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Molecules
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Antiproliferative Activities of Natural and Synthetic Compounds
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Antiproliferative Activities of Natural and Synthetic Compounds

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 31 May 2025 | Viewed by 2997

Special Issue Editor

Prof. Dr. Daniel Pereira Bezerra

E-Mail Website
Guest Editor
Gonçalo Moniz Institute, Oswaldo Cruz Foundation (IGM-FIOCRUZ/BA), Salvador, BA 40296-710, Brazil
Interests: natural products; experimental oncology; biotechnology; natural products biotechnology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The identification and selection of antiproliferative compounds is of particular importance in cancer research. Studies of natural and synthetic compounds with antiproliferative effects have provided new insights into their potential for cancer treatment. Understanding the mechanisms through which these compounds affect cell proliferation may lead to the development of more effective therapies that specifically target cancer cells.

This Special Issue encourages the submission of papers on the antiproliferative effects of synthetic and natural compounds on cancer cells from marine organisms, fungi, microorganisms, and medicinal plants. We only welcome submissions of well chemically characterized compounds. The following areas of natural and synthetic compounds with antiproliferative activities are covered:

  • Chemistryofnaturalproducts;
  • Syntheticchemistry;
  • Mechanismofaction;
  • Moleculartarget;
  • Formulations and delivery systems.

This Special Issue aims to publish original research papers and reviews from researchers worldwide.

Prof. Dr. Daniel Pereira Bezerra
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. Molecules is an international peer-reviewed open access semimonthly 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

  • cancer research
  • natural products
  • synthetic compounds

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Published Papers (2 papers)

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Research

16 pages, 2112 KiB  
Article
Extraction of Cannabinoids and Terpenes from Hemp Flowers and Leaves (Cannabis sativa L., Futura 75): Chemical Profiling and Evaluation of Anticancer Properties
by Monika Haczkiewicz, Marta Świtalska, Jacek Łyczko, Magdalena Pluta, Joanna Wietrzyk and Anna Gliszczyńska
Molecules 2025, 30(6), 1325; https://doi.org/10.3390/molecules30061325 - 15 Mar 2025
Viewed by 975
Abstract
This study investigated efficient extraction methods for cannabinoids and terpenes from the above-ground parts of Futura 75, focusing on two techniques: pressurized extraction and magnetic stirrer-assisted extraction. The effects of solvent type, temperature, time, and pressure were evaluated using five organic solvents and [...] Read more.
This study investigated efficient extraction methods for cannabinoids and terpenes from the above-ground parts of Futura 75, focusing on two techniques: pressurized extraction and magnetic stirrer-assisted extraction. The effects of solvent type, temperature, time, and pressure were evaluated using five organic solvents and two binary solvent systems. Cannabinoid profiles of obtained extracts were analyzed using gas chromatography coupled with mass spectrometry (GC-MS), while terpene profiles were characterized through solid-phase microextraction (SPME) combined with GC-MS. Next, two selected extracts with the highest content of cannabinoid and terpene fractions (Futu1 and Futu2) were tested for antiproliferative activity toward cancer cell lines (MV4-11, AGS, HT-29, MDA-MB-468, MCF-7) and their cytotoxicity was evaluated on non-tumorigenic MCF-10A cells. Extract Futu1 contained 51.57% cannabinoids, 9.8% monoterpenes, and 90.2% sesquiterpenes in the terpene fraction. Futu2 exhibited a higher proportion of monoterpenes in the terpene fraction (19.6% monoterpenes and 80.4% sesquiterpenes) and consisted of 49.49% cannabinoids. Both extracts exhibited higher selectivity for cancer cells over non-tumorigenic cells, with Futu2 demonstrating stronger antiproliferative properties. Interestingly, lower concentrations of extracts and tested free, single cannabinoids stimulated the growth of leukemia (MV4-11) and breast cancer (MDA-MB-468) cell lines while their higher concentrations suppressed proliferation. Full article
(This article belongs to the Special Issue Antiproliferative Activities of Natural and Synthetic Compounds)
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16 pages, 1206 KiB  
Article
Gouregine, an α-Gem-Dimethyltetradehydrocularine Alkaloid, and Other Aporphinoid Alkaloids from the Bark of Guatteria olivacea (Annonaceae) and Their In Vitro Cytotoxic Activities
by Emmanoel V. Costa, José Guilherme C. Freitas, Steve Pereira Manickchand, Morgana de S. Araújo, Valdenizia R. Silva, Luciano de S. Santos, Hector Henrique Ferreira Koolen, Felipe M. A. da Silva, Milena Botelho Pereira Soares and Daniel P. Bezerra
Molecules 2024, 29(16), 3834; https://doi.org/10.3390/molecules29163834 - 13 Aug 2024
Cited by 1 | Viewed by 1196
Abstract
Guatteria olivacea R.E. Fries is an Amazonian species known as ‘envira-bobó’ and ‘envira-fofa’ and is common in the states of Amazonas, Acre, and Pará. Recently, the essential oil from the leaves of this species has shown promising antitumor activity both in vitro and [...] Read more.
Guatteria olivacea R.E. Fries is an Amazonian species known as ‘envira-bobó’ and ‘envira-fofa’ and is common in the states of Amazonas, Acre, and Pará. Recently, the essential oil from the leaves of this species has shown promising antitumor activity both in vitro and in vivo. The presence of isoquinoline-derived alkaloids, including aporphinoids and tetrahydroprotoberberine alkaloids, has also been previously reported. In our ongoing search for bioactive compounds from Annonaceae Amazonian plants, the bark of G. olivacea was investigated via classical chromatography techniques, which revealed nine compounds, eight isoquinoline-derived alkaloids, a rare alkaloid with a α-gem-dimethyltetradehydrocularine structure known as gouregine, seven known aporphinoid alkaloids: isopiline, O-methylisopiline, melosmine, 9-hydroxyiguattescine, dihydromelosmine, lysicamine, and guattouregidine, and one known pimaradiene diterpene: acanthoic acid. All the isolated compounds were described for the first time in the bark of G. olivacea, and their structures were elucidated by extensive analyses of their 1D and 2D NMR spectra in combination with MS data. The NMR data of the alkaloids isopiline, O-methylisopiline, melosmine, dihydromelosmine, and guattouregidine were revised due to incomplete data in the literature and some ambiguities. The in vitro cytotoxic activities of the isolated compounds were evaluated against human cancer (HepG2, KG-1a, and HCT116) and noncancerous (MRC-5) cell lines via the Alamar blue assay after 72 h of incubation. Among the compounds evaluated against human cancer cell lines, the most active was the oxoaporphine alkaloid lysicamine, which has strong activity against HCT116 cells, with an IC50 value of 6.64 µg/mL (22.79 µmol/L). Melosmine had a moderate effect on HCT116 cells, with an IC50 value of 16.77 µg/mL (49.70 µmol/L), whereas acanthoic acid had moderate effects on HepG2 and HCT116 cells, with IC50 values of 14.63 µg/mL (48.37 µmol/L) and 21.25 µg/mL (70.25 µmol/L), respectively. Full article
(This article belongs to the Special Issue Antiproliferative Activities of Natural and Synthetic Compounds)
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