Screening of active ingredients of herbal medicine for interaction with CYP450 3A4

A two-step algorithm is adopted in the screening of herbal species which possess significant inhibitory effects on cytochrome P450 3A4 (CYP450 3A4). The algorithm comprises an initial stage of high throughput screening with Herbochip® for the identification of herbal fractions that exhibit interactions with CYP450 3A4. Fifty commonly used TCM species were screened with seven showing a positive signal reflecting interaction. In the inhibition assays that followed, six of the seven species gave a signal. Sophora flavescens stood out as it gave the highest number of wells with a response, the highest maximum index was 0.96, and the median index was 0.55. The selection of TCM species with inhibitory effects on CYP450 carries the potential role of its use to boost the effects of known therapeutic agents, a mechanism that has been exploited in the design of regimens for the treatment of HIV infection. Copyright © 2007 John Wiley & Sons, Ltd.