View Article and Find Full Text PDFA covalent conjugate between an antibacterial ionic liquid and an antimicrobial peptide was produced via "click" chemistry, and found to retain the parent peptide's activity against multidrug-resistant clinical isolates of Gram-negative bacteria, and antibiofilm action on a resistant clinical isolate of , while exhibiting much improved stability towards tyrosinase-mediated modifications. This unprecedented communication is a prelude for the promise held by ionic liquids -based approaches as tools to improve the action of bioactive peptides.
View Article and Find Full Text PDFMany efforts have been made in the past two decades into the search for novel natural and less-toxic anti-diabetic agents. Some clinical trials have assigned this ability to anthocyanins, although different factors like the food source, the amount ingested, the matrix effect and the time of consumption (before or after a meal) seem to result in contradictory conclusions. The possible mechanisms involved in these preventive or therapeutic effects will be discussed-giving emphasis to the latest in vitro and in silico approaches.
View Article and Find Full Text PDFThe effect of five different vinegars, applied as a seasoning, on the formation of polycyclic aromatic hydrocarbons (PAH) in charcoal-grilled pork loin was investigated. PAH were assayed using acetonitrile based-extraction and high-performance liquid chromatography with fluorescence detection. Unseasoned samples presented a mean value of 31.
View Article and Find Full Text PDFPhenolic compounds in plants are essential components of human nutrition, which provide various health benefits. However, some missing links became the research in phenolic compounds structures and potential applications in a challenging work. Despite universal extraction methods with mixtures of different organic solvents are generally adopted in the analysis of phenolic compounds, a need for establish a specific procedure is still open.
View Article and Find Full Text PDFMalvidin-3-O-glucoside, malvidin-3,5-O-diglucoside, malvidin-3-O-(6-O-coumaroyl)-glucoside-5-O-glucoside from Chinese Vitis davidii red wine were used to investigate the role of glucoside, diglucoside and coumaroylated glucoside moieties on their transport efficiency through MKN-28 gastric and Caco-2 intestinal cells. Due to the already described conversion of 3-O-glucosylated anthocyanins into 3-O-glucuronidated, the 3-O-glucuronidated metabolite of malvidin-3-O-glucoside was also tested. The antiproliferative activity was higher for the glucuronidated metabolite in both cell lines.
View Article and Find Full Text PDFAntimicrobial resistance is becoming one the most serious health threats worldwide, as it not only hampers effective treatment of infectious diseases using current antibiotics, but also increases the risks of medical procedures like surgery, transplantation, bone and dental implantation, chemotherapy, or chronic wound management. To date, there are no effective measures to tackle life-threatening nosocomial infections caused by multidrug resistant bacterial species, of which Gram-negative species within the so-called "ESKAPE" pathogens are the most worrisome. Many such bacteria are frequently isolated from severely infected skin lesions such as diabetic foot ulcers (DFU).
View Article and Find Full Text PDFThis study aims to exploit the molecular and cellular mechanisms concerning the functionality of dietary polyphenols (catechin, procyanidin B3, procyanidin C2, epigallocatechin and epigallocatechin gallate) in a nutritional context to prevent Celiac Disease (CD). In that sense, the interaction between the main CD bioactive peptide (32-mer peptide) and some polyphenols was fully characterized at the intestinal level under near physiological conditions by means of different spectroscopic techniques and dynamic simulations. Accordingly, it is proposed that the primarily polyphenol-binding sites on the 32-mer peptide correspond to leucine, tyrosine and phenylalanine containing domains being this interaction entropy-driven.
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