Natural Bioactives: Exploring Their Therapeutic Potential

A special issue of Life (ISSN 2075-1729). This special issue belongs to the section "Pharmaceutical Science".

Deadline for manuscript submissions: 29 November 2024 | Viewed by 9915

Special Issue Editor


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Guest Editor
Department of Clinical Pharmacy, Jagiellonian University, Krakow, Poland
Interests: plant-derived compounds; plant extracts; anti-cancer; anti-tumor; melanoma; anti-tyrosinase; neuropsychopharmacology; anti-inflammatory; behavioral testing; central nervous system; anxiolytic; anti-depressant; anti-psychotic
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Dear Colleagues,

Exploring therapeutic agents is a constant endeavor. Nature, a trove of biodiversity, continually offers us biologically active compounds. Time-tested natural bioactives such as artemisinin, which is isolated from the plant Artemisia annua and has for decades been a key treatment for malaria, or the Madagascar-periwinkle-derived anticancer agents vincristine and vinblastine, demonstrate nature's therapeutic potential. Today, at least 70,000 medicinal plants are known to be used worldwide, highlighting the vast potential yet to be fully explored.

During recent decades, research has been focused on exploring therapeutics for non-communicable diseases, which have become a growing and overwhelming medical problem. It has been shown in many studies that agents with antioxidant, anti-inflammatory, and cytotoxic properties (apparat from more specific activities) can be useful in the prophylaxis and/or treatment of central nervous system disorders, cancer, cardiovascular and metabolic diseases. Many phytochemicals, such as phenolic compounds (e.g., flavonoids, tannins, quinones or curcuminoids), terpenoids, steroids or alkaloids, have been found to possess complex and beneficial modes of biological action. Consequently, they have been a continuously important subject of research interest. Furthermore, the last few years have shown that infectious diseases can also be an unexpected global threat, and this time, nature-derived substances are being broadly explored as well, as herbs and microbes are known sources of antibiotic agents.

In this Special Issue, our aim is to bring together the latest discoveries and fresh insights, taking a closer look at diverse phytochemicals and compounds from plants, marine organisms, fungi, and microbes. Both original research articles and comprehensive reviews are welcomed.

For the publication of the previous edition, please see: https://www.mdpi.com/journal/life/special_issues/Natural_Anti_Tumor_Compounds

Dr. Dagmara Wróbel-Biedrawa
Guest Editor

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Keywords

  • bioactive compounds
  • medicinal plants
  • bioactive metabolites antioxidant properties
  • anti-inflammatory properties
  • antitumor properties
  • cytotoxic properties
  • antipsychotic properties
  • anxiolytic properties
  • neuroprotective properties
  • hypotensive properties
  • vasorelaxant properties
  • antimicrobial properties (antiviral, antibacterial, antifungal, and antiparasitic properties)

Published Papers (7 papers)

