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Bioactive Compounds with Applications in Health and Food
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Bioactive Compounds with Applications in Health and Food

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (30 September 2020) | Viewed by 75493

Special Issue Editor

Prof. Dr. Panagiotis Zoumpoulakis

E-Mail Website
Guest Editor
1. Department of Food Science and Technology, University of West Attica, 12243 Athens, Greece
2. Institute of Chemical Biology, National Hellenic Research Foundation, 116 35 Athens, Greece
Interests: molecular design; bioanalysis; metabolic profiling; design and development of dietary supplements; functional food; phytoconstituents
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Bioactive compounds constitute a significant field of natural products chemistry, mainly because of their structural biodiversity and their high exploitation potential. They are chemical entities that exhibit certain biological effects, related to their ability to modulate metabolic processes, and activate or inhibit receptors or enzymes with a beneficial response in the human body. Their consumption has been related to the prevention of multiple pathologies, and to the promotion of good health. Plant bioactive compounds are produced as secondary metabolites, and have singnificant and still unexplored health benefits. Natural bioactives (i.e., carotenoids, polyphenols), either isolated or in extracts, are mainly used for the development of food supplements and cosmetics, but are also widely incorporated into food products in order to enhance their sensory, nutritional, or health properties.

Stemming from the structure of natural bioactives, there is a growing trend towards the design and synthesis of new chemical entitites under the name “bio-inspired compounds”, with their structural motifs inspired by natural bioactives compounds.

This Special Issue aims to cover the current trends and the recent progress on bioactive compounds with applications in health and food. The objective of the Issue is to constitute a source of relevant information on either isolated bioactive or synthesized bioinspired compounds, as well as bioactive extracts, which could potentially be exploited for the development of pharmaceuticals, comeceuticals, and nutraceuticals.

Focus will be given to solid research findings for compounds or extracts with activities on specific biological targets or pharmacological models. Any kind of health topic related biological targtets is accepted. Papers with the main objective being the in vitro studies of the antioxidant/radical scavenging activities of plant extracts should at least provide a chemical profile of the extract, if not a complete identification and quantifiation of the relevant bioactive compounds. To this extent, studies focusing on the use of modern analytical techniques that allow for the identification of bioactive compounds and deepening the mechanisms that relate them to health are also accepted.

Types of contributions to this Special Isssue can be original research articles, short communications, and reviews/mini-reviews.
Submissions on, but not limited to, the following are welcome:

  • Isolation and characterization of bioactive compounds
  • Selective extraction of bioactive compounds
  • Biological evaluation of selected plant extracts/ isolated and/or synthetic compounds
  • Design and synthesis of bio-inspired compounds
  • Hit discovery and hit-to-lead optimization of bio-inspired compounds
  • Structure–activity relationship studies

Prof. Dr. Panagiotis Zoumpoulakis
Guest Editor

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

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Keywords

  • Bioactive compounds
  • Natural products
  • Extraction methodologies
  • Bio-inspired compounds
  • Design and synthesis
  • Hit discovery
  • Hit-to-lead optimization
  • Analytical techniques and methodologies
  • Structure–activity Relationship

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Published Papers (18 papers)

