Bioactivity of medicinal plants and extracts

Nature is an inexhaustible source of bioactive compounds and products with interest- ing medicinal properties and technological applications. Although natural products can be found in plants, animals, microorganisms and minerals, the vast majority of them come from plants ..

Rock tea (Jasonia glutinosa (L.) DC.) polyphenolic extract inhibits triglyceride accumulation in 3T3-L1 adipocyte-like cells and obesity related enzymes in vitro

Jasonia glutinosa (L.) DC., also known in Spain as "té de roca" (rock tea, RT), is an endemic plant species of the Iberian Peninsula and Southern France. Traditionally, it is used in infusions, prepared with the flowering aerial parts, as a digestive and anti-inflammatory herbal tea. Despite the traditional knowledge of this plant as a digestive after meals, there are hardly any scientific studies that support its use. The aim of this study is to assess the effects of RT extract on physiological targets related to metabolic diseases such as obesity. For this purpose, enzyme inhibition bioassays of lipase, a-glucosidase and fatty acid amide hydrolase were carried out in cell-free systems. Similarly, adipocytes derived from 3T3-L1 cells were employed to study the effects of the extract on adipocyte differentiation and triglyceride (TG) accumulation. RT extract was able to inhibit lipase, a-glucosidase and fatty acid amide hydrolase. Furthermore, the extract displayed anti-adipogenic properties in a dose-dependent manner as it significantly reduced TG accumulation during adipocyte differentiation. These results may explain from a molecular perspective the beneficial effects of RT in the prevention of metabolic-associated disorders such as obesity, diabetes and related complications

Evaluation of two different Cannabis sativa extracts as antioxidant and neuroprotective agents

Cannabis sativa L. is a plant that contains numerous chemically active compounds including cannabinoids such as trans-Δ-9-tetrahydrocannabinol (Δ9-THC) and cannabidiol (CBD), and flavone derivatives, such as luteolin-7-O-glucuronide and apigenin glucuronide. In particular, the polar fraction of hemp including many phenolic compounds has been overlooked when compared with the more lipophilic fraction containing cannabinoids. Therefore, the aim of this study was to assess two extracts of industrial hemp (C. sativa) of different polarity (aqueous and hexane) by evaluating their antioxidant profile and their neuroprotective potential on pharmacological targets in the central nervous system (CNS). Several assays on in vitro antioxidant capacity (DPPH, superoxide radical, FRAP, ORAC), as well as inhibition of physiological enzymes such as acetylcholinesterase (AChE) and monoaminooxidase A (MAO-A) were carried out in order to find out how these extracts may be helpful to prevent neurodegenerative disorders. Neuro-2a cell line was selected to test the cytotoxic and neuroprotective potential of these extracts. Both extracts showed striking antioxidant capacity in the FRAP and ORAC assays, particularly the hexane extract, and interesting results for the DPPH and superoxide radical uptake assays, with the aqueous extract standing out especially in the latter. In enzyme inhibition assays, the aqueous extract showed AChE and MAO-A inhibitory activity, while the hexane extract only reached IC50 value for AChE inhibitory bioassay. Neuro-2a assays demonstrated that polyphenolic extract was not cytotoxic and exhibited cytoprotective properties against hydrogen peroxide and antioxidant response decreasing reactive oxygen species (ROS) production. These extracts could be a source of compounds with potential benefit on human health, especially related to neurodegenerative disorders

Neuroprotective profile of edible flowers of borage (Borago officinalis L.) in two different models: Caenorhabditis elegans and Neuro-2a cells

The flowers of Borago officinalis L. (Boraginaceae), commonly known as borage, are widely used as a culinary ingredient. The aim of this study was to assess the potential benefits of fresh borage flower extract related to antioxidant, neuroprotective and anti-aging properties. The extract was obtained by Soxhlet extraction with ethanol as a solvent, and fatty acids were detected by GC-FID. The antioxidant activity was evaluated in vitro through the DPPH, FRAP and ORAC assays. Regarding the fatty acid (FA) composition, the extract showed high amounts of polyunsaturated FA. The Neuro-2a cell line was used to determine the cytoprotective capacity of the extract subjected to oxidative stress (H2O2). Moreover, the model organism Caenorhabditis elegans was used to assess antioxidant activity, delayed ageing as well as cytoprotection and reduced ß-amyloid toxicity. Cells treated with the extract and H2O2 showed a better response to oxidative stress than the control group, particularly in terms of mitochondrial activity (MTT assay), redox state (ROS formation) and the activity of antioxidant enzymes (catalase and superoxide dismutase). B. officinalis flower extract showed promising antioxidant activity in the selected models, without causing toxicity. Hence, the results obtained support the antioxidant properties of borage flowers in different bioassays using living organisms

Cytotoxic, antioxidant, and enzyme inhibitory properties of the traditional medicinal plant matthiola incana (L.) R. Br.

Matthiola incana (L.) R. Br. (Brassicaceae) is widely cultivated for ornamental purposes and utilized as a medicinal plant. In the present work, the hydroalcoholic extract from the aerial parts of this species has been evaluated in different bioassays in order to detect potential pharmacological applications. The cytotoxic capacity against the human colorectal adenocarcinoma (CaCo-2) and breast cancer (MCF-7) cell lines was tested using the MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) assay. The extract was investigated as a neuroprotective inhibitor of central nervous system (CNS) enzymes such as monoamine oxidase A, tyrosinase, acetylcholinesterase, and as a natural enzyme inhibitor of a-glucosidase and lipase involved in some metabolic disorders such as obesity or type 2 diabetes. The antioxidant ability was also evaluated in an enzymatic system (xanthine/xanthine oxidase assay). Results showed that the M. incana extract displayed moderate to low cytotoxicity vs. CaCo-2 cells. The extract acted as a superoxide radical scavenger and enzymatic inhibitor of monoamine oxidase A, tyrosinase, a-glucosidase, and lipase. The best results were found in the a-glucosidase assay, as M. incana hydroalcoholic extract was able to inhibit the enzyme a-glucosidase up to 100% without significant differences, compared to the antidiabetic drug acarbose. Matthiola incana has been demonstrated to exert different biological properties. These are important in order to consider this species as a source of bioactive compounds