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Research

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24 pages, 14590 KiB  
Article
Elucidation of Anti-Obesity Mechanisms of Phenolics in Artemisiae argyi Folium (Aiye) by Integrating LC-MS, Network Pharmacology, and Molecular Docking
by Yongxiang Liu, Jinhai Luo and Baojun Xu
Life 2024, 14(6), 656; https://doi.org/10.3390/life14060656 - 22 May 2024
Viewed by 418
Abstract
The global prevalence of obesity is a pressing health issue, increasing the medical burden and posing significant health risks to humans. The side effects and complications associated with conventional medication and surgery have spurred the search for anti-obesity drugs from plant resources. Previous [...] Read more.
The global prevalence of obesity is a pressing health issue, increasing the medical burden and posing significant health risks to humans. The side effects and complications associated with conventional medication and surgery have spurred the search for anti-obesity drugs from plant resources. Previous studies have suggested that Artemisiae argyi Folium (Aiye) water extracts could inhibit pancreatic lipase activities, control body weight increase, and improve the plasma lipids profile. However, the exact components and mechanisms were not precisely understood. Therefore, this research aims to identify the chemical profile of Aiye and provide a comprehensive prediction of its anti-obesity mechanisms. The water extract of Aiye was subjected to LC-MS analysis, which identified 30 phenolics. The anti-obesity mechanisms of these phenolics were then predicted, employing network pharmacology and molecular docking. Among the 30 phenolics, 21 passed the drug-likeness screening and exhibited 486 anti-obesity targets. The enrichment analysis revealed that these phenolics may combat obesity through PI3K-Akt signaling and MAPK, prolactin, and cAMP signaling pathways. Eight phenolics and seven central targets were selected for molecular docking, and 45 out of 56 docking had a binding affinity of less than −5 kcal/mol. This research has indicated the potential therapy targets and signaling pathways of Aiye in combating obesity. Full article
(This article belongs to the Special Issue Natural Bioactives: Exploring Their Therapeutic Potential)
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21 pages, 6387 KiB  
Article
Genistein–Aspirin Combination Exerts Cytotoxic and Anti-Migratory Effects in Human Colorectal Cancer Cells
by Claudia Iftode, Stela Iurciuc, Iasmina Marcovici, Ioana Macasoi, Dorina Coricovac, Cristina Dehelean, Sorin Ursoniu, Andreea Rusu and Simona Ardelean
Life 2024, 14(5), 606; https://doi.org/10.3390/life14050606 - 9 May 2024
Cited by 1 | Viewed by 702
Abstract
Colorectal cancer (CRC) is a heterogenous pathology with high incidence and mortality rates globally, but it is also preventable so finding the most promising candidates (natural compounds or repurposed drugs) to be chemopreventive alternatives has become a topic of interest in recent years. [...] Read more.
Colorectal cancer (CRC) is a heterogenous pathology with high incidence and mortality rates globally, but it is also preventable so finding the most promising candidates (natural compounds or repurposed drugs) to be chemopreventive alternatives has become a topic of interest in recent years. The present work aims to elucidate the potential effects of a combination between genistein (GEN), an isoflavone of natural origin, and aspirin (ASA) in CRC prevention/treatment by performing an in vitro evaluation in human colorectal cancer cells (HCT-116) and an in ovo analysis using the chick embryo chorioallantoic membrane (CAM) model. Cell viability was verified by an MTT (migratory potential by scratch) assay, and the expressions of MMP-2 and MMP-9 were analyzed using RT-qPCR. Our results indicated a dose-dependent cytotoxic effect of ASA (2.5 mM) + GEN (10–75 µM) combination characterized by reduced cell viability and morphological changes (actin skeleton reorganization and nuclei deterioration), an inhibition of HCT-116 cells’ migratory potential by down-regulating MMP-2 and MMP-9 mRNA expressions, and an antiangiogenic effect by modifying the vascular network. These promising results raise the possibility of future in-depth investigations regarding the chemopreventive/therapeutical potential of ASA+GEN combination. Full article
(This article belongs to the Special Issue Natural Bioactives: Exploring Their Therapeutic Potential)
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21 pages, 11029 KiB  
Article
Comparative Evaluation of Anticancer Activity of Natural Methoxylated Flavones Xanthomicrol and Eupatilin in A375 Skin Melanoma Cells
by Antonella Rosa, Franca Piras, Federica Pollastro, Valeria Sogos, Giovanni Appendino and Mariella Nieddu
Life 2024, 14(3), 304; https://doi.org/10.3390/life14030304 - 26 Feb 2024
Cited by 1 | Viewed by 3784
Abstract
Melanoma is a skin cancer caused by the malignant transformation of melanocytes and cutaneous melanoma represents the most aggressive and deadliest type of skin cancer with an increasing incidence worldwide. The main purpose of the present research was to evaluate the anticancer effects [...] Read more.