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24 pages, 4428 KiB  
Article
Exploring the 2′-Hydroxy-Chalcone Framework for the Development of Dual Antioxidant and Soybean Lipoxygenase Inhibitory Agents
by Ioanna Kostopoulou, Andromachi Tzani, Nestor-Ioannis Polyzos, Maria-Anna Karadendrou, Eftichia Kritsi, Eleni Pontiki, Thalia Liargkova, Dimitra Hadjipavlou-Litina, Panagiotis Zoumpoulakis and Anastasia Detsi
Molecules 2021, 26(9), 2777; https://doi.org/10.3390/molecules26092777 - 8 May 2021
Cited by 27 | Viewed by 4469
Abstract
2′-hydroxy-chalcones are naturally occurring compounds with a wide array of bioactivity. In an effort to delineate the structural features that favor antioxidant and lipoxygenase (LOX) inhibitory activity, the design, synthesis, and bioactivity profile of a series of 2′-hydroxy-chalcones bearing diverse substituents on rings [...] Read more.
2′-hydroxy-chalcones are naturally occurring compounds with a wide array of bioactivity. In an effort to delineate the structural features that favor antioxidant and lipoxygenase (LOX) inhibitory activity, the design, synthesis, and bioactivity profile of a series of 2′-hydroxy-chalcones bearing diverse substituents on rings A and B, are presented. Among all the synthesized derivatives, chalcone 4b, bearing two hydroxyl substituents on ring B, was found to possess the best combined activity (82.4% DPPH radical scavenging ability, 82.3% inhibition of lipid peroxidation, and satisfactory LOX inhibition value (IC50 = 70 μM). Chalcone 3c, possessing a methoxymethylene substituent on ring A, and three methoxy groups on ring B, exhibited the most promising LOX inhibitory activity (IC50 = 45 μM). A combination of in silico techniques were utilized in an effort to explore the crucial binding characteristics of the most active compound 3c and its analogue 3b, to LOX. A common H-bond interaction pattern, orienting the hydroxyl and carbonyl groups of the aromatic ring A towards Asp768 and Asn128, respectively, was observed. Regarding the analogue 3c, the bulky (-OMOM) group does not seem to participate in a direct binding, but it induces an orientation capable to form H-bonds between the methoxy groups of the aromatic ring B with Trp130 and Gly247. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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15 pages, 1790 KiB  
Article
On the Identification and Quantification of Ergothioneine and Lovastatin in Various Mushroom Species: Assets and Challenges of Different Analytical Approaches
by Konstantinos Tsiantas, Thalia Tsiaka, Georgios Koutrotsios, Eleni Siapi, Georgios I. Zervakis, Nick Kalogeropoulos and Panagiotis Zoumpoulakis
Molecules 2021, 26(7), 1832; https://doi.org/10.3390/molecules26071832 - 24 Mar 2021
Cited by 23 | Viewed by 5342
Abstract
In recent years, mushrooms have drawn the attention of agro-industries and food-industries as they were considered to be valuable natural sources of health promoting compounds such as β-glucans, ergothioneine, and lovastatin. The detection and quantification of such compounds by implementing reliable analytical approaches [...] Read more.
In recent years, mushrooms have drawn the attention of agro-industries and food-industries as they were considered to be valuable natural sources of health promoting compounds such as β-glucans, ergothioneine, and lovastatin. The detection and quantification of such compounds by implementing reliable analytical approaches is of the utmost importance in order to adjust mushrooms’ cultivation conditions and maximize the production in different species. Toward this direction, the current study focuses on the comparison of ultraviolet–visible (UV–Vis) spectrometry and liquid chromatography–mass spectrometry (LC–MS) methods (a) by evaluating the content of ergothioneine and lovastatin in mushrooms and (b) by highlighting any possible substrate-based interferences that hinder the accurate determination of these two compounds in order to propose the technique-of-choice for a standardized bioactive compounds monitoring. For this purpose, mushrooms produced by three species (i.e., Agaricus bisporus, Pleurotus ostreatus, and P. citrinopileatus) on various cultivation substrates, namely wheat straw (WS), winery (grape marc (GM)), and olive oil (OL) by-products, were examined. Among the two applied techniques, the developed and validated LC–MS methods, exhibiting relatively short analysis time and higher resolution, emerge as the methods-of-choice for detecting ergothioneine and lovastatin in mushrooms. On the contrary, UV–Vis methods were hindered due to co-absorbance of different constituents, resulting in invalid results. Among the studied mushrooms, P. citrinopileatus contained the highest amount of ergothioneine (822.1 ± 20.6 mg kg−1 dry sample), whereas A. bisporus contained the highest amounts of lovastatin (1.39 ± 0.014 mg kg−1 dry sample). Regarding the effect of different cultivation substrates, mushrooms produced on OL and WS contained the highest amount of ergothioneine, while mushrooms deriving from GM-based substrates contained the highest amount of lovastatin. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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19 pages, 11120 KiB  
Article
Design and Characterisation of Inhibitory Peptides against Bleg1_2478, an Evolutionary Divergent B3 Metallo-β-lactamase
by Gayathri Selvaraju, Thean Chor Leow, Abu Bakar Salleh and Yahaya M. Normi
Molecules 2020, 25(24), 5797; https://doi.org/10.3390/molecules25245797 - 9 Dec 2020
Cited by 5 | Viewed by 2693
Abstract
Previously, a hypothetical protein (HP) termed Bleg1_2437 (currently named Bleg1_2478) from Bacillus lehensis G1 was discovered to be an evolutionary divergent B3 subclass metallo-β-lactamase (MBL). Due to the scarcity of clinical inhibitors for B3 MBLs and the divergent nature of Bleg1_2478, this study [...] Read more.
