Special Issue "Biological Activity and Applications of Natural Compounds"

A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Applied Biosciences and Bioengineering".

Deadline for manuscript submissions: 15 January 2020.

Special Issue Editors

Prof. Dr. Ana M. L Seca
E-Mail Website
Guest Editor
Sciences of Chemistry, Physics and Engineering, University of the Azores, Ponta Delgada, Portugal
Interests: isolation by preparative chromatographic techniques, and identification, by 1D and 2D NMR and MS methods, of biologically active secondary metabolites; analyzing of secondary metabolite profile by GC-MS
Special Issues and Collections in MDPI journals
Prof. Dr. Laila M. Moujir
E-Mail Website
Guest Editor
Department of Biochemistry, Microbiology, Genetics and Cell Biology. Faculty of Pharmacy, University of La Laguna, Santa Cruz de Tenerife, Spain
Interests: i) determination of antimicrobial and cytotoxic activity of secondary metabolites; ii) enzymatic activity.
Prof. Dr. Farukh Sharopov
E-Mail Website
Guest Editor
Department of Pharmaceutical Technology, Avicenna Tajik State Medical University, Rudaki Avenue 139, Dushanbe, Tajikistan
Interests: Natural products; medicinal plants; isolation active compounds; essential oils; biological activity; cytotoxicity; antioxidants; chromatography; sorption; adsorbents; drug discovery.

Special Issue Information

Dear Colleagues,

Natural compounds, also known as secondary metabolites, obtained from terrestrial or marine species, are a research focal point, both from the point of view of isolation and structural characterization of new molecules that can be valuable scaffolds, as well as from the point of view of applications of these molecules in the pharmaceutical (e.g., to treat cancer, cardiovascular and infectious), food (e.g. as additive), cosmetic (e.g. as proposal of smart-aging), and environmental industries, among others.

As Guest Editors of this Special Issue of Applied Sciences “Biological Activity and Applications of Natural Compounds”, we invite you to provide original research contributions, as well as review articles, related with pure and completely characterized secondary metabolites from plants, seaweed, and sponges. Specifically, this issue will focus on the potential of these metabolites as therapeutic agents (due to their in vitro and in vivo antitumor, antioxidant, anti-inflammatory, anti-neurodegenerative, antimicrobial, and anti-aging activities) as well as environmental health agents and nutraceuticals.

We look forward to receiving your contributions to this Special Issue.

Prof. Dr. Ana M. L Seca
Prof. Dr. Laila M. Moujir
Prof. Dr. Farukh Sharopov
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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. Applied Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1500 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Natural compounds
  • bioactivities
  • industrial applications
  • drug discovery
  • nutraceutical
  • environmental health
  • anticancer
  • antioxidant
  • anti-aging
  • structure-activity relationship

Published Papers (7 papers)

