Synthesis and biological evaluation of deferiprone-resveratrol hybrids as antioxidants, Aβ 1–42 aggregation inhibitors and metal-chelating agents for Alzheimer's disease

Xu, Ping; Zhang, Minkui; Sheng, Rong; Ma, Yongmin

doi:10.1016/j.ejmech.2016.12.045

Cited by 79 publications

(69 citation statements)

References 33 publications

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“…5 Deferiprone is an iron chelating agent which is studied in phase 2 trials in participants with mild and prodromal AD. 4,53 A metal protein-attenuating compound, PBT2, has recently progressed in phase 2 AD treatment trials, as it demonstrated promising efficacy data in preclinical studies. 54 In a 3-month phase 2 study, PBT2 succeeded in a 13% reduction of CSF Aβ and an executive function improvement in a dose-related pattern in patients with early AD.…”

Section: Reduction Of Aβ-plaque Burden Via Drugs Interfering With Metmentioning

confidence: 99%

Current and Future Treatments in Alzheimer Disease: An Update

Yiannopoulou

Papageorgiou

2020

J Cent Nerv Syst Dis

600

378

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Disease-modifying treatment strategies for Alzheimer disease (AD) are still under extensive research. Nowadays, only symptomatic treatments exist for this disease, all trying to counterbalance the neurotransmitter disturbance: 3 cholinesterase inhibitors and memantine. To block the progression of the disease, therapeutic agents are supposed to interfere with the pathogenic steps responsible for the clinical symptoms, classically including the deposition of extracellular amyloid β plaques and intracellular neurofibrillary tangle formation. Other underlying mechanisms are targeted by neuroprotective, anti-inflammatory, growth factor promotive, metabolic efficacious agents and stem cell therapies. Recent therapies have integrated multiple new features such as novel biomarkers, new neuropsychological outcomes, enrollment of earlier populations in the course of the disease, and innovative trial designs. In the near future different specific agents for every patient might be used in a “precision medicine” context, where aberrant biomarkers accompanied with a particular pattern of neuropsychological and neuroimaging findings could determine a specific treatment regimen within a customized therapeutic framework. In this review, we discuss potential disease-modifying therapies that are currently being studied and potential individualized therapeutic frameworks that can be proved beneficial for patients with AD.

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Section: Reduction Of Aβ-plaque Burden Via Drugs Interfering With Metmentioning

confidence: 99%

Current and Future Treatments in Alzheimer Disease: An Update

Yiannopoulou

Papageorgiou

2020

J Cent Nerv Syst Dis

600

378

View full text Add to dashboard Cite

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“…Recently, resveratrol has been suggested to have neuroprotective effects against many neurological diseases (Porro et al, 2015; Abdel-Aleem et al, 2016; Ghaiad et al, 2016; Jeong et al, 2016; Shi et al, 2016; Xu et al, 2017), and several underlying mechanisms for this effect have been suggested. For example, resveratrol attenuates hypoxia-induced neurotoxicity by inhibiting microglial activation (Zhang et al, 2015), and similarly constrains amyloid-β-induced microglial activation via NOX (Yao et al, 2015).…”

Section: Pharmacological Approaches For Modulating Microglial Phenotypesmentioning

confidence: 99%

Pharmacological Modulation of Functional Phenotypes of Microglia in Neurodegenerative Diseases

Song

Suk

2017

Front. Aging Neurosci.

150

112

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Microglia are the resident innate immune cells of the central nervous system that mediate brain homeostasis maintenance. Microglia-mediated neuroinflammation is a hallmark shared by various neurodegenerative diseases, including Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis. Numerous studies have shown microglial activation phenotypes to be heterogeneous; however, these microglial phenotypes can largely be categorized as being either M1 or M2 type. Although the specific classification of M1 and M2 functionally polarized microglia remains a topic for debate, the use of functional modulators of microglial phenotypes as potential therapeutic approaches for the treatment of neurodegenerative diseases has garnered considerable attention. This review discusses M1 and M2 microglial phenotypes and their relevance in neurodegenerative disease models, as described in recent literature. The modulation of microglial polarization toward the M2 phenotype may lead to development of future therapeutic and preventive strategies for neuroinflammatory and neurodegenerative diseases. Thus, we focus on recent studies of microglial polarization modulators, with a particular emphasis on the small-molecule compounds and their intracellular target proteins.

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“…Recently, resveratrol has gained more interest to treat AD due to its greater neuroprotective effect, and many studies confirmed that resveratrol treatment significantly improved the cognition and biochemical parameters. [114][115][116][117][118][119][120][121][122][123] Recently, resveratrol-loaded SLN was studied for its bioavailability and brain delivery. Resveratrol was efficiently delivered to the brain and exhibited its potential bioactivity.…”

Section: Anti-alzheimer's Effectmentioning

confidence: 99%

Recent developments in solid lipid nanoparticle and surface-modified solid lipid nanoparticle delivery systems for oral delivery of phyto-bioactive compounds in various chronic diseases

Ganesan

Ramalingam

Karthivashan

et al. 2018

IJN

135

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Solid lipid nanoparticle (SLN) delivery systems have a wide applicability in the delivery of phyto-bioactive compounds to treat various chronic diseases, including diabetes, cancer, obesity and neurodegenerative diseases. The multiple benefits of SLN delivery include improved stability, smaller particle size, leaching prevention and enhanced lymphatic uptake of the bioactive compounds through oral delivery. However, the burst release makes the SLN delivery systems inadequate for the oral delivery of various phyto-bioactive compounds that can treat such chronic diseases. Recently, the surface-modified SLN (SMSLN) was observed to overcome this limitation for oral delivery of phyto-bioactive compounds, and there is growing evidence of an enhanced uptake of curcumin delivered orally via SMSLNs in the brain. This review focuses on different SLN and SMSLN systems that are useful for oral delivery of phyto-bioactive compounds to treat various chronic diseases.

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Synthesis and biological evaluation of deferiprone-resveratrol hybrids as antioxidants, Aβ 1–42 aggregation inhibitors and metal-chelating agents for Alzheimer's disease

Cited by 79 publications

References 33 publications

Current and Future Treatments in Alzheimer Disease: An Update

Current and Future Treatments in Alzheimer Disease: An Update

Pharmacological Modulation of Functional Phenotypes of Microglia in Neurodegenerative Diseases

Recent developments in solid lipid nanoparticle and surface-modified solid lipid nanoparticle delivery systems for oral delivery of phyto-bioactive compounds in various chronic diseases

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