Previously, a hypothetical protein (HP) termed Bleg1_2437 (currently named Bleg1_2478) from Bacillus lehensis G1 was discovered to be an evolutionary divergent B3 subclass metallo-β-lactamase (MBL). Due to the scarcity of clinical inhibitors for B3 MBLs and the divergent nature of Bleg1_2478, this study aimed to design and characterise peptides as inhibitors against Bleg1_2478. Through in silico docking, RSWPWH and SSWWDR peptides with comparable binding energy to ampicillin were obtained. In vitro assay results showed RSWPWH and SSWWDR inhibited the activity of Bleg1_2478 by 50% at concentrations as low as 0.90 µM and 0.50 µM, respectively. At 10 µM of RSWPWH and 20 µM of SSWWDR, the activity of Bleg1_2478 was almost completely inhibited. Isothermal titration calorimetry (ITC) analyses showed slightly improved binding properties of the peptides compared to ampicillin. Docked peptide–protein complexes revealed that RSWPWH bound near the vicinity of the Bleg1_2478 active site while SSWWDR bound at the center of the active site itself. We postulate that the peptides caused the inhibition of Bleg1_2478 by reducing or blocking the accessibility of its active site from ampicillin, thus hampering its catalytic function. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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10 pages, 634 KiB  
Article
Quantification of Cooking Method Effect on COP Content in Meat Types Using Triple Quadrupole GC-MS/MS
by Shazamawati Zam Hashari, Alina Abdul Rahim, Goh Yong Meng and Suriya Kumari Ramiah
Molecules 2020, 25(21), 4978; https://doi.org/10.3390/molecules25214978 - 28 Oct 2020
Cited by 7 | Viewed by 2708
Abstract
A diet containing cholesterol is an essential component of biological function; however, cholesterol oxidation products (COPs) remain a major public health concern. This study investigated the effects of cooking methods (boiling and frying) on the production levels of COPs in processed foods. Samples, [...] Read more.
A diet containing cholesterol is an essential component of biological function; however, cholesterol oxidation products (COPs) remain a major public health concern. This study investigated the effects of cooking methods (boiling and frying) on the production levels of COPs in processed foods. Samples, as represented by minced beef, chicken sausages, and fish fillets, were subjected to different cooking methods followed by COP extraction using a saponification method. Then, six common COPs, 5α-cholest, α-epoxy, β-epoxy, 25-HC, triol, and 7-keto, were quantified by triple quadrupole gas chromatography–mass spectrometry (GS-MS/MS). A significantly high number of COPs were detected in minced meat, of which 7-keto and triol were detected as major oxidation products, followed by chicken sausages and fish fillets (p ≤ 0.05). Compared to boiling, frying generated significantly more COPs, specifically triol (0.001–0.004 mg/kg) and 7-keto (0.001–0.200 mg/kg), in all samples. Interestingly, cholesterol level was found to be slightly (but not significantly) decreased in heat-treated samples due to oxidation during cooking, producing a higher number of COPs. Notably, the fish fillets were found to produce the fewest COPs due to the presence of a low amount of cholesterol and unsaturated fatty acids. In conclusion, adapting boiling as a way of cooking and choosing the right type of meat could serve to reduce COPs in processed foods. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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15 pages, 2905 KiB  
Article
In Vitro Antimicrobial and Antioxidant Activities of Lactobacillus coryniformis BCH-4 Bioactive Compounds and Determination of their Bioprotective Effects on Nutritional Components of Maize (Zea mays L.)
by Mahwish Salman, Anam Tariq, Anam Ijaz, Shazia Naheed, Abeer Hashem, Elsayed Fathi Abd_Allah, Mona H. Soliman and Muhammad Rizwan Javed
Molecules 2020, 25(20), 4685; https://doi.org/10.3390/molecules25204685 - 14 Oct 2020
Cited by 11 | Viewed by 3498
Abstract
Lactic acid bacteria (LAB) can synthesize antimicrobial compounds (AMCs) with nutritional and bioprotective properties in crops and food products. In the current study, AMCs of Lactobacillus coryniformis BCH-4 were evaluated to control fungal spoilage in maize grains. On maize grains treated with 75%–100% [...] Read more.
Lactic acid bacteria (LAB) can synthesize antimicrobial compounds (AMCs) with nutritional and bioprotective properties in crops and food products. In the current study, AMCs of Lactobacillus coryniformis BCH-4 were evaluated to control fungal spoilage in maize grains. On maize grains treated with 75%–100% (v/v) concentrated AMCs, no fungal growth was observed even after 72 h of Aspergillus flavus inoculation. Proximate analysis of treatments A1 (raw grains), A2 (A. flavus inoculated grains) and A3 (A. flavus + AMCs inoculated grains) revealed that moisture was significantly (p ≤ 0.05) high in A2 than A3 and A1. Meanwhile, protein, fat, fiber and ash contents were significantly decreased in A2 compared to A1 and A3. Moreover, β-carotene contents were not statistically different between A1 and A3, while in A2 it was significantly decreased. HPLC analysis revealed the presence of 2-oxopropanoic acid, 2-hydroxypropane-1,2,3-tricarboxylic acid, 2-hydroxybutanedioic acid, 2-hydroxypropanoic acid, propanedioic acid and butanedioic acid, which also showed antifungal activity against Aspergillus flavus. FTIR spectroscopy revealed the presence of hydroxyl, carbonyl and ester-groups along with organic and fatty acids, thereby indicating their participation in inhibitory action. Furthermore, the AMCs were found to be a good alternative to chemical preservatives, thereby not only preserving the nutritive qualities but increasing the shelf life as well. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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9 pages, 1282 KiB  
Article
In Silico Molecular Study of Tryptophan Bitterness
by Antonella Di Pizio and Alessandro Nicoli
Molecules 2020, 25(20), 4623; https://doi.org/10.3390/molecules25204623 - 11 Oct 2020
Cited by 12 | Viewed by 3993
Abstract
Tryptophan is an essential amino acid, required for the production of serotonin. It is the most bitter amino acid and its bitterness was found to be mediated by the bitter taste receptor TAS2R4. Di-tryptophan has a different selectivity profile and was found to [...] Read more.
Tryptophan is an essential amino acid, required for the production of serotonin. It is the most bitter amino acid and its bitterness was found to be mediated by the bitter taste receptor TAS2R4. Di-tryptophan has a different selectivity profile and was found to activate three bitter taste receptors, whereas tri-tryptophan activated five TAS2Rs. In this work, the selectivity/promiscuity profiles of the mono-to-tri-tryptophans were explored using molecular modeling simulations to provide new insights into the molecular recognition of the bitter tryptophan. Tryptophan epitopes were found in all five peptide-sensitive TAS2Rs and the best tryptophan epitope was identified and characterized at the core of the orthosteric binding site of TAS2R4. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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9 pages, 1117 KiB  