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Research

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Open AccessCommunication
Synthesis and Evaluation of the Lifespan-Extension Properties of Oleracones D–F, Antioxidative Flavonoids from Portulaca oleracea L.
Appl. Sci. 2019, 9(19), 4014; https://doi.org/10.3390/app9194014 - 25 Sep 2019
Abstract
Plant-derived antioxidants have been widely used as supplementary health foods, as well as having been regarded as drug candidates for aging and aging-associated diseases. Oleracones, a novel series of flavonoids isolated from Portulaca oleracea L., possess potent antioxidative activities and are expected to [...] Read more.
Plant-derived antioxidants have been widely used as supplementary health foods, as well as having been regarded as drug candidates for aging and aging-associated diseases. Oleracones, a novel series of flavonoids isolated from Portulaca oleracea L., possess potent antioxidative activities and are expected to exhibit therapeutic potential on the aging process. The current paper describes the concise sequential synthesis of oleracones D–F. Oleracones D and F were efficiently synthesized via selective intramolecular oxa-Michael addition from oleracone E. In addition, we investigated their possible lifespan-extension properties using Caenorhabditis elegans, which is excellently suited as an experimental model to study aging. A significant longevity effect was observed when nematodes were grown with 20 μM of oleracone E. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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Open AccessFeature PaperArticle
Essential Oil Compositions and Antifungal Activity of Sunflower (Helianthus) Species Growing in North Alabama
Appl. Sci. 2019, 9(15), 3179; https://doi.org/10.3390/app9153179 - 05 Aug 2019
Abstract
Helianthus species are North American members of the Asteraceae, several of which have been used as traditional medicines by Native Americans. The aerial parts of two cultivars of Helianthus annuus, “Chianti” and “Mammoth”, and wild-growing H. strumosus, were collected from locations [...] Read more.
Helianthus species are North American members of the Asteraceae, several of which have been used as traditional medicines by Native Americans. The aerial parts of two cultivars of Helianthus annuus, “Chianti” and “Mammoth”, and wild-growing H. strumosus, were collected from locations in north Alabama. The essential oils were obtained by hydrodistillation and analyzed by gas chromatography—mass spectrometry. The Helianthus essential oils were dominated by monoterpene hydrocarbons, in particular α-pinene (50.65%, 48.91%, and 58.65%, respectively), sabinene (6.81%, 17.01%, and 1.91%, respectively), β-pinene (5.79%, 3.27%, and 4.52%, respectively), and limonene (7.2%, 7.1%, and 3.8%, respectively). The essential oils were screened against three opportunistic pathogenic fungal species, Aspergillus niger, Candida albicans, and Cryptococcus neoformans. The most sensitive fungus was C. neoformans with minimum inhibitory concentration (MIC) values of 78, 156, and 78 μg/mL, respectively. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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Open AccessFeature PaperArticle
Structural Requirements for Antimicrobial Activity of Phenolic Nor-Triterpenes from Celastraceae Species
Appl. Sci. 2019, 9(15), 2957; https://doi.org/10.3390/app9152957 - 24 Jul 2019
Abstract
The emergence of pathogenic bacteria-resistant strains is a major public health issue. In this regard, natural product scaffolds offer a promising source of new antimicrobial drugs. In the present study, we report the antimicrobial activity against Gram-positive and Gram-negative bacteria and the yeast [...] Read more.
The emergence of pathogenic bacteria-resistant strains is a major public health issue. In this regard, natural product scaffolds offer a promising source of new antimicrobial drugs. In the present study, we report the antimicrobial activity against Gram-positive and Gram-negative bacteria and the yeast Candida albicans of five phenolic nor-triterpenes (15) isolated from Maytenus blepharodes and Maytenus canariensis in addition to four derivatives (69), three of them reported for the first time. Their stereostructures have been elucidated on the basis of spectroscopic analysis, including one-dimensional (1D) and two-dimensional (2D) NMR techniques, spectrometric methods, and comparison with data reported in the literature. To understand the structural basis for the antimicrobial activity of this type of compounds, we have performed an in-depth study of the structure–activity relationship (SAR) of a series of previously reported phenolic nor-triterpenes. The SAR analysis was based on the skeleton framework, oxidation degree, functional groups, and regiosubstitution patterns, revealing that these aspects modulate the antimicrobial activity. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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Open AccessArticle
Chalcones and Flavanones Bearing Hydroxyl and/or Methoxyl Groups: Synthesis and Biological Assessments
Appl. Sci. 2019, 9(14), 2846; https://doi.org/10.3390/app9142846 - 17 Jul 2019
Cited by 2
Abstract
Chalcones and flavanones are isomeric structures and also classes of natural products, belonging to the flavonoid family. Moreover, their wide range of biological activities makes them key scaffolds for the synthesis of new and more efficient drugs. In this work, the synthesis of [...] Read more.
Chalcones and flavanones are isomeric structures and also classes of natural products, belonging to the flavonoid family. Moreover, their wide range of biological activities makes them key scaffolds for the synthesis of new and more efficient drugs. In this work, the synthesis of hydroxy and/or methoxychalcones was studied using less common bases, such as sodium hydride (NaH) and lithium bis(trimethylsilyl)amide (LiHMDS), in the aldol condensation. The results show that the use of NaH was more effective for the synthesis of 2′-hydroxychalcone derivatives, while LiHMDS led to the synthesis of polyhydroxylated chalcones in a one-pot process. During this study, it was also possible to establish the conditions that favor their isomerization into flavanones, allowing at the same time the synthesis of hydroxy and/or methoxyflavanones. The chalcones and flavanones obtained were evaluated to disclose their antioxidant, anticholinesterasic, antibacterial and antitumor activities. 2′,4′,4-Trihydroxychalcone was the most active compound in terms of antioxidant, anti-butyrylcholinesterase (IC50 26.55 ± 0.55 μg/mL, similar to control drug donepezil, IC50 28.94 ± 1.76 μg/mL) and antimicrobial activity. 4′,7-Dihydroxyflavanone presented dual inhibition, that is, the ability to inhibit both cholinesterases. 4′-Hydroxy-5,7-dimethoxyflavanone and 2′-hydroxy-4-methoxychalcone were the compounds with the best antitumor activity. The substitution pattern and the biological assay results allowed the establishment of some structure/activity relationships. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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Open AccessArticle
Volatile Secondary Metabolites with Potent Antidiabetic Activity from the Roots of Prangos pabularia Lindl.—Computational and Experimental Investigations
Appl. Sci. 2019, 9(11), 2362; https://doi.org/10.3390/app9112362 - 10 Jun 2019
Abstract
(1) Background: Almost 500 million people worldwide are suffering from diabetes. Since ancient times, humans have used medicinal plants for the treatment of diabetes. Medicinal plants continue to serve as natural sources for the discovery of antidiabetic compounds. Prangos pabularia Lindl. is a [...] Read more.
(1) Background: Almost 500 million people worldwide are suffering from diabetes. Since ancient times, humans have used medicinal plants for the treatment of diabetes. Medicinal plants continue to serve as natural sources for the discovery of antidiabetic compounds. Prangos pabularia Lindl. is a widely distributed herb with large reserves in Tajikistan. Its roots and fruits have been used in Tajik traditional medicine. To our best knowledge, there are no previously published reports concerning the antidiabetic activity and the chemical composition of the essential oil obtained from roots of P. pabularia. (2) Methods: The volatile secondary metabolites were obtained by hydrodistillation from the underground parts of P. pabularia growing wild in Tajikistan and were analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). Protein tyrosine phosphatase 1B (PTP-1B) inhibition assay and molecular docking analysis were carried out to evaluate the potential antidiabetic activity of the P. pabularia essential oil. (3) Results: The main constituents of the volatile oil of P. pabularia were 5-pentylcyclohexa-1,3-diene (44.6%), menthone (12.6%), 1-tridecyne (10.9%), and osthole (6.0%). PTP-1B inhibition assay of the essential oil and osthole resulted in significant inhibitory activity with an IC50 value of 0.06 ± 0.01 and 0.93 ± 0.1 μg/mL. Molecular docking analysis suggests volatile compounds such as osthole inhibit PTP-1B, and the results are also in agreement with experimental investigations. (4) Conclusions: Volatile secondary metabolites and the pure isolated compound (osthole) from the roots of P. pabularia exhibited potent antidiabetic activity, twenty-five and nearly two times more than the positive control (3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-(4-(thiazol-2-ylsulfamyl)-phenyl)-amide)) with an IC50 value of 1.46 ± 0.4 μg/mL, respectively. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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Open AccessArticle
The Antifungal Potential of Carvacrol against Penicillium Digitatum through 1H-NMR Based Metabolomics Approach
Appl. Sci. 2019, 9(11), 2240; https://doi.org/10.3390/app9112240 - 30 May 2019
Abstract
Carvacrol (5-Isopropyl-2-methylphenol), a volatile oil constituent, mainly exists in Labiaceae family plants. Carvacrol has long been studied for its natural antifungal potential and food preservative potential. However, its exact mode of action, especially against Penicillium digitatum (P. digitatum), remains unexplored. Herein, [...] Read more.
Carvacrol (5-Isopropyl-2-methylphenol), a volatile oil constituent, mainly exists in Labiaceae family plants. Carvacrol has long been studied for its natural antifungal potential and food preservative potential. However, its exact mode of action, especially against Penicillium digitatum (P. digitatum), remains unexplored. Herein, a 1H-NMR-based metabolomic technique was used to investigate the antifungal mechanism of carvacrol against P. digitatum. The metabolomic profiling data showed that alanine, aspartate, glutamate, and glutathione metabolism were imbalanced in the fungal hyphae. A strong positive correlation was seen between aspartate, glutamate, alanine, and glutamine, with a negative correlation among glutathione and lactate. These metabolic changes revealed that carvacrol-induced oxidative stress had disturbed the energy production and amino acid metabolism of P. digitatum. The current study will improve the understanding of the metabolic changes posed by plant-based fungicides in order to control citrus fruit green mold caused by P. digitatum. Moreover, the study will provide a certain experimental and theoretical basis for the development of novel citrus fruit preservatives. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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Review

