These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Anti-inflammatory activity of the synthetic C-C biflavonoids.
    Author: Park H, Kim YH, Chang HW, Kim HP.
    Journal: J Pharm Pharmacol; 2006 Dec; 58(12):1661-7. PubMed ID: 17331331.
    Abstract:
    To find anti-inflammatory agents based on plant constituents, the effects of six synthetic C-C biflavonoids connecting with different positions of C-C bond between flavone monomers (a: 4'-4', b: 4'-3', c: 4'-6, d: 3'-6, e: 6-6, f: 4'-3) were examined on PGE(2) and nitric oxide (NO) production from lipopolysaccharide (LPS)-treated macrophages, RAW 264.7. Among the compounds tested, the biflavonoids d, e, and f showed a considerable inhibition of cyclooxygenase-2 (COX-2)-mediated PGE(2) production at concentrations up to 50 microM, while the derivative c exerted cytotoxic effects on RAW cells. Especially, the biflavonoid e possessed the most potent inhibitory activity of PGE(2) production with an IC50 of 3.7 microM, compared with an IC50 of 8.2-20.7 microM by ginkgetin (natural biflavonoid). Western blot and reverse transcriptase-polymerase chain reaction analyses have shown that the inhibition of PGE(2) production by these synthetic derivatives was mediated at least in part by COX-2 inhibition, but not by COX-2 down-regulation. Meanwhile, these synthetic biflavonoids did not considerably inhibit inducible nitric oxide synthase-mediated NO production at concentrations up to 50 microM. When intraperitoneally administered, the biflavonoid e showed a significant anti-inflammatory activity (22.2% inhibition) against rat carrageenan-induced paw oedema at 5 mg kg(-1). The biflavonoid e may be used as a synthetic lead for developing new anti-inflammatory agents.
    [Abstract] [Full Text] [Related] [New Search]