Comparative biophysical characterization: A screening tool for acetylcholinesterase inhibitors.
Among neurodegenerative diseases, Alzheimer's disease (AD) is one of the most grievous disease. The oldest cholinergic hypothesis is used to elevate the level of cognitive impairment and acetylcholinesterase (AChE) comprises the major targeted enzyme in AD. Thus, acetylcholinesterase inhibitors...
| Main Authors: | , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Public Library of Science (PLoS)
2019-01-01
|
| Series: | PLoS ONE |
| Online Access: | https://doi.org/10.1371/journal.pone.0215291 |
| _version_ | 1818590367574917120 |
|---|---|
| author | Devashree N Patil Sushama A Patil Srinivas Sistla Jyoti P Jadhav |
| author_facet | Devashree N Patil Sushama A Patil Srinivas Sistla Jyoti P Jadhav |
| author_sort | Devashree N Patil |
| collection | DOAJ |
| description | Among neurodegenerative diseases, Alzheimer's disease (AD) is one of the most grievous disease. The oldest cholinergic hypothesis is used to elevate the level of cognitive impairment and acetylcholinesterase (AChE) comprises the major targeted enzyme in AD. Thus, acetylcholinesterase inhibitors (AChEI) constitutes the essential remedy for the treatment of AD. The study aims to evaluate the interactions between natural molecules and AChE by Surface Plasmon Resonance (SPR). The molecules like alkaloids, polyphenols and substrates of AChE have been considered for the study with a major emphasis on affinity and kinetics. To better understand the activity of small molecules, the investigation is supported by both experimental and theoretical approach such as fluorescence, Circular Dichroism (CD) and molecular docking studies. Amongst the screened ones tannic acid showed promising results compared with others. The methodology followed here have highlighted many molecules with a higher affinity towards AChE and these findings may take lead molecules generated in preclinical studies to treat neurodegenerative diseases. Additionally, we suggest a unique signature for the heterogeneous analyte model using competitive experiments for analyzing simultanous interactions of both the analytes. |
| first_indexed | 2024-12-16T09:55:25Z |
| format | Article |
| id | doaj.art-ac29b446488f40039a7158a61273e437 |
| institution | Directory Open Access Journal |
| issn | 1932-6203 |
| language | English |
| last_indexed | 2024-12-16T09:55:25Z |
| publishDate | 2019-01-01 |
| publisher | Public Library of Science (PLoS) |
| record_format | Article |
| series | PLoS ONE |
| spelling | doaj.art-ac29b446488f40039a7158a61273e4372022-12-21T22:35:56ZengPublic Library of Science (PLoS)PLoS ONE1932-62032019-01-01145e021529110.1371/journal.pone.0215291Comparative biophysical characterization: A screening tool for acetylcholinesterase inhibitors.Devashree N PatilSushama A PatilSrinivas SistlaJyoti P JadhavAmong neurodegenerative diseases, Alzheimer's disease (AD) is one of the most grievous disease. The oldest cholinergic hypothesis is used to elevate the level of cognitive impairment and acetylcholinesterase (AChE) comprises the major targeted enzyme in AD. Thus, acetylcholinesterase inhibitors (AChEI) constitutes the essential remedy for the treatment of AD. The study aims to evaluate the interactions between natural molecules and AChE by Surface Plasmon Resonance (SPR). The molecules like alkaloids, polyphenols and substrates of AChE have been considered for the study with a major emphasis on affinity and kinetics. To better understand the activity of small molecules, the investigation is supported by both experimental and theoretical approach such as fluorescence, Circular Dichroism (CD) and molecular docking studies. Amongst the screened ones tannic acid showed promising results compared with others. The methodology followed here have highlighted many molecules with a higher affinity towards AChE and these findings may take lead molecules generated in preclinical studies to treat neurodegenerative diseases. Additionally, we suggest a unique signature for the heterogeneous analyte model using competitive experiments for analyzing simultanous interactions of both the analytes.https://doi.org/10.1371/journal.pone.0215291 |
| spellingShingle | Devashree N Patil Sushama A Patil Srinivas Sistla Jyoti P Jadhav Comparative biophysical characterization: A screening tool for acetylcholinesterase inhibitors. PLoS ONE |
| title | Comparative biophysical characterization: A screening tool for acetylcholinesterase inhibitors. |
| title_full | Comparative biophysical characterization: A screening tool for acetylcholinesterase inhibitors. |
| title_fullStr | Comparative biophysical characterization: A screening tool for acetylcholinesterase inhibitors. |
| title_full_unstemmed | Comparative biophysical characterization: A screening tool for acetylcholinesterase inhibitors. |
| title_short | Comparative biophysical characterization: A screening tool for acetylcholinesterase inhibitors. |
| title_sort | comparative biophysical characterization a screening tool for acetylcholinesterase inhibitors |
| url | https://doi.org/10.1371/journal.pone.0215291 |
| work_keys_str_mv | AT devashreenpatil comparativebiophysicalcharacterizationascreeningtoolforacetylcholinesteraseinhibitors AT sushamaapatil comparativebiophysicalcharacterizationascreeningtoolforacetylcholinesteraseinhibitors AT srinivassistla comparativebiophysicalcharacterizationascreeningtoolforacetylcholinesteraseinhibitors AT jyotipjadhav comparativebiophysicalcharacterizationascreeningtoolforacetylcholinesteraseinhibitors |