Table 4 PAMPA-BBB permeability of pterosin derivatives

From: Inhibition of β-site amyloid precursor protein cleaving enzyme 1 and cholinesterases by pterosins via a specific structure−activity relationship with a strong BBB permeability

Compounds

PAMPA-BBB permeability

Pe (10−6 cm/s)

(2S)-Pterosin A

6.26 ± 0.24

(2R)-Pterosin B

60.3 ± 9.8

(2S,3 R)-Pterosin C

2.34 ± 0.81

(2R,3 R)-Pterosin C

1.98 ± 0.17

(2S)-Pterosin P

7.92 ± 0.36

(2S)-Pteroside A2

0.54 ± 0.51

(2R)-Pteroside B

0.48 ± 0.29

(2S,3R)-Pteroside C

0.29 ± 0.34

(2R,3R)-Pteroside C

0.00 ± 0.00

(3S)-Pteroside D

0.00 ± 0.00

Pteroside Z

0.61 ± 0.17

Verapamila

34.6 ± 3.9

  1. PAMPA-BBB permeability Pe (10−6 cm/s) is expressed as the mean ± SD of quadruple experiments (Supplementary Information 4)
  2. “CNS+” (high BBB permeation predicted); Pe > 4.0, “CNS+/−” (BBB permeation uncertain); Pe from 4.0 to 2.0, “CNS−” (low BBB permeation predicted); Pe < 2.040
  3. PAMPA parallel artificial membrane permeation assay
  4. aVerapamil was used as positive control
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