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Open AccessReview
Therapeutic Potential of Rosmarinic Acid: A Comprehensive Review
Appl. Sci. 2019, 9(15), 3139; https://doi.org/10.3390/app9153139 - 02 Aug 2019
Abstract
Naturally occurring food-derived active ingredients have received huge attention for their chemopreventive and chemotherapy capabilities in several diseases. Rosmarinic acid (RA) is a caffeic acid ester and a naturally-occurring phenolic compound in a number of plants belonging to the Lamiaceae family, such as [...] Read more.
Naturally occurring food-derived active ingredients have received huge attention for their chemopreventive and chemotherapy capabilities in several diseases. Rosmarinic acid (RA) is a caffeic acid ester and a naturally-occurring phenolic compound in a number of plants belonging to the Lamiaceae family, such as Rosmarinus officinalis (rosemary) from which it was formerly isolated. RA intervenes in carcinogenesis through different ways, including in tumor cell proliferation, apoptosis, metastasis, and inflammation. On the other hand, it also exerts powerful antimicrobial, anti-inflammatory, antioxidant and even antidepressant, anti-aging effects. The present review aims to provide an overview on anticancer activities of RA and to deliberate its therapeutic potential against a wide variety of diseases. Given the current evidence, RA may be considered as part of the daily diet in the treatment of several diseases, with pre-determined doses avoiding cytotoxicity. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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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: Structural Requirements for Antimicrobial Activity of Phenolic nor-Triterpenes from Celastraceae species

Authors: Laila Moujira, Manuel R. Lópeza, Ignacio A. Jiménezb, Isabel L. Bazzocchib

 

 

Title: Hydroxyl or Methoxyl Chalcone and Flavanone Derivatives: Synthesis and Biological Applications

Authors: Gonçalo P. Rosa, Ana M. L. Seca, Maria do Carmo Barreto, Artur M. S. Silva and Diana C. G. A. Pinto

 

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