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FACT
Focus on Alternative and Complementary Therapies

Herbal alternatives to bear bile: effects of Scutellaria baicalensis Georgi on IL-6 promoter and CYP3A4 activities

Appiah SS1,3, Bremner P2, Heinrich M2, Kokubun T3, Simmonds MSJ3, Bell C1
1Middlesex University, Queensway, Enfield EN3 4SA, UK
2Centre for Pharmacognosy and Phytotherapy, School of Pharmacy, University of London, UK
3Royal Botanic Gardens, Kew, Richmond, Surrey TW9 3AB, UK

Objective

The aim of this study was to investigate a mechanism of anti-inflammatory action of extracts of the root of Scutellaria baicalensis (huang qin) and the effects of its constituents on the drug metabolising enzyme cytochrome P450-3A4.

Materials and methods

IL-6-Luciferease reporter assays were conducted using HeLa cells. Cytochrome P450-3A4 (CYP-3A4) was assessed using testosterone 6β-hydroxylation as a probe for enzyme activity in human liver microsomes.

Results

At 100 μg/ml an ethyl acetate extract, but not the water or the methanol extracts of S. baicalensis, inhibited IL-6 promoter activity. Fractions and compounds (chrysin and wogonin) isolated from the methanolic extract, as well as standard compounds (baicalin and scutellarein) of the herb, demonstrated anti-inflammatory effect by inhibiting IL-6 promoter activity. Chrysin (5,7-dihy-droxyflavone) dose-dependently inhibited IL-6 promoter activity by 63% (P < 0.001), 91% (P < 0.001) and 98% (P < 0.001), at 50, 100 and 393 μM, respectively. Chrysin (79 μM), baicalein (74 μM) and scutellarein (69 μM) inhibited CYP-3A4 enzyme activity by 74% (P < 0.001), 41% (P < 0.05) and 40% (P < 0.05), respectively.

Conclusion

Constituents of S. baicalensis were found to exert anti-inflammatory action through the inhibition of IL-6 promoter activity. Also, preliminary results suggest that some constituents of S. baicalensis with anti-inflammatory properties are also inhibitors of CYP-3A4 activity in vitro. Therefore, co-administration of S. baicalensis with herbs or drugs metabolised by CYP-3A4 could lead to possible herb–herb or drug–herb interactions. S. baicalensis is a herb proposed as a potential alternative to bear bile (used in traditional medicine as an anti-inflammatory agent), either as an individual herb or in combination with others.

Acknowledgements

We thank DEFRA and IFAW charitable trust for their financial support.

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