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Non-structural protein 5 (Nsp5) is a cysteine protease that plays a key role in SARS-CoV-2 replication, suppressing host protein synthesis and promoting immune evasion. The investigation of natural products as a potential strategy for Nsp5 inhibition is gaining attention as a means of developing antiviral agents. In this work, we have investigated the physicochemical properties and structure-activity relationships of ellagic acid and its gut metabolites, urolithins A–D, as ligands of Nsp5. Results allow us to identify urolithin D as promising ligand of Nsp5, with a dissociation constant in the nanomolar range of potency. Although urolithin D is able to bind to the catalytic cleft of Nsp5, the appraisal of its viral replication inhibition against SARS-CoV-2 in Vero E6 assay highlights a lack of activity. While these results are discussed in the framework of the available literature reporting conflicting data on polyphenol antiviral activity, they provide new clues for natural products as potential viral protease inhibitors. [ABSTRACT FROM AUTHOR]

Context: Ellagic acid (EA) is used in traditional medicine to treated hyperlipidaemia. Objective: This study examined if AMPK mediates the anti-steatotic effect of ellagic acid (EA) in streptozotocin (STZ)-induced type 1 diabetes mellitus in rats. Materials and methods: Adult male Wistar rats (130 ± 10 g) were divided into 6 groups (n=8 rats/group) as control, controlþEA, controlþEAþCC an AMPK inhibitor), T1DM, T1DMþEA, and T1DMþEAþCC. The treatments with EA (50 mg/kg/orally) and CC (200 ng/rat/i.p.) were given the desired groups for 12 weeks, daily. Results: In T1DM-rats, EA reduced fasting glucose levels (44.8%), increased fasting insulin levels (92.8%), prevented hepatic lipid accumulation, and decreased hepatic and serum levels of total triglycerides (54% & 61%), cholesterol (57% & 48%), and free fatty acids (40% & 37%). It also reduced hepatic levels of ROS (62%), MDA (52%), TNF-a (62%), and IL-6 (57.2%) and the nuclear activity of NF-jB p65 (54%) but increased the nuclear activity of Nrf-2 (4-fold) and levels of GSH (107%) and SOD (87%). Besides, EA reduced downregulated SREBP1 (35%), SREBP2 (34%), ACC-1 (36%), FAS (38%), and HMG-CoAR (49%) but stimulated mRNA levels of PPARa (1.7-fold) and CPT1a (1.8-fold), CPT1b (2.9-fold), and p-AMPK (4-fold). All these events were prevented by the co-administration of CC. Discussion and conclusions: These findings encourage the use of EA to treat hepatic disorders, and non-alcoholic fatty liver disease (NAFLD). Further in vivo and in vitro studies are needed to validate its potential in clinical medicine. [ABSTRACT FROM AUTHOR]

This study aimed to characterize the quality and bioactive compounds from five cultivars grown in Mexico´s northern region: Heritage, Summit, Harvest, and red and yellow Autumn. The physicochemical characteristics, DPPH anti-radical capacity, total phenolics, flavonoid and anthocyanins, polyphenolic profile, and ascorbic acid levels of the raspberries were assessed. The Harvest cultivar presented the highest weight and firmness and the lowest yield, total phenolics, and flavonoids. The yellow Autumn Bliss contained higher concentrations of polyphenols and ascorbic acid, and the red Autumn Bliss contained higher concentrations of flavonoids and anthocyanins and possessed a greater antioxidant capacity. The polyphenol profile indicated the presence of seven phenolic acids, namely, ellagic, gallic, caffeic, chlorogenic, p-coumaric, hydroxybenzoic, and protocatechuic acids; and four flavonoids, namely, catechin, quercetin-3-β-D-glucoside, quercetin-3-glucuronide, and rutin; these compounds were present in all the varieties, except for rutin, in yellow Autumn Bliss. The results of this study highlight the most valuable raspberry cultivars in terms of weight and firmness (Harvest), yield (Heritage), polyphenols and ascorbic acid (yellow Autumn Bliss), and anthocyanins and antioxidant capacity (red Autumn Bliss) in raspberries grown in northern Mexico. [ABSTRACT FROM AUTHOR]

Irvingia gabonensis, also known as 'bush mango', is a multipurpose fruit tree, native to tropical Africa. It is a priority indigenous fruit tree in western and central Africa since its wood is used for making utensils and fruits are mostly used as food and medicine. The objective of this work is to provide an updated review of the available knowledge about physicochemical characteristics of I. gabonensis fruit in order to evaluate its potential use in the food industry. The fruit mesocarp contains various phytochemicals and ascorbic acid concentration higher than some vitamin C rich fruits, then it is consumed fresh or dried, used to produce juice and wine, or as a flavourant. I. gabonensis fruit kernel is rich in oil (63%–69% crude fat), mainly composed of myristic and lauric acids. Its triacylglycerol composition and, resultantly, melting curve and polymorphism indicate an aptitude for diverse applications, as it is solid at room temperature. Forty-one phenolic compounds were identified in the seeds and derived extracts and supplements, being ellagic acid and its derivates the most present. This review enhances our knowledge about nutritional content and health benefits of I. gabonensis whole fruit, especially its pulp and seed, evidencing the need for safer and more efficient production of value-added products. [ABSTRACT FROM AUTHOR]

