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Biomolecules
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Chemistry, Biosynthesis and Biological Activity of Natural Substances: A Themed...
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Chemistry, Biosynthesis and Biological Activity of Natural Substances: A Themed Issue Dedicated to Professor Evidente

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Synthetic Biology and Bioengineering".

Deadline for manuscript submissions: closed (15 June 2022) | Viewed by 16932

Special Issue Editor

Prof. Dr. Alexander V Kornienko

E-Mail Website
Guest Editor
Department of Chemistry and Biochemistry, Texas State University, San Marcos, TX 78666, USA
Interests: organic synthesis; drug discovery; cancer research; natural products

Special Issue Information

Dear Colleagues,

Natural products are commonly regarded as “privileged structures” selected by evolution to manifest multiple biological activities. Because of such intrinsic biorelevance, compounds of nature have historically been a major source of novel pharmaceuticals. For example, in the area of cancer, the fraction of drugs whose origin can be attributed to natural products amounts to 60%, and identification of hits in biological screening of natural product-derived collections of compounds is much more frequent compared with high-throughput screens of combinatorial libraries. In this Special Issue, dedicated to Professor Evidente’s achievements in natural product research, reports covering the chemistry, biology and medicinal potential of natural substances are highly welcome, and novel developments in this generally broad area of research will undoubtedly be met with enthusiasm by the scientific community working on the interface of various scientific disciplines that natural products bring together. 

Prof. Dr. Alexander V Kornienko
Guest Editor

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. Biomolecules 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 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

  • natural products
  • drug discovery
  • structure elucidation
  • synthesis
  • biosynthesis

Published Papers (4 papers)

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Research

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20 pages, 6119 KiB  
Article
Amaryllidaceae Alkaloids Decrease the Proliferation, Invasion, and Secretion of Clinically Relevant Cytokines by Cultured Human Colon Cancer Cells
by Veronique Mathieu, Breana Laguera, Marco Masi, Sara Adriana Dulanto, Tanner W. Bingham, Lucas W. Hernandez, David Sarlah, Antonio Evidente, Denis L. J. Lafontaine, Alexander Kornienko and Michelle A. Lane
Biomolecules 2022, 12(9), 1267; https://doi.org/10.3390/biom12091267 - 9 Sep 2022
Cited by 8 | Viewed by 2652
Abstract
Alkaloids isolated from members of the Amaryllidaceae plant family are promising anticancer agents. The purpose of the current study was to determine if the isocarbostyrils narciclasine, pancratistatin, lycorane, lycorine, crinane, and haemanthamine inhibit phenomena related to cancer progression in vitro. To achieve this, [...] Read more.
Alkaloids isolated from members of the Amaryllidaceae plant family are promising anticancer agents. The purpose of the current study was to determine if the isocarbostyrils narciclasine, pancratistatin, lycorane, lycorine, crinane, and haemanthamine inhibit phenomena related to cancer progression in vitro. To achieve this, we examined the proliferation, adhesion, and invasion of cultured human colon cancer cells via MTT assay and Matrigel-coated Boyden chambers. In addition, Luminex assays were used to quantify the secretion of matrix metalloproteinases (MMP) and cytokines associated with poor clinical outcomes. We found that all alkaloids decreased cell proliferation regardless of TP53 status, with narciclasine exhibiting the greatest potency. The effects on cell proliferation also appear to be specific to cancer cells. Narciclasine, lycorine, and haemanthamine decrease both adhesion and invasion but with various potencies depending on the cell line. In addition, narciclasine, lycorine, and haemanthamine decreased the secretion of MMP-1, -2, and -7, as well as the secretion of the cytokines pentraxin 3 and vascular endothelial growth factor. In conclusion, the present study shows that Amaryllidaceae alkaloids decrease phenomena and cytokines associated with colorectal cancer progression, supporting future investigations regarding their potential as multifaceted drug candidates. Full article
(This article belongs to the Special Issue Chemistry, Biosynthesis and Biological Activity of Natural Substances: A Themed Issue Dedicated to Professor Evidente)
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Review

