Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease
Five novel tacrine-ferulic acid hybrid compounds (8a–e) were synthesized and their structures were identified on the basis of a detailed spectroscopic analysis. The activities of inhibiting acetyl cholinesterase (AChE) and butyryl cholinesterase (BuChE), reducing self-induced β-amyloid (Aβ) aggregat...
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| Format: | Article |
| Language: | English |
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MDPI AG
2016-10-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/21/10/1338 |
| _version_ | 1818574807874142208 |
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| author | Yingbo Fu Yu Mu Hui Lei Pu Wang Xin Li Qiao Leng Li Han Xiaodan Qu Zhanyou Wang Xueshi Huang |
| author_facet | Yingbo Fu Yu Mu Hui Lei Pu Wang Xin Li Qiao Leng Li Han Xiaodan Qu Zhanyou Wang Xueshi Huang |
| author_sort | Yingbo Fu |
| collection | DOAJ |
| description | Five novel tacrine-ferulic acid hybrid compounds (8a–e) were synthesized and their structures were identified on the basis of a detailed spectroscopic analysis. The activities of inhibiting acetyl cholinesterase (AChE) and butyryl cholinesterase (BuChE), reducing self-induced β-amyloid (Aβ) aggregation and chelating Cu2+ were evaluated in vitro. Among them, 8c and 8d displayed the higher selectivity in inhibiting AChE over BuChE. Moreover, 8d also showed dramatic inhibition of self-Aβ aggregation, activity of chelating Cu2+ and activity against Aβ-induced neurotoxicity in Neuro-2A cells. |
| first_indexed | 2024-12-15T00:31:01Z |
| format | Article |
| id | doaj.art-feb4148a2c2140a9b0aa5ecaf508429f |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-15T00:31:01Z |
| publishDate | 2016-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-feb4148a2c2140a9b0aa5ecaf508429f2022-12-21T22:42:02ZengMDPI AGMolecules1420-30492016-10-012110133810.3390/molecules21101338molecules21101338Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s DiseaseYingbo Fu0Yu Mu1Hui Lei2Pu Wang3Xin Li4Qiao Leng5Li Han6Xiaodan Qu7Zhanyou Wang8Xueshi Huang9Laboratory of Metabolic Disease Research and Drug Development, China Medical University, Shenyang 110001, ChinaInstitute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, ChinaInstitute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, ChinaInstitute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, ChinaLaboratory of Metabolic Disease Research and Drug Development, China Medical University, Shenyang 110001, ChinaLaboratory of Metabolic Disease Research and Drug Development, China Medical University, Shenyang 110001, ChinaInstitute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, ChinaInstitute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, ChinaLaboratory of Metabolic Disease Research and Drug Development, China Medical University, Shenyang 110001, ChinaLaboratory of Metabolic Disease Research and Drug Development, China Medical University, Shenyang 110001, ChinaFive novel tacrine-ferulic acid hybrid compounds (8a–e) were synthesized and their structures were identified on the basis of a detailed spectroscopic analysis. The activities of inhibiting acetyl cholinesterase (AChE) and butyryl cholinesterase (BuChE), reducing self-induced β-amyloid (Aβ) aggregation and chelating Cu2+ were evaluated in vitro. Among them, 8c and 8d displayed the higher selectivity in inhibiting AChE over BuChE. Moreover, 8d also showed dramatic inhibition of self-Aβ aggregation, activity of chelating Cu2+ and activity against Aβ-induced neurotoxicity in Neuro-2A cells.http://www.mdpi.com/1420-3049/21/10/1338β-amyloid aggregationcholinesteraseferulic acidmetal chelatortacrineneuroprotection |
| spellingShingle | Yingbo Fu Yu Mu Hui Lei Pu Wang Xin Li Qiao Leng Li Han Xiaodan Qu Zhanyou Wang Xueshi Huang Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease Molecules β-amyloid aggregation cholinesterase ferulic acid metal chelator tacrine neuroprotection |
| title | Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease |
| title_full | Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease |
| title_fullStr | Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease |
| title_full_unstemmed | Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease |
| title_short | Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease |
| title_sort | design synthesis and evaluation of novel tacrine ferulic acid hybrids as multifunctional drug candidates against alzheimer s disease |
| topic | β-amyloid aggregation cholinesterase ferulic acid metal chelator tacrine neuroprotection |
| url | http://www.mdpi.com/1420-3049/21/10/1338 |
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