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It remains to become determined whether or not danshen has any PXR activating effects in humans, offered that it really is commonly ingested as extracted powder or as one among the various herbs as component of a classic Chinese medicine regimen.

In recent years, it has been investigated like a hepatoprotectant. Docetaxel Dibenzocyclooctene lignans are the biologically active chemical constituents in the berries of S. chinensis. These include schisandrol A, schisandrol B, schisandrin A, and schisandrin B. Both aqueous and ethanolic extracts of wu wei zi at a concentration of 1:1,000 have been shown to activate human PXR transcriptional activity in a cell based reporter assay. The degree of PXR activation by the extracts is similar to that by rifampicin in the same experiment. Consistent with the nding that wu wei zi extract activates human PXR, it is also capable of increasing CYP2C9 and CYP3A4 gene expression in primary cultures of human hepatocytes.

The very limited amount of scientic information on tian xian suggests that it has immunomodulating effect and is capable of inhibiting proliferation of tumor cells by inducing apoptosis. An ethanolic extract of tian xian at concentrations of 16?250 ?g/ ml has been shown to activate human PXR transcriptional activity in a cell NSCLC based reporter gene assay. The fold induction in the reporter activity by the 250 ?g/ml concentration of the extract is comparable to that by rifampicin. As shown in the mammalian two hybrid assay, tian xian extract stimulates recruitment of a coactivator to human PXR and dissociation of a corepressor from the receptor, suggesting that the extract acts an agonist of human PXR. Tian xian extract also increases the expression of a PXR target gene in cultured hepatocytes from transgenic mice expressing human CYP3A4.

In some cases, such as H. perforatum, G. biloba, S. chinensis, and tian xian, the fold increase in reporter activity is similar to that obtained for rifampicin, which is a known agonist of human PXR.