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Biological Activities and Biomedical Application of Isatin and Its Analogues
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Biological Activities and Biomedical Application of Isatin and Its Analogues

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: closed (31 August 2020) | Viewed by 10638

Special Issue Editor

Prof. Dr. Alexei Medvedev

E-Mail Website
Guest Editor
Institute of Biomedical Chemistry, Moscow 119121, Russia
Interests: isatin; isatin metabolism; isatin analogues; isatin-based pharmacological agents; isatin binding proteins; neuroprotection; molecular mechanisms; ligand-receptor interaction; isatin-responsive genes; proteomics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Isatin (indol-2,3-dione), an endogenous oxidized indole found in the brain, peripheral tissues, and biological body fluids of humans and animals, exhibits a wide range of biological and pharmacological activities. They are realized via interactions with numerous biological targets. Proteomic profiling has revealed the existence of a representative group of isatin-binding proteins, including proteins involved in the development of neurodegenerative disorders. The isatin moiety is often used in the design of pharmacological agents, acting as an inhibitor of, e.g., apoptosis; anticonvulsants; and antiviral, anti-bacterial, and antitumor agents. In this context, there is a clear need for studies of mechanisms of action, regarding both isatin itself and its numerous analogues. Elucidation of the mechanisms responsible for different effects of isatin and its analogues requires the identification of particular targets, which would demonstrate susceptibility to this regulatory molecule at different levels of biological organization from the whole body to individual molecules.

This Special Issue of the International Journal of Molecular Sciences will focus on the multidisciplinary analysis of mechanisms responsible for the manifestation of biomedical (biological and pharmacological) effects of isatin and its analogues at various levels of structural organization of biological objects with a particular emphasis on their potential medical significance.

Authors are invited to submit their latest original research and reviews of recent experimental data within the scope of this Special Issue, which will cover all biomedical aspects related to both biological activities and biomedical applications of isatin and its analogues.

Prof. Dr. Alexei Medvedev
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

  • isatin
  • isatin analogues
  • molecular mechanisms
  • pharmacological activity
  • animal models
  • cell cultures
  • ligand-receptor interaction
  • genomics
  • proteomics
  • interactomics

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Published Papers (3 papers)