Melanoma is a skin cancer caused by the malignant transformation of melanocytes and cutaneous melanoma represents the most aggressive and deadliest type of skin cancer with an increasing incidence worldwide. The main purpose of the present research was to evaluate the anticancer effects of the natural bioactive compounds xanthomicrol (XAN) and eupatilin (EUP) in human A375 malignant skin melanoma cells, a cell line widely used as an in vitro model of cutaneous melanoma. XAN and EUP are lipophilic methoxylated flavones with antioxidant, anti-inflammatory, and antitumor properties. The effects of XAN and EUP on cell viability, morphology, lipid profile, oxidative status, apoptosis, and mitochondrial membrane polarization were determined and compared in A375 cells. At 24 h-incubation (MTT assay), XAN significantly reduced viability at the dose range of 2.5–200 μM, while EUP showed a significant cytotoxicity from 25 μM. Moreover, both methoxylated flavones induced (at 10 and 25 μM, 24 h-incubation) marked cell morphological alterations (presence of rounded and multi-nucleated cells), signs of apoptosis (NucView 488 assay), and a noteworthy mitochondrial membrane depolarization (MitoView 633 assay), coupled to a marked lipid profile modulation, including variations in the ratio of phospholipid/cholesterol and a decrease in the oleic, palmitic, and palmitoleic acid amounts. Moreover, a remarkable time-dependent ROS generation (2′,7′-dichlorodihydrofluorescein diacetate assay) was observed during 3 h-incubation of A375 cancer cells in the presence of XAN and EUP (10 and 25 μM). Our results confirm the potential antitumor effect of natural EUP and XAN in cutaneous melanoma by the activation of multiple anticancer mechanisms. Full article
(This article belongs to the Special Issue Natural Bioactives: Exploring Their Therapeutic Potential)
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13 pages, 1353 KiB  
Article
Heteroctenus junceus Scorpion Venom Modulates the Concentration of Pro-Inflammatory Cytokines in F3II Tumor Cells
by Arianna Yglesias-Rivera, Hermis Sánchez-Rodríguez, Carmen Soto-Febles and Lianet Monzote
Life 2023, 13(12), 2287; https://doi.org/10.3390/life13122287 - 30 Nov 2023
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Abstract
The ability of Heteroctenus junceus scorpion venom to modulate the concentration of cytokines related to its antitumoral effect is unknown. F3II cells were treated with ¼ IC50, ½ IC50 and the IC50 of H. junceus scorpion venom. Tumor growth [...] Read more.
The ability of Heteroctenus junceus scorpion venom to modulate the concentration of cytokines related to its antitumoral effect is unknown. F3II cells were treated with ¼ IC50, ½ IC50 and the IC50 of H. junceus scorpion venom. Tumor growth kinetics in F3II-bearing mice were evaluated after 24 days of oral administration of venom doses. The effect of tumor lysates on F3II cell viability was evaluated by MTT assay, while cytokines present in each sample were determined by ELISA. In supernatant, H. junceus scorpion venom decreased the concentration of IL-6 (p < 0.001), IFN-γ (p < 0.001), IL-1β (p < 0.01); meanwhile IL-12 (p < 0.001) and TNF-α (p < 0.001) levels increased significantly, according to the concentration and the time of incubation. Heteroctenus junceus scorpion venom effectively inhibits in vivo tumor progression. In the sera, a significant decrease was observed in TNF-α levels (p < 0.05). In tumor lysates, IL-6 decreased significantly in the groups treated with 12.5 mg/kg (p < 0.001) and 25 mg/kg (p < 0.05). Heteroctenus junceus scorpion venom is capable of modulating other proinflammatory and protumoral cytokines involved in the inflammation associated with cancer. Full article
(This article belongs to the Special Issue Natural Bioactives: Exploring Their Therapeutic Potential)
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12 pages, 2718 KiB  
Article
Protective Effect of Urtica dioica Extract against Oxidative Stress in Human Skin Fibroblasts
by Agnieszka Skalska-Kamińska, Weronika Wójciak, Magdalena Żuk, Roman Paduch and Magdalena Wójciak
Life 2023, 13(11), 2182; https://doi.org/10.3390/life13112182 - 9 Nov 2023
Cited by 2 | Viewed by 997
Abstract
Urtica dioica is a species with well-established significance in folk medicine in many countries. It was utilized to support the treatment of arthritis, allergies, and urinary tract disorders; however, the substantial presence of antioxidants suggests that nettle extract could also have a positive [...] Read more.
Urtica dioica is a species with well-established significance in folk medicine in many countries. It was utilized to support the treatment of arthritis, allergies, and urinary tract disorders; however, the substantial presence of antioxidants suggests that nettle extract could also have a positive impact on the skin. The objective of this study was to assess the impact of nettle extract on human skin fibroblasts subjected to oxidative stress. Various solvents were tested to prepare an extract rich in polyphenolic compounds with high antioxidant potential. The chemical composition was determined using ultra-high-performance liquid chromatography with mass spectrometry (UPLC-DAD-MS). H2O2 treatment was used to induce oxidative stress and cell viability, and the metabolism was evaluated through NR and MTT assays. Our study demonstrated that extraction with 80% ethanol, followed by the drying and re-dissolving of the extract in pure water, was more efficient than direct extraction with water. This yielded an extract rich in polyphenolic compounds, with chlorogenic acid and caffeoylmalic acid as the predominant compounds, averaging 64.9 and 114.4 µg/mL, respectively. The extract exhibited antioxidant properties in the DPPH and ABTS assays. Furthermore, it did not exhibit cytotoxicity and did not negatively affect cell metabolism. In addition, it effectively reduced ROS in the H2O2-stimulated cells, and at the highest concentration tested, the ROS levels returned to those of the untreated control. The extract also protected against H2O2-induced cytotoxicity. The cell viability was maintained at the level of the untreated control when the cells were pretreated with the extract before H2O2 exposure. These findings indicate that U. dioica extract is a valuable and safe additive in skincare products. Full article
(This article belongs to the Special Issue Natural Bioactives: Exploring Their Therapeutic Potential)
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18 pages, 583 KiB  
