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Bioactive Compounds from Plants with Pharmaceutical Interest II

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

Deadline for manuscript submissions: closed (31 July 2024) | Viewed by 13570

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Prof. Dr. Neda Mimica-Dukić

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Guest Editor

Biochemistry and Environmental Protection, Department of Chemistry, University of Novi Sad, Trg Dositeja Obradovića 3, 21000 Novi Sad, Serbia
Interests: chemotaxonomy; volatile compounds; antioxidant activity; anti-inflammatory; plant phenolics
Special Issues, Collections and Topics in MDPI journals

Prof. Dr. Maja Karaman

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Department of Biology and Ecology, Faculty of Sciences, University of Novi Sad, 21000 Novi Sad, Serbia
Interests: microbiology; mycology; biodiversity; environment; biochemistry; biotechnology; bioactive compounds of medicinal mushrooms; lignicolous macrofungi; bioactivity of fungal metabolites; fungal based biomaterials
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Special Issue Information

Dear Colleagues,

According to the WHO, 65–80% of the world’s population in developing countries uses plants for primary healthcare. Nearly 30% of all prescriptions issued in the EU and USA contain herbs, extracts, or active compounds derived from herbs. In the case of anticancer and antimicrobial drugs, nearly 80% are of natural origin or contain an active component whose structure is inspired by some natural products. Numerous studies have revealed antioxidant and anti-inflammatory activity of natural plant products that could be related to their protective role in human immune response and the development of various chronic diseases. Although a great number of natural bioactive products have already been isolated and investigated, this is still less than 10% of the plant medical treasury. Nature is still an endless source of medical drugs that are waiting to be discovered.

This Special Issue aims at providing the state of the art in the field of bioactive secondary plant products of special pharmaceutical interest and to bring together contemporary research of the chemical, biological, and pharmacological properties of natural plant products. Special emphasis is given to the mechanism of action, structure–activity relationships (SAR), bioavailability and efficacy, novel improved herbal drug formulation, etc. We expect that combined, submitted articles will give a realistic assessment of the value of natural plant products to future pharmaceutical discovery.

Prof. Dr. Neda Mimica-Dukić
Dr. Maja Karaman
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. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

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Keywords

herbal drugs
flavonoids
alkaloids
volatile substances
anti-inflammatory
antioxidant
anticancer activity
bioavailability
drug delivery system

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Related Special Issue

Bioactive Compounds from Plants with Pharmaceutical Interest in Molecules (8 articles)

Published Papers (5 papers)

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Research

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14 pages, 3374 KiB

Open AccessArticle

Determination of Bioactive Compound Kynurenic Acid in Linum usitatissimum L.

by Magdalena Wróbel-Kwiatkowska, Waldemar Turski, Grażyna Silska, Magdalena Rakicka-Pustułka, Lucyna Dymińska and Waldemar Rymowicz

Molecules 2024, 29(8), 1702; https://doi.org/10.3390/molecules29081702 - 9 Apr 2024

Cited by 1 | Viewed by 1569

Abstract

Kynurenic acid (KYNA) is a bioactive compound exhibiting multiple actions and positive effects on human health due to its antioxidant, anti-inflammatory and neuroprotective properties. KYNA has been found to have a beneficial effect on wound healing and the prevention of scarring. Despite notable progress in the research focused on KYNA observed during the last 10 years, KYNA’s presence in flax (Linum usitatissimum L.) has not been proven to date. In the present study, parts of flax plants were analysed for KYNA synthesis. Moreover, eight different cultivars of flax seeds were tested for the presence of KYNA, resulting in a maximum of 0.432 µg/g FW in the seeds of the cultivar Jan. The level of KYNA was also tested in the stems and roots of two selected flax cultivars: an oily cultivar (Linola) and a fibrous cultivar (Nike). The exposure of plants to the KYNA precursors tryptophan and kynurenine resulted in higher levels of KYNA accumulation in flax shoots and roots. Thus, the obtained results indicate that KYNA might be synthesized in flax. The highest amount of KYNA (295.9 µg/g dry weight [DW]) was detected in flax roots derived from plants grown in tissue cultures supplemented with tryptophan. A spectroscopic analysis of KYNA was performed using the FTIR/ATR method. It was found that, in tested samples, the characteristic KYNA vibration bands overlap with the bands corresponding to the vibrations of biopolymers (especially pectin and cellulose) present in flax plants and fibres. Full article

(This article belongs to the Special Issue Bioactive Compounds from Plants with Pharmaceutical Interest II)

