| In vitro: |
| