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Pharmaceuticals
Special Issues
Bioactive Peptides from Natural Sources: Current Applications and Future Directions
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Bioactive Peptides from Natural Sources: Current Applications and Future Directions

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: closed (15 September 2024) | Viewed by 3494

Special Issue Editors

Dr. Daniel Dias Rufino Arcanjo

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Guest Editor
AFMOL–Laboratory of Functional and Molecular Studies in Physiopharmacology, Department of Biophysics and Physiology, Federal University of Piauí, Teresina 64049-550, Brazil
Interests: bioactive peptides; cardiovascular; diabetes; dyslipidemia; endothelium; hypertension; medicinal plants; natural products; pharmacology; preclinical toxicology; vasorelaxant
Special Issues, Collections and Topics in MDPI journals
Dr. José Roberto Souza Almeida Leite

E-Mail Website
Guest Editor
Research Center in Applied Morphology and Immunology (NuPMIA), Faculty of Medicine (FM), University of Brasília (UnB), Brasília 70910-900, DF, Brazil
Interests: biotechnology; bionanotechnology; bioprospection; biomolecules; health and environment
Special Issues, Collections and Topics in MDPI journals
Dr. Alexandra Plácido

E-Mail Website
Guest Editor
LAQV/REQUIMTE, Department of Chemistry and Biochemistry, Faculty of Sciences, University of Porto, 4169-007 Porto, Portugal
Interests: secondary metabolites; natural antioxidants; in vitro, in vivo, and in silico models; structure–activity relationship; natural product chemistry; oxidative stress and antioxidant defense; free-radical-mediated chain reactions; extraction and separation methods; antioxidant ingredients and biomaterials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Venomous animals are considered specialized predators which have developed the most sophisticated apparatus regarding chemistry and pharmacology of bioactive peptides, able to produce a wide range of toxins with incredible structural and functional diversity and directed against a variety of pharmacological targets and with potential therapeutic applications.

For example, studies on the molecular characterization of toxins from Bothrops jararaca snake venom resulted in the discovery of bradykinin and bradykinin-potentiating peptides (BPPs), recognized as the first natural inhibitors of angiotensin I-converting enzyme (ACE) and a model for the development of captopril, the first ACE inhibitor and the first commercially available drug for the treatment of arterial hypertension. In this sense, several peptides obtained from venoms of amphibians, snakes, scorpions, and spiders have been reported in the literature as important bioactive compounds with important pharmacological effects and potential therapeutic applications.

The aim of this Special Issue is to report the current advances in bioactive peptides from natural sources. Research areas of interest include, but are not limited to, the following: discovery and characterization of novel bioactive peptides, including pharmacological studies and the development of bioproducts. We are inviting the submission of original research articles or reviews that relate to the above topics.

Dr. Daniel Dias Rufino Arcanjo
Prof. Dr. José Roberto Souza Almeida Leite
Dr. Alexandra Plácido
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. Pharmaceuticals is an international peer-reviewed open access monthly 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 2900 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

  • bioactivity
  • synthesis
  • pharmacology
  • toxicology
  • immunogenicity
  • snake venom
  • scorpion venom
  • skin secretion
  • nanoparticles
  • bioassays

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Published Papers (3 papers)

