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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2023
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my-usm-ep.603722024-04-12T08:35:38Z Synthesis Of Blood-Brain Barrier Permeable Aurones As Modulators Of Microglia 2023-03 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 http://eprints.usm.my/60372/ http://eprints.usm.my/60372/1/Pages%20from%20CHIA%20SHI%20YI%20-%20TESIS.pdf application/pdf en public masters Universiti Sains Malaysia Pusat Pengajian Sains Farmasi (School of Pharmacy) |
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Universiti Sains Malaysia |
| collection |
USM Institutional Repository |
| language |
English |
| topic |
RS1-441 Pharmacy and materia medica |
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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 |
| qualification_level |
Master's degree |
| 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 |
| granting_institution |
Universiti Sains Malaysia |
| granting_department |
Pusat Pengajian Sains Farmasi (School of Pharmacy) |
| publishDate |
2023 |
| url |
http://eprints.usm.my/60372/1/Pages%20from%20CHIA%20SHI%20YI%20-%20TESIS.pdf |
| _version_ |
1804888924389113856 |