Compounds from Natural Products as Sources for Drug Discovery

A special issue of Biomedicines (ISSN 2227-9059). This special issue belongs to the section "Drug Discovery, Development and Delivery".

Deadline for manuscript submissions: 30 September 2024 | Viewed by 464

Special Issue Editors


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Guest Editor
School of Medicine, Keele University, Keele, UK
Interests: cardiovascular; sex hormones; pain; oxidative stress

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Co-Guest Editor
School of Medicine, Keele University, Staffordshire ST5 5BG, UK
Interests: malaria; Plasmodium falciparum; cell biology; drug action; pharmacodynamics; leishmaniasis; assay development; natural products; medical education; postgraduate research

Special Issue Information

Dear Colleagues,

This Special Issue aims to comprehensively showcase the diverse landscape of bioactive compounds derived from natural products and their profound significance in contemporary drug discovery endeavours. Contributions are invited to delve into various facets of this dynamic field, encompassing the isolation, structural elucidation, pharmacological evaluation, and mechanistic insights of individual compounds sourced from a diverse array of natural reservoirs, including plants, microorganisms, and marine organisms. We encourage the submission of research articles, reviews, and perspectives that shed light on innovative methodologies for compound isolation and characterisation, as well as studies elucidating the therapeutic potential and molecular mechanisms underlying the bioactivity of these natural compounds. Furthermore, we seek to highlight the crucial role of sustainable sourcing practices and ethical considerations in the utilisation of individual compounds for pharmaceutical purposes. Through collaborative efforts, this Special Issue aims to advance our understanding of the intricate interplay between nature's chemical diversity and its implications for the development of novel therapeutics, fostering meaningful contributions to the field of drug discovery.

Dr. Suzanne A. Nasser
Prof. Dr. Paul Horrocks
Guest Editors

Manuscript Submission Information

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Keywords

  • natural products
  • drug discovery
  • bioactive compounds
  • medicinal plants
  • marine natural products
  • pharmacological screening
  • pharmacognosy
  • sustainable drug development
  • purification techniques
  • compound isolation

Published Papers (1 paper)

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Research

11 pages, 3611 KiB  
Article
Cannabielsoin (CBE), a CBD Oxidation Product, Is a Biased CB1 Agonist
by Mehdi Haghdoost, Scott Young, Matthew Roberts, Caitlyn Krebs and Marcel O. Bonn-Miller
Biomedicines 2024, 12(7), 1551; https://doi.org/10.3390/biomedicines12071551 - 12 Jul 2024
Viewed by 296
Abstract
Cannabielsoin (CBE) is primarily recognized as an oxidation byproduct of cannabidiol (CBD) and a minor mammalian metabolite of CBD. The pharmacological interactions between CBE and cannabinoid receptors remain largely unexplored, particularly with respect to cannabinoid receptor type 1 (CB1). The present [...] Read more.
Cannabielsoin (CBE) is primarily recognized as an oxidation byproduct of cannabidiol (CBD) and a minor mammalian metabolite of CBD. The pharmacological interactions between CBE and cannabinoid receptors remain largely unexplored, particularly with respect to cannabinoid receptor type 1 (CB1). The present study aimed to elucidate the interaction dynamics of CBE in relation to CB1 by employing cyclic adenosine monophosphate (cAMP) and β-arrestin assays to assess its role as an agonist, antagonist, and positive allosteric modulator (PAM). To our knowledge, this is the first publication to investigate CBE’s receptor activity in vitro. Our findings reveal that S-CBE acts as an agonist to CB1 with EC50 = 1.23 µg/mL (3.7 µM) in the cAMP assay. No agonist activity was observed in the β-arrestin assay in concentrations up to 12 µM, suggesting a noteworthy affinity towards G-protein activation and the cAMP signaling pathway. Furthermore, in silico molecular docking simulations were conducted to provide a structural basis for the interaction between CBE and CB1, offering insights into the molecular determinants of its receptor affinity and functional selectivity. Full article
(This article belongs to the Special Issue Compounds from Natural Products as Sources for Drug Discovery)
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