Comparison of the anti-inflammatory and analgesic effects of Gentiana macrophylla Pall. and Gentiana straminea Maxim., and identification of their active constituents.

BACKGROUND

Tibetan medicine get used to use the flowers of Gentiana straminea Maxim. to cure inflammation of stomach and intestines, hepatitis, cholecystitis, etc. The flowers of Gentiana macrophylla Pall. have been traditionally treated as an anti-inflammatory agent to clear heat in Mongolian medicine. In traditional Chinese medicine, Gentiana macrophylla Pall. and Gentiana straminea Maxim. have also been used under the name "Gentianae Macrophyllae Radix" and prescribed for the treatment of pain and inflammatory conditions.

OBJECTIVE

The present study evaluated the pharmacological effects of two species of "Radix Gentianae Macrophyllae" in experimental inflammation and pain models, and determined the chemical compounds that may correlate with their pharmacological activities. The comparison is needed to identify whether the two related plants can be used interchangeably.

METHODS

We evaluated the pharmacological effects of the flowers of Gentiana macrophylla Pall. and Gentiana straminea Maxim. in experimental inflammation and pain models. An HPLC-MS method was developed to analyze the chemical composition. The effects of Gentiana macrophylla Pall. and Gentiana straminea Maxim. on the p65 and p50 phosphorylation were examined by immunblotting. NF-κB transcriptional activity was measured using the luciferase assay, in vitro kinase assay and Griess reaction.

RESULTS

The extracts of Gentiana macrophylla Pall. and Gentiana straminea Maxim. possessed significant antinociceptive and anti-inflammatory activities. Flavonoids, secoiridoid glycosides and triterpines were determined in the extracts and may be the basis of the observed pharmacological effects. Nuclear translocation of p65, p50 and NF-κB transcriptional activity induced by LPS were suppressed by Gentiana macrophylla Pall. and Gentiana straminea Maxim.

CONCLUSIONS

The results clearly demonstrated that the chemical composition and pharmacological activities of the two herbs were similar, which support the interchangeability among the two herbs when using them in folk medicine.