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Boron-based hybrids...
Boron-based hybrids as novel scaffolds for the development of drugs with neuroprotective properties
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Cacciatore, I. (författare)
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Turkez, H. (författare)
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Di Rienzo, A. (författare)
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Ciulla, M. (författare)
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- Mardinoglu, Adil (författare)
- KTH,Science for Life Laboratory, SciLifeLab,Systembiologi,Centre for Host-Microbiome Interactions, Dental Institute, King's College London, London SE1 9RT, UK
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Di Stefano, A. (författare)
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(creator_code:org_t)
- 2021
- 2021
- Engelska.
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Ingår i: RSC Medicinal Chemistry. - : Royal Society of Chemistry (RSC). - 2632-8682. ; 12:11, s. 1944-1949
- Relaterad länk:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- Novel boron-based compounds (BBCs) were synthesized and evaluated as potential candidates for the development of novel drugs against Alzheimer's disease (AD). The neuroprotective profile of novel BBCs was evaluated using Aβ1-42-treated-SH-SY5Y cells while their antioxidant activity was evaluated by total antioxidant capacity (TAC) and total oxidative status (TOS) assays. Results showed that BLA (a novel boron-based hybrid containing an antioxidant portion) inhibited cell death induced by Aβ1-42-exposure in differentiated SH-SY5Y cells, resulting in an increase in cell viability by 25-33% (MTT assay) and by 63-71% (LDH assay) in a concentration range of 25-100 μM. Antioxidant assays demonstrated a good capability of BLA to counteract the oxidative status. Moreover, BLA possessed a significant ability to inhibit acetylcholinesterase (AChE) (22.96% at 50 μM), an enzyme whose enzymatic activity is increased in AD patients. In the present work, absorption and distribution properties of boron-based hybrids were predicted using Pre-ADMET software. In vitro preliminary results suggested that boron-based hybrids could be new structural scaffolds for the development of novel drugs for the management of AD.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Pediatrik (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Pediatrics (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Gastroenterologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Gastroenterology and Hepatology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Cell- och molekylärbiologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Cell and Molecular Biology (hsv//eng)
Nyckelord
- acetylcholinesterase
- amyloid beta protein[1-42]
- boron derivative
- Alzheimer disease
- antioxidant activity
- Article
- cell differentiation
- cell protection
- computer model
- concentration response
- controlled study
- drug structure
- drug synthesis
- enzyme activity
- enzyme inhibition
- human
- human cell
- in vitro study
- MTT assay
- neuroprotection
- SH-SY5Y cell line
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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