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Active Molecules and Complexes for Neurodegenerative Prevention

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

Deadline for manuscript submissions: closed (30 April 2022) | Viewed by 4727

Special Issue Editor


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Guest Editor
Laboratoire d’Ingénierie des Biomolécules (LIBio), Université de Lorraine, 54518 Vandoeuvre CEDEX, France
Interests: nanoliposome; biomaterials; molecular transfer; vectorization; multiscale characterization
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Natural active molecules such as antioxidants are real sources of healthcare for the population, in particular for the prevention and treatment of neurodegenerative diseases including Alzheimer's. In function of the physico-chemical properties of these compounds, such as hydrophilicity or hydrophobicity, they do not have the same stability and bioavailability in certain physiological environments. The chemical or physical modification of active molecules with hydrophobic property will improve their stability and bioavailability, among other functionalities. Various strategies could be proposed to improve these properties, including click chemistry or the vectorization of active molecules. The chemical and physical modification of an active molecule can modify the functional properties of the initial compound and change its solubility in function of its new chemical structure. In addition, this modification impacts its biological efficiency.

The purpose of this Special Issue “Active Molecules and Complexes for Neurodegenerative Prevention” is to explore the potential solution to improve the physico-chemical properties of active molecules.

Prof. Dr. Elmira Arab-Tehrany
Guest Editor

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Keywords

  • natural active compound
  • conjugates
  • antioxidants
  • click chemistry
  • neurodegenerative diseases

Published Papers (2 papers)

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Research

15 pages, 3209 KiB  
Article
A Novel Cu(II)-Binding Peptide Identified by Phage Display Inhibits Cu2+-Mediated Aβ Aggregation
by Xiaoyu Zhang, Xiancheng Zhang, Manli Zhong, Pu Zhao, Chuang Guo, You Li, He Xu, Tao Wang and Huiling Gao
Int. J. Mol. Sci. 2021, 22(13), 6842; https://doi.org/10.3390/ijms22136842 - 25 Jun 2021
Cited by 12 | Viewed by 2300
Abstract
Copper (Cu) has been implicated in the progression of Alzheimer’s disease (AD), and aggregation of Cu and amyloid β peptide (Aβ) are considered key pathological features of AD. Metal chelators are considered to be potential therapeutic agents for AD because of their capacity [...] Read more.
Copper (Cu) has been implicated in the progression of Alzheimer’s disease (AD), and aggregation of Cu and amyloid β peptide (Aβ) are considered key pathological features of AD. Metal chelators are considered to be potential therapeutic agents for AD because of their capacity to reduce metal ion-induced Aβ aggregation through the regulation of metal ion distribution. Here, we used phage display technology to screen, synthesize, and evaluate a novel Cu(II)-binding peptide that specifically blocked Cu-triggered Aβ aggregation. The Cu(II)-binding peptide (S-A-Q-I-A-P-H, PCu) identified from the phage display heptapeptide library was used to explore the mechanism of PCu inhibition of Cu2+-mediated Aβ aggregation and Aβ production. In vitro experiments revealed that PCu directly inhibited Cu2+-mediated Aβ aggregation and regulated copper levels to reduce biological toxicity. Furthermore, PCu reduced the production of Aβ by inhibiting Cu2+-induced BACE1 expression and improving Cu(II)-mediated cell oxidative damage. Cell culture experiments further demonstrated that PCu had relatively low toxicity. This Cu(II)-binding peptide that we have identified using phage display technology provides a potential therapeutic approach to prevent or treat AD. Full article
(This article belongs to the Special Issue Active Molecules and Complexes for Neurodegenerative Prevention)
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13 pages, 2812 KiB  
Article
Synthesis of New Water Soluble β-Cyclodextrin@Curcumin Conjugates and In Vitro Safety Evaluation in Primary Cultures of Rat Cortical Neurons
by Amina Ben Mihoub, Samir Acherar, Céline Frochot, Catherine Malaplate, Frances T. Yen and Elmira Arab-Tehrany
Int. J. Mol. Sci. 2021, 22(6), 3255; https://doi.org/10.3390/ijms22063255 - 23 Mar 2021
Cited by 5 | Viewed by 1912
Abstract
Self-aggregation of Curcumin (Cur) in aqueous biological environment decreases its bioavailability and in vivo therapeutic efficacy, which hampers its clinical use as candidate for reducing risk of neurodegenerative diseases. Here, we focused on the design of new Cur- β-Cyclodextrin nanoconjugates to improve the [...] Read more.
Self-aggregation of Curcumin (Cur) in aqueous biological environment decreases its bioavailability and in vivo therapeutic efficacy, which hampers its clinical use as candidate for reducing risk of neurodegenerative diseases. Here, we focused on the design of new Cur- β-Cyclodextrin nanoconjugates to improve the solubility and reduce cell toxicity of Cur. In this study, we described the synthesis, structural characterization, photophysical properties and neuron cell toxicity of two new water soluble β-CD/Cur nanoconjugates as new strategy for reducing risks of neurodegenerative diseases. Cur was coupled to one or two β-CD molecules via triazole rings using CuAAC click chemistry strategy to yield β-CD@Cur and (β-CD)2@Cur nanoconjugates, respectively. The synthesized nanoconjugates were found to be able to self-assemble in aqueous condition and form nano-aggregates of an average diameter size of around 35 and 120 nm for β-CD@Cur and (β-CD)2@Cur, respectively. The photophysical properties, water solubility and cell toxicity on rat embryonic cortical neurons of the designed nanoconjugates were investigated and compared to that of Cur alone. The findings revealed that both new nanoconjugates displayed better water solubility and in vitro biocompatibility than Cur alone, thus making it possible to envisage their use as future nano-systems for the prevention or risk reduction of neurodegenerative diseases. Full article
(This article belongs to the Special Issue Active Molecules and Complexes for Neurodegenerative Prevention)
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