Therapeutic Potential of Natural Compounds: In Vitro and In Vivo Approaches

A special issue of Plants (ISSN 2223-7747). This special issue belongs to the section "Phytochemistry".

Deadline for manuscript submissions: 31 October 2024 | Viewed by 3133

Special Issue Editors


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Department of Pharmacognosy, University of Medicine and Pharmacy “Victor Babeş“, Eftimie Murgu Square, No. 2, 300041 Timişoara, Romania
Interests: phytochemical characterization; extraction, isolation and characterization of pure bioactive compounds from plants extracts; assessment of the biological activity of plant extracts/pure active phytochemicals; in vitro, in vivo evaluations; clinical trials
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Department of Pharmacognosy, Lithuanian University of Health Sciences, Sukileliu Av. 13, LT-50162 Kaunas, Lithuania
Interests: phytochemical and antioxidant investigation of herbal raw material and isolated compounds; qualitative–quantitative analysis of proteins; lectins; investigation of proteins; lectins’ biological activity tested in vitro and in vivo; search for new herbal drugs and pharmacological activities; clinical investigation of natural antioxidants on the development of Diabetes mellitus complications; periodontitis
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Pharmacology, School of Medicine, Faculty of Health Sciences, University of Pretoria, Pretoria, South Africa
Interests: phytopharmacology; medicinal plants; toxicology; drug development
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Special Issue Information

Dear Colleagues,

Natural compounds derived from plants, animals, and microorganisms have long been recognized for their diverse pharmacological properties. Many researchers have investigated the therapeutic potential of selected natural compounds through comprehensive in vitro and in vivo evaluations in order to assess the efficacy and safety of these compounds in various disease models, shedding light on their mechanisms of action and clinical applications.

As revealed by various search engines, the number of studies containing the keywords ‘medicinal plants’, ‘natural compounds’, and ‘phytochemicals’ is growing annually. Moreover, approximately a quarter of the newly approved drugs within the past four decades have been derived from natural sources. The aim of this Special Issue is to disseminate the latest findings regarding the identification of new plant sources with therapeutic potential, along with phytochemical characterization and biological evaluation (pre-clinical/clinical studies), identification of new biological activities of plant extracts or pure active phytochemicals together with their mechanism of action (pre-clinical/clinical studies), identification of extracts or pure isolated phytocompounds with synergistic action and associated mechanism of action, (pre-clinical/clinical studies), physico-chemical modulation and evaluation of bioactive phytochemicals  (pre-clinical/clinical studies), green-synthesis of nanoparticles (physico-chemical characterisation, pre-clinical/clinical studies), nutraceuticals, and cosmeceuticals of natural origin (physico-chemical characterisation, pre-clinical/clinical studies). As Guest Editors, we welcome experimental/clinical research papers and in-depth reviews.

Prof. Dr. Corina Danciu
Prof. Dr. Nijole Savickienė
Prof. Dr. Vanessa Steenkamp
Guest Editors

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Keywords

  • natural compounds
  • plant extracts
  • in vitro
  • in vivo
  • biological activity

Published Papers (2 papers)

