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150th Anniversary of the Creation of the Faculty of Pharmacy...
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150th Anniversary of the Creation of the Faculty of Pharmacy of Nancy, Université de Lorraine, France

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

Deadline for manuscript submissions: closed (31 December 2023) | Viewed by 12955

Special Issue Editors

Prof. Dr. Raphaël E. Duval

E-Mail Website
Guest Editor
Dean, Faculty of Pharmacy, Université de Lorraine, CNRS, L2CM, 54000 Nancy, France
Interests: research of new anti-infectives; development of new strategies to fight antimicrobial resistance
Special Issues, Collections and Topics in MDPI journals
Dr. Julien Perrin

E-Mail Website
Guest Editor
Vice-Dean of the Faculty of Pharmacy, Université de Lorraine, UMR_S 1116 INSERM, DCAC, F-54000 Nancy, France
Interests: hemostasis; thrombin generation test; sepsis; red blood cells and related disorders; diagnosis
Dr. Caroline Gaucher

E-Mail Website
Guest Editor
President of the Research Council, Faculty of Pharmacy, Université de Lorraine, CITHEFOR, F-54000 Nancy, France
Interests: NO donors; oxidative stress; nitro redox signalling; vascular pharmacology; vascular physiopathology

Special Issue Information

Dear Colleagues,

On October 1, 1872, following the transfer of the “Ecole Supérieure de Pharmacie de Strasbourg”, the “Ecole Supérieure de Pharmacie de Nancy” was created. This Special Issue therefore aims to mark the 150th anniversary of the creation of the “Ecole Supérieure de Pharmacie de Nancy” (which will become a Faculty in 1920).

This Special Issue may include original research, review as well as comment articles on research works that have been carried out at the “Faculté de Pharmacie de Nancy” during its 150 years.

Prof. Dr. Raphaël E. Duval
Dr. Julien Perrin
Dr. Caroline Gaucher
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.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 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

  • analytical chemistry: methods/assays development, alcohol dosage, nanoparticles
  • nanotechnology/vectorization: calixarenes, cyclodextrins, macrocycles, eudragit
  • physiology/pharmacology: regulation of major functions by nitric oxide, renin angiotensin system
  • microbiology: antimicrobial resistance, antibiotics, viruses and environment, biofilms
  • hematology: hemoglobin substitutes, hemostasis
  • theoretical chemistry: molecular modeling, theoretical calculations
  • hearing care professional, hearing aids
  • oncology: PTEN inhibitors, tumor markers, nanoparticles, peptidomimetics
  • pharmacognosy/botany: oxidative stress and plants, antioxidants
  • immunotherapy
  • biomaterials
  • nutrition: vitamins

Published Papers (7 papers)

