Discovery of boron-containing compounds as Aβ aggregation inhibitors and antioxidants for the treatment of Alzheimer's disease

Abstract

A novel series of boron-containing compounds were designed, synthesized and evaluated as multi-target-directed ligands against Alzheimer's disease.

Ameliorative Properties of Boronic Compounds in In Vitro and In Vivo Models of Alzheimer’s Disease

“…Although we did not measure the boron levels in the TBSA-treated mice brain tissue, previous studies have shown that boron compounds can cross the blood brain barrier and penetrate the brain tissue [ 32 ] and decrease inflammatory responses [ 33 ]. Combined with previous research showing efficacy of boron compounds in the brain [ 3 , 4 , 5 , 6 , 7 ], our findings of the efficacy of TBSA in the present study strongly suggest that TBSA is sufficiently permeable to brain tissue to reduce AD pathology.…”

“…Although as a trace element, boron has yet to be established as an essential nutrient for humans, recent experimental and clinical studies suggest that it might be an important mineral for cell membrane function [ 7 ]. Because of their anti-inflammatory properties, boron compounds have been used as dietary supplements for the treatment of neuroinflammation and in neurodegeneration [ 4 ]. Boron compounds have been tested to treat a host of disorders, from arthritis to vascular dysfunction [ 13 , 22 ].…”

“…Therefore, developing new drugs for the treatment of AD is a challenging task for researchers. One area of drug development receiving renewed attention is the use of boron compounds which, because of their anti-inflammatory properties, are being proposed as potential treatments for reducing AD-induced neuroinflammation and cognitive deficits [ 3 , 4 , 5 , 6 ].…”

“…Recently, Kucukdogru and colleagues reported that boron nitride nanoparticles have neuroprotective effects in the experimental Parkinson’s disease model against MPP+-induced apoptosis [ 3 ]. Similarly, Lu and colleagues discovered a series of boron-containing compounds to be Aβ aggregation inhibitors and antioxidants for the treatment of AD [ 4 ]. In our previous study, we found evidence of the reduction of Aβ plaque-induced neurodegeneration in C. elegans overexpressed with Aβ42 after treatment with trans-2-phenylvinylboronic acid (TPVA; unpublished data).…”

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“…This important characteristic enabled the development of specic enzyme inhibitors that can be used for Alzheimer's disease and cancer treatments. [11][12][13] For instance, the peptidylboronic antineoplastic agent Bortezomib has been used in cancer treatment since 2003. 14 Phenylboronic acid (PBA) belongs to a class of organic ligands that are widely employed for molecular recognition.…”