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Biomedicines
Special Issues
Compounds from Natural Products as Sources for Drug Discovery
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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: 31 August 2025 | Viewed by 7054

Special Issue Editors

Dr. Suzanne A. Nasser

E-Mail Website
Guest Editor
School of Medicine, Keele University, Keele, UK
Interests: cardiovascular; sex hormones; pain; oxidative stress
Prof. Dr. Paul Horrocks

E-Mail Website
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

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. Biomedicines 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 2600 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
  • bioactive compounds
  • medicinal plants
  • marine natural products
  • pharmacological screening
  • pharmacognosy
  • sustainable drug development
  • purification techniques
  • compound isolation

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Published Papers (5 papers)

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20 pages, 11005 KiB  
Article
Synthesis and Evaluation of Isosteviol Derivatives: Promising Anticancer Therapies for Colon Cancer
by Yecang Chen, Feifei Zhu, Yuxin Ding, Lin Xing, Enxiao Wang, Yixiang Fang, Ruilong Sheng, Qidong Tu and Ruihua Guo
Biomedicines 2025, 13(4), 793; https://doi.org/10.3390/biomedicines13040793 - 25 Mar 2025
Viewed by 244
Abstract
Background: Isosteviol, a tetracyclic diterpenoid with a beyerene-type skeleton, exhibited wide pharmacological activities and an inhibitory impact on tumor proliferation in colon cancer; Methods: 22 isosteviol derivatives were synthesized by modifying the C-16 and C-19 position of isosteviol, and then the inhibitory activities [...] Read more.
Background: Isosteviol, a tetracyclic diterpenoid with a beyerene-type skeleton, exhibited wide pharmacological activities and an inhibitory impact on tumor proliferation in colon cancer; Methods: 22 isosteviol derivatives were synthesized by modifying the C-16 and C-19 position of isosteviol, and then the inhibitory activities of derivatives 2–22 were evaluated by CCK8 method. Next, the structure–activity relationships (SARs) of these isosteviol derivatives in HCT116 cells were discussed in detail. Network pharmacology was employed to predict and analyze the targets of isosteviol in the treatment of colon cancer; Results: The results indicated derivative 8 possessed stronger inhibitory activity against HCT116 and HepG2 cells (IC50 = 6.20 ± 0.61 μM for HCT116, and IC50 = 39.84 ± 0.43 μM for HepG2). Additionally, cell cycle analysis indicated that derivative 8 arrested HCT116 cells at the G1 phase and increased the percentage of apoptotic cells. Moreover, the molecular docking showed that derivative 8 could interact with TP53 through its Tyr-1600 and Leu-1534 residues (docking energy: −11.84 kcal/mol); Conclusions: With these results, we can conclude that derivative 8 may be a promising candidate for anticancer chemotherapy. Full article
(This article belongs to the Special Issue Compounds from Natural Products as Sources for Drug Discovery)
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14 pages, 655 KiB  
Article
Combination of Cannabidiol with Cisplatin or Paclitaxel Analysis Using the Chou–Talalay Method and Chemo-Sensitization Evaluation in Platinum-Resistant Ovarian Cancer Cells
by Jana Ismail, Wassim Shebaby, Shirine Azar Atallah, Robin I. Taleb, Sara Kawrani, Wissam Faour and Mohamad Mroueh
Biomedicines 2025, 13(2), 520; https://doi.org/10.3390/biomedicines13020520 - 19 Feb 2025
Viewed by 773
Abstract
Background/Objectives: Cannabidiol (CBD) is known for its anti-cancer properties in preclinical models and is increasingly used alongside conventional chemotherapy in cancer treatment. This study aims to evaluate the anti-cancer activity of CBD from Lebanese Cannabis sativa as a monotherapy and in combination with [...] Read more.
Background/Objectives: Cannabidiol (CBD) is known for its anti-cancer properties in preclinical models and is increasingly used alongside conventional chemotherapy in cancer treatment. This study aims to evaluate the anti-cancer activity of CBD from Lebanese Cannabis sativa as a monotherapy and in combination with cisplatin or paclitaxel on human ovarian adenocarcinoma cells. Methods: Cytotoxicity of CBD was tested on OVCAR-3 and SK-OV-3 cell lines using the MTS assay. The Chou–Talalay method and CompuSyn software were used to determine the combination indices (CIs) for predicting interactions between CBD and chemotherapeutic agents. CBD showed dose-dependent tumor growth inhibition at 72 h with comparable IC50 values for both cell lines. Results: The combination of CBD with cisplatin or paclitaxel showed significant antagonistic interaction in SK-OV-3 cells (CI > 1), but mild synergism (CI < 1) at high growth inhibition rates (95% and 97%) was observed in SK-OV-3 cells with CBD/cisplatin. Pure antagonism was found in OVCAR-3 cells with CBD/cisplatin. Priming SK-OV-3 cells with CBD reduced the IC50 values of both drugs significantly, with a similar effect seen when cells were primed with cisplatin or paclitaxel before CBD treatment. Conclusions: Integrating CBD with chemotherapy could improve cancer therapy and address drug resistance. Sequential administration of CBD and chemotherapeutic agents is more beneficial than simultaneous administration. Further in vivo studies are necessary to validate these findings and understand CBD’s interactions with other drugs fully. Full article
(This article belongs to the Special Issue Compounds from Natural Products as Sources for Drug Discovery)
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14 pages, 442 KiB  
Article
Phenolic Content, Antioxidant Activity and In Vitro Anti-Inflammatory and Antitumor Potential of Selected Bulgarian Propolis Samples
