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Therapeutic Potential of Natural Compounds: Insights into Mechanisms, Molecular Docking, and Biological Activities

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

Deadline for manuscript submissions: 25 July 2024 | Viewed by 2360

Special Issue Editor


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Guest Editor
Department of Pharmaceutical Microbiology, Medical University of Gdańsk, 80-416 Gdańsk, Poland
Interests: antimicrobials plant secondary metabolites; plant extracts; synthetic derivatives; bacterial antibiotic resistance; antimicrobial assay; mechanism of action; clinical microbiology; diagnostic microbiology; microbial pathogenesis; hospital epidemiology

Special Issue Information

Dear Colleagues,

For centuries, folk medicine has been used to treat various ailments afflicting people and animals stemming from plants, lichens, mushrooms, etc. The accurate determination of the biological properties of chemical compounds (i.e., those responsible for the healing properties of natural products) have progressed in tandem with the development of science. Naturally occurring compounds have become the basis for modern synthetic modifications, leading to the creation of active substances with more effective mechanisms of action, improved pharmacological parameters, and low side effects. Unfortunately, new or known diseases that are resistant to current preparations have been detected.Therefore, there is a constant need to identify new compounds/mixtures of compounds that can combat new diseases,or allow us to control diseases that are immune to current treatments.

Led by Dr. Rafał Hałasa and assisted by the Topical Advisory Panel Member Dr. Katarzyna Turecka (Medical University of Gdańsk), this Special Issue is devoted to natural compounds and their derivatives, including their biological activity and mechanisms of action that may have therapeutic uses in the fight against diseases. Original research articles and reviews on these and related topics will be considered for publication in this Special Issue.

Dr. Rafał Hałasa
Guest Editor

Manuscript Submission Information

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Keywords

  • natural compounds
  • synthetic derivatives of natural compounds
  • biological activity
  • mechanism of action
  • molecular docking
  • therapeutic potential
  • anticancer
  • antimicrobial
  • antiviral
  • anti-civilization diseases
  • antiobesity
  • antidiabetes
  • preventing the development of cardiovascular diseases, including myocardial infarction, hypertension and ischemic heart disease
  • food hypersensitivity
  • antiallergy

Published Papers (2 papers)

