Bioactive Compounds
A topical collection in Molecules (ISSN 1420-3049). This collection belongs to the section "Natural Products Chemistry".
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Interests: cancer chemoprevention; nutrition; olive oil; polyphenols; natural bioactive compounds; antioxidants; oxidative stress; genotoxicity; mutagenicity; apoptosis; cell cycle regulation
Special Issues, Collections and Topics in MDPI journals
Interests: chemistry of natural products; emerging conservation technologies; gamma and electron beam irradiation; development of functional food; recovery of biological waste; bio-based ingredients
Special Issues, Collections and Topics in MDPI journals
Topical Collection Information
Dear Colleagues,
Consumers increasingly believe that foods contribute directly to their health and well-being. In this context, extranutritional constituents that typically occur in small quantities in foods, "Bioactive compounds", play a very significant role. Bioactive compounds are being intensively studied to evaluate their effects on health, including antioxidant, antiallergic, antimicrobial, antithrombotic, antiatherogenic, hypoglycaemic, anti-inflammatory, antitumor, cytostatic, immunosuppressive properties, and hepatoprotective activities. Contributions for this issue, both in form of original research and review articles, may cover all aspects of bioactive compounds with proven activities in various biological screenings and pharmacological models, e.g. quantification, variability and efficacy of bioactive compounds; development of new protocols and methods based on chemical or biological systems for the evaluation of in vivo and in vitro bioactivity; clinical and nutritional trials focused on the bioactive properties of bioactive compounds synthesized or isolated; elucidation of bioactive compounds mechanisms; innovative techniques of bioactive compounds delivery and protocols for the extraction, isolation, structural characterization of new bioactive compounds will be welcomed, on condition that an adequate evaluation of their efficacy is provided. Papers regarding the development of pharmaceuticals from bioactive compounds will be also taken into consideration.
Dr. Roberto Fabiani
Dr. Eliana Pereira
Collection Editors
Prof. Dr. Isabel C.F.R. Ferreira
Dr. Nancy D. Turner
Former Collection Editors
Manuscript Submission Information
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Keywords
- bioactivity
- natural products
- synthesised compounds
- isolation techniques
- structure elucidation
- mechanism of action
Related Special Issue
- Bioactive Compounds in Pharmaceuticals (1 article)
Planned Papers
The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.
Title: Carpesium divaricatum Sieb. & Zucc. revisited: New constituents from aerial parts of the plant and their possible contribution to the biological activity of the plant
Authors: Natalia Kłeczek, Janusz Malarz, Barbara Michalak, Anna Karolina Kiss and Anna Stojakowska
Abstract: Composition of hydroalcoholic extract from aerial parts of Carpesium divaricatum Sieb. & Zucc. was analysed, by HPLC-DAD- MSn, revealing the presence of numerous caffeic acid derivatives, of known antioxidative activity. The compounds were formerly unknown as constituents of the plant. In all, 17 compounds including commonly found chlorogenic acids and rarely occurring butyryl and methylbutyryl tricaffeoylhexaric acids were tentatively identified. Fractionation of nonpolar extract from shoots of the plant led to the isolation of 12-oxo-phytodienoic acid (12-OPDA) – a newly identified constituent of the plant. En effect of 12-OPDA on excretion of some pro-inflammatory cytokines from human neutrophils was also assessed. The compound, at concentrations 1.0 and 2.5 μM, significantly reduced IL-8 excretion by LPS stimulated human neutrophils and f-MLP induced ROS generation in the cells. Release of IL-1β and CCL2 from the LSP stimulated neutrophils were less affected.
Title: Metabolic engineering approaches to enhance pharmaceutically important plant-derived diterpenes
Article Type: Review
Authors: Antonietta Leone and Mara Alfieri
Title: In vitro human metabolism and inhibition potency of verbascoside for CYP enzymes
Article Type: Article
Authors: Anna-Mari Reid 1, Risto Juvonen 2, Pasi Huuskonen 2, Marko Lehtonen 3, Markku Pasanen 2 and
Namrita Lall 2,*
Abstract: This study investigates the potential of verbascoside as an adjuvant during tuberculosis treatment.
This study reports on the in vitro metabolism in human hepatic microsomes and cytosol incubations
as well as the presence of verbascoside within Lippia scaberrima. Additionally, studied are the
inhibitory properties on human hepatic CYP enzymes together with antioxidant and cytotoxic
properties. Five different methylated conjugates could be found in the S-adenosylmethionine
incubation, three different sulphate conjugates with the 3′-phosphoadenosine 5′-phosphosulfate
(PAPS) incubation with human liver samples and very low levels of glucuronide metabolites after
incubation with recombinant human uridine 5'-diphospho-glucuronosyltransferase (UGT) 1A7,
UGT1A8 and UGT1A10. Additionally, verbascoside showed weak inhibitory potency against
CYP1A2 and CYP1B1 with IC50-values of 83 μM and 86 μM, respectively. Potent antioxidant and low
cytotoxic potential were observed. Based on this data, verbascoside does not possess any clinically
relevant CYP-mediated interaction potential but effective biological activity. Therefore, verbascoside
could be considered as a lead compound for further drug development and as an adjuvant during
tuberculosis treatment.