Research concerning the benefits derived from dietary polyphenols, a significant class within the family of phytonutrients, has increased considerably in the last decade. Prior to the late 1990s, the nutritional spotlight focused on the antioxidant capabilities of carotenoids, vitamins, and minerals. More recently, however, research has emerged in strong support of the antioxidant capacity of polyphenols and their role in the prevention and/or treatment of certain cancers, diabetes, cardiovascular diseases, and inflammation. Polyphenols are categorized according to the nature of their carbon skeleton, ranging from basic phenolic molecules to highly complex compounds, such as flavonoids, the most common and widely studied of all phenolic compounds. The most prevalent phenolic acids include ellagic acid, gallic acid, tannic acid, and capsaicin. [ABSTRACT FROM AUTHOR]

Epidemiological reports as well as experimental studies have demonstrated the significant health benefits provided by regular berry consumption. Berries possess both prophylactic and therapeutic potential against several chronic illnesses, such as cardiovascular, neurodegenerative, and neoplastic diseases. Berries owe their health benefits to phytoconstituents, such as polyphenolic anthocyanins, ellagic acid, and a diverse array of phytochemicals bestowed with potent antioxidant and anti-inflammatory effects as well as the ability to engage a multitude of signaling pathways. This review highlights the principal chemical constituents present in berries and their primary molecular targets. The article presents and critically analyzes the chemopreventive and therapeutic potential of berry extracts, fractions, and bioactive components on various cancers of the gastrointestinal tract (GIT), including esophageal, stomach, intestinal, and colorectal cancers as well as cancers of the upper aerodigestive tract, such as oral cancer. The current status of clinical studies evaluating berry products in several aforementioned cancers is presented. Various emerging issues including dose-ranging and dosage forms, the role of synergy and the usage of combination therapy as well as other relevant areas essential for the development of berry phytoconstituents as mainstream chemopreventive and therapeutic agents against aerodigestive and GIT cancers are critically discussed. [ABSTRACT FROM AUTHOR]

In recent years, the therapeutic use of non-drug substances such as herbal and medicinal foods is increasing progressively. Of these substances, Punica granatum L., which is an ancient and highly distinctive fruit, has been proposed for treatment of several different illnesses. Ellagic acid (EA) is one of those biological molecules found in pomegranate and may have therapeutic potential in many diseases. EA has been detected not only in pomegranate but also in a wide variety of fruits and nuts such as raspberries, strawberries, walnuts, grapes and black currants, and is becoming an increasingly popular dietary supplement over recent years. Similar to other ellagitannins (ETs), EA is quite stable under physiological conditions in the stomach. EA and ETs as active agents induce vasorelaxation, oxygen free radical scavenging, hypolipidemic, anti-inflammatory and anti-carcinogenic activities in various animal preparations call an attention to the need for designing adequate tests in humans to assess these potentially useful properties in diseased states. [ABSTRACT FROM AUTHOR]

Interest in ellagitannins and ellagic acid has increased over the past few years due to its properties as a micronutrient. Ellagitannins are complex plant polyphenols composed of hexahydroxydiphenoyl moieties esterified to a sugar. Fruits (especially berries and nuts) are rich sources of ellagitannins and ellagic acid, a hydrolytic product of ellagitannins. These secondary metabolites give the characteristic taste to the fruits and their products, and also play an important role in food processing. This paper reviews research about occurrence in foods, change during process, and antioxidant activity of ellagitannins and ellagic acid. [ABSTRACT FROM AUTHOR]

Maple syrup of four grades (extra-light, light, medium, and dark) of the 2007 crop was provided by three local (St. Joseph's Island, Ontario, Canada) producers. Twenty-four phenolic compounds were isolated from a medium-grade syrup and identified on the basis of spectral and chemical evidence. They were (a) benzoic acid and several hydroxylated and methoxylated derivatives (gallic acid, 1-O-galloyl-β-d-glucose, γ-resorcylic acid); (b) cinnamic acid derivatives (p-coumaric acid, 4-methoxycinnamic acid, caffeic acid, ferulic acid, sinapic acid, and the ester chlorogenic acid); (c) flavonoids, the flavanols catechin and epicatechin, and the flavonols kaempferol and its 3-O-β-d-glucoside, 3-O-β-d-galactoside, quercetin and its 3-O-β-d-glucoside, 3-O-β-L-rhamnoside and 3-O-rhamnoglucoside (rutin). Traces obtained at 280 and 350 nm in HPLC runs of the ethyl acetate-soluble fractions of eight samples indicated the presence of many more phenolic substances, most at very low concentration with some varibilities in peak heights, but not in retention times, among the syrups. In view of the well-established antioxidant activity these substances possess, it is suggested that it is the complexity of the mixture rather than any one compound that may serve to counter the unhealthful presence of the high concentration of sugars in the syrup. [ABSTRACT FROM AUTHOR]

Ellagic acid (EA) is a naturally occurring polyphenol found in a variety of plants in its free form or in the form of ellagitannin glycosides. In this study, the ellagic acid content of the methanol extracts of Juglans regia L. (Juglandaceae) leaves, Castanea sativa Mill. (Fagaceae) stem bark, and Eucalyptus camaldulensis Dehnh. (Myrtaceae) leaves was determined to develop melanogenesis inhibitors. An improved NaNO2 assay was used for determination of EA. The tyrosinase inhibitory activity of the extracts and synthetic EA was tested in vitro by monitoring the appearance of dopachrome, an intermediate in the melanogenesis process. The results were compared keeping the same total concentration of inhibitor. The efficacy of EA (1%) was compared with arbutin (1%) and hydroquinone monomethyl ether (1%) as reference substances, and it was found to be a more efficient suppressor of pigmentation. The effect of formulation variables on the tyrosinase inhibitory activity was also evaluated. Based on dopachrome tests performed in the formulations, it could be concluded that the combination with plant extracts had a synergistic effect, and gel formulation could be suggested as an effective carrier for treating uneven skin pigmentation. [ABSTRACT FROM AUTHOR]