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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| Format: | Thèse |
| Langue: | anglais |
| Publié: |
2023
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| Accès en ligne: | http://eprints.usm.my/60372/ |
| Abstract | Abstract here |
| _version_ | 1855633056040222720 |
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| author | Chia, Shi Yi |
| author_facet | Chia, Shi Yi |
| author_sort | Chia, Shi Yi |
| 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). |
| first_indexed | 2025-10-17T08:48:39Z |
| format | Thesis |
| id | usm-60372 |
| institution | Universiti Sains Malaysia |
| language | English |
| last_indexed | 2025-10-17T08:48:39Z |
| publishDate | 2023 |
| record_format | EPrints |
| record_pdf | Restricted |
| spelling | usm-603722024-04-12T08:35:38Z 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. |
| spellingShingle | RS1-441 Pharmacy and materia medica Chia, Shi Yi Synthesis Of Blood-Brain Barrier Permeable Aurones As Modulators Of Microglia |
| thesis_level | Master |
| title | 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_short | Synthesis Of Blood-Brain Barrier Permeable Aurones As Modulators Of Microglia |
| title_sort | synthesis of blood brain barrier permeable aurones as modulators of microglia |
| topic | RS1-441 Pharmacy and materia medica |
| url | http://eprints.usm.my/60372/ |
| work_keys_str_mv | AT chiashiyi synthesisofbloodbrainbarrierpermeableauronesasmodulatorsofmicroglia |