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. 2007 Sep 5;55(18):7323-31.
doi: 10.1021/jf0710074. Epub 2007 Aug 15.

Inhibition of Prostaglandin E(2) Production by Anti-Inflammatory Hypericum Perforatum Extracts and Constituents in RAW264.7 Mouse Macrophage Cells

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Free PMC article

Inhibition of Prostaglandin E(2) Production by Anti-Inflammatory Hypericum Perforatum Extracts and Constituents in RAW264.7 Mouse Macrophage Cells

Kimberly D P Hammer et al. J Agric Food Chem. .
Free PMC article

Abstract

Hypericum perforatum (Hp) is commonly known for its antiviral, antidepressant, and cytotoxic properties, but traditionally Hp was also used to treat inflammation. In this study, the anti-inflammatory activity and cytotoxicity of different Hp extractions and accessions and constituents present within Hp extracts were characterized. In contrast to the antiviral activity of Hp, the anti-inflammatory activity observed with all Hp extracts was light-independent. When pure constituents were tested, the flavonoids, amentoflavone, hyperforin, and light-activated pseudohypericin, displayed anti-inflammatory activity, albeit at concentrations generally higher than the amount present in the Hp extracts. Constituents that were present in the Hp extracts at concentrations that inhibited the production of prostaglandin E(2) (PGE(2)) were pseudohypericin and hyperforin, suggesting that they are the primary anti-inflammatory constituents along with the flavonoids, and perhaps the interactions of these constituents and other unidentified compounds are important for the anti-inflammatory activity of the Hp extracts.

Figures

Figure 1
Figure 1
Anti-inflammatory activity was screened using the PGE2 assay (n = 8 for each). Data are presented as mean LPS-induced PGE2 level ± standard error. Data represent light-activated and dark treatments combined as there were no significant differences between light-activated and dark treatments for each extract. Addition of LPS to the culture media +DMSO control increased the level of PGE2 20-fold over media +DMSO control alone (0.1 ± 0.05 ng/mL for media + DMSO, 2.4 ± 0.3 ng/mL for media + LPS + DMSO). Extracts in the culture media without LPS did not affect the concentration of PGE2 as compared to the media + DMSO control. *, p < 0.05, as compared to media + DMSO control.
Figure 2
Figure 2
Anti-inflammatory activity was screened using the PGE2 assay (n = 8 for each). Data are presented as mean LPS-induced PGE2 level ± standard error. Controls were the same for each accession tested and are represented as a single bar. Elixir at 5 and 1 μg/mL did not significantly reduce PGE2 levels as compared to control with values of 1.7 ± 0.3 and 2.1 ± 0.5, respectively (data not shown). Data represent light-activated and dark treatments combined as there were no significant differences between light-activated and dark treatments for each extract. Addition of LPS to the culture media + DMSO control increased the level of PGE2 13-fold over media + DMSO control alone (0.1 ± 0.02 ng/mL for media + DMSO, 1.7 ± 0.2 ng/mL for media + LPS + DMSO). Extracts in the culture media without LPS did not affect the concentration of PGE2 as compared to the media + DMSO control. *, p < 0.05, as compared to media + DMSO control.
Figure 3
Figure 3
Anti-inflammatory activity (mean PGE2 level ± standard error) of hypericin and pseudohypericin was screened using the PGE2 assay (n = 4). Addition of LPS to the culture media + DMSO control increased the level of PGE2 12-fold over media + DMSO control alone (0.18 ± 0.09 ng/mL for media + DMSO, 2.1 ± 0.3 ng/mL for media + LPS + DMSO) for pseudohypericin and 18-fold (0.17 ± 0.02 ng/mL for media + DMSO, 3.0 ± 0.6 ng/mL for media + DMSO + LPS) for hypericin. *, p < 0.05, as compared to media + DMSO or media + LPS + DMSO control. #, p < 0.05, significant difference between light-activated and dark treatments for corresponding dose.

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