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Research

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17 pages, 4938 KiB  
Article
Increased Range of Catalytic Activities of Immobilized Compared to Colloidal Gold Nanoparticles
by Célia Boukoufi, Ariane Boudier and Igor Clarot
Molecules 2023, 28(22), 7558; https://doi.org/10.3390/molecules28227558 - 13 Nov 2023
Viewed by 901
Abstract
Gold nanoparticles (AuNPs) can be described as nanozymes, species that are able to mimic the catalytic activities of several enzymes, such as oxidase/peroxidase, reductase, or catalase. Most studies in the literature focus on the colloidal suspension of AuNPs, and it is obvious that [...] Read more.
Gold nanoparticles (AuNPs) can be described as nanozymes, species that are able to mimic the catalytic activities of several enzymes, such as oxidase/peroxidase, reductase, or catalase. Most studies in the literature focus on the colloidal suspension of AuNPs, and it is obvious that their immobilization could open the doors to new applications thanks to their increased stability in this state. This work aimed to investigate the behavior of surfaces covered by immobilized AuNPs (iAuNPs). Citrate-stabilized AuNPs (AuNPs-cit) were synthesized and immobilized on glass slides using a simple dip coating method. The resulting iAuNPs were characterized (surface plasmon resonance, microscopy, quantification of immobilized AuNPs), and their multi-enzymatic-like activities (oxidase-, peroxidase-, and catalase-like activity) were evaluated. The comparison of their activities versus AuNPs-cit highlighted their added value, especially the preservation of their activity in some reaction media, and their ease of reuse. The huge potential of iAuNPs for heterogeneous catalysis was then applied to the degradation of two model molecules of hospital pollutants: metronidazole and methylene blue. Full article
(This article belongs to the Special Issue 150th Anniversary of the Creation of the Faculty of Pharmacy of Nancy, Université de Lorraine, France)
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28 pages, 2783 KiB  
Article
Screening of Anti-Inflammatory Activity and Metabolomics Analysis of Endophytic Fungal Extracts; Identification and Characterization of Perylenequinones and Terpenoids from the Interesting Active Alternaria Endophyte
by Rosella Spina, Armelle Ropars, Sihem Bouazzi, Safa Dadi, Pascal Lemiere, François Dupire, Afra Khiralla, Sakina Yagi, Jean-Pol Frippiat and Dominique Laurain-Mattar
Molecules 2023, 28(18), 6531; https://doi.org/10.3390/molecules28186531 - 9 Sep 2023
Viewed by 1496
Abstract
Patients suffering from inflammatory chronic diseases are classically treated with anti-inflammatory drugs but unfortunately are highly susceptible to becoming resistant to their treatment. Finding new drugs is therefore crucial and urgent and research on endophytic fungi is a promising way forward. Endophytic fungi [...] Read more.
Patients suffering from inflammatory chronic diseases are classically treated with anti-inflammatory drugs but unfortunately are highly susceptible to becoming resistant to their treatment. Finding new drugs is therefore crucial and urgent and research on endophytic fungi is a promising way forward. Endophytic fungi are microorganisms that colonize healthy plants and live within their intercellular tissues. They are able to produce a large variety of secondary metabolites while allowing their host to stay healthy. A number of these molecules are endowed with antioxidant or antimicrobial as well as cytotoxic properties, making them very interesting/promising in the field of human therapy. The aim of our study was to investigate whether extracts from five endophytic fungi isolated from plants are endowed with anti-inflammatory activity. Extracts of the endophytic fungi Alternaria alternata from Calotropis procera leaves and Aspergillus terreus from Trigonella foenum-graecum seeds were able to counteract the lipopolysaccharide (LPS) pro-inflammatory effect on THP-1 cells differentiated into macrophages. Moreover, they were able to induce an anti-inflammatory state, rendering them less sensitive to the LPS pro-inflammatory stimulus. Taken together, these results show that these both endophytic fungi could be interesting alternatives to conventional anti-inflammatory drugs. To gain more detailed knowledge of their chemical richness, phytochemical analysis of the ethyl acetate extracts of the five endophytic fungi studied was performed using HPTLC, GC-MS and LC-MS with the Global Natural Products Social (GNPS) platform and the MolNetEnhancer tool. A large family of metabolites (carboxylic acids and derivatives, steroid derivatives, alkaloids, hydroxyanthraquinones, valerolactones and perylenequinones) were detected. The purification of endophytic fungus extract of Alternaria alternate, which diminished TNF-α production of 66% at 20 µg/mL, incubated one hour before LPS addition, led to the characterization of eight pure compounds. These molecules are altertoxins I, II, III, tricycloalternarenes 3a, 1b, 2b, anthranilic acid, and o-acetamidobenzoic acid. In the future, all these pure compounds will be evaluated for their anti-inflammatory activity, while altertoxin II has been shown in the literature as the most active mycotoxin in terms of anti-inflammatory activity. Full article
