| Autor: |
Frank, Annika, Abu-Lafi, Saleh, Adawi, Azmi, Schwed, Johannes, Stark, Holger, Rayan, Anwar |
| Předmět: |
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| Zdroj: |
Inflammation Research; Oct2017, Vol. 66 Issue 10, p923-929, 7p |
| Abstrakt: |
Objectives: The aim was to evaluate the activity of seven medicinal, anti-inflammatory plants at the hHR with focus on defined chemical compounds from Curcuma longa. Materials: Activities were analyzed with membrane preparations from Sf9 cells, transiently expressing the hHR, G and G subunits. Methods: From the methanolic extract of C. longa curcumin ( 1), demethoxycurcumin ( 2) and bis(4-hydroxy-cinnamoyl)methane ( 3) were isolated, purified with HPLC (elution-time 10.20, 9.66, 9.20 min, respectively) and together with six additional extracts, were characterized via radioligand binding studies at the hHR. Results: Compounds from C. longa were the most potent ligands at the hHR. They exhibited estimated K values of 4.26-6.26 µM (1.57-2.31 µg/mL) ( 1); 6.66--8.97 µM (2.26-3.04 µg/mL) ( 2) and 10.24-14.57 µM (3.16-4.49 µg/mL) ( 3) (95% CI). The estimated K value of the crude extract of curcuma was 0.50-0.81 µg/mL. Fractionated curcumin and the crude extract surpassed the effect of pure curcumin with a K value of 5.54 µM or 2.04 µg/mL [95% CI (4.47-6.86 µM), (1.65-2.53 µg/mL)]. Conclusion: Within this study, defined compounds of C. longa were recognized as potential ligands and reasonable lead structures at the hHR. The mode of anti-inflammatory action of curcumin was further elucidated and the role of extracts in traditional phytomedicine was strengthened. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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