Article
Screening of Phytochemical, Antimicrobial, and Antioxidant Properties of Juncus acutus from Northeastern Morocco
by Yousra Hammouti, Amine Elbouzidi, Mohamed Taibi, Reda Bellaouchi, El Hassania Loukili, Mohamed Bouhrim, Omar M. Noman, Ramzi A. Mothana, Mansour N. Ibrahim, Abdeslam Asehraou, Bouchra El Guerrouj and Mohamed Addi
Life 2023, 13(11), 2135; https://doi.org/10.3390/life13112135 - 29 Oct 2023
Cited by 1 | Viewed by 1471
Abstract
Juncus acutus, acknowledged through its indigenous nomenclature “samar”, is part of the Juncaceae taxonomic lineage, bearing considerable import as a botanical reservoir harboring conceivable therapeutic attributes. Its historical precedence in traditional curative methodologies for the alleviation of infections and inflammatory conditions is [...] Read more.
Juncus acutus, acknowledged through its indigenous nomenclature “samar”, is part of the Juncaceae taxonomic lineage, bearing considerable import as a botanical reservoir harboring conceivable therapeutic attributes. Its historical precedence in traditional curative methodologies for the alleviation of infections and inflammatory conditions is notable. In the purview of Eastern traditional medicine, Juncus species seeds find application for their remedial efficacy in addressing diarrhea, while the botanical fruits are subjected to infusion processes targeting the attenuation of symptoms associated with cold manifestations. The primary objective of this study was to unravel the phytochemical composition of distinct constituents within J. acutus, specifically leaves (JALE) and roots (JARE), originating from the indigenous expanse of the Nador region in northeastern Morocco. The extraction of plant constituents was executed utilizing an ethanol-based extraction protocol. The subsequent elucidation of chemical constituents embedded within the extracts was accomplished employing analytical techniques based on high-performance liquid chromatography (HPLC). For the purpose of in vitro antioxidant evaluation, a dual approach was adopted, encompassing the radical scavenging technique employing 2,2-diphenyl-1-picrylhydrazyl (DPPH) and the total antioxidant capacity (TAC) assay. The acquired empirical data showcase substantial radical scavenging efficacy and pronounced relative antioxidant activity. Specifically, the DPPH and TAC methods yielded values of 483.45 ± 4.07 µg/mL and 54.59 ± 2.44 µg of ascorbic acid (AA)/mL, respectively, for the leaf extracts. Correspondingly, the root extracts demonstrated values of 297.03 ± 43.3 µg/mL and 65.615 ± 0.54 µg of AA/mL for the DPPH and TAC methods. In the realm of antimicrobial evaluation, the assessment of effects was undertaken through the agar well diffusion technique. The minimum inhibitory concentration, minimum bactericidal concentration, and minimum fungicidal concentration were determined for each extract. The inhibitory influence of the ethanol extracts was observed across bacterial strains including Staphylococcus aureus, Micrococcus luteus, and Pseudomonas aeruginosa, with the notable exception of Escherichia coli. However, fungal strains such as Candida glabrata and Rhodotorula glutinis exhibited comparatively lower resistance, whereas Aspergillus niger and Penicillium digitatum exhibited heightened resistance, evincing negligible antifungal activity. An anticipatory computational assessment of pharmacokinetic parameters was conducted, complemented by the application of the Pro-tox II web tool to delineate the potential toxicity profile of compounds intrinsic to the studied extracts. The culmination of these endeavors underpins the conceivable prospects of the investigated extracts as promising candidates for oral medicinal applications. Full article
(This article belongs to the Special Issue Natural Bioactives: Exploring Their Therapeutic Potential)
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18 pages, 1665 KiB  
Review
Beneficial Effect of Olive Oil and Its Derivates: Focus on Hematological Neoplasm
by Chiara Campo, Sebastiano Gangemi, Giovanni Pioggia and Alessandro Allegra
Life 2024, 14(5), 583; https://doi.org/10.3390/life14050583 - 30 Apr 2024
Viewed by 608
Abstract
Olive oil (Olea europaea) is one of the major components of the Mediterranean diet and is composed of a greater percentage of monounsaturated fatty acids, such as oleic acid; polyunsaturated fatty acids, such as linoleic acid; and minor compounds, such as [...] Read more.
Olive oil (Olea europaea) is one of the major components of the Mediterranean diet and is composed of a greater percentage of monounsaturated fatty acids, such as oleic acid; polyunsaturated fatty acids, such as linoleic acid; and minor compounds, such as phenolic compounds, and particularly hydroxytyrosol. The latter, in fact, are of greater interest since they have found widespread use in popular medicine. In recent years, it has been documented that phenolic acids and in particular hydroxytyrosol have anti-inflammatory, antioxidant, and antiproliferative action and therefore interest in their possible use in clinical practice and in particular in neoplasms, both solid and hematological, has arisen. This work aims to summarize and analyze the studies present in the literature, both in vitro and in vivo, on the possible use of minor components of olive oil in some hematological neoplasms. In recent years, in fact, interest in nutraceutical science has expanded as a possible adjuvant in the treatment of neoplastic pathologies. Although it is worth underlining that, regarding the object of our study, there are still few preclinical and clinical studies, it is, however, possible to document a role of possible interest in clinical practice. Full article
(This article belongs to the Special Issue Natural Bioactives: Exploring Their Therapeutic Potential)
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