|
Cytochrome enzyme
|
Percentage of control activity
|
|---|
| |
1 μM IQ-143
|
10 μM IQ-143
|
100 μM IQ-143
|
|---|
|
1A2
|
106.9
|
127.3
|
126.2
|
|
2C8
|
142.8
|
144.0
|
146.0
|
|
2C9
|
122.7
|
130.0
|
142.0
|
|
2C19
|
102.2
|
101.8
|
90.1
|
|
2D6
|
99.1
|
100.9
|
58.7
|
|
3A4
|
98.6
|
95.3
|
6.6
|
- CYP enzymes derived from baculovirus-infected insect cells were incubated with the corresponding substrates and IQ-143 at concentrations of 1 μM, 10 μM, and 100 μM as described by Unger and Frank [34]. As shown here (and in Figure S3), only very high doses of IQ-143 reduced the activity of the CYP isoenzymes 2C19, 2D6, and 3A4. At concentrations below 100 μM IQ-143, the activities were even higher compared to those of the control group.
