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Pharmacological Activity, Biochemical Properties, and Clinical Applications of Synthetic and Natural Compounds

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A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Applied Biosciences and Bioengineering".

Deadline for manuscript submissions: 20 June 2024 | Viewed by 4572

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Special Issue Editor

Dr. Anna Szewczyk

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Guest Editor

Department of Molecular and Cellular Biology, Faculty of Pharmacy, Wroclaw Medical University, 211A 50-556 Wroclaw, Poland
Interests: cell culture; cell line culture; cell proliferation; flow cytometry; apoptosis; cancer biology; cell signaling; western blot analysis; immunofluorescence; immunofluorescence staining

Special Issue Information

Dear Colleagues,

This issue aims to provide an extensive overview of the latest research in the field of pharmacology and drug discovery.

The articles in the Special Issue cover a wide range of topics, including the development and optimization of synthetic compounds, the isolation and characterization of natural compounds, and their mechanisms of action. We also explore the clinical applications of these compounds in the treatment of various diseases such as cancer, neurodegenerative diseases, and metabolic disorders.

As we all know, pharmacological activity, biochemical properties, and clinical applications of synthetic and natural compounds are areas of research that have gained significant interest in recent years. The presented studies within can help researchers, clinicians, and drug developers better understand the pharmacokinetics and pharmacodynamics of synthetic and natural compounds.

We hope that this Special Issue will stimulate further research and inspire exciting ideas for the development of novel therapies.

Dr. Anna Szewczyk
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. Applied Sciences 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 2400 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

pharmacokinetics
pharmacodynamics
innovative therapies
drugs
natural compounds
in vitro
in vivo
clinical trials
intracellular pathways
inhibitors

Published Papers (5 papers)

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Research

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14 pages, 1618 KiB

Open AccessArticle

Phenolic Profiles and Antitumor Activity against Colorectal Cancer Cells of Seeds from Selected Ribes Taxa

by Svetlana Lyashenko, Rosalía López-Ruiz, Ana Minerva García-Cervantes, Ignacio Rodríguez-García, Svetlana Yunusova and José Luis Guil-Guerrero

Appl. Sci. 2024, 14(6), 2428; https://doi.org/10.3390/app14062428 - 13 Mar 2024

Viewed by 452

Abstract

Seeds from several Ribes taxa were surveyed for phenolic compounds and in vitro antiproliferative activity against HT-29 colorectal cancer cells. Total phenolic compounds were analyzed through the Folin–Ciocalteu procedure, while LC coupled to a single mass spectrometer (MS) Orbitrap using an electrospray interface (ESI) was performed to determine the phenolic profiles. Antitumor effects were established using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Total phenolics ranged from 11.4 in R. alpinum to 94.8 mg of caffeic acid equivalents (CAE)/g in R. nigrum ‘Koksa’. Concerning phenolic compounds, four were hydroxylated benzoic acids, four cinnamic acid derivatives, eight flavonoids, and nine flavonoid glycosides. The growth inhibition against HT-29 cancer cells was exercised much better by R. nigrum ‘Koksa’ and Ribes ‘Erkeeni’ (GI₅₀ 37 and 42 µg/mL). All Ribes extracts, except for R. nigrum ‘Hara katarlik’, showed higher activity than R. rubrum (GI₅₀ at 72 h: 99 µg/mL). Interestingly, the extract from Ribes ‘Erkeeni’, which exhibited high bioactivity, contains all detected phenolic compounds, unlike R. nigrum ‘Koksa’, which lacks only populnin. Therefore, the high bioactivity found for such extracts could be due to a synergy of all detected compounds. This work constitutes a comprehensive action for expanding knowledge on the phenolic profiles and antitumor activity of GLA-rich Ribes seeds. Full article

(This article belongs to the Special Issue Pharmacological Activity, Biochemical Properties, and Clinical Applications of Synthetic and Natural Compounds)

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15 pages, 2249 KiB

Open AccessArticle

Adjuvant Effects of Lavandula angustifolia Oil in Experimental Carrageenan-Induced Thrombosis

by Valeriu Mihai But, Vasile Rus, Tamás Ilyés, Mădălina Luciana Gherman, Ioana Cristina Stănescu, Sorana D. Bolboacă and Adriana Elena Bulboacă

Appl. Sci. 2024, 14(5), 1852; https://doi.org/10.3390/app14051852 - 23 Feb 2024

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Abstract

Antinociceptive, sedative, anti-inflammatory, and antioxidant effects of lavender oil (LO) have been documented. The aim of our study was to evaluate the adjuvant effects of pretreatment with LO compared to standard treatment (low molecular weight heparin) in thrombosis. We evaluated the effects of two doses of LO in addition to nadroparin calcium (NC) on experimentally induced thrombosis in rats. The groups were as follows: the control (C) group received intraperitoneal (i.p.) saline and vehicle (DMSO), the thrombosis (T) group received saline plus vehicle pretreatment, nadroparin calcium (NC) was administrated subcutaneously (s.c.), TNCL1 and TNCL2 received pretreatment with LO (TNCL1—100 mg/kg body weight (b.w.) i.p. and TNCL2—200 mg/kg b.w. i.p. and NC s.c.). Thrombosis was successfully obtained in all groups, except the C group. Statistically significant differences between groups (p-values < 0.001) were found for the levels of oxidative stress biomarkers (malondialdehyde, nitric oxide, and total oxidative stress) and antioxidant parameters (total antioxidant capacity and thiols), TNF-α, MCP-1, and RANTES. Dose-dependent effects are seen on the biomarkers under evaluation, with higher LO doses producing the best outcomes. When compared to the group receiving standard treatment (NC alone), the LO pretreatment led to an increase in antioxidant levels (p-values < 0.001) and a decrease in oxidative stress and pro-inflammatory levels (p-values < 0.001). Lavender oil associated with NC treatment alleviates the inflammatory components of experimental carrageenan-induced thrombosis in rats by decreasing oxidative stress and inflammatory cytokines and improving antioxidant activity. Full article

