Extended Chalcones: Synthesis, In Vitro Analysis, and In Vivo Testing Against a <i>Drosophila melanogaster</i> Alzheimer’s Disease Model
Alzheimer’s Disease (AD) is the most common form of dementia in individuals over the age of 65. There is no known prevention for the progression of the disease, although the FDA recently approved two drugs for AD. The exact etiology of AD is still under debate; however, it is commonly associated wit...
Saved in:
| Main Authors: | , , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2024-11-01
|
| Series: | Chemistry |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2624-8549/6/6/89 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1850241511864664064 |
|---|---|
| author | Aadya Jaipuria Madison Castillo James Boksanski Greg Landry Ji Hyung Beak Michelle Young David T. Priefer Kaïs Guessab Crystal N. Ellis Ronny Priefer |
| author_facet | Aadya Jaipuria Madison Castillo James Boksanski Greg Landry Ji Hyung Beak Michelle Young David T. Priefer Kaïs Guessab Crystal N. Ellis Ronny Priefer |
| author_sort | Aadya Jaipuria |
| collection | DOAJ |
| description | Alzheimer’s Disease (AD) is the most common form of dementia in individuals over the age of 65. There is no known prevention for the progression of the disease, although the FDA recently approved two drugs for AD. The exact etiology of AD is still under debate; however, it is commonly associated with the aggregation of amyloid-beta (Aβ) plaques in the brain. Recently some extended chalcones were reported to be potential anti-amyloidogenic agents. In this study, a larger library of extended chalcone analogs were synthesized with modifications on both rings. These were tested using the Thioflavin T fluorescence assay to measure their anti-Aβ aggregation properties. Three notably active compounds were further evaluated for potential neurotoxicity and neuroprotection using an MTT cell viability assay. These compounds were non-neurotoxic and displayed a trend toward neuroprotection. These were further assessed in a <i>Drosophila melanogaster</i> animal AD model. A forced climbing assay revealed statistically significant changes in flies’ movement by ~30% when fed these anti-amyloidogenic agents. |
| format | Article |
| id | doaj-art-45cbbdaf4d1646839ba1243a3e32c211 |
| institution | OA Journals |
| issn | 2624-8549 |
| language | English |
| publishDate | 2024-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Chemistry |
| spelling | doaj-art-45cbbdaf4d1646839ba1243a3e32c2112025-08-20T02:00:35ZengMDPI AGChemistry2624-85492024-11-01661477149410.3390/chemistry6060089Extended Chalcones: Synthesis, In Vitro Analysis, and In Vivo Testing Against a <i>Drosophila melanogaster</i> Alzheimer’s Disease ModelAadya Jaipuria0Madison Castillo1James Boksanski2Greg Landry3Ji Hyung Beak4Michelle Young5David T. Priefer6Kaïs Guessab7Crystal N. Ellis8Ronny Priefer9Massachusetts College of Pharmacy and Health Sciences, Boston, MA 02115, USAMassachusetts College of Pharmacy and Health Sciences, Boston, MA 02115, USAMassachusetts College of Pharmacy and Health Sciences, Boston, MA 02115, USAMassachusetts College of Pharmacy and Health Sciences, Boston, MA 02115, USAMassachusetts College of Pharmacy and Health Sciences, Boston, MA 02115, USAMassachusetts College of Pharmacy and Health Sciences, Boston, MA 02115, USAMassachusetts College of Pharmacy and Health Sciences, Boston, MA 02115, USAMassachusetts College of Pharmacy and Health Sciences, Boston, MA 02115, USAMassachusetts College of Pharmacy and Health Sciences, Boston, MA 02115, USAMassachusetts College of Pharmacy and Health Sciences, Boston, MA 02115, USAAlzheimer’s Disease (AD) is the most common form of dementia in individuals over the age of 65. There is no known prevention for the progression of the disease, although