(This article belongs to the Special Issue 150th Anniversary of the Creation of the Faculty of Pharmacy of Nancy, Université de Lorraine, France)
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20 pages, 2918 KiB  
Article
Characterization of Biological Properties of Individual Phenolamides and Phenolamide-Enriched Leaf Tomato Extracts
by Marwa Roumani, Armelle Ropars, Christophe Robin, Raphaël E. Duval, Jean-Pol Frippiat, Michel Boisbrun and Romain Larbat
Molecules 2023, 28(4), 1552; https://doi.org/10.3390/molecules28041552 - 6 Feb 2023
Cited by 2 | Viewed by 1571
Abstract
Resistance to conventional treatments renders urgent the discovery of new therapeutic molecules. Plant specialized metabolites such as phenolamides, a subclass of phenolic compounds, whose accumulation in tomato plants is mediated by the biotic and abiotic environment, constitute a source of natural molecules endowed [...] Read more.
Resistance to conventional treatments renders urgent the discovery of new therapeutic molecules. Plant specialized metabolites such as phenolamides, a subclass of phenolic compounds, whose accumulation in tomato plants is mediated by the biotic and abiotic environment, constitute a source of natural molecules endowed with potential antioxidant, antimicrobial as well as anti-inflammatory properties. The aim of our study was to investigate whether three major phenolamides found in Tuta absoluta-infested tomato leaves exhibit antimicrobial, cytotoxic and/or anti-inflammatory properties. One of them, N1,N5,N14-tris(dihydrocaffeoyl)spermine, was specifically synthesized for this study. The three phenolamides showed low to moderate antibacterial activities but were able to counteract the LPS pro-inflammatory effect on THP-1 cells differentiated into macrophages. Extracts made from healthy but not T. absoluta-infested tomato leaf extracts were also able to reduce inflammation using the same cellular approach. Taken together, these results show that phenolamides from tomato leaves could be interesting alternatives to conventional drugs. Full article
(This article belongs to the Special Issue 150th Anniversary of the Creation of the Faculty of Pharmacy of Nancy, Université de Lorraine, France)
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23 pages, 4814 KiB  
Article
Succinimido–Ferrocidiphenol Complexed with Cyclodextrins Inhibits Glioblastoma Tumor Growth In Vitro and In Vivo without Noticeable Adverse Toxicity
by Feten Najlaoui, Benoit Busser, Germain Sotoing Taïwe, Pascal Pigeon, Nathalie Sturm, Diane Giovannini, Naziha Marrakchi, Ali Rhouma, Gérard Jaouen, Stéphane Gibaud and Michel De Waard
Molecules 2022, 27(14), 4651; https://doi.org/10.3390/molecules27144651 - 21 Jul 2022
Cited by 2 | Viewed by 1904
Abstract
SuccFerr (N-[4-ferrocenyl,5-5-bis (4-hydroxyphenyl)-pent-4-enyl]-succinimide) has remarkable antiproliferative effects in vitro, attributed to the formation of a stabilized quinone methide. The present article reports in vivo results for a possible preclinical study. SuccFerr is lipophilic and insoluble in water, so the development of a formulation [...] Read more.
SuccFerr (N-[4-ferrocenyl,5-5-bis (4-hydroxyphenyl)-pent-4-enyl]-succinimide) has remarkable antiproliferative effects in vitro, attributed to the formation of a stabilized quinone methide. The present article reports in vivo results for a possible preclinical study. SuccFerr is lipophilic and insoluble in water, so the development of a formulation to obviate this inconvenience was necessary. This was achieved by complexation with randomly methylated cyclodextrins (RAMEßCDs). This supramolecular water-soluble system allowed the in vivo experiments below to proceed. Application of SuccFerr on the glioblastoma cancer cell line U87 indicates that it affects the cellular cycle by inducing a blockade at G0/G1 phase, linked to apoptosis, and another one at the S phase, associated with senescence. Using healthy Fischer rats, we show that both intravenous and subcutaneous SuccFerr: RAMEßCD administration at 5 mg/kg lacks toxic effects on several organs. To reach lethality, doses higher than 200 mg/kg need to be administered. These results prompted us to perform an ectopic in vivo study at 1 mg/kg i.v. ferrocidiphenol SuccFerr using F98 cells xenografted in rats. Halting of cancer progression was observed after six days of injection, associated with an immunological defense response linked to the active principle. These results demonstrate that the properties of the selected ferrocidiphenol SuccFerr transfer successfully to in vivo conditions, leading to interesting therapeutic perspectives based on this chemistry. Full article
(This article belongs to the Special Issue 150th Anniversary of the Creation of the Faculty of Pharmacy of Nancy, Université de Lorraine, France)
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Review