(This article belongs to the Special Issue Pharmacological Activity, Biochemical Properties, and Clinical Applications of Synthetic and Natural Compounds)

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23 pages, 2651 KiB

Open AccessArticle

Seaweed Calliblepharis jubata and Fucus vesiculosus Pigments: Anti-Dermatophytic Activity

by Louisa Gomes, João Cotas, Chantal Fernandes, Teresa Gonçalves and Leonel Pereira

Appl. Sci. 2024, 14(4), 1456; https://doi.org/10.3390/app14041456 - 10 Feb 2024

Viewed by 1179

Abstract

Seaweeds have been explored as a natural resource of compounds of interest due to their bioactivities. Although many studies report the interest and the application of seaweeds in various areas, from food or human health to the economy, these data mostly focus on raw extracts and not on specific compounds, such as seaweed pigments. Fungal infections of the skin, nails, and hair caused by dermatophytes are the most common fungal infections worldwide. These pathologies require long periods of topical and/or systemic treatment associated with adverse effects and increased antifungal resistance. So, this study had two objectives: the first was to isolate and characterize the pigments of the seaweeds Calliblepharis jubata and Fucus vesiculosus; the second was to assess their antifungal activity. The extraction of pigments was performed using a method of extraction by exhaustion, and the purification was achieved via column chromatography. Three techniques were used to characterize the pigments: thin-layer chromatography (TLC), UV–visible spectrophotometry, and Fourier-transform infrared spectroscopy (FTIR). The antifungal activity against the three most common dermatophytes, Trichophyton rubrum, Trichophyton mentagrophytes, and Microsporum canis, was evaluated using a microdilution methodology, following the EUCAST international standards. It was possible to observe that the extracts obtained from the seaweed C. jubata, corresponding to the purified pigment phycobiliprotein, and the crude extract (an enriched extract) showed antifungal activity against the three fungal agents of human skin infection. Full article

(This article belongs to the Special Issue Pharmacological Activity, Biochemical Properties, and Clinical Applications of Synthetic and Natural Compounds)

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13 pages, 1216 KiB

Open AccessArticle

Inhalation with Vitamin D3 Metabolites—A Novel Strategy to Restore Vitamin D3 Deficiencies in Lung Tissue

by Michał Chojnacki, Jakub Anisiewicz, Ilona Leśniowska and Marta Kinga Lemieszek

Appl. Sci. 2023, 13(19), 10672; https://doi.org/10.3390/app131910672 - 25 Sep 2023

Viewed by 974

Abstract

Vitamin D3 deficiency has been recognized as a pandemic with serious health consequences including chronic respiratory diseases. Unfortunately, improvement in this situation by using vitamin D supplementation has failed. The direct delivery of 1,25(OH)₂-vitamin D3 and its precursor into the respiratory tract, by nebulization, seemed to be a better option, as verified in the presented study. To induce vitamin D deficiency, mice received a diet with 0.05 IU/g cholecalciferol, while control animals were given feed with 0.5 IU/g cholecalciferol. Vitamin-D-deficient mice were exposed to different doses of calcidiol or calcitriol via nebulization for at least 7 days. At the end of the experiment, whole-body plethysmography was conducted. Pulmonary and serum levels of calcitriol were examined using ELISA. The calcitriol concentrations in mice on standard vs. deficient diet were 30.31/18.20 pg/mg (lungs) and 132.24/98.61 pg/mL (serum), respectively. Restoration of the physiological level of calcitriol in vitamin-D-deficient mice required 1-week exposure to 100 pg/g of calcidiol or 5 pg/g of calcitriol. The inhalations did not cause any side changes in murine respiratory function. The presented study revealed the usefulness and safety of chronic inhalation with a bioactive form of vitamin D3 or its precursor for the restoration of physiological calcitriol levels in animals with vitamin D deficiencies. Full article

(This article belongs to the Special Issue Pharmacological Activity, Biochemical Properties, and Clinical Applications of Synthetic and Natural Compounds)

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Review

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20 pages, 4144 KiB

Open AccessReview

Flavone Hybrids and Derivatives as Bioactive Agents

by László Hazai, Bernadett Zsoldos, Mónika Halmai and Péter Keglevich

Appl. Sci. 2024, 14(3), 1039; https://doi.org/10.3390/app14031039 - 25 Jan 2024

Viewed by 613

Abstract

Hybrid molecules can be defined as chemical entities with two or more structural domains, namely pharmacophores, having a specific biological effect. In many cases, when at least one of the components is biologically inactive, it is rather correct to call them “derivatives”, despite the fact that in the literature they are often mentioned also as hybrids. We have summarized such types of molecules, in which one of the components is mostly a real pharmacophore, i.e., flavone, which is one of the best-known natural bioactive substances. Structures, synthetic methods, medicinal indications, and more important activity data are presented. Full article

(This article belongs to the Special Issue Pharmacological Activity, Biochemical Properties, and Clinical Applications of Synthetic and Natural Compounds)

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