Phytochemicals and Enzyme Inhibitory Capacities of the Methanolic Extracts from the Italian Apple cultivar Mela Rosa dei Monti Sibillini

The phytochemical profile of the methanolic extracts (pulp and peel) obtained from two dehydration methods (drying and freeze-lyophilization) of the traditional Italian apple Mela Rosa dei Monti Sibillini, as well as their inhibitory properties against some biological enzymes (α-glucosidase, lipase, monoamine oxidase A, tyrosinase and acetylcholinesterase) were assessed in this study. HPLC-DAD-MS technique was used for the determination of polyphenolic and triterpenic compounds. The determination of the enzymes inhibitory effect was made through spectrophotometric techniques. The peel extracts were richer in bioactive compounds than the pulp. In this regard, the extracts from freeze-lyophilization displayed higher levels of flavan-3-ols, flavonol glycosides and dihydrochalcones. However, the extracts obtained from dried material displayed a stronger enzyme inhibition. Notably, the peel extracts showed a higher activity than the pulp ones, especially in terms of α-glucosidase whereby some samples exerted a similar enzymatic inhibition than acarbose (100% inhibition) at high concentrations (1 mg/mL). These results encourage thus further studies on this traditional Italian apple as a potential source of nutraceuticals helpful to prevent the insurgence of some pathologies

Everlasting flower (Helichrysum stoechas Moench) as a potential source of bioactive molecules with antiproliferative, antioxidant, antidiabetic and neuroprotective properties

Helichrysum stoechas (L.) Moench is one of the scientific names of everlasting flower, which has traditionally been used as an ornamental, medicinal and food plant. The aim of this study was to identify the main phytochemical constituents as well as to evaluate the potential of this plant in terms of antioxidant, antidiabetic and neuroprotective activities. The phytochemical analysis of the methanolic extract allowed for the identification of ten constituents mainly of phenolic nature and with chemosystematic relevance: two heterodimeric phloroglucinols, arzanol (1) and compound (3), one homodimeric α-pyrone, helipyrone (2), three phenolic acids, p-hydroxybenzoic (4), caffeic (5) and neochlorogenic (6) acids, one polymethoxylated and two glycosidic flavonoids, 5,7-dihydroxy-3,6,8-trimethoxyflavone (7), isoquercitrin (8) and quercetagetin-7-O-glucopyranoside (9) together with santinol B (10). Bioassays showed significant antioxidant and antiproliferative effects and for the first time the potential of Helichrysum stoechas to inhibit the MAO-A, AChE and TYR enzymes, as well as to exert anti-α-glucosidase and anti-dipeptidyl peptidase-4 activities

Natural essential oils as a new therapeutic tool in colorectal cancer

Colorectal cancer (CRC) is the third most revalent type of cancer in the world and the second most common cause of cancer death (about 1 million per year). Historically, natural compounds and their structural analogues have contributed to the development of new drugs useful in the treatment of various diseases, including cancer. Essential oils are natural odorous products made up of a complex mixture of low molecular weight compounds with recognized biological and pharmacological properties investigated also for the prevention and treatment of cancer. The aim of this paper is to highlight the possible role of essential oils in CRC, their composition and the preclinical studies involving them. It has been reviewed the preclinical pharmacological studies to determine the experimental models used and the anticancer potential mechanisms of action of natural essential oils in CRC. Searches were performed in the following databases PubMed/Medline, Web of science, TRIP database, Scopus, Google Scholar using appropriate MeSH terms. The results of analyzed studies showed that EOs exhibited a wide range of bioactive effects like cytotoxicity, antiproliferative, and antimetastatic effects on cancer cells through various mechanisms of action. This updated review provides a better quality of scientific evidence for the efficacy of EOs as chemotherapeutic/chemopreventive agents in CRC. Future translational clinical studies are needed to establish the effective dose in humans as well as the most suitable route of administration for maximum bioavailability and efficacy. Given the positive anticancer results obtained from preclinical pharmacological studies, EOs can be considered efficient complementary therapies in chemotherapy in CRC

The ANTI-Vea-UGR Platform: A Free Online Resource to Measure Attentional Networks (Alertness, Orienting, and Executive Control) Functioning and Executive/Arousal Vigilance

The Attentional Networks Test for Interactions and Vigilance—executive and arousal components (ANTI-Vea) is a computerized task of 32 min duration in the standard format. The task simultaneously assesses the main effects and interactions of the three attentional networks (i.e., phasic alertness, orienting, and executive control) and two dissociated components of vigilance with reasonable reliability (executive and arousal vigilance). We present this free and publicly accessible resource (ANTI-Vea-UGR; https://anti-vea.ugr.es/) developed to easily run, collect, and analyze data with the ANTI-Vea (or its subtasks measuring some attentional and/or vigilance components embedded in the ANTI-Vea). Available in six different languages, the platform allows for the adaptation of stimulus timing and procedure to facilitate data collection from different populations (e.g., clinical patients, children). Collected data can be freely downloaded and easily analyzed with the provided scripts and tools, including a Shiny app. We discuss previous evidence supporting that attention and vigilance components can be assessed in typical lab conditions as well as online and outside the laboratory. We hope this tutorial will help researchers interested in measuring attention and vigilance with a tool useful to collect data from large sample sizes and easy to use in applied contexts