Article
Isolation and FTIR-ATR and 1H NMR Characterization of Alginates from the Main Alginophyte Species of the Atlantic Coast of Morocco
by Zahira Belattmania, Soukaina Kaidi, Samir El Atouani, Chaimaa Katif, Fouad Bentiss, Charafeddine Jama, Abdeltif Reani, Brahim Sabour and Vitor Vasconcelos
Molecules 2020, 25(18), 4335; https://doi.org/10.3390/molecules25184335 - 22 Sep 2020
Cited by 62 | Viewed by 6187
Abstract
Alginates are widely used as gelling agents in textile print pastes, medical industries, impression material in dentistry, and anticoagulant material in toothpaste. In the present study, the content and spectroscopic characterization (1H NMR and FT-IR) of the sodium alginates were investigated [...] Read more.
Alginates are widely used as gelling agents in textile print pastes, medical industries, impression material in dentistry, and anticoagulant material in toothpaste. In the present study, the content and spectroscopic characterization (1H NMR and FT-IR) of the sodium alginates were investigated in the eight brown seaweeds Sargassum muticum, Fucus vesiculosus f. volubilis, Carpodesmia tamariscifolia, Bifurcaria bifurcata, Laminaria ochroleuca, Cystoseira humilis, Saccorhiza polyschides, and Fucus guiryi harvested from the NW Atlantic coast of Morocco. The results proved that the most studied algae depicted alginate yields higher than 18% dry weight. The FT-IR analysis showed that the spectra of the extracted alginates exhibited significant similarities to the commercial alginate from Sigma-Aldrich. The 1H NMR spectroscopy indicated that the extracted alginates have a high content of β-d-mannuronic (M) than α-l-guluronic acid (G) with M/G ratio values ranging from 1.04 to 4.41. The homopolymeric fractions FMM are remarkably high compared to the FGG and heteropolymeric fractions (FGM = FMG) especially for F. guiryi, C humilis, C. tamariscifolia, L. ochroleuca, and S. polyschides. Nevertheless, the heteropolymeric fractions (FGM/FMG) are quite abundant in the alginates of S. muticum, F. vesiculosus f. volubilis, and B. bifurcata accounting for more than 52% of the polymer diads. Based on these results, the investigated algal species (except Fucus guiryi and Bifurcaria bifurcata) could be regarded as potential sources of alginates for industrial uses. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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19 pages, 2502 KiB  
Article
Nature-Identical Compounds and Organic Acids Ameliorate and Prevent the Damages Induced by an Inflammatory Challenge in Caco-2 Cell Culture
by Andrea Toschi, Barbara Rossi, Benedetta Tugnoli, Andrea Piva and Ester Grilli
Molecules 2020, 25(18), 4296; https://doi.org/10.3390/molecules25184296 - 19 Sep 2020
Cited by 21 | Viewed by 4217
Abstract
Bioactive compounds, such as organic acids (OA) and nature-identical compounds (NIC), can exert a role in the protection of intestinal mucosa functionality due to their biological properties. The aim of this study was to understand the role of 2 OA (citric and sorbic [...] Read more.
Bioactive compounds, such as organic acids (OA) and nature-identical compounds (NIC), can exert a role in the protection of intestinal mucosa functionality due to their biological properties. The aim of this study was to understand the role of 2 OA (citric and sorbic acid) and 2 NIC (thymol and vanillin), alone or combined in a blend (OA + NIC), on intestinal barrier functionality, either during homeostatic condition or during an inflammatory challenge performed with pro-inflammatory cytokines and lipopolysaccharides (LPS). The study was performed on the human epithelial cell line Caco-2, a well-known model of the intestinal epithelial barrier. The results showed how OA and NIC alone can improve transepithelial electrical resistance (TEER) and mRNA levels of tight junction (TJ) components, but OA + NIC showed stronger efficacy compared to the single molecules. When an inflammatory challenge occurred, OA + NIC blend was able both to ameliorate, and prevent, damage caused by the pro-inflammatory stimulus, reducing or preventing the drop in TEER and improving the TJ mRNA expression. The data support the role of OA + NIC in modulating gut barrier functionality and reducing the negative effects of inflammation in intestinal epithelial cells, thereby supporting the gut barrier functionality. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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15 pages, 694 KiB  
Article
Effect of the Solvent on Propolis Phenolic Profile and its Antifungal, Antioxidant, and In Vitro Cytoprotective Activity in Human Erythrocytes Under Oxidative Stress
by Magdalena Woźniak, Lucyna Mrówczyńska, Patrycja Kwaśniewska-Sip, Agnieszka Waśkiewicz, Piotr Nowak and Izabela Ratajczak
Molecules 2020, 25(18), 4266; https://doi.org/10.3390/molecules25184266 - 17 Sep 2020
Cited by 39 | Viewed by 3712
Abstract
Propolis is a natural bee product with various beneficial biological effects. The health-promoting properties of propolis depend on its chemical composition, particularly the presence of phenolic compounds. The aim of this study was to evaluate the relationship between extraction solvent (acetone 100%, ethanol [...] Read more.