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Research

14 pages, 4252 KiB  
Article
Mechanism of the Affinity-Enhancing Effect of Isatin on Human Ferrochelatase and Adrenodoxin Reductase Complex Formation: Implication for Protein Interactome Regulation
by Pavel V. Ershov, Alexander V. Veselovsky, Yuri V. Mezentsev, Evgeniy O. Yablokov, Leonid A. Kaluzhskiy, Anastasiya M. Tumilovich, Anton A. Kavaleuski, Andrei A. Gilep, Taisiya V. Moskovkina, Alexei E. Medvedev and Alexis S. Ivanov
Int. J. Mol. Sci. 2020, 21(20), 7605; https://doi.org/10.3390/ijms21207605 - 14 Oct 2020
Cited by 7 | Viewed by 2170
Abstract
Isatin (indole-2, 3-dione) is a non-peptide endogenous bioregulator exhibiting a wide spectrum of biological activity, realized in the cell via interactions with numerous isatin-binding proteins, their complexes, and (sub) interactomes. There is increasing evidence that isatin may be involved in the regulation of [...] Read more.
Isatin (indole-2, 3-dione) is a non-peptide endogenous bioregulator exhibiting a wide spectrum of biological activity, realized in the cell via interactions with numerous isatin-binding proteins, their complexes, and (sub) interactomes. There is increasing evidence that isatin may be involved in the regulation of complex formations by modulating the affinity of the interacting protein partners. Recently, using Surface Plasmon Resonance (SPR) analysis, we have found that isatin in a concentration dependent manner increased interaction between two human mitochondrial proteins, ferrochelatase (FECH), and adrenodoxine reductase (ADR). In this study, we have investigated the affinity-enhancing effect of isatin on the FECH/ADR interaction. The SPR analysis has shown that FECH forms not only homodimers, but also FECH/ADR heterodimers. The affinity-enhancing effect of isatin on the FECH/ADR interaction was highly specific and was not reproduced by structural analogues of isatin. Bioinformatic analysis performed using three dimensional (3D) models of the interacting proteins and in silico molecular docking revealed the most probable mechanism involving FECH/isatin/ADR ternary complex formation. In this complex, isatin is targeted to the interface of interacting FECH and ADR monomers, forming hydrogen bonds with both FECH and ADR. This is a new regulatory mechanism by which isatin can modulate protein–protein interactions (PPI). Full article
(This article belongs to the Special Issue Biological Activities and Biomedical Application of Isatin and Its Analogues)
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38 pages, 6021 KiB  
Article
Design, Synthesis and Biological Evaluation of Biphenylglyoxamide-Based Small Molecular Antimicrobial Peptide Mimics as Antibacterial Agents
by Tsz Tin Yu, Rajesh Kuppusamy, Muhammad Yasir, Md. Musfizur Hassan, Amani Alghalayini, Satyanarayana Gadde, Evelyne Deplazes, Charles Cranfield, Mark D.P. Willcox, David StC Black and Naresh Kumar
Int. J. Mol. Sci. 2020, 21(18), 6789; https://doi.org/10.3390/ijms21186789 - 16 Sep 2020
Cited by 15 | Viewed by 4683
Abstract
There has been an increasing interest in the development of antimicrobial peptides (AMPs) and their synthetic mimics as a novel class of antibiotics to overcome the rapid emergence of antibiotic resistance. Recently, phenylglyoxamide-based small molecular AMP mimics have been identified as potential leads [...] Read more.
There has been an increasing interest in the development of antimicrobial peptides (AMPs) and their synthetic mimics as a novel class of antibiotics to overcome the rapid emergence of antibiotic resistance. Recently, phenylglyoxamide-based small molecular AMP mimics have been identified as potential leads to treat bacterial infections. In this study, a new series of biphenylglyoxamide-based small molecular AMP mimics were synthesised from the ring-opening reaction of N-sulfonylisatin bearing a biphenyl backbone with a diamine, followed by the conversion into tertiary ammonium chloride, quaternary ammonium iodide and guanidinium hydrochloride salts. Structure–activity relationship studies of the analogues identified the octanesulfonyl group as being essential for both Gram-positive and Gram-negative antibacterial activity, while the biphenyl backbone was important for Gram-negative antibacterial activity. The most potent analogue was identified to be chloro-substituted quaternary ammonium iodide salt 15c, which possesses antibacterial activity against both Gram-positive (MIC against Staphylococcus aureus = 8 μM) and Gram-negative bacteria (MIC against Escherichia coli = 16 μM, Pseudomonas aeruginosa = 63 μM) and disrupted 35% of pre-established S. aureus biofilms at 32 μM. Cytoplasmic membrane permeability and tethered bilayer lipid membranes (tBLMs) studies suggested that 15c acts as a bacterial membrane disruptor. In addition, in vitro toxicity studies showed that the potent compounds are non-toxic against human cells at therapeutic dosages. Full article
(This article belongs to the Special Issue Biological Activities and Biomedical Application of Isatin and Its Analogues)
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21 pages, 3436 KiB  
Article
A Neuroprotective Dose of Isatin Causes Multilevel Changes Involving the Brain Proteome: Prospects for Further Research
by Alexei Medvedev, Arthur Kopylov, Olga Buneeva, Leonid Kurbatov, Olga Tikhonova, Alexis Ivanov and Victor Zgoda
Int. J. Mol. Sci. 2020, 21(11), 4187; https://doi.org/10.3390/ijms21114187 - 11 Jun 2020
Cited by 20 | Viewed by 3229
Abstract
Isatin (indole-2,3-dione) is an endogenous regulator, exhibiting a wide range of biological and pharmacological activities. At doses of 100 mg/kg and above, isatin is neuroprotective in different experimental models of neurodegeneration. Good evidence exists that its effects are realized via interaction with numerous [...] Read more.
Isatin (indole-2,3-dione) is an endogenous regulator, exhibiting a wide range of biological and pharmacological activities. At doses of 100 mg/kg and above, isatin is neuroprotective in different experimental models of neurodegeneration. Good evidence exists that its effects are realized via interaction with numerous isatin-binding proteins identified in the brain and peripheral tissues studied. In this study, we investigated the effect of a single dose administration of isatin to mice (100 mg/kg, 24 h) on differentially expressed proteins and a profile of the isatin-binding proteins in brain hemispheres. Isatin administration to mice caused downregulation of 31 proteins. However, these changes cannot be attributed to altered expression of corresponding genes. Although at this time point isatin influenced the expression of more than 850 genes in brain hemispheres (including 433 upregulated and 418 downregulated genes), none of them could account for the changes in the differentially expressed proteins. Comparative proteomic analysis of brain isatin-binding proteins of control and isatin-treated mice revealed representative groups of proteins sensitive to isatin administration. Control-specific proteins (n = 55) represent specific targets that interact directly with isatin. Appearance of brain isatin-binding proteins specific to isatin-treated mice (n = 94) may be attributed to the formation of new clusters of protein–protein interactions and/or novel binding sites induced by a high concentration of this regulator (ligand-induced binding sites). Thus, isatin administration produces multiple effects in the brain, which include changes in gene expression and also profiles of isatin-binding proteins and their interactomes. Further studies are needed for deeper insight into the mechanisms of the multilevel changes in the brain proteome induced by isatin. In the context of the neuroprotective action, these changes may be aimed at interruption of pathological links that begin to form after initiation of pathological processes. Full article
(This article belongs to the Special Issue Biological Activities and Biomedical Application of Isatin and Its Analogues)
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