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17 pages, 3068 KiB

Open AccessArticle

Thymus Vulgaris Oil Nanoemulsion: Synthesis, Characterization, Antimicrobial and Anticancer Activities

by Ahmed S. Doghish, Amr M. Shehabeldine, Hesham A. El-Mahdy, Mahmoud M. H. Hassanin, Abdulaziz A. Al-Askar, Samy A. Marey, Hamada AbdElgawad and Amr H. Hashem

Molecules 2023, 28(19), 6910; https://doi.org/10.3390/molecules28196910 - 2 Oct 2023

Cited by 22 | Viewed by 2580

Abstract

Essential oil nanoemulsions have received much attention due to their biological activities. Thus, a thyme essential oil nanoemulsion (Th-nanoemulsion) was prepared using a safe and eco-friendly method. DLS and TEM were used to characterize the prepared Th-nanoemulsion. Our findings showed that the nanoemulsion was spherical and ranged in size from 20 to 55.2 nm. The micro-broth dilution experiment was used to evaluate the in vitro antibacterial activity of a Th-emulsion and the Th-nanoemulsion. The MIC50 values of the thymol nanoemulsion were 62.5 mg/mL against Escherichia coli and Klebsiella oxytoca, 250 mg/mL against Bacillus cereus, and 125 mg/mL against Staphylococcus aureus. Meanwhile, it emerged that the MIC50 values of thymol against four strains were not detected. Moreover, the Th-nanoemulsion exhibited promising antifungal activity toward A. brasiliensis and A. fumigatus, where inhibition zones and MIC50 were 20.5 ± 1.32 and 26.4 ± 1.34 mm, and 12.5 and 6.25 mg/mL, respectively. On the other hand, the Th-nanoemulsion displayed weak antifungal activity toward C. albicans where the inhibition zone was 12.0 ± 0.90 and MIC was 50 mg/mL. Also, the Th-emulsion exhibited antifungal activity, but lower than that of the Th-nanoemulsion, toward all the tested fungal strains, where MIC was in the range of 12.5–50 mg/mL. The in vitro anticancer effects of Taxol, Th-emulsion, and Th-nanoemulsion were evaluated using the standard MTT method against breast cancer (MCF-7) and hepatocellular carcinoma (HepG2). Additionally, the concentration of VEGFR-2 was measured, and the activities of caspase-8 (casp-8) and caspase-9 (casp-9) were evaluated. The cytotoxic effect was the most potent against the MCF-7 breast cancer cell line after the Th-nanoemulsion treatment (20.1 ± 0.85 µg/mL), and was 125.1 ± 5.29 µg/mL after the Th-emulsion treatment. The lowest half-maximal inhibitory concentration (IC50) value, 20.1 ± 0.85 µg/mL, was achieved when the MCF-7 cell line was treated with the Th-nanoemulsion. In addition, Th-nanoemulsion treatments on MCF-7 cells led to the highest elevations in casp-8 and casp-9 activities (0.66 ± 0.042 ng/mL and 17.8 ± 0.39 pg/mL, respectively) compared to those with Th-emulsion treatments. In comparison to that with the Th-emulsion (0.982 0.017 ng/mL), the VEGFR-2 concentration was lower with the Th-nanoemulsion treatment (0.672 ± 0.019ng/mL). In conclusion, the Th-nanoemulsion was successfully prepared and appeared in nanoform with a spherical shape according to DLS and TEM, and also exhibited antibacterial, antifungal, as well as anticancer activities. Full article

(This article belongs to the Special Issue Bioactive Compounds from Plants with Pharmaceutical Interest II)

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14 pages, 1086 KiB

Open AccessArticle

Biological Activity of Genus Hypericum Sect. Hypericum Species—H. tetrapterum, H. maculatum subsp. immaculatum, H. triquetrifolium

by Nebojša Kladar, Biljana Božin, Katarina Bijelić, Mirjana Bogavac, Maja Karaman, Branislava Srđenović Čonić, Milica Rat and Goran Anačkov

Molecules 2023, 28(17), 6218; https://doi.org/10.3390/molecules28176218 - 24 Aug 2023

Cited by 4 | Viewed by 1446

Abstract

St. John’s wort (Hypericum perforatum, Hypericaceae) has long been used in traditional medicine as a potent remedy, while many other species of this genus have not been thoroughly investigated. The study aimed to detect the biological activity, including antioxidant, antihyperglycemic, anticholinergic, antimicrobial and monoaminoxidase inhibitory potential, of water-alcoholic extracts of three species autochthonous for Serbia and Greece from plant genus Hypericum (section Hypericum—H. tetrapterum, H. maculatum ssp. immaculatum and H. triquetrifolium), followed by phytochemical profiling. The highest amount of phenolics was recorded in H. maculatum subsp. immaculatum extract, while the highest abundance of flavonoids was characteristic of H. tetrapterum extract. Hypericin and hyperforin, quercetin, and its flavonoid, rutin, were present in all of the evaluated species. The evaluated species were good scavengers of DPPH, OH and NO radicals, as well as potent reducers of ferric ions in FRAP assay. Furthermore, the evaluated species were shown as potent inhibitors of monoaminoxidase A and α-glucosidase and modest inhibitors of acetylcholinesterase, monoaminoxidase B and α-amylase. No anti-Candida activity was recorded, but the extracts were effective against MRSA Staphylococcus aureus and Enterococcus sp., as well as against Proteus mirabilis. The obtained results strongly highlight the need for further in vivo studies in order to better define the potential of the medicinal application of the studied species. Full article

