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Applied Sciences
Special Issues
Bioactive Compounds for the Treatment of Neurological and Neurodegenerative Disorders
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Bioactive Compounds for the Treatment of Neurological and Neurodegenerative Disorders

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

Deadline for manuscript submissions: closed (30 July 2022) | Viewed by 5216

Special Issue Editor

Prof. Dr. Hoon Kim

E-Mail Website
Guest Editor
College of Pharmacy and Research Institute of Life and Pharmaceutical Sciences, Sunchon National University, Suncheon 57922, Republic of Korea
Interests: monoamine oxidase inhibitors; acetylcholinesterase inhibitors; pharmaceutical biochemistry; cell wall lytic enzyme; laccase enzyme; rumen microbial metagenome; microorganism with host
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are inviting manuscript submissions to this Special Issue on “Bioactive Compounds for the Treatment of Neurological and Neurodegenerative Disorders”.

Depression, Alzheimer’s disease (AD), and Parkinson’s disease (PD) are recently being recognized as major neurological and neurodegenerative disorders. Many countries have focused on the development of therapeutic agents, and many studies have been reported about the molecular mechanisms of the diseases. However, only a tiny portion has been uncovered due to their complex systems. Several enzymes have been targeted, such as monoamine oxidases (MAOs; MAO-A and MAO-B), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-secretase 1 (BACE1). MAO catalyzes the oxidative deamination of neurotransmitter monoamines, and two types of isoforms of MAO (i.e., MAO-A and MAO-B) are localized in the mitochondrial outer membrane. In addition, MAO is critically related to amyloid plaque formation in AD, and MAO-B is expressed at high levels in the AD brain with secretases, and it is also related to PD. AChE hydrolyzes the neurotransmitter acetylcholine, and it is the main target in the palliative therapy of AD, being present in both central and peripheral nervous system and in muscular motor plaques. BChE is present in the brain peripheral tissues and in the serum, and is up-regulated in advanced AD. BACE1 is an aspartic acid protease, and it is the major β-secretase for the generation of amyloid-β peptides in the neurons. A number of papers have been published on MAO-A, MAO-B, AChE, BChE, and BACE1 inhibitors for their roles in these neurodegenerative disorders.

In this Special Issue, we invite eminent submissions describing recent advances in the fields of “Bioactive Compounds for the Treatment of Neurological and Neurodegenerative Disorders”. Both experimental articles and comprehensive reviews are welcome.

Prof. Dr. Hoon Kim
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

  • Bioactive compounds
  • Neurological and neurodegenerative disorders
  • Depression
  • Alzheimer’s disease
  • Parkinson’s disease
  • Monoamine oxidase
  • Cholinesterase
  • β-secretase 1
  • Inhibitors

Published Papers (2 papers)

