Synthesis Of Blood-Brain Barrier Permeable Aurones As Modulators Of Microglia

In the present study, a series of aurones incorporating basic amines and lipophilic functionalities at ring A and/or ring B were synthesized to improve upon present sulfuretin activity towards targeting brain microglia while overcoming the blood-brain barrier. The effects of the synthesized aurones...

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Main Author: Chia, Shi Yi
Format: Thesis
Language:English
Published: 2023
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Online Access:http://eprints.usm.my/60372/1/Pages%20from%20CHIA%20SHI%20YI%20-%20TESIS.pdf
http://eprints.usm.my/60372/
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spelling my.usm.eprints.60372 http://eprints.usm.my/60372/ Synthesis Of Blood-Brain Barrier Permeable Aurones As Modulators Of Microglia Chia, Shi Yi RS1-441 Pharmacy and materia medica In the present study, a series of aurones incorporating basic amines and lipophilic functionalities at ring A and/or ring B were synthesized to improve upon present sulfuretin activity towards targeting brain microglia while overcoming the blood-brain barrier. The effects of the synthesized aurones on LPS-stimulated BV-2 microglial cells were examined and their modulation to an activated M1 phenotype and alternatively activated M2 phenotype were characterized. Also, the BBB permeability of the aurones were determined using the parallel artificial membrane permeability assay for blood-brain barrier (PAMPA-BBB) model. The results revealed that several aurones showing significant inhibitory activities against nitric oxide (NO) levels of more than 50% at 1 to 10 μM (p < 0.01 versus control). 2023-03 Thesis NonPeerReviewed application/pdf en http://eprints.usm.my/60372/1/Pages%20from%20CHIA%20SHI%20YI%20-%20TESIS.pdf Chia, Shi Yi (2023) Synthesis Of Blood-Brain Barrier Permeable Aurones As Modulators Of Microglia. Masters thesis, Universiti Sains Malaysia.
institution Universiti Sains Malaysia
building Hamzah Sendut Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Sains Malaysia
content_source USM Institutional Repository
url_provider http://eprints.usm.my/
language English
topic RS1-441 Pharmacy and materia medica
spellingShingle RS1-441 Pharmacy and materia medica
Chia, Shi Yi
Synthesis Of Blood-Brain Barrier Permeable Aurones As Modulators Of Microglia
description In the present study, a series of aurones incorporating basic amines and lipophilic functionalities at ring A and/or ring B were synthesized to improve upon present sulfuretin activity towards targeting brain microglia while overcoming the blood-brain barrier. The effects of the synthesized aurones on LPS-stimulated BV-2 microglial cells were examined and their modulation to an activated M1 phenotype and alternatively activated M2 phenotype were characterized. Also, the BBB permeability of the aurones were determined using the parallel artificial membrane permeability assay for blood-brain barrier (PAMPA-BBB) model. The results revealed that several aurones showing significant inhibitory activities against nitric oxide (NO) levels of more than 50% at 1 to 10 μM (p < 0.01 versus control).
format Thesis
author Chia, Shi Yi
author_facet Chia, Shi Yi
author_sort Chia, Shi Yi
title Synthesis Of Blood-Brain Barrier Permeable Aurones As Modulators Of Microglia
title_short Synthesis Of Blood-Brain Barrier Permeable Aurones As Modulators Of Microglia
title_full Synthesis Of Blood-Brain Barrier Permeable Aurones As Modulators Of Microglia
title_fullStr Synthesis Of Blood-Brain Barrier Permeable Aurones As Modulators Of Microglia
title_full_unstemmed Synthesis Of Blood-Brain Barrier Permeable Aurones As Modulators Of Microglia
title_sort synthesis of blood-brain barrier permeable aurones as modulators of microglia
publishDate 2023
url http://eprints.usm.my/60372/1/Pages%20from%20CHIA%20SHI%20YI%20-%20TESIS.pdf
http://eprints.usm.my/60372/
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score 13.211869