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From Bioactive Compounds to New Drugs: Commemorative Issue Dedicated to...
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From Bioactive Compounds to New Drugs: Commemorative Issue Dedicated to Professor Ernesto Fattorusso (1937-2012)

A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: closed (31 July 2018) | Viewed by 34207

Special Issue Editors

Prof. Dr. Patrizia Ciminiello

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Dipartimento di Chimica delle Sostanze Naturali, Università di Napoli "Federico II", Via D. Montesano 49, I-80131 Napoli, Italy
Interests: marine natural products; marine plankton; structure elucidation; marine biotoxins; dinoflagellates
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Alfonso Mangoni

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Department of Pharmacy, University of Naples Federico II, Naples, Italy
Interests: marine natural products; structural elucidation; biosynthetic gene clusters; metagenomics; computational chemistry
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Prof. Dr. Marialuisa Menna

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Department of Pharmacy, School of Medicine and Surgery, University of Naples Federico II, Via Domenico Montesano, 49 – 80131, Naples, Italy
Interests: natural products chemistry; NMR spectroscopy; small molecules structure elucidation; bioactive marine metabolites; synthetic and medicinal chemistry; chemical libraries; marine-inspired leads to drugs
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Prof. Dr. Orazio Taglialatela-Scafati

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Department of Pharmacy, University of Naples Federico II, Naples, Italy
Interests: marine and terrestrial natural products; pharmaceutical biology; stereostructure elucidation; bioactivity
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Marine Drugs and Molecules are pleased to announce a joint commemorative Special Issue dedicated to Professor Ernesto Fattorusso, on the occasion of his 80th birthday in 2017, for his outstanding contribution in the research field of bioactive natural products.

Prof. Fattorusso (born in 1937) has been Professor of Organic Chemistry at the University of Naples Federico II since 1975. He was one of the founding fathers of the chemistry of marine natural products, and, more recently, he was also involved in the investigation of therapeutically active terrestrial plants of the Mediterranean flora. His prolific scientific activity is documented by more than 350 papers describing the isolation and identification of bioactive natural products, potential leads for drug, cosmetic, and biotechnological applications. Prof. Fattorusso founded a multidisciplinary research group, the NeaNat group, based at the Department of Pharmacy of the University of Naples Federico II, which will be continuing to work on these topics.

Since 1980, Prof. Fattorusso has coordinated many national and international projects (NOMATEC, BIOTOXmarin, NatPharma, BLUEGENICS among others) and established fruitful collaborations with several institutions around the world. Prof. Fattorusso has received a remarkable number of awards, including the prestigious Paul Scheuer Award in 2010 for his studies in the field of marine natural products: he was the first European scientist to receive this award.

This commemorative issue welcomes submission of previously unpublished manuscripts (original researches or reviews) on the investigation of biologically active chemical entities, with particular regard to natural products isolated from plants, marine invertebrates and microorganisms, potentially useful as lead compounds for the development of new drugs or biological tools.

We plan to receive submissions from November 2016 to the end of September 2017. Manuscripts will be published on an ongoing basis after being processed.

Prof. Dr. Patrizia Ciminiello
Prof. Dr. Alfonso Mangoni
Prof. Dr. Marialuisa Menna
Prof. Dr. Orazio Taglialatela-Scafati
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 submissions that pass pre-check are 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 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 2700 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

  • Lead compounds
  • Natural products
  • Biological tools
  • Drug development
  • Structure elucidation-
  • Organic synthesis

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Related Special Issue

Published Papers (4 papers)

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Research

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8 pages, 738 KiB  
Article
TRPA1 Modulating C14 Polyacetylenes from the Iranian Endemic Plant Echinophora platyloba
by Giuseppina Chianese, Carmina Sirignano, Yalda Shokoohinia, Zeynab Mohammadi, Leili Bazvandi, Fataneh Jafari, Fereshteh Jalilian, Aniello Schiano Moriello, Luciano De Petrocellis, Orazio Taglialatela-Scafati and Daniela Rigano
Molecules 2018, 23(7), 1750; https://doi.org/10.3390/molecules23071750 - 17 Jul 2018
Cited by 9 | Viewed by 4132
Abstract
Phytochemical investigation of the apolar extract obtained from aerial parts of the Iranian endemic plant Echinophora platyloba DC (Apiaceae) resulted in the characterization of the polyacetylene fraction of this plant. This resulted to be composed of the known echinophorins A and B, embedding [...] Read more.
Phytochemical investigation of the apolar extract obtained from aerial parts of the Iranian endemic plant Echinophora platyloba DC (Apiaceae) resulted in the characterization of the polyacetylene fraction of this plant. This resulted to be composed of the known echinophorins A and B, embedding the very rare α-pyrone terminal, and of the new echinophorin D (3), including also three conjugated triple bonds. The chemical structures of these compounds were secured by detailed inspection of MS and 1D/2D NMR spectra. The isolated polyacteylenes were evaluated for their modulation of six thermo-TRP channels and they revealed a selective activity on TRPA1, an ion channel involved in the mediation of neuropathic and inflammatory pain. This is the first report on the activity of plant polyacetylenes on transient receptor potential (TRP) channels. Full article
(This article belongs to the Special Issue From Bioactive Compounds to New Drugs: Commemorative Issue Dedicated to Professor Ernesto Fattorusso (1937-2012))
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1893 KiB  
Article
Characterization and Trypanocidal Activity of a Novel Pyranaphthoquinone
by Elen Diana Dantas, Fabia Julliana Jorge De Souza, William Nascimento Litaiff Nogueira, Cláudia Cândida Silva, Pedro Henrique Antunes De Azevedo, Cícero Flávio Soares Aragão, Patricia Danielle Oliveira de Almeida, Mariana Filomena do Carmo Cardoso, Fernando De Carvalho Da Silva, Eduardo Pereira De Azevedo, Euzébio Guimarães Barbosa, Emerson Silva Lima, Vitor Francisco Ferreira and Ádley Antonini Neves de Lima
Molecules 2017, 22(10), 1631; https://doi.org/10.3390/molecules22101631 - 30 Sep 2017
Cited by 11 | Viewed by 4572
Abstract
Chagas disease is an endemic parasitic infection that occurs in 21 Latin American countries. New therapies for this disease are urgently needed, as the only two drugs available (nifurtimox and benznidazol) have high toxicity and variable efficacy in the disease’s chronic phase. Recently, [...] Read more.
Chagas disease is an endemic parasitic infection that occurs in 21 Latin American countries. New therapies for this disease are urgently needed, as the only two drugs available (nifurtimox and benznidazol) have high toxicity and variable efficacy in the disease’s chronic phase. Recently, a new chemical entity (NCE) named Pyranaphthoquinone (IVS320) was synthesized from lawsone. We report herein, a detailed study of the physicochemical properties and in vitro trypanocidal activity of IVS320. A series of assays were performed for characterization, where thermal, diffractometric, and morphological analysis were performed. In addition, the solubility, permeability, and hygroscopicity of IVS320 were determined. The results show that its poor solubility and low permeability may be due to its high degree of crystallinity (99.19%), which might require the use of proper techniques to increase the IVS320’s aqueous solubility and permeability. The trypanocidal activity study demonstrated that IVS320 is more potent than the reference drug benznidazole, with IC50/24 h of 1.49 ± 0.1 μM, which indicates that IVS320 has potential as a new drug candidate for the treatment of Chagas disease. Full article
(This article belongs to the Special Issue From Bioactive Compounds to New Drugs: Commemorative Issue Dedicated to Professor Ernesto Fattorusso (1937-2012))
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Review