Propolis is a natural bee product with various beneficial biological effects. The health-promoting properties of propolis depend on its chemical composition, particularly the presence of phenolic compounds. The aim of this study was to evaluate the relationship between extraction solvent (acetone 100%, ethanol 70% and 96%) and the antifungal, antioxidant, and cytoprotective activity of the extracts obtained from propolis. Concentrations of flavonoids and phenolic acids in the propolis extracts were determined using ultrahigh-performance liquid chromatography. The antioxidant potential of different extracts was assessed on the basis of 2,2-diphenyl-1-picrylhydrazyl (DPPH·) free-radical-scavenging activity, Fe3+-reducing power, and ferrous ion (Fe2+)-chelating activity assays. The ability of the extracts to protect human red blood cell membranes against free-radical-induced damage and their antifungal activity was also determined. The results showed that the concentration of flavonoids in the propolis extracts was dependent on the solvent used in the extraction process and pinocembrin, chrysin, galangin, and coumaric acid were the most abundant phenols. All extracts exhibited high antioxidant potential and significantly protected human erythrocytes against oxidative damage. On the other hand, the antifungal activity of the propolis extracts depended on the solvent used in extraction and the fungal strains tested. It needs to be stressed that, to the best of our knowledge, there is no study relating the effect of solvent used for extraction of Polish propolis to its phenolic profile, and its antifungal, antioxidant, and cytoprotective activity. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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23 pages, 6312 KiB  
Article
Plant Milking Technology—An Innovative and Sustainable Process to Produce Highly Active Extracts from Plant Roots
by Hanane Chajra, Aleksander Salwinski, Agnès Guillaumin, Benoit Mignard, Paul Hannewald, Léonor Duriot, Pierre Warnault, Carine Guillet-Claude, Mathilde Fréchet and Frédéric Bourgaud
Molecules 2020, 25(18), 4162; https://doi.org/10.3390/molecules25184162 - 11 Sep 2020
Cited by 3 | Viewed by 5168
Abstract
We have used an original technology (Plant Milking Technology) based on aeroponic cultivation of plants associated with the gentle recovery of active ingredients from roots. Extraction of bioactive molecules was achieved by soaking the roots, still attached to the living plants, into a [...] Read more.
We have used an original technology (Plant Milking Technology) based on aeroponic cultivation of plants associated with the gentle recovery of active ingredients from roots. Extraction of bioactive molecules was achieved by soaking the roots, still attached to the living plants, into a nontoxic solvent for a 2 h period. This nondestructive recovery process allows using the same root biomass for successive harvesting dates, in a recyclable way. We have applied this technology to Morus alba L. (mulberry tree), an emblematic tree of the Traditional Chinese Medicine (TCM). Trees were aeroponically grown in large-scale devices (100 m2) and were submitted to nitrogen deprivation to increase the content in active molecules (prenylated flavonoids). The Plant Milking technology applied to Morus alba L. allowed to produce an extract enriched in prenylated compounds (18-fold increase when compared to commercial root extract). Prenylated flavonoids (moracenin A and B, kuwanon C, wittiorumin F, morusin) presented a high affinity for the aged-associated collagenase enzyme, which was confirmed by activity inhibition. In accordance, M. alba extract presents efficient properties to regulate the skin matrisome, which is critical during skin aging. The benefits have been especially confirmed in vivo on wrinkle reduction, in a clinical study that involved aged women. Plant Milking technology is an optimal solution to produce active ingredients from plant roots, including trees, that meet both customer expectations around sustainability, as well as the need for an efficient production system for biotechnologists. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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8 pages, 921 KiB  
Article
Isolation and Cytotoxic Activity of Phyllocladanes from the Roots of Acacia schaffneri (Leguminosae)
by José de Jesús Manríquez-Torres, Marco Antonio Hernández-Lepe, José Román Chávez-Méndez, Susana González-Reyes, Idanya Rubí Serafín-Higuera, Genaro Rodríguez-Uribe and Jesús Martín Torres-Valencia
Molecules 2020, 25(17), 3944; https://doi.org/10.3390/molecules25173944 - 28 Aug 2020
Cited by 4 | Viewed by 2550
Abstract
In research on natural molecules with cytotoxic activity that can be used for the development of new anticancer agents, the cytotoxic activity of hexane, chloroform, and methanol extracts from the roots of Acacia schaffneri against colon, lung, and skin cancer cell lines was [...] Read more.
In research on natural molecules with cytotoxic activity that can be used for the development of new anticancer agents, the cytotoxic activity of hexane, chloroform, and methanol extracts from the roots of Acacia schaffneri against colon, lung, and skin cancer cell lines was explored. The hexane extract showed the best activity with an average IC50 of 10.6 µg mL−1. From this extract, three diterpenoids, phyllocladan-16α,19-diol (1), phyllocladan-16α-ol (2), and phylloclad-16-en-3-ol (3), were isolated and characterized by their physical and spectroscopic properties. Diterpenoids 1 and 2 were tested against the same cancer cell lines, as well as their healthy counterparts, CCD841 CoN, MRC5, and VH10, respectively. Compound 1 showed moderate activity (IC50 values between 24 and 70 μg mL−1), although it showed a selective effect against cancer cell lines. Compound 2 was practically inactive. The cytotoxicity mechanism of 1 was analyzed by cell cycle, indicating that the compound induces G0/G1 cell cycle arrest. This effect might be generated by DNA alkylation damage. In addition, compound 1 decreased migration of HT29 cells. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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22 pages, 1794 KiB  
Article
Extracts Characterization and In Vitro Evaluation of Potential Immunomodulatory Activities of the Moss Hypnum cupressiforme Hedw.
by Tanja M. Lunić, Mariana M. Oalđe, Marija R. Mandić, Aneta D. Sabovljević, Marko S. Sabovljević, Uroš M. Gašić, Sonja N. Duletić-Laušević, Bojan Dj. Božić and Biljana Dj. Božić Nedeljković
Molecules 2020, 25(15), 3343; https://doi.org/10.3390/molecules25153343 - 23 Jul 2020
Cited by 17 | Viewed by 5628
Abstract
Recently, there has been an increasing interest in the chemistry and biological potential of mosses, since a large number of biologically active compounds have been found within these species. This study aimed at examining the chemical composition and immunomodulatory potential (antioxidant, antidiabetic, anti-neuroinflammatory/antineurodegenerative, [...] Read more.
