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Special Issue "Biological Activity of Secondary Metabolites"

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

Deadline for manuscript submissions: 28 February 2018

Special Issue Editors

Guest Editor
Prof. Dr. Helen D. Skaltsa

Department of Pharmacognosy and Chemistry of Natural Products, School of Pharmacy, University of Athens, 15771 Athens, Greece
Website | E-Mail
Phone: +30 210 7274593
Interests: chemistry of natural products; analytical methods; NMR; GC-MS; terpenes (iridoids, sesquiterpene lactones, triterpenes); phenolics (flavonoids, phenols, phenolic acids, lignans); essential oils; ethnopharmacology; history of pharmacy
Guest Editor
Dr. Marina Sokovic

Institute for Biological Research “Siniša Stanković”, University of Belgrade, Belgrade, Serbia
Website | E-Mail
Interests: Microfungi, macrofungi, antimcirobial activity, natural products

Special Issue Information

Dear Colleagues,

This Special Issue is related to the biological activities of natural products. Secondary metabolites are largely found in plants, marine organisms, bacteria, fungi, and insects. Natural products are used and marketed as medicines or food supplements for a number of health reasons, like the prevention or treatment of an illness or the reduction of health risks, or the maintenance of good health.

Past practices of compound drugs containing different natural ingredients predominately of plant origin were highly esteemed over centuries, but only recently are scientifically confirmed. The ethno pharmacological properties of healing plants have been used as a primary source of medicines for early drug discovery. The investigation of biological and chemical properties of natural products has, not only revealed new bioactive entities for the treatment of several diseases, but also enabled the development of synthetic organic chemistry. Natural products are the most successful source of leads for potential drug discovery and play a highly significant role in medicinal chemistry.

We particularly have interest in manuscripts dealing with the most recent research on bio-active natural products, including: Isolation and structure elucidation, metabolomic analyses, bio-assays, mechanisms of action of bioactive natural products, SAR studies, ethno-pharmacological studies.

Prof. Dr. Helen D. Skaltsa
Dr. Marina Sokovic
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. Molecules is an international peer-reviewed open access monthly 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 1800 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

  • Secondary Metabolites
  • Analytical Techniques
  • Structure elucidation
  • Biological activities
  • Predicting biological activities
  • Structure-activity relationship
  • Target-based assays
  • Ligand-based drug design
  • Ethnopharmacological studies
  • Metabolomic analysis of medicinal plants

Published Papers (2 papers)

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Research

Open AccessArticle Asperflavin, an Anti-Inflammatory Compound Produced by a Marine-Derived Fungus, Eurotium amstelodami
Molecules 2017, 22(11), 1823; doi:10.3390/molecules22111823
Received: 21 September 2017 / Revised: 15 October 2017 / Accepted: 24 October 2017 / Published: 29 October 2017
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Abstract
In the present study, 16 marine-derived fungi were isolated from four types of marine materials including float, algae, animals and drift woods along with the coast of Jeju Island, Korea and evaluated for anti-inflammatory effects in lipopolysaccharide (LPS)-stimulated RAW 24.7 cells. The broth
[...] Read more.
In the present study, 16 marine-derived fungi were isolated from four types of marine materials including float, algae, animals and drift woods along with the coast of Jeju Island, Korea and evaluated for anti-inflammatory effects in lipopolysaccharide (LPS)-stimulated RAW 24.7 cells. The broth and mycelium extracts from the 16 fungi were prepared and the broth extract (BE) of Eurotium amstelodami (015-2) inhibited nitric oxide (NO) production in LPS-stimulated RAW 264.7 cells without cytotoxicity. By further bioassay-guided isolation, three compounds including asperflavin, neoechinulin A and preechinulin were successfully isolated from the BE of E. amstelodami. It was revealed that asperflavin showed no cytotoxicity up to 200 μM and significantly inhibited LPS-induced NO and PGE2 production in a dose-dependent manner. In the western blot results, asperflavin suppressed only inducible NOS (iNOS), but COX-2 were slightly down-regulated. Asperflavin was also observed to inhibit the production of pro-inflammatory cytokines including TNF-α, IL-1β, and IL-6. In conclusion, this study reports a potential use of asperflavin isolated from a marine fungus, E. amstelodami as an anti-inflammatory agent via suppression of iNOS and pro-inflammatory cytokines as well as no cytotoxicity. Full article
(This article belongs to the Special Issue Biological Activity of Secondary Metabolites)
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Open AccessArticle Inhibition of Human Kallikrein 5 Protease by Triterpenoids from Natural Sources
Molecules 2017, 22(11), 1829; doi:10.3390/molecules22111829
Received: 29 September 2017 / Revised: 16 October 2017 / Accepted: 24 October 2017 / Published: 27 October 2017
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Abstract
Stratum corneum tryptic enzyme kallikrein 5 (KLK5) is a serine protease that is involved in the cell renewal and maintenance of the skin barrier function. The excessive activation of KLK5 causes an exacerbation of dermatoses, such as rosacea and atopic dermatitis. Some triterpenoids
[...] Read more.
Stratum corneum tryptic enzyme kallikrein 5 (KLK5) is a serine protease that is involved in the cell renewal and maintenance of the skin barrier function. The excessive activation of KLK5 causes an exacerbation of dermatoses, such as rosacea and atopic dermatitis. Some triterpenoids are reported to suppress the serine proteases. We aimed to investigate whether bioactive triterpenoids modulate the KLK5 protease. Nineteen triterpenoids occurring in medicinal crude drugs were evaluated using an enzymatic assay to measure the anti-KLK5 activity. The KLK5-dependent cathelicidin peptide LL-37 production in human keratinocytes was examined using immunoprecipitation and Western blotting. Screening assays for evaluating the anti-KLK5 activity revealed that ursolic acid, oleanolic acid, saikosaponin b1, tumulosic acid and pachymic acid suppressed the KLK5 protease activity, although critical molecular moieties contributing to anti-KLK5 activity were unclarified. Ursolic acid and tumulosic acid suppressed the proteolytic processing of LL-37 in keratinocytes at ≤10 μM; no cytotoxicity was observed. Both triterpenoids were detected in the plasma of rats administered orally with triterpenoid-rich crude drug Jumihaidokuto. Our study reveals that triterpenoids, such as ursolic acid and tumulosic acid, modulate the KLK5 protease activity and cathelicidin peptide production. Triterpenoids may affect the skin barrier function via the regulation of proteases. Full article
(This article belongs to the Special Issue Biological Activity of Secondary Metabolites)
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