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Secondary Metabolites and Their Synthetic Derivatives as Potential Plant Protection Products

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Plant Sciences".

Deadline for manuscript submissions: 28 July 2024 | Viewed by 727

Special Issue Editor


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Guest Editor
Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Viale delle Scienze, 90128 Palermo, Italy
Interests: bioactive natural products; phytochemistry; medicinal natural products; structural modification; structural identification
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Special Issue Information

Dear Colleagues,

The world of terrestrial and aquatic plants offers diversified molecules which continue, to this day, to be the most interesting therapeutic option for the treatment of various pathologies that affect human beings.

The process leading to the discovery of new drugs is certainly long and troubled, but nevertheless, simple compounds, with 15 or 20 carbon atoms, such as sesquiterpenes or diterpenes, are still classes of chemical compounds that offer, even when derivatized, important applications for human health. The complex structure of these organic compounds, which is characterized by numerous chiral centers, can increase their biological potency and selectivity. For this reason, it is essential to carefully evaluate all the synthetic processes implemented for the discovery and development of new drugs.

This Special Issue focuses on those natural molecules, in particular terpenes, naturally present in plants and on synthetic derivatives. Different pathologies, such as anti-inflammatory, antiproliferative, antioxidant, and antibacterial activities, will be evaluated, both in vitro and in vivo, to find their correlations with the structural diversity in the compound or compounds investigated.

Dr. Natale Badalamenti
Guest Editor

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Keywords

  • terpenoids
  • biological activities
  • natural products
  • NMR
  • synthetic derivatives
  • structural modification
  • mechanism of action

Published Papers (1 paper)

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Research

27 pages, 4441 KiB  
Article
Synthetic Derivatives of Natural ent-Kaurane Atractyligenin Disclose Anticancer Properties in Colon Cancer Cells, Triggering Apoptotic Cell Demise
by Natale Badalamenti, Antonella Maggio, Gianfranco Fontana, Maurizio Bruno, Marianna Lauricella and Antonella D’Anneo
Int. J. Mol. Sci. 2024, 25(7), 3925; https://doi.org/10.3390/ijms25073925 - 31 Mar 2024
Viewed by 562
Abstract
The antitumor activity of different ent-kaurane diterpenes has been extensively studied. Several investigations have demonstrated the excellent antitumor activity of synthetic derivatives of the diterpene atractyligenin. In this research, a series of new synthetic amides and their 15,19-di-oxo analogues obtained from atractyligenin [...] Read more.
The antitumor activity of different ent-kaurane diterpenes has been extensively studied. Several investigations have demonstrated the excellent antitumor activity of synthetic derivatives of the diterpene atractyligenin. In this research, a series of new synthetic amides and their 15,19-di-oxo analogues obtained from atractyligenin by modifying the C-2, C-15, and C-19 positions were designed in order to dispose of a set of derivatives with different substitutions at the amidic nitrogen. Using different concentrations of the obtained compounds (10–300 μM) a reduction in cell viability of HCT116 colon cancer cells was observed at 48 h of treatment. All the di-oxidized compounds were more effective than their alcoholic precursors. The di-oxidized compounds had already reduced the viability of two colon cancer cells (HCT116 and Caco-2) at 24 h when used at low doses (2.5–15 μM), while they turned out to be poorly effective in differentiated Caco-2 cells, a model of polarized enterocytes. The data reported here provide evidence that di-oxidized compounds induced apoptotic cell death, as demonstrated by the appearance of condensed and fragmented DNA in treated cells, as well as the activation of caspase-3 and fragmentation of its target PARP-1. Full article
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