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Research

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19 pages, 3239 KiB  
Article
Enhanced Cytotoxicity and Antimelanoma Activity of Novel Semisynthetic Derivatives of Betulinic Acid with Indole Conjugation
by Adelina Lombrea, Claudia Geanina Watz, Larisa Bora, Cristina Adriana Dehelean, Zorita Diaconeasa, Stefania Dinu, Māris Turks, Jevgeņija Lugiņina, Uldis Peipiņš and Corina Danciu
Plants 2024, 13(1), 36; https://doi.org/10.3390/plants13010036 - 21 Dec 2023
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Abstract
The prevalence and severity of skin cancer, specifically malignant melanoma, among Caucasians remains a significant concern. Natural compounds from plants have long been explored as potential anticancer agents. Betulinic acid (BI) has shown promise in its therapeutic properties, including its anticancer effects. However, [...] Read more.
The prevalence and severity of skin cancer, specifically malignant melanoma, among Caucasians remains a significant concern. Natural compounds from plants have long been explored as potential anticancer agents. Betulinic acid (BI) has shown promise in its therapeutic properties, including its anticancer effects. However, its limited bioavailability has hindered its medicinal applications. To address this issue, two recently synthesized semisynthetic derivatives, N-(2,3-indolo-betulinoyl)diglycylglycine (BA1) and N-(2,3-indolo-betulinoyl)glycylglycine (BA2), were compared with previously reported compounds N-(2,3-indolo-betulinoyl)glycine (BA3), 2,3-indolo-betulinic acid (BA4), and BI. These compounds were evaluated for their effects on murine melanoma cells (B164A5) using various in vitro assays. The introduction of an indole framework at the C2 position of BI resulted in an increased cytotoxicity. Furthermore, the cytotoxicity of compound BA4 was enhanced by conjugating its carboxylic group with an amino acid residue. BA2 and BA3, with glycine and glycylglycine residues at C28, exhibited approximately 2.20-fold higher inhibitory activity compared to BA4. The safety assessment of the compounds on human keratinocytes (HaCaT) has revealed that concentrations up to 10 µM slightly reduced cell viability, while concentrations of 75 µM resulted in lower cell viability rates. LDH leakage assays confirmed cell membrane damage in B164A5 cells when exposed to the tested compounds. BA2 and BA3 exhibited the highest LDH release, indicating their strong cytotoxicity. The NR assay revealed dose-dependent lysosome disruption for BI and 2,3-indolo-betulinic acid derivatives, with BA1, BA2, and BA3 showing the most cytotoxic effects. Scratch assays demonstrated concentration-dependent inhibition of cell migration, with BA2 and BA3 being the most effective. Hoechst 3342 staining revealed that BA2 induced apoptosis, while BA3 induced necrosis at lower concentrations, confirming their anti-melanoma properties. In conclusion, the semisynthetic derivatives of BI, particularly BA2 and BA3, show promise as potential candidates for further research in developing effective anti-cancer therapies. Full article
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Review

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25 pages, 3012 KiB  
Review
Bioactive Compounds in Moringa oleifera: Mechanisms of Action, Focus on Their Anti-Inflammatory Properties
by Adina Chiș, Paul Aimé Noubissi, Oana-Lelia Pop, Carmen Ioana Mureșan, Michel Archange Fokam Tagne, René Kamgang, Adriana Fodor, Adela-Viviana Sitar-Tăut, Angela Cozma, Olga Hilda Orășan, Simona Codruța Hegheș, Romana Vulturar and Ramona Suharoschi
Plants 2024, 13(1), 20; https://doi.org/10.3390/plants13010020 (registering DOI) - 20 Dec 2023
Cited by 1 | Viewed by 1863
Abstract
Moringa oleifera (M. oleifera) is a tropical tree native to Pakistan, India, Bangladesh, and Afghanistan; it is cultivated for its nutritious leaves, pods, and seeds. This scientific study was conducted to outline the anti-inflammatory properties and mechanisms of action of bioactive [...] Read more.
Moringa oleifera (M. oleifera) is a tropical tree native to Pakistan, India, Bangladesh, and Afghanistan; it is cultivated for its nutritious leaves, pods, and seeds. This scientific study was conducted to outline the anti-inflammatory properties and mechanisms of action of bioactive compounds from M. oleifera. The existing research has found that the plant is used in traditional medicine due to its bioactive compounds, including phytochemicals: flavonoids and polyphenols. The compounds are thought to exert their anti-inflammatory effects due to: (1) inhibition of pro-inflammatory enzymes: quercetin and kaempferol inhibit the pro-inflammatory enzymes (cyclooxygenase and lipoxygenase); (2) regulation of cytokine production: isothiocyanates modulate signaling pathways involved in inflammation, such as the nuclear factor-kappa B (NF-kappa B) pathway; isothiocyanates inhibit the production of pro-inflammatory cytokines such as TNF-α (tumor necrosis factor α) and IL-1β (interleukin-1β); and (3) antioxidant activity: M. oleifera contains flavonoids, polyphenols, known to reduce oxidative stress and inflammation. The review includes M. oleifera’s effects on cardiovascular protection, anti-hypertensive activities, type 2 diabetes, inflammatory bowel disease, and non-alcoholic fatty liver disease (NAFLD). This research could prove valuable for exploring the pharmacological potential of M. oleifera and contributing to the prospects of developing effective medicines for the benefit of human health. Full article
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