Authors: Raquel Bridi, Ady Giordano, Maria Fernanda Peñalillo, Gloria Montenegro
Abstract: A large number of researches have indicated that complex extracts from plants, such as fruits,
vegetables, herbs and spices were good sources of natural. For food industry, the preservation of meat
products has been of constant concern, in order to maintain both the quality and safety of the product. To
mitigate the oxidative process, the most important mechanisms behind the deterioration of meat, the
industry has used several molecules with antioxidant activity. The products of natural origin have been
prioritized mainly due to the growing concern among consumers about synthetic antioxidants and their
potential adverse effects. The oxidation processes can affect both lipids and proteins, and is facilitated by
the presence of various oxidizing agents, for example the peroxyl radicals (ROO•). Lipid peroxidation is
the main cause of deterioration of meat products, causing the appearance of stale odors, changes in the
taste and color of the meat and partly responsible for protein oxidation. Protein oxidation corresponds to
chemical modifications produced in the structure of the protein.
In this sense, this work focused on the study of the antioxidant potential and the ability to inhibit lipid and
protein oxidation of the meat of four native Chilean species canelo, Drimys winteri J.R. Forst. & G. Forst.
(Winteraceae); nalca, Gunnera tinctoria (Molina) Mirb (Gunneraceae); tiaca, Caldcluvia paniculata (Cav.) D.
Don (Cunoniaceae) and ulmo, Eucryphia cordifolia Cav. (Cunoniaceae). For the characterization of plant
extracts, total phenols and flavonoids were quantified and the main phenolic compounds were identified
by HPLC-MS. The antioxidant capacity of plant extracts was evaluated using the oxygen radical absorption
capacity-red pyrogallol method (ORAC-PGR) and ferric ion reducing antioxidant power (FRAP) assay.
Furthermore, the antioxidant ability of these plant extracts in inhibit to oxidative modifications induced by
peroxyl radicals (ROO•) in bovine meat were evaluated. The oxidative modifications generated from lipid
peroxidation were evaluated using the TBARS technique, which is based on the measurement of
malondialdehyde (MDA). While the oxidative modifications generated by protein oxidation were evaluated by quantification of carbonyl and sulfhydryl groups, and electrophoresis in polyacrylamide gels (SDS-page). Of the extracts studied, the one of canelo presented greater phenolic content, of flavonoids and greater antioxidant capacity (ORAC-PGR), identifying the presence of 13 phenolic compounds. All the extracts analyzed exhibited protection in peroxyl radical induced lipid peroxidation. As for the quantification of carbonyl groups, the extracts of ulmo, canelo and nalca exhibited protection by decreasing the amount of carbonyl groups generated by peroxyl radicals. No extract exhibited protection against the loss of sulfhydryl groups. In the analysis of electrophoresis in polyacrylamide gels, only the extract of canelo demonstrated a mild protection against protein oxidation.
Title: Therapeutic potential of cannabinoids for the control of obesity: a systematic review
Article Type: Review
Authors: Santos Medina, Rafael 1; Loyola, Mário 1; Piovan, Silvano; Mareze-Costa, Cecília Edna 1,*
Abstract: Cannabis sativa, popularly known as marijuana, has a large therapeutic importance that has been known for a long time, but only recently with the discovery of the chemical structure of cannabinoids and later of the endocannabinoid system is that there were a greater number of studies related to this therapeutic power. A systematic review of the literature was carried out with a search on PubMed and SciELO databases to gather the main information contained in published articles about the endocannabinoid system with a focus on its role on energy metabolism and / or therapeutic potential for the control of obesity. Experimental studies and systematic reviews that investigated the effects of cannabinoids on energy metabolism were included, as well as their possible therapeutic potential for the control of obesity. Regarding the methodological quality and the design of the study, original experimental studies, as well as systematic reviews that focused on the therapeutic potential of cannabinoids and / or their mechanisms of action on energy metabolism, were selected. The results of the research have proven to be promising and most have contributed to delineate the effects of cannabinoids on energy homeostasis and how they could be used for medicinal purposes, such as obesity control.
Keywords: Cannabis sativa. Cannabinoids. Endocannabinoids. Energy metabolism. Obesity.