the FDA recently approved two drugs for AD. The exact etiology of AD is still under debate; however, it is commonly associated with the aggregation of amyloid-beta (Aβ) plaques in the brain. Recently some extended chalcones were reported to be potential anti-amyloidogenic agents. In this study, a larger library of extended chalcone analogs were synthesized with modifications on both rings. These were tested using the Thioflavin T fluorescence assay to measure their anti-Aβ aggregation properties. Three notably active compounds were further evaluated for potential neurotoxicity and neuroprotection using an MTT cell viability assay. These compounds were non-neurotoxic and displayed a trend toward neuroprotection. These were further assessed in a <i>Drosophila melanogaster</i> animal AD model. A forced climbing assay revealed statistically significant changes in flies’ movement by ~30% when fed these anti-amyloidogenic agents.https://www.mdpi.com/2624-8549/6/6/89Alzheimer’s Diseaseanti-amyloidogenicextended chalconesneuroprotection |
| spellingShingle | Aadya Jaipuria Madison Castillo James Boksanski Greg Landry Ji Hyung Beak Michelle Young David T. Priefer Kaïs Guessab Crystal N. Ellis Ronny Priefer Extended Chalcones: Synthesis, In Vitro Analysis, and In Vivo Testing Against a <i>Drosophila melanogaster</i> Alzheimer’s Disease Model Chemistry Alzheimer’s Disease anti-amyloidogenic extended chalcones neuroprotection |
| title | Extended Chalcones: Synthesis, In Vitro Analysis, and In Vivo Testing Against a <i>Drosophila melanogaster</i> Alzheimer’s Disease Model |
| title_full | Extended Chalcones: Synthesis, In Vitro Analysis, and In Vivo Testing Against a <i>Drosophila melanogaster</i> Alzheimer’s Disease Model |
| title_fullStr | Extended Chalcones: Synthesis, In Vitro Analysis, and In Vivo Testing Against a <i>Drosophila melanogaster</i> Alzheimer’s Disease Model |
| title_full_unstemmed | Extended Chalcones: Synthesis, In Vitro Analysis, and In Vivo Testing Against a <i>Drosophila melanogaster</i> Alzheimer’s Disease Model |
| title_short | Extended Chalcones: Synthesis, In Vitro Analysis, and In Vivo Testing Against a <i>Drosophila melanogaster</i> Alzheimer’s Disease Model |
| title_sort | extended chalcones synthesis in vitro analysis and in vivo testing against a i drosophila melanogaster i alzheimer s disease model |
| topic | Alzheimer’s Disease anti-amyloidogenic extended chalcones neuroprotection |
| url | https://www.mdpi.com/2624-8549/6/6/89 |
| work_keys_str_mv | AT aadyajaipuria extendedchalconessynthesisinvitroanalysisandinvivotestingagainstaidrosophilamelanogasterialzheimersdiseasemodel AT madisoncastillo extendedchalconessynthesisinvitroanalysisandinvivotestingagainstaidrosophilamelanogasterialzheimersdiseasemodel AT jamesboksanski extendedchalconessynthesisinvitroanalysisandinvivotestingagainstaidrosophilamelanogasterialzheimersdiseasemodel AT greglandry extendedchalconessynthesisinvitroanalysisandinvivotestingagainstaidrosophilamelanogasterialzheimersdiseasemodel AT jihyungbeak extendedchalconessynthesisinvitroanalysisandinvivotestingagainstaidrosophilamelanogasterialzheimersdiseasemodel AT michelleyoung extendedchalconessynthesisinvitroanalysisandinvivotestingagainstaidrosophilamelanogasterialzheimersdiseasemodel AT davidtpriefer extendedchalconessynthesisinvitroanalysisandinvivotestingagainstaidrosophilamelanogasterialzheimersdiseasemodel AT kaisguessab extendedchalconessynthesisinvitroanalysisandinvivotestingagainstaidrosophilamelanogasterialzheimersdiseasemodel AT crystalnellis extendedchalconessynthesisinvitroanalysisandinvivotestingagainstaidrosophilamelanogasterialzheimersdiseasemodel AT ronnypriefer extendedchalconessynthesisinvitroanalysisandinvivotestingagainstaidrosophilamelanogasterialzheimersdiseasemodel |