Discovery of alkenylboronic acids as neuroprotective agents affecting multiple biological targets involved in Alzheimer's disease

Karim Jiménez-Aligaga; Paloma Bermejo-Bescós; Sagrario Martín-Aragón; Aurelio G. Csákÿ

doi:10.1016/j.bmcl.2012.11.068

Discovery of alkenylboronic acids as neuroprotective agents affecting multiple biological targets involved in Alzheimer's disease

Karim Jiménez-Aligaga, Paloma Bermejo-Bescós, Sagrario Martín-Aragón, Aurelio G. Csákÿ

Research output: Contribution to journal › Article › peer-review

14 Scopus citations

Abstract

Alkenylboronic acids have shown important biological activities that contribute to neuroprotection. We have determined their influence on the β-amyloid (βA) aggregation process, β-secretase and acethylcholinesterase activities on cell-free systems, on the redox and lipid peroxidation status, and on the vulnerability to apoptotic death in an APPswe neuroblastoma cell line, before and after hydrogen peroxide treatment. We have discovered that 2-arylvinylboronic acids and some of their esters possess a set of properties which makes them highly useful as neuroprotective agents affecting multiple biological targets involved in AD. These properties are not paralleled by the related 2-arylboronic acids.

Original language	English
Pages (from-to)	426-429
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	23
Issue number	2
DOIs	https://doi.org/10.1016/j.bmcl.2012.11.068
State	Published - 15 Jan 2013
Externally published	Yes

Bibliographical note

Funding Information:
This work was supported by grant CTQ2010-6170 from the Ministerio de Economía y Competitividad from the government of Spain. We thank Fundación Folch for a pre-doctoral grant to K. J.-A.

Keywords

Boronic acids
Caspase
Glutathione
Lipid peroxidation
β-Amyloid fibrillogenesis

Access to Document

10.1016/j.bmcl.2012.11.068

Cite this

@article{fc371810707f4bae829fcaf81e4201bc,

title = "Discovery of alkenylboronic acids as neuroprotective agents affecting multiple biological targets involved in Alzheimer's disease",

abstract = "Alkenylboronic acids have shown important biological activities that contribute to neuroprotection. We have determined their influence on the β-amyloid (βA) aggregation process, β-secretase and acethylcholinesterase activities on cell-free systems, on the redox and lipid peroxidation status, and on the vulnerability to apoptotic death in an APPswe neuroblastoma cell line, before and after hydrogen peroxide treatment. We have discovered that 2-arylvinylboronic acids and some of their esters possess a set of properties which makes them highly useful as neuroprotective agents affecting multiple biological targets involved in AD. These properties are not paralleled by the related 2-arylboronic acids.",

keywords = "Boronic acids, Caspase, Glutathione, Lipid peroxidation, β-Amyloid fibrillogenesis",

author = "Karim Jim{\'e}nez-Aligaga and Paloma Bermejo-Besc{\'o}s and Sagrario Mart{\'i}n-Arag{\'o}n and Cs{\'a}k{\"y}, {Aurelio G.}",

note = "Funding Information: This work was supported by grant CTQ2010-6170 from the Ministerio de Econom{\'i}a y Competitividad from the government of Spain. We thank Fundaci{\'o}n Folch for a pre-doctoral grant to K. J.-A. ",

year = "2013",

month = jan,

day = "15",

doi = "10.1016/j.bmcl.2012.11.068",

language = "Ingl{\'e}s",

volume = "23",

pages = "426--429",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

number = "2",

}

Discovery of alkenylboronic acids as neuroprotective agents affecting multiple biological targets involved in Alzheimer's disease. / Jiménez-Aligaga, Karim; Bermejo-Bescós, Paloma; Martín-Aragón, Sagrario et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 23, No. 2, 15.01.2013, p. 426-429.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - Discovery of alkenylboronic acids as neuroprotective agents affecting multiple biological targets involved in Alzheimer's disease

AU - Jiménez-Aligaga, Karim

AU - Bermejo-Bescós, Paloma

AU - Martín-Aragón, Sagrario

AU - Csákÿ, Aurelio G.

N1 - Funding Information: This work was supported by grant CTQ2010-6170 from the Ministerio de Economía y Competitividad from the government of Spain. We thank Fundación Folch for a pre-doctoral grant to K. J.-A.

PY - 2013/1/15

Y1 - 2013/1/15

N2 - Alkenylboronic acids have shown important biological activities that contribute to neuroprotection. We have determined their influence on the β-amyloid (βA) aggregation process, β-secretase and acethylcholinesterase activities on cell-free systems, on the redox and lipid peroxidation status, and on the vulnerability to apoptotic death in an APPswe neuroblastoma cell line, before and after hydrogen peroxide treatment. We have discovered that 2-arylvinylboronic acids and some of their esters possess a set of properties which makes them highly useful as neuroprotective agents affecting multiple biological targets involved in AD. These properties are not paralleled by the related 2-arylboronic acids.

AB - Alkenylboronic acids have shown important biological activities that contribute to neuroprotection. We have determined their influence on the β-amyloid (βA) aggregation process, β-secretase and acethylcholinesterase activities on cell-free systems, on the redox and lipid peroxidation status, and on the vulnerability to apoptotic death in an APPswe neuroblastoma cell line, before and after hydrogen peroxide treatment. We have discovered that 2-arylvinylboronic acids and some of their esters possess a set of properties which makes them highly useful as neuroprotective agents affecting multiple biological targets involved in AD. These properties are not paralleled by the related 2-arylboronic acids.

KW - Boronic acids

KW - Caspase

KW - Glutathione

KW - Lipid peroxidation

KW - β-Amyloid fibrillogenesis

UR - http://www.scopus.com/inward/record.url?scp=84871712446&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2012.11.068

DO - 10.1016/j.bmcl.2012.11.068

M3 - Artículo

C2 - 23219701

AN - SCOPUS:84871712446

SN - 0960-894X

VL - 23

SP - 426

EP - 429

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 2

ER -

Discovery of alkenylboronic acids as neuroprotective agents affecting multiple biological targets involved in Alzheimer's disease

Abstract

Bibliographical note

Keywords

Access to Document

Other files and links

Fingerprint

Cite this