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Table 7 Effects on human cytochrome P450 function in vitro

From: Modeling antibiotic and cytotoxic effects of the dimeric isoquinoline IQ-143 on metabolism and its regulation in Staphylococcus aureus, Staphylococcus epidermidisand human cells

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
  1. 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.