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25 pages, 1657 KiB  
Review
Minor Phytocannabinoids: A Misleading Name but a Promising Opportunity for Biomedical Research
by Diego Caprioglio, Hawraz Ibrahim M. Amin, Orazio Taglialatela-Scafati, Eduardo Muñoz and Giovanni Appendino
Biomolecules 2022, 12(8), 1084; https://doi.org/10.3390/biom12081084 - 6 Aug 2022
Cited by 10 | Viewed by 3034
Abstract
Despite the very large number of phytocannabinoids isolated from Cannabis (Cannabis sativa L.), bioactivity studies have long remained focused on the so called “Big Four” [Δ9-THC (1), CBD (2), CBG (3) and CBC ( [...] Read more.
Despite the very large number of phytocannabinoids isolated from Cannabis (Cannabis sativa L.), bioactivity studies have long remained focused on the so called “Big Four” [Δ9-THC (1), CBD (2), CBG (3) and CBC (4)] because of their earlier characterization and relatively easy availability via isolation and/or synthesis. Bioactivity information on the chemical space associated with the remaining part of the cannabinome, a set of ca 150 compounds traditionally referred to as “minor phytocannabinoids”, is scarce and patchy, yet promising in terms of pharmacological potential. According to their advancement stage, we sorted the bioactivity data available on these compounds, better referred to as the “dark cannabinome”, into categories: discovery (in vitro phenotypical and biochemical assays), preclinical (animal models), and clinical. Strategies to overcome the availability issues associated with minor phytocannabinoids are discussed, as well as the still unmet challenges facing their development as mainstream drugs. Full article
(This article belongs to the Special Issue Chemistry, Biosynthesis and Biological Activity of Natural Substances: A Themed Issue Dedicated to Professor Evidente)
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15 pages, 824 KiB  
Review
Biotechnological Approaches to Optimize the Production of Amaryllidaceae Alkaloids
by Manoj Koirala, Vahid Karimzadegan, Nuwan Sameera Liyanage, Natacha Mérindol and Isabel Desgagné-Penix
Biomolecules 2022, 12(7), 893; https://doi.org/10.3390/biom12070893 - 25 Jun 2022
Cited by 8 | Viewed by 3292
Abstract
Amaryllidaceae alkaloids (AAs) are plant specialized metabolites with therapeutic properties exclusively produced by the Amaryllidaceae plant family. The two most studied representatives of the family are galanthamine, an acetylcholinesterase inhibitor used as a treatment of Alzheimer’s disease, and lycorine, displaying potent in vitro [...] Read more.
Amaryllidaceae alkaloids (AAs) are plant specialized metabolites with therapeutic properties exclusively produced by the Amaryllidaceae plant family. The two most studied representatives of the family are galanthamine, an acetylcholinesterase inhibitor used as a treatment of Alzheimer’s disease, and lycorine, displaying potent in vitro and in vivo cytotoxic and antiviral properties. Unfortunately, the variable level of AAs’ production in planta restricts most of the pharmaceutical applications. Several biotechnological alternatives, such as in vitro culture or synthetic biology, are being developed to enhance the production and fulfil the increasing demand for these AAs plant-derived drugs. In this review, current biotechnological approaches to produce different types of bioactive AAs are discussed. Full article
(This article belongs to the Special Issue Chemistry, Biosynthesis and Biological Activity of Natural Substances: A Themed Issue Dedicated to Professor Evidente)
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11 pages, 1158 KiB  
Review
Cannabis Biomolecule Effects on Cancer Cells and Cancer Stem Cells: Cytotoxic, Anti-Proliferative, and Anti-Migratory Activities
by Hadar Peeri and Hinanit Koltai
Biomolecules 2022, 12(4), 491; https://doi.org/10.3390/biom12040491 - 24 Mar 2022
Cited by 17 | Viewed by 7401
Abstract
Cancer is a complex family of diseases affecting millions of people worldwide. Gliomas are primary brain tumors that account for ~80% of all malignant brain tumors. Glioblastoma multiforme (GBM) is the most common, invasive, and lethal subtype of glioma. Therapy resistance and intra-GBM [...] Read more.
Cancer is a complex family of diseases affecting millions of people worldwide. Gliomas are primary brain tumors that account for ~80% of all malignant brain tumors. Glioblastoma multiforme (GBM) is the most common, invasive, and lethal subtype of glioma. Therapy resistance and intra-GBM tumoral heterogeneity are promoted by subpopulations of glioma stem cells (GSCs). Cannabis sativa produces hundreds of secondary metabolites, such as flavonoids, terpenes, and phytocannabinoids. Around 160 phytocannabinoids have been identified in C. sativa. Cannabis is commonly used to treat various medical conditions, and it is used in the palliative care of cancer patients. The anti-cancer properties of cannabis compounds include cytotoxic, anti-proliferative, and anti-migratory activities on cancer cells and cancer stem cells. The endocannabinoids system is widely distributed in the body, and its dysregulation is associated with different diseases, including various types of cancer. Anti-cancer activities of phytocannabinoids are mediated in glioma cells, at least partially, by the endocannabinoid receptors, triggering various cellular signaling pathways, including the endoplasmic reticulum (ER) stress pathway. Specific combinations of multiple phytocannabinoids act synergistically against cancer cells and may trigger different anti-cancer signaling pathways. Yet, due to scarcity of clinical trials, there remains no solid basis for the anti-cancer therapeutic potential of cannabis compounds. Full article
(This article belongs to the Special Issue Chemistry, Biosynthesis and Biological Activity of Natural Substances: A Themed Issue Dedicated to Professor Evidente)
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