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14 pages, 8768 KiB  
Review
Antiviral Activities of Oleanolic Acid and Its Analogues
by Vuyolwethu Khwaza, Opeoluwa O. Oyedeji and Blessing A. Aderibigbe
Molecules 2018, 23(9), 2300; https://doi.org/10.3390/molecules23092300 - 9 Sep 2018
Cited by 69 | Viewed by 8490
Abstract
Viral diseases, such as human immune deficiency virus (HIV), influenza, hepatitis, and herpes, are the leading causes of human death in the world. The shortage of effective vaccines or therapeutics for the prevention and treatment of the numerous viral infections, and the great [...] Read more.
Viral diseases, such as human immune deficiency virus (HIV), influenza, hepatitis, and herpes, are the leading causes of human death in the world. The shortage of effective vaccines or therapeutics for the prevention and treatment of the numerous viral infections, and the great increase in the number of new drug-resistant viruses, indicate that there is a great need for the development of novel and potent antiviral drugs. Natural products are one of the most valuable sources for drug discovery. Most natural triterpenoids, such as oleanolic acid (OA), possess notable antiviral activity. Therefore, it is important to validate how plant isolates, such as OA and its analogues, can improve and produce potent drugs for the treatment of viral disease. This article reports a review of the analogues of oleanolic acid and their selected pathogenic antiviral activities, which include HIV, the influenza virus, hepatitis B and C viruses, and herpes viruses. Full article
(This article belongs to the Special Issue From Bioactive Compounds to New Drugs: Commemorative Issue Dedicated to Professor Ernesto Fattorusso (1937-2012))
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1493 KiB  
Review
Molecular Targets for Components of Essential Oils in the Insect Nervous System—A Review
by Milena Jankowska, Justyna Rogalska, Joanna Wyszkowska and Maria Stankiewicz
Molecules 2018, 23(1), 34; https://doi.org/10.3390/molecules23010034 - 23 Dec 2017
Cited by 265 | Viewed by 15930
Abstract
Essential oils (EOs) are lipophilic secondary metabolites obtained from plants; terpenoids represent the main components of them. A lot of studies showed neurotoxic actions of EOs. In insects, they cause paralysis followed by death. This feature let us consider components of EOs as [...] Read more.
Essential oils (EOs) are lipophilic secondary metabolites obtained from plants; terpenoids represent the main components of them. A lot of studies showed neurotoxic actions of EOs. In insects, they cause paralysis followed by death. This feature let us consider components of EOs as potential bioinsecticides. The inhibition of acetylcholinesterase (AChE) is the one of the most investigated mechanisms of action in EOs. However, EOs are rather weak inhibitors of AChE. Another proposed mechanism of EO action is a positive allosteric modulation of GABA receptors (GABArs). There are several papers that prove the potentiation of GABA effect on mammalian receptors induced by EOs. In contrast, there is lack of any data concerning the binding of EO components in insects GABArs. In insects, EOs act also via the octopaminergic system. Available data show that EOs can increase the level of both cAMP and calcium in nervous cells. Moreover, some EO components compete with octopamine in binding to its receptor. Electrophysiological experiments performed on Periplaneta americana have shown similarity in the action of EO components and octopamine. This suggests that EOs can modify neuron activity by octopamine receptors. A multitude of potential targets in the insect nervous system makes EO components interesting candidates for bio-insecticides. Full article
(This article belongs to the Special Issue From Bioactive Compounds to New Drugs: Commemorative Issue Dedicated to Professor Ernesto Fattorusso (1937-2012))
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