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New Research on Bioactive Natural Products
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New Research on Bioactive Natural Products

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: 20 February 2025 | Viewed by 4972

Special Issue Editor

Dr. Alexandros Tsoupras

E-Mail Website
Guest Editor
Hephaestus Laboratory, Department of Chemistry, School of Science, Democritus University of Thrace, Kavala University Campus, St Lucas, GR 65404 Kavala, Greece
Interests: inflammation; thrombosis; oxidative stress; chronic disorders; cardiovascular disoases; cancer; renal disorders; neurodegenerative disorders; persistent infections; anti-inflammatory; antithrombotic; antioxidant; cardio-protective; antitumor; antidiabetic; skin protection; anti-ageing; anti-UV protection; natural bioactives; bioactives; bioactive compounds; bioactive ingredients; valorization of by-products; phenolics; polar lipids; vitamins; functional foods; supplements; nutraceuticals; drugs; cosmetics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Chronic disorders like cardiovascular diseases (CVD), cancer, renal and neurodegenerative disorders, allergy and autoimmune diseases, persistent infections and associated manifestations, etc., are a global burden. Even though current approaches for prevention and therapy have high efficacy, they nevertheless usually come along with high costs, undesirable side effects and environmental issues. Hence, there is an increasing necessity for developing novel products containing natural bioactives, especially those derived from sustainable natural sources.

The objective of this Special Issue is to promote research in the field and outline the current status and future perspectives on the valorization of bioactives from sustainable natural sources, such as the rich-in-natural-bioactives bio-cultures of several microorganisms and/or several by-products of the agro-food sector, as well as to highlight their importance as ingredients for the design and production of high-value, bio-functional medicinal products, including supplements, nutraceuticals and drugs, with promising health-promoting effects, against the aforementioned inflammation-related chronic disorders. Emphasis will be given to work with state-of-the-art methods of isolation and molecular analysis applied to several natural sources for obtaining/extracting and fractionating such natural micro-/macro-bioactives from the prime extracts/mixtures/filtrates/isolates/etc. derived from a sustainable natural source, as well as to the OMICS-based full chemical characterization and structural elucidation, in tandem with designed and tailored bioassays and in vitro/ex vivo/in vivo approaches, in order to evaluate structure–activity relationships and potential synergism(s) against specific bio-molecular pathways and cell/tissue/organ biological responses, which is of paramount importance in assessing structure–activity and causality, and will provide the molecular evidence for the utilization of the most optimum bio-functional natural bioactives or their mixtures for the production of targeted bio-functional products, based on current legislations and according to the needs of the industry and consumers.

Studies containing such targeted biomolecular experiments accompanied by appropriately designed approaches for evaluating the clinical safety and efficacy of products containing such natural bioactives, through tandem animal studies and clinical trials, are also welcomed. Special attention will be given to work on such sustainable natural bioactives with higher safety, efficacy and bioavailability–biodigestibility. Finally, relative reviews and meta-analysis articles in the field are also welcomed in this Special Issue.

Dr. Alexandros Tsoupras
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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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

  • chronic disorders
  • bioactives
  • natural sources
  • sustainable sources
  • biomolecular
  • structure–activity relationship
  • synergism
  • health promoting
  • bio-functional
  • products
  • supplements
  • nutraceuticals
  • drugs

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Published Papers (4 papers)