Recently, there has been an increasing interest in the chemistry and biological potential of mosses, since a large number of biologically active compounds have been found within these species. This study aimed at examining the chemical composition and immunomodulatory potential (antioxidant, antidiabetic, anti-neuroinflammatory/antineurodegenerative, and antitumor activities) of moss Hypnum cupressiforme Hedw. extracts. Corresponding extracts have been obtained applying Soxhlet extractor. The chemical characterization was performed using spectrophotometric assays and liquid chromatography–mass spectrometry (LC-MS). The extracts were analyzed for antioxidant activity and for inhibitory activities on α-glucosidase, α-amylase, acetylcholinesterase, and tyrosinase. Additionally, extracts were tested against four cell lines—MRC-5, BV2, HCT-116, and MDA-MB-231—for antitumor and anti-inflammatory activities. Chemical analysis of extracts revealed the presence of flavonoids, phenolic acids, and triterpenoids. Major compounds identified by LC-MS in H. cupressiforme were kaempferol and five phenolic acids: p-hydroxybenzoic, protocatechuic, p-coumaric, gallic, and caffeic acid. According to biochemical assays the investigated extracts exhibited significant immunomodulatory potential. Significant antiproliferative potential against MDA-MB-231 cells has been observed together with the promising anti-neuroinflammatory application. The obtained data suggest that moss H. cupressiforme is a valuable natural source of biologically active compounds with potential application in the pharmaceutical industry. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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13 pages, 1329 KiB  
Article
Determining the Effect of Pterostilbene on Insulin Secretion Using Chemoproteomics
by Chiara Cassiano, Daniela Eletto, Alessandra Tosco, Raffaele Riccio, Maria Chiara Monti and Agostino Casapullo
Molecules 2020, 25(12), 2885; https://doi.org/10.3390/molecules25122885 - 23 Jun 2020
Cited by 7 | Viewed by 2767
Abstract
Pterostilbene, the 3,5-dimethoxy derivative of resveratrol, is a well-known polyphenolic compound, mainly found in blueberries, grapevines, and Pterocarpus marsupium heartwood, which has recently attracted a great deal of attention due to its wide bio-pharmacological profile. Moreover, pterostilbene is more lipophilic than resveratrol, with [...] Read more.
Pterostilbene, the 3,5-dimethoxy derivative of resveratrol, is a well-known polyphenolic compound, mainly found in blueberries, grapevines, and Pterocarpus marsupium heartwood, which has recently attracted a great deal of attention due to its wide bio-pharmacological profile. Moreover, pterostilbene is more lipophilic than resveratrol, with a consequently better bioavailability and a more interesting therapeutic potential. In this work, a chemoproteomic approach, based on affinity chromatography, was applied on pterostilbene in the attempt to identify the biological targets responsible for its bioactivity. On this basis, syntaxins, a group of proteins involved in the formation of SNARE complexes mediating vesicles exocytosis, were selected among the most interesting pterostilbene interactors. In vitro and in cell assays gave evidence of the pterostilbene ability to reduce insulin secretion on glucose-stimulated pancreatic beta cells, opening the way to potential applications of pterostilbene as a supplement in the care of insulin-dependent metabolic disorders. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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25 pages, 4072 KiB  
Article
Expanding the Role of Sub-Exploited DOE-High Energy Extraction and Metabolomic Profiling towards Agro-Byproduct Valorization: The Case of Carotenoid-Rich Apricot Pulp
by Thalia Tsiaka, Charalambos Fotakis, Dimitra Z. Lantzouraki, Konstantinos Tsiantas, Eleni Siapi, Vassilia J. Sinanoglou and Panagiotis Zoumpoulakis
Molecules 2020, 25(11), 2702; https://doi.org/10.3390/molecules25112702 - 11 Jun 2020
Cited by 13 | Viewed by 3257
Abstract
Traditional extraction remains the method-of-choice for phytochemical analyses. However, the absence of an integrated analytical platform, focusing on customized, validated extraction steps, generates tendentious and non-reproducible data regarding the phytochemical profile. Such a platform would also support the exploration and exploitation of plant [...] Read more.
Traditional extraction remains the method-of-choice for phytochemical analyses. However, the absence of an integrated analytical platform, focusing on customized, validated extraction steps, generates tendentious and non-reproducible data regarding the phytochemical profile. Such a platform would also support the exploration and exploitation of plant byproducts, which are a valuable source of bioactive metabolites. This study deals with the incorporation of (a) the currently sub-exploited high energy extraction methods (ultrasound (UAE)- and microwave-assisted extraction (MAE)), (b) experimental design (DOE), and (c) metabolomics, in an integrated analytical platform for the extensive study of plant metabolomics and phytochemical profiling. The recovery of carotenoids from apricot by-products (pulp) is examined as a case study. MAE, using ethanol as solvent, achieved higher carotenoid yields compared to UAE, where 1:1 chloroform-methanol was employed, and classic extraction. Nuclear magnetic resonance (NMR)-based metabolomic profiling classified extracts according to the variations in co-extractives in relation to the extraction conditions. Extracts with a lower carotenoid content contained branched-chain amino acids as co-extractives. Medium carotenoid content extracts contained choline, unsaturated fatty acids, and sugar alcohols, while the highest carotenoid extracts were also rich in sugars. Overall, the proposed pipeline can provide different the phytochemical fractions of bioactive compounds according to the needs of different industrial sectors (cosmetics, nutraceuticals, etc.). Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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23 pages, 1333 KiB  
Article
Phytosterol, Lipid and Phenolic Composition, and Biological Activities of Guava Seed Oil
by Adchara Prommaban, Niramon Utama-ang, Anan Chaikitwattana, Chairat Uthaipibull, John B. Porter and Somdet Srichairatanakool
Molecules 2020, 25(11), 2474; https://doi.org/10.3390/molecules25112474 - 27 May 2020
Cited by 17 | Viewed by 4554
Abstract
