Table 1.
Main features of cholinesterase inhibitors.
| Classic/derivatives/analogues/hybrid natural and synthetic | Enzyme specificity (AChE/BuChE) | Additional targets | Type of experimentation | Pre-clinical/clinical studies/in use |
|---|---|---|---|---|
| Single target | ||||
| Tacrine | AChE/BuChE | In use 1993-2013 | ||
| Donepezil | AChE | In use since 1996 | ||
| Rivastigmine | AChE (G1 isoform) and BuChE | In use since 2000 | ||
| Galantamine | AChE | In use since 2001 | ||
| Huperzine-A | AChE | ‘In vitro’ and ‘In vivo’ studies | Phase IV in China | |
| Tolserine (Physostigmine derivate) | AChE, especially human AChE | Theoretical chemistry studies | ||
| Eseroline (Physostigmine derivate) | AChE | Opioids agonist | Theoretical chemistry studies | |
| Tacrine analogues (N-alkyl-7-methoxytacrine hydrochloride) | AChE better than tacrine | Theoretical chemistry studies | ||
| Cardanol (Anacardium occidentale nutshell) derivatives [N, N-dimethycarbamoyl, N, N-dimethylamine, and pyrrolidine substitutions)] | AChE | Theoretical chemistry studies | ||
| Multi-target | ||||
| Phenserine (physostigmine derivate) | AChE | APP cleavage | Phase II | |
| Ladostigil N-propargyl-(3R) aminoindan-5yl)-ethyl methyl carbamate) | AChE | APP cleavage; MAO | Phase II | |
| Galangin (flavonoid extracted from Alpiniae officinarum sp.) | AChE | Free radical scavenger | ‘In vitro’ studies | |
| Liquiritigenin (chalcone isoliquiritigenin derivate) | AChE | MAO; BDNF; ERK; CREB and free radicals’ production | ‘In vivo’ studies | |
| Hybrid compounds (tacrine/donepezil; tacrine/ferulic acid; tacrine-8-hydroxyquinoline; donepezil-AP2238) | AChE; BuChE | Aβ mediated toxicity; MAO; antioxidant properties | ‘In vitro’ studies | |
| Fucoxanthin (Brown seaweed) | AChE | Oxidative stress; inflammation via MAPK pathway | Enzymatic assay; ‘in vitro’ and ‘in vivo’ studies | |
| Phloroglucinol (Ecklonia maxima) | AChE | Aβ 1-42-induced neuritic loss | Enzymatic assay; ‘in vitro’ and ‘in vivo’ studies | |
| Dibenzodioxine-2,4,7,9-tetraol (Ecklonia maxima) | AChE | Aβ mediated toxicity | Enzymatic assay; ‘in vitro’ and ‘in vivo’ studies | |
| Eckol (Ecklonia maxima) | AChE | Aβ 25-35-induced toxicity | Enzymatic assay; ‘in vitro’ and ‘in vivo’ studies | |
| Fucosterol (Ecklonia stolonifera) | BuChE | Aβ 1-42-induced memory impairment; inflammation via NFkB pathway | Enzymatic assay; ‘in vitro’ and ‘in vivo’ studies | |
| Fucosterol (Panida australis) | AChE/BuChE | Enzymatic assay; ‘in vitro’ and ‘in vivo’ studies | ||
| Fucosterol (Sargassum horridum) | AChE | Enzymatic assay; ‘in vitro’ and ‘in vivo’ studies | ||