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24 pages, 4759 KiB  
Article
TnP and AHR-CYP1A1 Signaling Crosstalk in an Injury-Induced Zebrafish Inflammation Model
by Geonildo Rodrigo Disner, Thales Alves de Melo Fernandes, Milton Yutaka Nishiyama-Jr, Carla Lima, Emma Wincent and Monica Lopes-Ferreira
Pharmaceuticals 2024, 17(9), 1155; https://doi.org/10.3390/ph17091155 - 31 Aug 2024
Viewed by 980
Abstract
Aryl Hydrocarbon Receptor (AHR) signaling is crucial for regulating the biotransformation of xenobiotics and physiological processes like inflammation and immunity. Meanwhile, Thalassophryne nattereri Peptide (TnP), a promising anti-inflammatory candidate from toadfish venom, demonstrates therapeutic effects through immunomodulation. However, its influence on [...] Read more.
Aryl Hydrocarbon Receptor (AHR) signaling is crucial for regulating the biotransformation of xenobiotics and physiological processes like inflammation and immunity. Meanwhile, Thalassophryne nattereri Peptide (TnP), a promising anti-inflammatory candidate from toadfish venom, demonstrates therapeutic effects through immunomodulation. However, its influence on AHR signaling remains unexplored. This study aimed to elucidate TnP’s molecular mechanisms on the AHR–cytochrome P450, family 1 (CYP1) pathway upon injury-induced inflammation in wild-type (WT) and Ahr2-knockdown (KD) zebrafish larvae through transcriptomic analysis and Cyp1a reporters. TnP, while unable to directly activate AHR, potentiated AHR activation by the high-affinity ligand 6-Formylindolo [3,2-b]carbazole (FICZ), implying a role as a CYP1A inhibitor, confirmed by in vitro studies. This interplay suggests TnP’s ability to modulate the AHR-CYP1 complex, prompting investigations into its influence on biotransformation pathways and injury-induced inflammation. Here, the inflammation model alone resulted in a significant response on the transcriptome, with most differentially expressed genes (DEGs) being upregulated across the groups. Ahr2-KD resulted in an overall greater number of DEGs, as did treatment with the higher dose of TnP in both WT and KD embryos. Genes related to oxidative stress and inflammatory response were the most apparent under inflamed conditions for both WT and KD groups, e.g., Tnfrsf1a, Irf1b, and Mmp9. TnP, specifically, induces the expression of Hspa5, Hsp90aa1.2, Cxcr3.3, and Mpeg1.2. Overall, this study suggests an interplay between TnP and the AHR-CYP1 pathway, stressing the inflammatory modulation through AHR-dependent mechanisms. Altogether, these results may offer new avenues in novel therapeutic strategies, such as based on natural bioactive molecules, harnessing AHR modulation for targeted and sustained drug effects in inflammatory conditions. Full article
(This article belongs to the Special Issue Bioactive Peptides from Natural Sources: Current Applications and Future Directions)
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20 pages, 5747 KiB  
Article
Bioactive Properties of Venoms Isolated from Whiptail Stingrays and the Search for Molecular Mechanisms and Targets
by Craig A. Doupnik, Carl A. Luer, Catherine J. Walsh, Jessica Restivo and Jacqueline Xinlan Brick
Pharmaceuticals 2024, 17(4), 488; https://doi.org/10.3390/ph17040488 - 11 Apr 2024
Viewed by 1288
Abstract
The venom-containing barb attached to their ‘whip-like’ tail provides stingrays a defensive mechanism for evading predators such as sharks. From human encounters, dermal stingray envenomation is characterized by intense pain often followed by tissue necrosis occurring over several days to weeks. The bioactive [...] Read more.
The venom-containing barb attached to their ‘whip-like’ tail provides stingrays a defensive mechanism for evading predators such as sharks. From human encounters, dermal stingray envenomation is characterized by intense pain often followed by tissue necrosis occurring over several days to weeks. The bioactive components in stingray venoms (SRVs) and their molecular targets and mechanisms that mediate these complex responses are not well understood. Given the utility of venom-derived proteins from other venomous species for biomedical and pharmaceutical applications, we set out to characterize the bioactivity of SRV extracts from three local species that belong to the Dasyatoidea ‘whiptail’ superfamily. Multiple cell-based assays were used to quantify and compare the in vitro effects of these SRVs on different cell lines. All three SRVs demonstrated concentration-dependent growth-inhibitory effects on three different human cell lines tested. In contrast, a mouse fibrosarcoma cell line was markedly resistant to all three SRVs, indicating the molecular target(s) for mediating the SRV effects are not expressed on these cells. The multifunctional SRV responses were characterized by an acute disruption of cell adhesion leading to apoptosis. These findings aim to guide future investigations of individual SRV proteins and their molecular targets for potential use in biomedical applications. Full article
(This article belongs to the Special Issue Bioactive Peptides from Natural Sources: Current Applications and Future Directions)
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11 pages, 1584 KiB  
Brief Report
Ultrasound-Assisted Solid-Phase Affibody Synthesis Using ZEGFR:1907 as an Example—Superior to the Conventional Protocol?
by Marie Prochiner, Benedikt Judmann, Alina Ruder, Björn Wängler, Ralf Schirrmacher and Carmen Wängler
Pharmaceuticals 2024, 17(10), 1280; https://doi.org/10.3390/ph17101280 - 27 Sep 2024
Viewed by 597
Abstract
Background: Affibody molecules represent a class of highly specific binders of particular interest for the development of highly affine target-specific radiopharmaceuticals. Their chemical synthesis is, however, intricate due to their considerable length of 58 amino acids; thus, approaches to optimize their preparation are [...] Read more.
Background: Affibody molecules represent a class of highly specific binders of particular interest for the development of highly affine target-specific radiopharmaceuticals. Their chemical synthesis is, however, intricate due to their considerable length of 58 amino acids; thus, approaches to optimize their preparation are constantly being sought. Methods: As ultrasound assistance has recently been shown to increase the efficiency of amino acid conjugation during solid-phase peptide synthesis (SPPS), the influence of ultrasonication on the outcome of the SPPS-based preparation of the EGFR-specific affibody ZEGFR:1907 was compared to a common protocol relying on mechanical shaking. Results: After the identification of a suitable solid support for the study, the execution of the systematic comparison of both approaches showed that conventional and ultrasound-assisted syntheses yielded equivalent results with analogous composition of the raw products. Further, both approaches produced the affibody in good isolated yields of >20% when applying the same optimal reagent excesses and coupling times for the conjugation of each amino acid. This indicates that, under optimal reaction conditions, the choice of solid support used has a much stronger influence on the outcome of the preparation of ZEGFR:1907 than the application of ultrasound, which did not further improve the synthesis results. Conclusions: Therefore, for the chemical synthesis of affibodies, great attention should be paid to the choice of a suitable solid support, enabling this highly interesting class of biomolecules to be obtained in good yields and to bring them more into the focus of radiopharmaceutical research. Full article
(This article belongs to the Special Issue Bioactive Peptides from Natural Sources: Current Applications and Future Directions)
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