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氟化分子与纳米技术:对抗阿尔茨海默病的未来“复仇者”?

Fluorinated Molecules and Nanotechnology: Future 'Avengers' against the Alzheimer's Disease?

机构信息

LEPABE, Department of Chemical Engineering, Faculty of Engineering of the University of Porto, s/n, R. Dr. Roberto Frias, 4200-465 Porto, Portugal.

出版信息

Int J Mol Sci. 2020 Apr 23;21(8):2989. doi: 10.3390/ijms21082989.


DOI:10.3390/ijms21082989
PMID:32340267
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7216102/
Abstract

Alzheimer's disease (AD) is a serious health concern, affecting millions of people globally, which leads to cognitive impairment, dementia, and inevitable death. There is still no medically accepted treatment for AD. Developing therapeutic treatments for AD is an overwhelming challenge in the medicinal field, as the exact mechanics underlying its devastating symptoms is still not completely understood. Rather than the unknown mechanism of the disease, one of the limiting factors in developing new drugs for AD is the blood-brain barrier (BBB). A combination of nanotechnology with fluorinated molecules is proposed as a promising therapeutic treatment to meet the desired pharmacokinetic/physiochemical properties for crossing the BBB passage. This paper reviews the research conducted on fluorine-containing compounds and fluorinated nanoparticles (NPs) that have been designed and tested for the inhibition of amyloid-beta (Aβ) peptide aggregation. Additionally, this study summarizes fluorinated molecules and NPs as promising agents and further future work is encouraged to be effective for the treatment of AD.

摘要

阿尔茨海默病(AD)是一个严重的健康问题,影响着全球数百万人,导致认知障碍、痴呆和不可避免的死亡。目前还没有医学上公认的 AD 治疗方法。开发 AD 的治疗方法是医学领域的一个巨大挑战,因为其破坏性症状的确切机制仍不完全清楚。对于开发治疗 AD 的新药来说,除了未知的疾病机制,一个限制因素是血脑屏障(BBB)。将纳米技术与含氟分子结合,被提议作为一种有前途的治疗方法,以满足穿过 BBB 所需的药代动力学/物理化学特性。本文综述了对含氟化合物和氟化物纳米粒子(NPs)的研究,这些化合物和氟化物纳米粒子已被设计和测试用于抑制淀粉样β(Aβ)肽聚集。此外,本研究总结了氟化物分子和 NPs 作为有前途的药物,并鼓励进一步开展工作,以有效治疗 AD。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a76/7216102/ee8515d6c14e/ijms-21-02989-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a76/7216102/7c7985d78d3a/ijms-21-02989-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a76/7216102/36083f63a0b5/ijms-21-02989-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a76/7216102/ee8515d6c14e/ijms-21-02989-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a76/7216102/7c7985d78d3a/ijms-21-02989-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a76/7216102/36083f63a0b5/ijms-21-02989-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a76/7216102/ee8515d6c14e/ijms-21-02989-g003.jpg

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Fluorinated Molecules and Nanotechnology: Future 'Avengers' against the Alzheimer's Disease?

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[2]
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[3]
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引用本文的文献

[1]
Exploring the Benzazoles Derivatives as Pharmacophores for AChE, BACE1, and as Anti-Aβ Aggregation to Find Multitarget Compounds against Alzheimer's Disease.

Molecules. 2024-10-9

[2]
Fluorine-modified polymers reduce the adsorption of immune-reactive proteins to PEGylated gold nanoparticles.

Nanomedicine (Lond). 2024

[3]
The Role of Small Molecules Containing Fluorine Atoms in Medicine and Imaging Applications.

Pharmaceuticals (Basel). 2024-2-22

[4]
Monofluoromethylation of -Heterocyclic Compounds.

Int J Mol Sci. 2023-12-18

[5]
On the Question of Zwitterionic Intermediates in the [3 + 2] Cycloaddition Reactions between C-arylnitrones and Perfluoro 2-Methylpent-2-ene.

Molecules. 2021-11-25

[6]
Perfluorocarbons in Chemical Biology.

Chembiochem. 2020-12-11

本文引用的文献

[1]
Fluorinated beta-sheet breaker peptides.

J Mater Chem B. 2014-4-28

[2]
Recent progress in the strategic incorporation of fluorine into medicinally active compounds.

J Fluor Chem. 2019-1

[3]
The Dark Side of Fluorine.

ACS Med Chem Lett. 2019-6-20

[4]
Fluorine-Containing Drugs Approved by the FDA in 2018.

Chemistry. 2019-7-8

[5]
Natural Compounds for Alzheimer's Disease Therapy: A Systematic Review of Preclinical and Clinical Studies.

Int J Mol Sci. 2019-5-10

[6]
BACE-1 and γ-Secretase as Therapeutic Targets for Alzheimer's Disease.

Pharmaceuticals (Basel). 2019-3-19

[7]
New evolutions in the BACE1 inhibitor field from 2014 to 2018.

Bioorg Med Chem Lett. 2019-1-4

[8]
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.

J Med Chem. 2018-8-8

[9]
Memantine loaded PLGA PEGylated nanoparticles for Alzheimer's disease: in vitro and in vivo characterization.

J Nanobiotechnology. 2018-3-27

[10]
Diastereoselective synthesis of fused cyclopropyl-3-amino-2,4-oxazine β-amyloid cleaving enzyme (BACE) inhibitors and their biological evaluation.

Bioorg Med Chem Lett. 2018-4-1

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