(This article belongs to the Special Issue Bioactive Compounds from Plants with Pharmaceutical Interest II)

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16 pages, 3850 KiB

Open AccessArticle

Antimicrobial, Antibiofilm, and Anticancer Activities of Syzygium aromaticum Essential Oil Nanoemulsion

by Amr M. Shehabeldine, Ahmed S. Doghish, Walaa A. El-Dakroury, Mahmoud M. H. Hassanin, Abdulaziz A. Al-Askar, Hamada AbdElgawad and Amr H. Hashem

Molecules 2023, 28(15), 5812; https://doi.org/10.3390/molecules28155812 - 1 Aug 2023

Cited by 38 | Viewed by 5079 | Correction

Abstract

In the current study, clove oil nanoemulsion (CL-nanoemulsion) and emulsion (CL-emulsion) were prepared through an ecofriendly method. The prepared CL-nanoemulsion and CL-emulsion were characterized using dynamic light scattering (DLS) and a transmission electron microscope (TEM), where results illustrated that CL-nanoemulsion droplets were approximately 32.67 nm in size and spherical in shape, while CL-nanoemulsion droplets were approximately 225.8 nm with a spherical shape. The antibacterial activity of CL-nanoemulsion and CL-emulsion was carried out using a microbroth dilution method. Results revealed that the preferred CL-nanoemulsion had minimal MIC values between 0.31 and 5 mg/mL. The antibiofilm efficacy of CL-nanoemulsion against S. aureus significantly decreased the development of biofilm compared with CL-emulsion. Furthermore, results illustrated that CL-nanoemulsion showed antifungal activity significantly higher than CL-emulsion. Moreover, the prepared CL-nanoemulsion exhibited outstanding antifungal efficiency toward Candida albicans, Cryptococcus neoformans, Aspergillus brasiliensis, A. flavus, and A. fumigatus where MICs were 12.5, 3.12, 0.78, 1.56, and 1.56 mg/mL, respectively. Additionally, the prepared CL-nanoemulsion was analyzed for its antineoplastic effects through a modified MTT assay for evaluating apoptotic and cytotoxic effects using HepG2 and MCF-7 cell lines. MCF-7 breast cancer cells showed the lowest IC₅₀ values (3.4-fold) in CL-nanoemulsion relative to that of CL-emulsion. Thus, CL-nanoemulsion induces apoptosis in breast cancer cells by inducing caspase-8 and -9 activity and suppressing VEGFR-2. In conclusion, the prepared CL-nanoemulsion had antibacterial, antifungal, and antibiofilm as well as anticancer properties, which can be used in different biomedical applications after extensive studies in vivo. Full article

(This article belongs to the Special Issue Bioactive Compounds from Plants with Pharmaceutical Interest II)

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Review

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18 pages, 6268 KiB

Open AccessReview

Carvacrol and Thymol Hybrids: Potential Anticancer and Antibacterial Therapeutics

by Sijongesonke Peter, Namhla Sotondoshe and Blessing A. Aderibigbe

Molecules 2024, 29(10), 2277; https://doi.org/10.3390/molecules29102277 - 12 May 2024

Cited by 2 | Viewed by 2147

Abstract

Cancer is ranked among lethal diseases globally, and the increasing number of cancer cases and deaths results from limited access to effective therapeutics. The use of plant-based medicine has been gaining interest from several researchers. Carvacrol and its isomeric compound, thymol, are plant-based extracts that possess several biological activities, such as antimalarial, anticancer, antifungal, and antibacterial. However, their efficacy is compromised by their poor bioavailability. Thus, medicinal scientists have explored the synthesis of hybrid compounds containing their pharmacophores to enhance their therapeutic efficacy and improve their bioavailability. Hence, this review is a comprehensive report on hybrid compounds containing carvacrol and its isomer, thymol, with potent anticancer and antibacterial agents reported between 2020 and 2024. Furthermore, their structural activity relationship (SAR) and recommended future strategies to further enhance their therapeutic effects will be discussed. Full article

(This article belongs to the Special Issue Bioactive Compounds from Plants with Pharmaceutical Interest II)

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