Published September 30, 2019
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Table 2 h AChE, h in Amaryllidaceae alkaloids from Narcissus pseudonarcissus L. cv. Dutch Master as potential drugs in treatment of Alzheimer's disease
Authors/Creators
- 1. ∗ & ADINACO Research Group, Department of Pharmaceutical Botany, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05, Hradec Králové, Czech & Department of Pharmacognosy, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05, Hradec Králové, Czech Republic
Description
Table 2 h AChE, h BuChE, POP and GSK-3β inhibitory activities of the tested Amaryllidaceae alkaloids isolated from Narcissus pseudonarcissus cv. Dutch Master expressed as IC50.
| Compound | h AChE IC (μM) a 50 | h BuChE IC (μM) a 50 | SI for h AChE b | POP IC a (μM) 50 | GSK-3β (% inhib.) c | GSK-3β IC a (μM) 50 |
|---|---|---|---|---|---|---|
| Homolycorine (1) | 64 ± 4 | 151 ± 20 | 2.4 | 173 ± 41 | 54 ± 1 | n.d. |
| Masonine (2) | 305 ± 34 | 229 ± 24 | 0.8 | 314 ± 34 | 66 ± 4 | 27.9 ± 0.8 |
| Seco-isopowellaminone (3) | 294 ± 33 | > 500 | > 1.7 | > 500 | 38 ± 1 | n.d. |
| O -Ethyllycorenine (4) | > 500 | > 500 | n.d. | > 500 | 58 ± 3 | n.d. |
| N -Demethylmasonine (5) | > 500 | 474 ± 13 | <0.9 | > 500 | n.d. | n.d. |
| Narcimatuline (6) | 489 ± 60 | 5.9 ± 0.2 | 0.01 | 29.2 ± 1.0 | 67 ± 3 | 20.7 ± 2.4 |
| O -Acetylpluviine (7) | > 500 | > 500 | n.d. | n.d. | n.d. | n.d. |
| Tazettine (8) | > 500 | > 500 | n.d. | > 500 | 49 ± 0 | n.d. |
| Galanthine (9) | 606 ± 60 | > 500 | > 1.7 | > 500 | 26 ± 7 | n.d. |
| Galanthamine (10) | 1.7 ± 0.1 | 42.3 ± 1.3 | 24.9 | > 500 | n.d. | n.d. |
| Narwedine (11) | 281 ± 34 | 911 ± 69 | 3.2 | 907 ± 87 | n.d. | n.d. |
| Caranine (12) | 321 ± 42 | 487 ± 55 | 1.5 | > 1000 | 58 ± 9 | 30.8 ± 0.3 |
| Lycoraminone (13) | > 500 | > 500 | n.d. | n.d. | 39 ± 1 | n.d. |
| Lycoramine (14) | 456 ± 57 | > 500 | > 1.1 | > 500 | n.d. | n.d. |
| O -Methyllycorenine (15) | > 500 | > 500 | n.d. | > 500 | n.d. | n.d. |
| Lycorenine (16) | > 500 | > 500 | n.d. | > 500 | 48 ± 3 | n.d. |
| Oduline (17) | > 500 | > 500 | n.d. | 252 ± 27 | 58 ± 4 | n.d. |
| Haemanthamine (18) | > 500 | > 500 | n.d. | > 500 | 52 ± 0 | n.d. |
| Tetrahydromasonine (19) | > 500 | > 500 | n.d. | > 500 | 22 ± 0 | n.d. |
| Hippeastrine (20) | > 500 | > 500 | n.d. | > 500 | 11 ± 2 | n.d. |
| Crinine (21) | > 500 | > 500 | n.d. | > 500 | 40 ± 5 | n.d. |
| Epimaritidine (22) | > 500 | > 500 | n.d. | n.d. | n.d. | n.d. |
| Huperzine A c | 0.033 ± 0.001 | > 500 | > 15.151 | n.d. | n.d. | n.d. |
| Berberine c | n.d. | n.d. | n.d. | 142 ± 21 | n.d. | n.d. |
| Z -Pro-prolinal c | n.d. | n.d. | n.d. | 2.75 × 10−3 | n.d. | n.d. |
| SB-415286 c | n.d. | n.d. | n.d. | n.d. | n.d. | 70 nM |
a Compound concentration required to decrease enzyme activity by 50%; the values are the mean ± SEM of three independent measurements, each performed in triplicate; b Selectivity index (SI) for h AChE is determined as ratio h BuChE IC / h AChE IC; c tested at 10 μM compound concentration; n.d. stands for not determined.
Notes
Published as part of Hulcová, Daniela, Maříková, Jana, Korábečný, Jan, Hošťálková, Anna, Jun, Daniel, Kuneš, Jiří, Chlebek, Jakub, Opletal, Lubomír, Simone, Angela De, Nováková, Lucie, Andrisano, Vincenza, Růžička, Aleš & Cahlíková, Lucie, 2019, Amaryllidaceae alkaloids from Narcissus pseudonarcissus L. cv. Dutch Master as potential drugs in treatment of Alzheimer's disease, pp. 5 in Phytochemistry 165 on page 5, DOI: 10.1016/j.phytochem.2019.112055, http://zenodo.org/record/10483285
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