Plant seeds have been found to contain bioactive compounds that have potential nutraceutical benefits. Guava seeds (Psidium guajava) are by-products in the beverage and juice industry; however, they can be utilized for a variety of commercial purposes. This study was designed [...] Read more.
Plant seeds have been found to contain bioactive compounds that have potential nutraceutical benefits. Guava seeds (Psidium guajava) are by-products in the beverage and juice industry; however, they can be utilized for a variety of commercial purposes. This study was designed to analyze the phytochemicals of the n-hexane extract of guava seed oil (GSO), to study its free-radical scavenging activity, and to monitor the changes in serum lipids and fatty acid profiles in rats that were fed GSO. The GSO was analyzed for phytochemicals using chromatographic methods. It was also tested for free-radical scavenging activity in hepatoma and neuroblastoma cells, and analyzed in terms of serum lipids and fatty acids. GSO was found to contain phenolic compounds (e.g., chlorogenic acid and its derivatives) and phytosterols (e.g., stimasterol, β-sitosterol and campesterol), and exerted radical-scavenging activity in cell cultures in a concentration-dependent manner. Long-term consumption of GSO did not increase cholesterol and triglyceride levels in rat serum, but it tended to decrease serum fatty acid levels in a concentration-dependent manner. This is the first study to report on the lipid, phytosterol and phenolic compositions, antioxidant activity, and the hepato- and neuro-protection of hydrogen peroxide-induced oxidative stress levels in the GSO extract. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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19 pages, 2410 KiB  
Article
Phenolic and Non-Polar Fractions of the Extracts from Fruits, Leaves, and Twigs of Elaeagnus rhamnoides (L.) A. Nelson—The Implications for Human Barrier Cells
by Beata Sadowska, Joanna Rywaniak, Anna Cichocka, Kinga Cichocka, Jerzy Żuchowski, Urszula Wójcik-Bojek, Marzena Więckowska-Szakiel and Barbara Różalska
Molecules 2020, 25(9), 2238; https://doi.org/10.3390/molecules25092238 - 9 May 2020
Cited by 6 | Viewed by 3887
Abstract
Biological potential of plant extracts are widely described. Because their oral or topical administration is usually recommended, intestinal mucous and skin are the first surfaces exposed to such preparations. Therefore, we asked the question whether phenolic and non-polar fractions of the extracts from [...] Read more.
Biological potential of plant extracts are widely described. Because their oral or topical administration is usually recommended, intestinal mucous and skin are the first surfaces exposed to such preparations. Therefore, we asked the question whether phenolic and non-polar fractions of the extracts from fruits, twigs, and leaves of sea buckthorn (Elaeagnus rhamnoides (L.) A. Nelson) would be able to modulate the functions of human physiological barrier. The study was carried on caucasian colon epithelial-like Caco-2 cells and human foreskin fibroblasts HFF-1 line. Cell secretory activity (ELISA), the expression of cell surface molecules (flow cytometry), cell migration during wound healing in vitro (scratch assay) were assessed. It was demonstrated for the first time, that sea buckthorn extracts can improve intestinal and skin barrier by increasing of ICAM-1 expression on colon epithelial cells and intensification of IL-8 production by fibroblasts. On the other hand, an inhibition of fibroblasts migration in the presence of those preparations was noted. Therefore, greater attention should be paid on precise description of plant extracts effect depended on target cells and their role to give adequate recommendations for such preparations use. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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17 pages, 1449 KiB  
Article
Copper Complexing Capacity and Trace Metal Content in Common and Balsamic Vinegars: Impact of Organic Matter
by Sotirios Karavoltsos, Aikaterini Sakellari, Vassilia J. Sinanoglou, Panagiotis Zoumpoulakis, Marta Plavšić, Manos Dassenakis and Nick Kalogeropoulos
Molecules 2020, 25(4), 861; https://doi.org/10.3390/molecules25040861 - 15 Feb 2020
Cited by 4 | Viewed by 3162
Abstract
Complex formation is among the mechanisms affecting metal bioaccessibility. Hence, the quantification of organic metal complexation in food items is of interest. Organic ligands in solutions of environmental and/or food origin function as buffering agents against small changes in dissolved metal concentrations, being [...] Read more.
Complex formation is among the mechanisms affecting metal bioaccessibility. Hence, the quantification of organic metal complexation in food items is of interest. Organic ligands in solutions of environmental and/or food origin function as buffering agents against small changes in dissolved metal concentrations, being able to maintain free metal ion concentrations below the toxicity threshold. Organic matter in vinegars consists of bioactive compounds, such as polyphenols, Maillard reaction endproducts, etc., capable of complexing metal ions. Furthermore, transition metal ions are considered as micronutrients essential for living organisms exerting a crucial role in metabolic processes. In this study, differential pulse anodic stripping voltammetry (DPASV), a sensitive electrochemical technique considered to be a powerful tool for the study of metal speciation, was applied for the first time in vinegar samples. The concentrations of Cu complexing ligands (LT) in 43 vinegars retailed in Greece varied between 0.05 and 52 μM, with the highest median concentration determined in balsamic vinegars (14 μM), compared to that of common vinegars (0.86 μM). In 21% of the vinegar samples examined, LT values were exceeded by the corresponding total Cu concentrations, indicating the presence of free Cu ion and/or bound within labile inorganic/organic complexes. Red grape balsamic vinegars exhibited the highest density of Cu ligands per mass unit of organic matter compared to other foodstuffs such as herbal infusions, coffee brews, and beers. Among the 16 metals determined in vinegars, Pb is of particular importance from a toxicological point of view, whereas further investigation is required regarding potential Rb biomagnification. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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Review