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Research

16 pages, 2869 KiB  
Article
Synthesis of N′-(4-/3-/2-/Non-substituted benzylidene)-4-[(4-methylphenyl)sulfonyloxy] Benzohydrazides and Evaluation of Their Inhibitory Activities against Monoamine Oxidases and β-Secretase
by Hasan Erdinç Sellitepe, Jong Min Oh, İnci Selin Doğan, Sercan Yildirim, Ahmet Buğra Aksel, Geum Seok Jeong, Ahmed Khames, Mohamed A. Abdelgawad, Nicola Gambacorta, Orazio Nicolotti, Bijo Mathew and Hoon Kim
Appl. Sci. 2021, 11(13), 5830; https://doi.org/10.3390/app11135830 - 23 Jun 2021
Cited by 5 | Viewed by 1777
Abstract
Nineteen tosylated acyl hydrazone derivatives were synthesized, and their inhibitory activities against monoamine oxidases (MAOs), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-secretase (BACE-1) were evaluated. Compound 3o was the most potent inhibitor of MAO-A, with an IC50 value of 1.54 µM, followed by [...] Read more.
Nineteen tosylated acyl hydrazone derivatives were synthesized, and their inhibitory activities against monoamine oxidases (MAOs), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-secretase (BACE-1) were evaluated. Compound 3o was the most potent inhibitor of MAO-A, with an IC50 value of 1.54 µM, followed by 3a (IC50 = 3.35 µM). A structural comparison with 3a indicated that the 3-F group in 3o increased its inhibitory activity against MAO-A. Compound 3s was the most potent inhibitor of MAO-B, with an IC50 value of 3.64 µM, followed by 3t (IC50 = 5.69 µM). The MAO-B inhibitory activity increased in the order of 3- > 4- > 2-NO2 groups in 3s, 3t, and 3r, respectively. All the compounds weakly inhibited AChE and BChE, which retained >50% residual activity at 10 µM, except for 3a, which inhibited BChE with an IC50 value of 16.1 µM. Interestingly, 3e, 3f, and 3n inhibited BACE-1 with IC50 values of 8.63, 9.92, and 8.47 µM, respectively, which were lower than the IC50 of the quercetin reference. Compounds 3o and 3s were found to be reversible competitive inhibitors of MAO-A and MAO-B, respectively, with Ki values of 0.35 ± 0.074 and 1.97 ± 0.65 µM, respectively. Moreover, compounds 3e, 3f, and 3n were effective BACE-1 inhibitors. The lead molecules were further investigated by molecular docking studies to elucidate the binding interactions with the target enzymes. Full article
(This article belongs to the Special Issue Bioactive Compounds for the Treatment of Neurological and Neurodegenerative Disorders)
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12 pages, 1787 KiB  
Article
Antidepressant-Like Effects of Ethanol Extract of Ziziphus jujuba Mill Seeds in Mice
by Jong Min Oh, Moongi Ji, Mi-Jin Lee, Geum Seok Jeong, Man-Jeong Paik, Hoon Kim and Joo-Won Suh
Appl. Sci. 2020, 10(20), 7374; https://doi.org/10.3390/app10207374 - 21 Oct 2020
Cited by 7 | Viewed by 2770
Abstract
The antidepressant-like activity of ethanol extract of Ziziphus jujuba Mill var. spinosa seeds (Semen Ziziphi Spinosae, SZS) was investigated by behavioral tests, such as a forced swimming test (FST), a tail-suspension test (TST), and an open field test (OFT), using mice exposed to [...] Read more.
The antidepressant-like activity of ethanol extract of Ziziphus jujuba Mill var. spinosa seeds (Semen Ziziphi Spinosae, SZS) was investigated by behavioral tests, such as a forced swimming test (FST), a tail-suspension test (TST), and an open field test (OFT), using mice exposed to chronic unpredictable mild stress (CUMS). In the TST, immobility times of the extract-treated groups E100 and E300 (CUMS + 100 and 300 mg/kg extract, respectively) were significantly decreased in a dose-dependent manner compared with the negative control (CUMS; p < 0.01, though those of E100 and E300 were higher than those of the positive control (CUMS + 15 mg/kg fluoxetine). In the FST, immobility times of E100 and E300 were decreased compared to the normal control. In the OFT, total and zone distances of E100 and E300 were significantly higher than those of negative controls (p < 0.01) with a dose dependency. In liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis after behavioral tests, norepinephrine (NE) and 5-hydroxytryptamine (5-HT) levels in the hippocampus tissues of E100 and E300 were significantly higher than those of negative controls. Brain-derived neurotrophic factor (BDNF) levels in the hippocampus tissues of E100 and E300 were higher than those of negative controls. From these results, the SZS ethanol extract exhibited significant antidepressant-like effects via immobility decrease, distance increase, hippocampal NE and 5-HT increase, and BDNF expression. These results suggest that the extract could be a potential antidepressant agent. Full article
(This article belongs to the Special Issue Bioactive Compounds for the Treatment of Neurological and Neurodegenerative Disorders)
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