Browsing by Author "León-González, Antonio J."

Chalcones constitute a group of phenolic compounds that command an increasing interest on cancer research. Natural chalcones are widespread through the plant kingdom. The most abundant and investigated chalcones are isoliquiritigenin, flavokawain and xanthohumol, which are present in the Fabaceae, Piperaceae, Cannabaceae, and Moraceae families. These chalcones have been shown to be promising lead antitumor-chemopreventive drugs by three different activities: antioxidants, cytotoxic and apoptosis inducers. In recent years, SAR (structure-activity relationship) has contributed towards the improvement of anticancer properties of chalcones by substituting aryl rings and introducing heterocyclic moieties. This review summarizes the anticancer activities shown by natural chalcones and the SAR and describes how different chemical moiety modifications could lead them to be therapeutically useful in the treatment of cancer.

Background/Objectives: Corema album berries are edible fruits from the Iberian Atlantic coast, characterized by a rich polyphenolic composition, which endows their juice with potential protective effects against neurodegeneration. This study aimed to evaluate the potential of the relatively lesser-known C. album berries as a novel neuroprotective agent against neurodegenerative diseases. Methods: The phenolic compounds of the juice were characterized using UHPLC-HRMS (Orbitrap). The SH-SY5Y neuroblastoma line was used to determine the preventive effect of the juice against H2O2-induced oxidative stress. Furthermore, neuronal cells were differentiated into dopaminergic and cholinergic lines and exposed to 6-hydroxydopamine and okadaic acid, respectively, to simulate in vitro models of Parkinson’s disease and Alzheimer’s disease. The ability of the juice to enhance neuronal viability under toxic conditions was examined. Additionally, its inhibitory effects on neuroprotective-related enzymes, including MAO-A and MAO-B, were assessed in vitro. Results: Phytochemical characterization reveals that 5-O-caffeoylquinic acid constitutes 80% of the total phenolic compounds. Higher concentrations of the juice effectively protected both differentiated and undifferentiated SH-SY5Y cells from H2O2-induced oxidative damage, reducing oxidative stress by approximately 20% and suggesting a dose-dependent mechanism. Moreover, the presence of the juice significantly enhanced the viability of dopaminergic and cholinergic cells exposed to neurotoxic agents. In vitro, the juice inhibited the activity of MAO-A (IC50 = 87.21 μg/mL) and MAO-B (IC50 = 56.50 μg/mL). Conclusions: While these findings highlight C. album berries as a promising neuroprotective agent, further research is required to elucidate its neuroprotective mechanisms in cell and animal models and, ultimately, in human trials.

Plants of the genus Retama (Fabaceae) are used in traditional medicine of the Mediterranean Basin as an emetic, purgative, and vermifuge. Certain Retama species are also employed to treat a multitude of disorders, including diabetes, hepatitis, jaundice, sore throat, skin diseases, joint pain, rheumatism, fever, and inflammation. This review deals with updated information on the distribution, botanical characteristics, ethnopharmacology, phytochemistry, pharmacological activities, and toxicity of the Retama species in order to support their therapeutic potential and to provide an input for future research prospects. The Retama species are mainly employed as ethnomedicinal remedies in Mediterranean countries, including Algeria, Egypt, Italy, Lebanon, Libya, Morocco, and Spain. Previous phytochemical studies show a complex composition, rich in carbohydrates (galactomannans), polyols (pinitol), fatty acids, phenolic compounds (genistein, daidzein) and alkaloids (retamine, lupanine). The pharmacological activity of their various extracts has been widely studied, revealing, among others, the anti-microbial, anti-inflammatory, and anti-diabetic effects of these species. The potential toxicity of these medicinal plants has also been discussed. Although recent experimental evidence confirms the pharmacological interest of this genus, further studies are necessary.

The rhizomes of Acanthus mollis have traditionally been used for the treatment of several ailments involving inflammation. However, to the best of our knowledge, their chemical composition and pharmacological properties have not been studied until now. As a first approach, this study analyses the A. mollis rhizome hexane extract phytochemistry and its anti-inflammatory and antioxidant capacities in HepG2 and RAW 264.7 cell culture assays. Chemical profiling was performed with gas chromatography mass spectrometry without the modification of native molecules. Free phytosterols (such as -sitosterol) account for 70% of detected compounds. The anti-inflammatory capacity of the rhizome extract of A. mollis is mediated by the decrease in the NO production in RAW 264.7 that has previously been stimulated with lipopolysaccharide in a dose-dependent manner. Furthermore, HepG2 pre-treatment with the rhizome extract prevents any damage being caused by oxidative stress, both through ROS scavenge and through the antioxidant cellular enzyme system. In this respect, the extract reduced the activity of glutathione peroxidase and reductase, which were stimulated under oxidative stress conditions. Our results suggest that the extract from the rhizomes of A. mollis may constitute a potential source of natural products with anti-inflammatory activity and could validate the traditional use of A. mollis.

Corema album (L.) D. Don (Ericaceae) is an endemic bush that grows along the Atlantic littoral of the Iberian Peninsula. Its edible white berries (known as camarinas, camariñas, camarinhas, white crowberry, among other vernacular names) have been used in popular medicine as an antipyretic and are consumed in localised areas of Portugal and Spain as appetisers and in the preparation of juices and jams. The aim of the present review is to summarise the knowledge of the chemical composition and pharmacological studies performed with C. album fruit and extracts. These berries are rich in phenolic compounds, including phenolic acids, stilbenes, flavonols, flavanones, prenylated flavanone, flavanols, and anthocyanins. The total phenolic content of various extracts of the pulp of these berries has been positively correlated with their antioxidant capacity. In this respect, the treatment with acetone, ethyl acetate, and aqueous extracts of this fruit has protected HepG2 cells against chemically induced oxidative stress. The chemoprotective effect of these extracts is mediated by preventing reactive oxygen species formation, reduced glutathione (GSH) depletion, antioxidant enzyme over-activity, and oxidative damage to proteins and lipids. Furthermore, the presence of pentacyclic triterpenes, such as ursolic and oleanolic acids, in C. album berries confers reflectance UV properties to this fruit and derived extracts. In short, existing studies suggest that the development of C. album crops should be considered as a promising opportunity to obtain these remarkable berries. Moreover, further experiments should also be designed to evaluate their in vivo effect and to ascertain the underlying mechanism of action.