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The extraction, isolation and characterization of 29 natural products contained in Ginkgo biloba have been described, which we have now tested for their in‐vitro capacity to inhibit the five major human cytochrome P450 (CYP) isoforms in human liver microsomes. Weak or negligible inhibitory activity was found for the terpene trilactones (ginkgolides A, B, C and J, and bilobalide), and the flavonol glycosides. However 50% inhibitory activity (IC50) was found at concentrations less than 10 μg mL⁻¹ for the flavonol aglycones (kaempferol, quercetin, apigenin, myricetin, tamarixetin) with CYP1A2 and CYP3A. Quercetin, the biflavone amentoflavone, sesamin, as well as (Z,Z)‐4,4′‐(1,4‐pentadiene‐1,5‐diyl)diphenol and 3‐nonadec‐8‐enyl‐benzene‐1,2‐diol, were also inhibitors of CYP2C9. The IC50 of amentoflavone for CYP2C9 was 0.019 μg mL⁻¹ (0.035 μm). Thus, the principal components of Ginkgo biloba preparations in clinical use (terpene trilactones and flavonol glycosides) do not significantly inhibit these human CYPs in‐vitro. However, flavonol aglycones, the biflavonol amentoflavone and several other non‐glycosidic constituents are significant in‐vitro inhibitors of CYP. The clinical importance of these potential inhibitors will depend on their amounts in ginkgo preparations sold to the public, and the extent to which their bioavailability allows them to reach the CYP enzymes in‐situ.