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23 pages, 1936 KiB  
Review
Effects of Lipid-Based Encapsulation on the Bioaccessibility and Bioavailability of Phenolic Compounds
by Gulay Ozkan, Tina Kostka, Tuba Esatbeyoglu and Esra Capanoglu
Molecules 2020, 25(23), 5545; https://doi.org/10.3390/molecules25235545 - 26 Nov 2020
Cited by 63 | Viewed by 6110
Abstract
Phenolic compounds (quercetin, rutin, cyanidin, tangeretin, hesperetin, curcumin, resveratrol, etc.) are known to have health-promoting effects and they are accepted as one of the main proposed nutraceutical group. However, their application is limited owing to the problems related with their stability and water [...] Read more.
Phenolic compounds (quercetin, rutin, cyanidin, tangeretin, hesperetin, curcumin, resveratrol, etc.) are known to have health-promoting effects and they are accepted as one of the main proposed nutraceutical group. However, their application is limited owing to the problems related with their stability and water solubility as well as their low bioaccessibility and bioavailability. These limitations can be overcome by encapsulating phenolic compounds by physical, physicochemical and chemical encapsulation techniques. This review focuses on the effects of encapsulation, especially lipid-based techniques (emulsion/nanoemulsion, solid lipid nanoparticles, liposomes/nanoliposomes, etc.), on the digestibility characteristics of phenolic compounds in terms of bioaccessibility and bioavailability. Full article
(This article belongs to the Special Issue Bioactive Compounds with Applications in Health and Food)
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