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Research

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17 pages, 753 KiB  
Article
German Chamomile (Matricaria chamomilla L.) Flower Extract, Its Amino Acid Preparations and 3D-Printed Dosage Forms: Phytochemical, Pharmacological, Technological, and Molecular Docking Study
by Oleh Koshovyi, Janne Sepp, Valdas Jakštas, Vaidotas Žvikas, Igor Kireyev, Yevhen Karpun, Vira Odyntsova, Jyrki Heinämäki and Ain Raal
Int. J. Mol. Sci. 2024, 25(15), 8292; https://doi.org/10.3390/ijms25158292 - 29 Jul 2024
Viewed by 1097
Abstract
German chamomile (Matricaria chamomilla L.) is an essential oil- containing medicinal plant used worldwide. The aim of this study was to gain knowledge of the phytochemical composition and the analgesic and soporific activity of Matricaria chamomilla L. (German chamomile) flower extract and [...] Read more.
German chamomile (Matricaria chamomilla L.) is an essential oil- containing medicinal plant used worldwide. The aim of this study was to gain knowledge of the phytochemical composition and the analgesic and soporific activity of Matricaria chamomilla L. (German chamomile) flower extract and its amino acid preparations, to predict the mechanisms of their effects by molecular docking and to develop aqueous printing gels and novel 3D-printed oral dosage forms for the flower extracts. In total, 22 polyphenolic compounds and 14 amino acids were identified and quantified in the M. chamomilla extracts. In vivo animal studies with rodents showed that the oral administration of such extracts revealed the potential for treating of sleep disorders and diseases accompanied by pain. Amino acids were found to potentiate these effects. Glycine enhanced the analgesic activity the most, while lysine and β-alanine improved the soporific activity. The molecular docking analysis revealed a high probability of γ-aminobutyric acid type A (GABAA) and N-methyl-D-aspartate (NMDA) receptor antagonism and 5-lipoxygenase (LOX-5) inhibition by the extracts. A polyethylene oxide (PEO)-based gel composition with the M. chamomilla extracts was proposed for preparing a novel 3D-printed dosage form for oral administration. These 3D-printed extract preparations can be used, for example, in dietary supplement applications. Full article
(This article belongs to the Special Issue New Research on Bioactive Natural Products)
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19 pages, 3584 KiB  
Article
Analysis of Active Components and Transcriptome of Freesia refracta Callus Extract and Its Effects against Oxidative Stress and Wrinkles in Skin
by Euihyun Kim, Morgane De Tollenaere, Benedicte Sennelier, Carole Lambert, Anais Durduret, Soo-Yun Kim, Hyo-Hyun Seo, Jung-Hun Lee, Amandine Scandolera, Romain Reynaud and Sang-Hyun Moh
Int. J. Mol. Sci. 2024, 25(15), 8150; https://doi.org/10.3390/ijms25158150 - 26 Jul 2024
Viewed by 805
Abstract
Freesia refracta (FR), a perennial flower of the Iris family (Iridaceae), is widely used in cosmetics despite limited scientific evidence of its skin benefits and chemical composition, particularly of FR callus extract (FCE). This study identified biologically active compounds in FCE and assessed [...] Read more.
Freesia refracta (FR), a perennial flower of the Iris family (Iridaceae), is widely used in cosmetics despite limited scientific evidence of its skin benefits and chemical composition, particularly of FR callus extract (FCE). This study identified biologically active compounds in FCE and assessed their skin benefits, focusing on anti-aging. FR calli were cultured, extracted with water at 40 °C, and analyzed using Centrifugal Partition Chromatography (CPC), Nuclear Magnetic Resonance (NMR), and HCA, revealing key compounds, namely nicotinamide and pyroglutamic acid. FCE significantly increased collagen I production by 52% in normal and aged fibroblasts and enhanced fibroblast–collagen interaction by 37%. An in vivo study of 43 female volunteers demonstrated an 11.1% reduction in skin roughness and a 2.3-fold increase in collagen density after 28 days of cream application containing 3% FCE. Additionally, the preservation tests of cosmetics containing FCE confirmed their stability over 12 weeks. These results suggest that FCE offers substantial anti-aging benefits by enhancing collagen production and fibroblast–collagen interactions. These findings highlighted the potential of FCE in cosmetic applications, providing significant improvements in skin smoothness and overall appearance. This study fills a gap in the scientific literature regarding the skin benefits and chemical composition of FR callus extract, supporting its use in the development of effective cosmeceuticals. Full article
(This article belongs to the Special Issue New Research on Bioactive Natural Products)
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19 pages, 5939 KiB  
Article
Antimicrobial Properties of Flavonoid Derivatives with Bromine, Chlorine, and Nitro Group Obtained by Chemical Synthesis and Biotransformation Studies
by Martyna Perz, Daria Szymanowska, Tomasz Janeczko and Edyta Kostrzewa-Susłow
Int. J. Mol. Sci. 2024, 25(10), 5540; https://doi.org/10.3390/ijms25105540 - 19 May 2024
Cited by 5 | Viewed by 1003
Abstract
The search for new substances of natural origin, such as flavonoids, is necessary in the fight against the growing number of diseases and bacterial resistance to antibiotics. In our research, we wanted to check the influence of flavonoids with chlorine or bromine atoms [...] Read more.
The search for new substances of natural origin, such as flavonoids, is necessary in the fight against the growing number of diseases and bacterial resistance to antibiotics. In our research, we wanted to check the influence of flavonoids with chlorine or bromine atoms and a nitro group on pathogenic and probiotic bacteria. We synthesized flavonoids using Claisen–Schmidt condensation and its modifications, and through biotransformation via entomopathogenic filamentous fungi, we obtained their glycoside derivatives. Biotransformation yielded two new flavonoid glycosides: 8-amino-6-chloroflavone 4′-O-β-D-(4″-O-methyl)-glucopyranoside and 6-bromo-8-nitroflavone 4′-O-β-D-(4″-O-methyl)-glucopyranoside. Subsequently, we checked the antimicrobial properties of the aforementioned aglycon flavonoid compounds against pathogenic and probiotic bacteria and yeast. Our studies revealed that flavones have superior inhibitory effects compared to chalcones and flavanones. Notably, 6-chloro-8-nitroflavone showed potent inhibitory activity against pathogenic bacteria. Conversely, flavanones 6-chloro-8-nitroflavanone and 6-bromo-8-nitroflavanone stimulated the growth of probiotic bacteria (Lactobacillus acidophilus and Pediococcus pentosaceus). Our research has shown that the presence of chlorine, bromine, and nitro groups has a significant effect on their antimicrobial properties. Full article
(This article belongs to the Special Issue New Research on Bioactive Natural Products)
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Review