by Yulian Tumbarski, Ivan Ivanov, Mina Todorova, Sonia Apostolova, Rumiana Tzoneva and Krastena Nikolova
Biomedicines 2025, 13(2), 334; https://doi.org/10.3390/biomedicines13020334 - 1 Feb 2025
Cited by 1 | Viewed by 999
Abstract
Background/objectives: Propolis (bee glue) is a valuable bee product widely used as a natural remedy, a cosmetic ingredient, a nutritional value enhancer and a food biopreservative. The present research aims to investigate the phenolic content, antioxidant activity and in vitro anti-inflammatory and antitumor [...] Read more.
Background/objectives: Propolis (bee glue) is a valuable bee product widely used as a natural remedy, a cosmetic ingredient, a nutritional value enhancer and a food biopreservative. The present research aims to investigate the phenolic content, antioxidant activity and in vitro anti-inflammatory and antitumor potential of six propolis samples from three regions of Bulgaria (Vidin, Gabrovo and Lovech). Methods: the analysis of propolis phenolic compounds was determined by high-performance liquid chromatography (HPLC); the antioxidant activity of ethanolic propolis extracts was assessed by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and ferric-reducing antioxidant power (FRAP) assay; the in vitro anti-inflammatory activity was assessed by the inhibition of albumin denaturation method; the in vitro antitumor activity was determined in human metastatic breast cancer cell line MDA-MB-231 using 3-(4,5-Dimethyl -2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. Results: The ethanolic propolis extracts exhibited the total phenolic content from 190.4 to 317.0 mg GAE/g, total flavonoid content from 53.4 to 79.3 mg QE/g and total caffeic acid derivatives content from 5.9 to 12.1 mg CAE/g. The studied propolis extracts showed significant antioxidant capacity (between 1000.3 and 1606.0 mM TE/g determined by the DPPH assay, and between 634.1 and 1134.5 mM TE/g determined by the FRAP assay). The chemical composition analysis indicated high concentrations of caffeic acid benzyl ester, chrysin, pinocembrin and pinobanksin-3-O-propionate, predominantly in three of the propolis samples originating from Gabrovo and Lovech regions. All propolis samples demonstrated promising in vitro anti-inflammatory activity, expressed as the inhibition of thermally induced albumin denaturation by 73.59% to 78.44%, which was higher than that of the conventional anti-inflammatory drugs Aspirin (58.44%) and Prednisolone Cortico (57.34%). The propolis samples exhibited high in vitro cytotoxicity against cancer cells MDA-MB-231 with IC50 values ranging between 9.24 and 13.62 µg/mL as determined by MTT assay. Conclusions: Overall, we can suggest that the high phenolic content of Bulgarian propolis from respective areas contributes to its enhanced antioxidant, anti-inflammatory and antitumor activity. Taken together, our results support the beneficial properties of Bulgarian propolis, with potential application as a promising therapeutic agent. Full article
(This article belongs to the Special Issue Compounds from Natural Products as Sources for Drug Discovery)
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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 2545
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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19 pages, 2473 KiB  
Systematic Review
The Role of Curcumin in Modulating Vascular Function and Structure during Menopause: A Systematic Review
by Amanina Athirah Mad Azli, Norizam Salamt, Amilia Aminuddin, Nur Aishah Che Roos, Mohd Helmy Mokhtar, Jaya Kumar, Adila A. Hamid and Azizah Ugusman
Biomedicines 2024, 12(10), 2281; https://doi.org/10.3390/biomedicines12102281 - 8 Oct 2024
Cited by 1 | Viewed by 1882
Abstract
The risk of developing cardiovascular disease (CVD) escalates in women during menopause, which is associated with increased vascular endothelial dysfunction, arterial stiffness, and vascular remodeling. Meanwhile, curcumin has been demonstrated to enhance vascular function and structure in various studies. Therefore, this study systematically [...] Read more.
The risk of developing cardiovascular disease (CVD) escalates in women during menopause, which is associated with increased vascular endothelial dysfunction, arterial stiffness, and vascular remodeling. Meanwhile, curcumin has been demonstrated to enhance vascular function and structure in various studies. Therefore, this study systematically reviewed the recent literature regarding the potential role of curcumin in modulating vascular function and structure during menopause. The Ovid MEDLINE, PubMed, Scopus, and Web of Science electronic databases were searched to identify relevant articles. Clinical and preclinical studies involving menopausal women and postmenopausal animal models with outcomes related to vascular function or structure were included. After thorough screening, seven articles were selected for data extraction, comprising three animal studies and four clinical trials. The findings from this review suggested that curcumin has beneficial effects on vascular function and structure during menopause by addressing endothelial function, arterial compliance, hemodynamic parameters, and the formation of atherosclerotic lesions. Therefore, curcumin has the potential to be utilized as a supplement to enhance vascular health in menopausal women. However, larger-scale clinical trials employing gold-standard techniques to evaluate vascular health in menopausal women are necessary to validate the preliminary results obtained from small-scale randomized clinical trials involving curcumin supplementation (INPLASY, INPLASY202430043). Full article
(This article belongs to the Special Issue Compounds from Natural Products as Sources for Drug Discovery)
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