Natural Products-Assisted Organic Synthesis in Medicinal Chemistry

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 25 June 2025 | Viewed by 1872

Special Issue Editors


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Guest Editor
Department of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University in Bratislava, Kalinčiakova 8, 83104 Bratislava, Slovakia
Interests: palladium complexes; curcuminoids; cytotoxicity; structural characterization of organic compounds; synthesis of organic compounds; synthesis of bio-inorganic compounds; coordination chemistry

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Guest Editor
Institute of Oncology "Prof.Dr.I.Chiricuta", 34-36 Republicii, 400015 Cluj-Napoca, Romania
Interests: oncology; biomarkers; bioinorganic chemistry; immunology; chemotherapy; biochemistry; translational medicine; cell biology; radiobiology; nanostructures

Special Issue Information

Dear Colleagues,

Natural products have been used as remedies as a form alternative medicine since ancient times. Many of the isolated organic compounds from plants have been proven to be biologically active and used as antifungal, antimicrobial, anti-inflammatory, antitussive, analgetic, antipyretic, and antioxidant agents, essentially contributing to medicine and pharmacotherapy. Generally, plant extracts also have disadvantages, whereby either the extracted amount of an active compound does not fulfill the requested quantity due to low natural abundance or the isolation of the active component as a pure biological active substance can be a strenuous process, which causes adverse side effects of the naturally extracted drug. The total synthesis of natural organic compounds and their derivatives supports the preparative aspects of a range of molecules of plant origins. In this regard, the limitations of the extracts are reduced, and the possibility of deriving natural products by generating synthetic analogs with improved biological activity can be afforded. Currently, various synthetic organic compounds are used in the prevention and treatment of cancer; rheumatic, cardiovascular, and neurodegenerative illnesses; and so forth. The diversity and availability of synthetic methods of organic compounds similar to natural products afford benefits, especially in the medical area.

Dr. Natalia Miklášová
Dr. Eva Fischer-Fodor
Guest Editors

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Keywords

  • total organic synthesis
  • preparative methods of natural products
  • natural carboxylic acids
  • derivatives of organic carboxylic acids
  • amino acids
  • carbonyl derivatives
  • phenolic compounds
  • heterocyclic compounds
  • antioxidant activity
  • antifungal activity
  • antimicrobial activity
  • anti-inflammatory activity
  • cytotoxicity
  • anti-cancer activity
  • ROS activity
  • DNA damages
  • structure-activity studies
  • DFT calculations for synthetic organic products
  • molecular docking

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Published Papers (2 papers)

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Research

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18 pages, 3508 KiB  
Article
Synthesis and Characterization of PEGylated Liposomes and Nanostructured Lipid Carriers with Entrapped Bioactive Triterpenoids: Comparative Fingerprints and Quantification by UHPLC-QTOF-ESI+-MS, ATR-FTIR Spectroscopy, and HPLC-DAD
by Carmen Socaciu, Florinela Fetea and Mihai Adrian Socaciu
Pharmaceuticals 2025, 18(1), 33; https://doi.org/10.3390/ph18010033 - 31 Dec 2024
Viewed by 975
Abstract
Background/Objectives: Pentacyclic triterpenoids, as bioactive phytochemicals, have proven to exhibit significant bioactivity (antioxidant, anti-inflammatory, hypoglycemic, and anticancer) and low cytotoxicity. This study developed convenient methods for extracting and characterizing a birch bark extract enriched in pentacyclic triterpenoids (betulin, betulinic acid, and lupeol) [...] Read more.
Background/Objectives: Pentacyclic triterpenoids, as bioactive phytochemicals, have proven to exhibit significant bioactivity (antioxidant, anti-inflammatory, hypoglycemic, and anticancer) and low cytotoxicity. This study developed convenient methods for extracting and characterizing a birch bark extract enriched in pentacyclic triterpenoids (betulin, betulinic acid, and lupeol) and entrapped in two bioavailable nanoformulations. The performance of ATR-FTIR spectroscopy as a cost-effective and non-destructive method was evaluated comparatively with accurate HPLC-based methods. Methods: The bark extract and pure betulin or betulinic acid were used to obtain PEGylated liposomes and nano lipid carriers (NLCs). Their size was characterized by light scattering diffraction. UV–Vis spectrometry was applied as a preliminary evaluation (1), as well as UHPLC-QTOF-ESI+-MS for structure identification (2), ATR-FTIR spectroscopy (for semi-quantitative evaluation) (3), and HPLC-DAD for an accurate quantification of each component, either in the organic solvents or in the nanoformulations (4). Results: The PEGylated liposomes had smaller sizes, and higher entrapment efficiency, significantly correlated between the three analytical methods. The performance of ATR-FTIR spectroscopy was positively correlated with HPLC-DAD data and confirmed the potential of this cheaper and reliable semi-quantitative method to evaluate the entrapment efficiency of TTs in liposome and NLC nanoformulations. Conclusions: The results recommend using liposomal nanoformulations for the entrapment of bioactive terpenoids and their characterization by ATR-FTIR after validation by HPLC-DAD. The ATR-FTIR spectroscopy also offers the possibility of screening in a short time different recipes of nanoformulations as well as their stability and bioavailability, which is useful for investigations in vitro and in vivo, which may confirm their efficacy as therapeutic agents. Full article
(This article belongs to the Special Issue Natural Products-Assisted Organic Synthesis in Medicinal Chemistry)
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Review

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30 pages, 16466 KiB  
Review
Natural Antifungal Alkaloids for Crop Protection: An Overview of the Latest Synthetic Approaches
by Denise Dozio, Francesca Sacchi, Andrea Pinto, Sabrina Dallavalle, Francesca Annunziata and Salvatore Princiotto
Pharmaceuticals 2025, 18(4), 589; https://doi.org/10.3390/ph18040589 - 18 Apr 2025
Viewed by 501
Abstract
Alkaloids are nitrogen-containing compounds naturally occurring in plants, microorganisms, and marine organisms. Potent biological activities have been reported to date, ranging from neuroprotective to antioxidant and anticancer effects. Alkaloids have recently gained attention as potential antifungal agents for crop protection due to their [...] Read more.
Alkaloids are nitrogen-containing compounds naturally occurring in plants, microorganisms, and marine organisms. Potent biological activities have been reported to date, ranging from neuroprotective to antioxidant and anticancer effects. Alkaloids have recently gained attention as potential antifungal agents for crop protection due to their broad spectrum of activity, eco-friendly nature, and ability to overcome some of the issues associated with synthetic fungicides, such as resistance development and environmental contamination. Several efforts have been made to obtain natural and nature-derived alkaloids endowed with significant activity against numerous pathogenic fungal strains. In this review, we collect synthetic strategies developed over the past decade to produce alkaloid fungicides for crop protection. Special emphasis is given to recent advancements in obtaining pure natural compounds and more potent analogs endowed with tailored and optimized properties. Full article
(This article belongs to the Special Issue Natural Products-Assisted Organic Synthesis in Medicinal Chemistry)
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