A galantamine–curcumin hybrid lacks the depressant side effect of acetylcholinesterase inhibitors
Acetylcholinesterase inhibitors (AChEIs) are drugs that enhance cholinergic neuro-transmission and are used for the treatment of Alzheimer’s disease and myasthenia gravis. Common AChEIs include rivastigmine, donepezil and galantamine (GAL), but they can cause side effects like nausea, vomiting, depr...
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2024-12-01
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| Series: | Biotechnology & Biotechnological Equipment |
| Subjects: | |
| Online Access: | https://www.tandfonline.com/doi/10.1080/13102818.2024.2305903 |
| _version_ | 1826939193451872256 |
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| author | Ivanka Kostadinova Mariyana Atanasova Georgi Stavrakov Irena Philipova Irini Doytchinova |
| author_facet | Ivanka Kostadinova Mariyana Atanasova Georgi Stavrakov Irena Philipova Irini Doytchinova |
| author_sort | Ivanka Kostadinova |
| collection | DOAJ |
| description | Acetylcholinesterase inhibitors (AChEIs) are drugs that enhance cholinergic neuro-transmission and are used for the treatment of Alzheimer’s disease and myasthenia gravis. Common AChEIs include rivastigmine, donepezil and galantamine (GAL), but they can cause side effects like nausea, vomiting, depression and bradycardia. A potential link exists between AChEIs and increased depression risk. Recently, we have discovered a hybrid compound (4b) combining GAL and curcumin (CCN), which shows improved anticholinesterase activity and neuroprotective effects. It could be developed as a potential multitarget agent for neurodegenerative disorders. Here, we examine the compound’s depressant side effect on mice, comparing it to GAL and CCN. Tests were conducted twice using the tail suspension test (TST) and the forced swim test over an 8-day treatment period. The results showed that 4b lacked the depressant effect of GAL and even displayed a mild antidepressant effect similar to CCN in TST. This suggests that incorporating antidepressant fragments, like CCN, into AChEIs can potentially neutralize their depressive side effects. |
| first_indexed | 2024-03-07T21:40:39Z |
| format | Article |
| id | doaj.art-a5a283a085034d828ddf35935f9dfff5 |
| institution | Directory Open Access Journal |
| issn | 1310-2818 1314-3530 |
| language | English |
| last_indexed | 2025-02-17T19:09:37Z |
| publishDate | 2024-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Biotechnology & Biotechnological Equipment |
| spelling | doaj.art-a5a283a085034d828ddf35935f9dfff52024-12-10T05:42:51ZengTaylor & Francis GroupBiotechnology & Biotechnological Equipment1310-28181314-35302024-12-0138110.1080/13102818.2024.2305903A galantamine–curcumin hybrid lacks the depressant side effect of acetylcholinesterase inhibitorsIvanka Kostadinova0Mariyana Atanasova1Georgi Stavrakov2Irena Philipova3Irini Doytchinova4Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University of Sofia, Sofia, BulgariaDepartment of Chemistry, Faculty of Pharmacy, Medical University of Sofia, Sofia, BulgariaDepartment of Chemistry, Faculty of Pharmacy, Medical University of Sofia, Sofia, BulgariaInstitute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Sofia, BulgariaDepartment of Chemistry, Faculty of Pharmacy, Medical University of Sofia, Sofia, BulgariaAcetylcholinesterase inhibitors (AChEIs) are drugs that enhance cholinergic neuro-transmission and are used for the treatment of Alzheimer’s disease and myasthenia gravis. Common AChEIs include rivastigmine, donepezil and galantamine (GAL), but they can cause side effects like nausea, vomiting, depression and bradycardia. A potential link exists between AChEIs and increased depression risk. Recently, we have discovered a hybrid compound (4b) combining GAL and curcumin (CCN), which shows improved anticholinesterase activity and neuroprotective effects. It could be developed as a potential multitarget agent for neurodegenerative disorders. Here, we examine the compound’s depressant side effect on mice, comparing it to GAL and CCN. Tests were conducted twice using the tail suspension test (TST) and the forced swim test over an 8-day treatment period. The results showed that 4b lacked the depressant effect of GAL and even displayed a mild antidepressant effect similar to CCN in TST. This suggests that incorporating antidepressant fragments, like CCN, into AChEIs can potentially neutralize their depressive side effects.https://www.tandfonline.com/doi/10.1080/13102818.2024.2305903Galantaminecurcuminfluoxetineacetylcholinesterase inhibitorstail suspension testforced swim test |
| spellingShingle | Ivanka Kostadinova Mariyana Atanasova Georgi Stavrakov Irena Philipova Irini Doytchinova A galantamine–curcumin hybrid lacks the depressant side effect of acetylcholinesterase inhibitors Biotechnology & Biotechnological Equipment Galantamine curcumin fluoxetine acetylcholinesterase inhibitors tail suspension test forced swim test |
| title | A galantamine–curcumin hybrid lacks the depressant side effect of acetylcholinesterase inhibitors |
| title_full | A galantamine–curcumin hybrid lacks the depressant side effect of acetylcholinesterase inhibitors |
| title_fullStr | A galantamine–curcumin hybrid lacks the depressant side effect of acetylcholinesterase inhibitors |
| title_full_unstemmed | A galantamine–curcumin hybrid lacks the depressant side effect of acetylcholinesterase inhibitors |
| title_short | A galantamine–curcumin hybrid lacks the depressant side effect of acetylcholinesterase inhibitors |
| title_sort | galantamine curcumin hybrid lacks the depressant side effect of acetylcholinesterase inhibitors |
| topic | Galantamine curcumin fluoxetine acetylcholinesterase inhibitors tail suspension test forced swim test |
| url | https://www.tandfonline.com/doi/10.1080/13102818.2024.2305903 |
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