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The chemical constituents of danshen contain water soluble phenolic acids, for example salvianolic acid and lithospermic acid B, along with the more lipophilic abietane kind diterpene quinones, for example tanshinone I, tanshinone IIA, tanshinone IIB, and cryptotanshinone.

On the other hand, tanshinone IIA and cryptotanshinone, but not tanshinone I, are capable of escalating human PXR transcriptional action when analyzed at a concentration of 2 ?M. Danshen could also be an activator of mouse PXR, as suggested by the nding that an ethyl acetate extract of danshen increases hepatic microsomal CYP3A protein levels in mice. It remains to be determined histone deacetylase inhibitor whether danshen has any PXR activating effects in humans, given that it is usually ingested as extracted powder or as one of the several herbs as part of a traditional Chinese medicine regimen. Schisandra chinensis is a deciduous woody vine found in the northwestern China, far eastern Russia, and Korea. As one of the commonly used herbs in traditional Chinese medicine, the berries of S.

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. Experiments with individual dibenzocyclooctene lignans indicate that schisandrol B, schisandrin A, and schisandrin IEM 1754 B activate human PXR with a similar efcacy and potency as rifampicin. Relative to these compounds, schisandrol A is also efcacious, but it is less potent. Wu wei zi extract and the four dibenzocyclooctene lignans are also able to activate mouse and rat PXR. Tian xian is a Chinese herbal remedy that consists of multiple herbs, including Hedyotis diffusae, Radix ginseng, Radix astragali, Polyporus umbellatus, Radix clematidis, Radix trichosanthis, Semen impatientis, Solanium nigrum, Calculus bovis, and Venenum bufonis.

As shown in Table I, various other herbal medicines have also been identied as activators of human PXR, as assessed by cell based reporter assays.