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46 pages, 16647 KiB  
Review
Functionalized Calixarenes as Promising Antibacterial Drugs to Face Antimicrobial Resistance
by Maxime Mourer, Jean-Bernard Regnouf-de-Vains and Raphaël E. Duval
Molecules 2023, 28(19), 6954; https://doi.org/10.3390/molecules28196954 - 6 Oct 2023
Cited by 3 | Viewed by 1511
Abstract
Since the discovery of polyphenolic resins 150 years ago, the study of polymeric compounds named calix[n]arene has continued to progress, and those skilled in the art perfectly know now how to modulate this phenolic ring. Consequently, calix[n]arenes are now [...] Read more.
Since the discovery of polyphenolic resins 150 years ago, the study of polymeric compounds named calix[n]arene has continued to progress, and those skilled in the art perfectly know now how to modulate this phenolic ring. Consequently, calix[n]arenes are now used in a large range of applications and notably in therapeutic fields. In particular, the calix[4]arene exhibits multiple possibilities for regioselective polyfunctionalization on both of its rims and offers researchers the possibility of precisely tuning the geometry of their structures. Thus, in the crucial research of new antibacterial active ingredients, the design of calixarenes finds its place perfectly. This review provides an overview of the work carried out in this aim towards the development of intrinsically active prodrogues or metallic calixarene complexes. Out of all the work of the community, there are some excellent activities emerging that could potentially place these original structures in a very good position for the development of new active ingredients. Full article
(This article belongs to the Special Issue 150th Anniversary of the Creation of the Faculty of Pharmacy of Nancy, Université de Lorraine, France)
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31 pages, 3292 KiB  
Review
The AT1/AT2 Receptor Equilibrium Is a Cornerstone of the Regulation of the Renin Angiotensin System beyond the Cardiovascular System
by Mélissa Colin, Céline Delaitre, Sébastien Foulquier and François Dupuis
Molecules 2023, 28(14), 5481; https://doi.org/10.3390/molecules28145481 - 18 Jul 2023
Cited by 5 | Viewed by 1996
Abstract
The AT1 receptor has mainly been associated with the pathological effects of the renin-angiotensin system (RAS) (e.g., hypertension, heart and kidney diseases), and constitutes a major therapeutic target. In contrast, the AT2 receptor is presented as the protective arm of this [...] Read more.
The AT1 receptor has mainly been associated with the pathological effects of the renin-angiotensin system (RAS) (e.g., hypertension, heart and kidney diseases), and constitutes a major therapeutic target. In contrast, the AT2 receptor is presented as the protective arm of this RAS, and its targeting via specific agonists is mainly used to counteract the effects of the AT1 receptor. The discovery of a local RAS has highlighted the importance of the balance between AT1/AT2 receptors at the tissue level. Disruption of this balance is suggested to be detrimental. The fine tuning of this balance is not limited to the regulation of the level of expression of these two receptors. Other mechanisms still largely unexplored, such as S-nitrosation of the AT1 receptor, homo- and heterodimerization, and the use of AT1 receptor-biased agonists, may significantly contribute to and/or interfere with the settings of this AT1/AT2 equilibrium. This review will detail, through several examples (the brain, wound healing, and the cellular cycle), the importance of the functional balance between AT1 and AT2 receptors, and how new molecular pharmacological approaches may act on its regulation to open up new therapeutic perspectives. Full article
(This article belongs to the Special Issue 150th Anniversary of the Creation of the Faculty of Pharmacy of Nancy, Université de Lorraine, France)
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25 pages, 2958 KiB  
Review
Nature-Inspired Bioactive Compounds: A Promising Approach for Ferroptosis-Linked Human Diseases?
by Sarah El Hajj, Laetitia Canabady-Rochelle and Caroline Gaucher
Molecules 2023, 28(6), 2636; https://doi.org/10.3390/molecules28062636 - 14 Mar 2023
Cited by 7 | Viewed by 2786
Abstract
Ferroptosis is a type of cell death driven by iron overload and lipid peroxidation. It is considered a key mechanism in the development of various diseases such as atherosclerosis, Alzheimer, diabetes, cancer, and renal failure. The redox status of cells, such as the [...] Read more.
Ferroptosis is a type of cell death driven by iron overload and lipid peroxidation. It is considered a key mechanism in the development of various diseases such as atherosclerosis, Alzheimer, diabetes, cancer, and renal failure. The redox status of cells, such as the balance between intracellular oxidants (lipid peroxides, reactive oxygen species, free iron ions) and antioxidants (glutathione, glutathione Peroxidase 4), plays a major role in ferroptosis regulation and constitutes its principal biomarkers. Therefore, the induction and inhibition of ferroptosis are promising strategies for disease treatments such as cancer or neurodegenerative and cardiovascular diseases, respectively. Many drugs have been developed to exert ferroptosis-inducing and/or inhibiting reactions, such as erastin and iron-chelating compounds, respectively. In addition, many natural bioactive compounds have significantly contributed to regulating ferroptosis and ferroptosis-induced oxidative stress. Natural bioactive compounds are largely abundant in food and plants and have been for a long time, inspiring the development of various low-toxic therapeutic drugs. Currently, functional bioactive peptides are widely reported for their antioxidant properties and application in human disease treatment. The scientific evidence from biochemical and in vitro tests of these peptides strongly supports the existence of a relationship between their antioxidant properties (such as iron chelation) and ferroptosis regulation. In this review, we answer questions concerning ferroptosis milestones, its importance in physiopathology mechanisms, and its downstream regulatory mechanisms. We also address ferroptosis regulatory natural compounds as well as provide promising thoughts about bioactive peptides. Full article
(This article belongs to the Special Issue 150th Anniversary of the Creation of the Faculty of Pharmacy of Nancy, Université de Lorraine, France)
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