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Research

19 pages, 5628 KiB  
Article
An In Vitro Study on the Cytotoxic, Antioxidant, and Antimicrobial Properties of Yamogenin—A Plant Steroidal Saponin and Evaluation of Its Mechanism of Action in Gastric Cancer Cells
by Justyna Stefanowicz-Hajduk, Piotr Graczyk, Anna Hering, Magdalena Gucwa, Anna Nowak and Rafał Hałasa
Int. J. Mol. Sci. 2024, 25(9), 4627; https://doi.org/10.3390/ijms25094627 - 24 Apr 2024
Viewed by 758
Abstract
Yamogenin is a steroidal saponin occurring in plant species such as Asparagus officinalis, Dioscorea collettii, Trigonella foenum-graecum, and Agave sp. In this study, we evaluated in vitro cytotoxic, antioxidant, and antimicrobial properties of yamogenin. The cytotoxic activity was estimated on [...] Read more.
Yamogenin is a steroidal saponin occurring in plant species such as Asparagus officinalis, Dioscorea collettii, Trigonella foenum-graecum, and Agave sp. In this study, we evaluated in vitro cytotoxic, antioxidant, and antimicrobial properties of yamogenin. The cytotoxic activity was estimated on human colon cancer HCT116, gastric cancer AGS, squamous carcinoma UM-SCC-6 cells, and human normal fibroblasts with MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay. The amount of apoptotic and dead AGS cells after treatment with yamogenin was estimated with flow cytometry. Also, in yamogenin-treated AGS cells we investigated the reactive oxygen species (ROS) production, mitochondrial membrane depolarization, activity level of caspase-8 and -9, and gene expression at mRNA level with flow cytometry, luminometry, and RT-PCR, respectively. The antioxidant properties of yamogenin were assessed with DPPH (2,2-diphenyl-1-picrylhydrazyl) and ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) assays. The antimicrobial potential of the compound was estimated on Staphylococcus aureus, Bacillus cereus, Klebsiella pneumoniae, Escherichia coli, Salmonella enterica, Helicobacter pylori, Campylobacter coli, Campylobacter jejuni, Listeria monocytogenes, Lactobacillus paracasei, and Lactobacillus acidophilus bacteria strains. Yamogenin showed the strongest cytotoxic effect on AGS cells (IC50 18.50 ± 1.24 µg/mL) among the tested cell lines. This effect was significantly stronger in combinations of yamogenin with oxaliplatin or capecitabine than for the single compounds. Furthermore, yamogenin induced ROS production, depolarized mitochondrial membrane, and increased the activity level of caspase-8 and -9 in AGS cells. RT-PCR analysis revealed that this sapogenin strongly up-regulated TNFRSF25 expression at the mRNA level. These results indicate that yamogenin induced cell death via the extrinsic and intrinsic way of apoptosis. Antioxidant study showed that yamogenin had moderate in vitro potential (IC50 704.7 ± 5.9 µg/mL in DPPH and 631.09 ± 3.51 µg/mL in ABTS assay) as well as the inhibition of protein denaturation properties (with IC50 1421.92 ± 6.06 µg/mL). Antimicrobial test revealed a weak effect of yamogenin on bacteria strains, the strongest one being against S. aureus (with MIC value of 350 µg/mL). In conclusion, yamogenin may be a potential candidate for the treatment and prevention of gastric cancers. Full article
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21 pages, 3717 KiB  
Article
New Chalcone Derivatives Containing 2,4-Dichlorobenzenesulfonamide Moiety with Anticancer and Antioxidant Properties
by Anita Bułakowska, Jarosław Sławiński, Anna Hering, Magdalena Gucwa, J. Renata Ochocka, Rafał Hałasa, Łukasz Balewski and Justyna Stefanowicz-Hajduk
Int. J. Mol. Sci. 2024, 25(1), 274; https://doi.org/10.3390/ijms25010274 - 24 Dec 2023
Cited by 1 | Viewed by 1140
Abstract
Chalcones and their derivatives, both natural and synthetic, exhibit diverse biological activities. In this study, we focused on designing and synthesizing (E)-2,4-dichloro-N-(4-cinnamoylphenyl)-5-methylbenzenesulfonamides 48 with the following two pharmacophore groups: 2,4-dichlorobenzenesulfonamide and chalcone. The obtained compounds displayed notable [...] Read more.
Chalcones and their derivatives, both natural and synthetic, exhibit diverse biological activities. In this study, we focused on designing and synthesizing (E)-2,4-dichloro-N-(4-cinnamoylphenyl)-5-methylbenzenesulfonamides 48 with the following two pharmacophore groups: 2,4-dichlorobenzenesulfonamide and chalcone. The obtained compounds displayed notable anticancer effects on various human cancer cells, such as cervical HeLa, acute promyelocytic leukemia HL-60, and gastric adenocarcinoma AGS, when assessed with the MTT test. The activity of all compounds against cancer cells was significant, and the obtained IC50 values were in the range of 0.89–9.63 µg/mL. Among all the tested compounds, derivative 5 showed the highest activity on the AGS cell line. Therefore, it was tested for cell cycle inhibition, induction of mitochondrial membrane depolarization, and activation of caspase-8 and -9. These results showed that this compound strongly arrested the cell cycle in the subG0 phase, depolarized the mitochondrial membrane, and activated caspase-8 and -9. Similar to the anticancer effects, all the obtained compounds 4–8 were also assessed for their antioxidant activity. The highest antiradical effect was demonstrated for derivative 5, which was able to inhibit DPPH and ABTS radicals. All examined compounds showed dose-dependent activity against neutrophil elastase. Notably, derivatives 7 and 8 demonstrated inhibitory properties similar to oleanolic acid, with IC50 values of 25.61 ± 0.58 and 25.73 ± 0.39 µg/mL, respectively. To determine the antibacterial activity of derivatives 48, the minimum bacteriostatic concentration (MIC) values were estimated (>500 µg/mL for all the tested bacterial strains). The findings demonstrate the substantial potential of sulfonamide-based chalcone 5 as a promising drug in anticancer therapy. Full article
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