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32 pages, 2441 KiB  
Review
A Review on Apple Pomace Bioactives for Natural Functional Food and Cosmetic Products with Therapeutic Health-Promoting Properties
by Maria Vandorou, Christos Plakidis, Ilektra Maria Tsompanidou, Theodora Adamantidi, Eirini A. Panagopoulou and Alexandros Tsoupras
Int. J. Mol. Sci. 2024, 25(19), 10856; https://doi.org/10.3390/ijms251910856 - 9 Oct 2024
Viewed by 1371
Abstract
Apples are consumed lavishly worldwide, while demand is increasing for the management of the huge apple-waste amounts that lead to significant disposal costs and ecological issues. Additionally, apples represent fruits with several bioactive constituents, which are key factors in a healthy, balanced diet. [...] Read more.
Apples are consumed lavishly worldwide, while demand is increasing for the management of the huge apple-waste amounts that lead to significant disposal costs and ecological issues. Additionally, apples represent fruits with several bioactive constituents, which are key factors in a healthy, balanced diet. In the present study, an extensive review is presented regarding the bioactive compounds of an apple processing by-product, namely apple pomace, mentioning their significance as viable ingredients/substances in foods and cosmetics aiming at chronic disease prevention and health promotion. Apple pomace contains several constituents, such as polar lipids, phenolics, vitamins and dietary fibers, with potential antioxidant, anti-inflammatory, anti-thrombotic, anti-aging and skin-protecting properties, and thus, they may contribute to minimizing the risk of various health conditions. Additionally, the mechanisms of action of such functional bioactives from apple pomace exert health benefits that will be examined, while the potential synergistic effects will also be investigated. Moreover, we will present the methods and techniques needed for the utilization of apple pomace in the appropriate form, such as powder, extracts, essential oil and so on, and their several applications in the food and cosmeceutical industry sectors, which summarize that apple pomace represents an ideal alternative to synthetic bioactive compounds. Full article
(This article belongs to the Special Issue New Research on Bioactive Natural Products)
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