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. 2019 Apr 3;24(7):1307. doi: 10.3390/molecules24071307

Table 1.

Results of biological activities connected to AD of haemanthamine derivatives (1a–1m).

Compound hAChE
IC50 (µM) a 		hBuChE
IC50 (µM) a 		SI for hAChE b GSK-3β (% inhib.) c GSK-3β IC50 a (µM) PAMPA-BBB
Permeability
(Pe; 10−6 cm s−1) d 		logBB e
1 > 500 > 500 n.d. n.d. n.d. n.d. n.c.
1a > 500 > 500 n.d. n.d. n.d. n.d. n.c.
1b > 500 437 ± 38 < 0.9 n.d. n.d. n.d. n.c.
1c > 500 203 ± 8 < 0.4 n.d. n.d. n.d. n.c.
1d > 500 > 500 n.d. n.d. n.d. n.d. n.c.
1e > 500 273 ± 18 < 0.5 n.d. n.d. n.d. n.c.
1f > 500 140 ± 21 < 0.3 n.d. n.d. n.d. n.c.
1g 294 ± 25 5.8 ± 0.3 0.02 11 ± 2 n.d. 8.4 ± 0.2 (CNS+) 0.285
1h 85.1 ± 6.4 80.2 ± 10.2 0.9 n.d. n.d. n.d. n.c.
1i 112 ± 21 129 ± 25 1.1 n.d. n.d. n.d. n.c.
1j 18.2 ± 1.3 6.6 ± 1.2 0.4 15 ± 6 n.d. 5.8 ± 0.9 (CNS+) 0.175
1k 180 ± 17 75.5 ± 12.5 0.4 n.d. n.d. n.d. n.c.
1m 14.7 ± 1.8 > 500 34.0 27 ± 9 34.8 ± 0.01 7.1 ± 0.3 (CNS+) 0.007
Huperzine A f 0.03 ± 0.00 > 500 > 15,151 n.d. n.d. n.d. n.c.
Galanthamine f 1.7 ± 0.1 42.3 ± 1.3 24.9 n.d. n.d. n.d n.c.
SB-415286 f n.d. n.d. n.d. n.d. n.d. 70 nM n.c.

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 for hAChE is determined as ratio hBuChE IC50/hAChE IC50; c tested at 10 µM compound concentration; n.d. stands for not determined; d CNS(+): high BBB permeation predicted with Pe (10−6 cm.s−1) > 4.0, CNS(−): low BBB permeation predicted with Pe (10−6 cm.s−1) < 2.0, CNS(+/−): BBB permeation uncertain with Pe (10−6 cm.s−1) from 4.0 to 2.0; e calculated at http://www.way2drug.com/geb/; n.c. stands for not calculated; f Reference compound; n.d. not determined; n.c. not calculated.