Table 2. Effect of (a) analogues of resveratrol (compound 1) and (b) (hydroxyphenyl)ethylphenols on inhibition (IC50) of the epoxide hydrolase (LTB4 generation) and aminopeptidase (PGP degradation) activities of LTA4H as described in Materials and methods.
Cmpd. No. | R1 | R2 | R3 | Epoxide Hydrolase IC50 ± SEM (μM) | Aminopeptidase IC50 ± SEM (μM) | |||
---|---|---|---|---|---|---|---|---|
1 | OH | OH | OH | 32.2 ± 5.9 | >100 | |||
2a | OH | OH | OH | 14.3 ± 2.1 | 85.3 ± 33.9 | |||
3 | OMe | OMe | OMe | 41.2 ± 5.5 | 68.8 ± 9.9 | |||
4 | OCOMe | OCOMe | OCOMe | 38.6 ± 5.9 | >100 | |||
5 | OMe | OH | OH | 3.9 ± 0.4 | 99.5 ± 22.6 | |||
Cmpd. No. | R1 | R2 | R3 | R4 | R5 | Epoxide Hydrolase IC50 ± SEM (μM) | Aminopeptidase IC50 ± SEM (μM) | |
6 | OMe | OH | H | H | OH | 6.4 ± 0.7 | >100 | |
7 | OEt | OH | H | H | OH | 3.2 ± 0.7 | >100 | |
8 | OMe | OH | H | OH | H | 1.7 ± 0.25 | >100 | |
9 | OMe | OH | OH | H | H | 0.50 ± 0.04 | >100 |
IC50 curves were generated from 3 technical replicates at each concentration of test compound and at least 2 biological replicates. Results depicted as mean ± SEM.
aZ-isomer.