Chalcones are among the leading bioactive flavonoids with a therapeutic potential implicated to an array of bioactivities investigated by a series of preclinical and clinical studies. In this article, different scientific databases were searched to retrieve studies depicting the biological activities of chalcones and their derivatives. This review comprehensively describes preclinical studies on chalcones and their derivatives describing their immense significance as antidiabetic, anticancer, anti-inflammatory, antimicrobial, antioxidant, antiparasitic, psychoactive, and neuroprotective agents. Besides, clinical trials revealed their use in the treatment of chronic venous insufficiency, skin conditions, and cancer. Bioavailability studies on chalcones and derivatives indicate possible hindrance and improvement in relation to its nutraceutical and pharmaceutical applications. Multifaceted and complex underlying mechanisms of chalcone actions demonstrated their ability to modulate a number of cancer cell lines, to inhibit a number of pathological microorganisms and parasites, and to control a number of signaling molecules and cascades related to disease modification. Clinical studies on chalcones revealed general absence of adverse effects besides reducing the clinical signs and symptoms with decent bioavailability. Further studies are needed to elucidate their structure activity, toxicity concerns, cellular basis of mode of action, and interactions with other molecules.

The genusCinnamomumincludes a number of plant species largely used as food, food additives and spices for a long time. Different traditional healing systems have used these plants as herbal remedies to cure diverse ailments. The aim of this comprehensive and updated review is to summarize the biodiversity of the genusCinnamomum, its bioactive compounds, the mechanisms that underlie the pharmacological activities and molecular targets and toxicological safety. All the data in this review have been collected from databases and recent scientific literature including Web of Science, PubMed, ScienceDirect etc. The results showed that the bioactive compounds ofCinnamomumspecies possess antimicrobial, antidiabetic, antioxidant, anti-inflammatory, anticancer and neuroprotective effects. The preclinical (in vitro/in vivo) studies provided the possible molecular mechanisms of these action. As a novelty, recent clinical studies and toxicological data described in this paper support and confirm the pharmacological importance of the genusCinnamomum.In conclusion, the obtained results from preclinical studies and clinical trials, as well as reduced side effects provide insights into future research of new drugs based on extracts and bioactive compounds fromCinnamomumplants.

Urolithin A is a metabolite generated from ellagic acid and ellagitannins by the intestinal microbiota after consumption of fruits such as pomegranates or strawberries. The objective of this study was to determine the cytoprotective capacity of this polyphenol in Neuro-2a cells subjected to oxidative stress, as well as its direct radical scavenging activity and properties as an inhibitor of oxidases. Cells treated with this compound and H₂O₂ showed a greater response to oxidative stress than cells only treated with H₂O₂, as mitochondrial activity (MTT assay), redox state (ROS formation, lipid peroxidation), and the activity of antioxidant enzymes (CAT: catalase, SOD: superoxide dismutase, GR: glutathione reductase, GPx: glutathione peroxidase) were significantly ameliorated; additionally, urolithin A enhanced the expression of cytoprotective peroxiredoxins 1 and 3. Urolithin A also acted as a direct radical scavenger, showing values of 13.2 μM Trolox Equivalents for Oxygen Radical Absorbance Capacity (ORAC) and 5.01 µM and 152.66 µM IC₅₀ values for superoxide and 2,2-diphenyss1-picrylhydrazyl (DPPH) radicals, respectively. Finally, inhibition of oxidizing enzymes, such as monoamine oxidase A and tyrosinase, was also detected in a dose-dependent manner. The cytoprotective effects of urolithin A could be attributed to the improvement of the cellular antioxidant battery, but also to its role as a direct radical scavenger and enzyme inhibitor of oxidases.

Cranberry (Vaccinium macrocarpon) and blueberry (Vaccinium myrtillus) juices are commonly consumed as a source of antioxidants. The aim of this study was to compare bioactivities as well as the differences in the polyphenol content and anthocyanin profile of both juices. Polyphenol and anthocyanin contents were quantified using spectrophotometric and chromatographic methods. Bioassays were carried out in terms of antioxidant properties in cell and cell free systems as well as inhibition of physiological enzymes that are targets involved in the prevention of chronic diseases (monoamine oxidase A, tyrosinase, acetylcholinesterase, α-glucosidase and dipeptidyl peptidase-4). Both juices contained a significant amount of anthocyanins (3.909 mg anthocyanins per mg extract for blueberry juice and 0.398 for cranberry juice) and also exhibited antioxidant properties against DPPH, superoxide radicals and hydrogen peroxide. These juices showed inhibitory effects on the enzymes, showing substantial potential as antioxidant, neuroprotective and anti-hyperglycaemic agents. The total anthocyanin and polyphenol content was higher in blueberry juice, which is indicative of a higher antioxidant activity. Both juices were also able to inhibit monoamine oxidase A, tyrosinase, α-glucosidase and dipeptidyl peptidase-4 in a dose-dependent manner. However, cranberry juice had a greater capacity than blueberry juice as an α-glucosidase inhibitor, revealing a similar activity to acarbose.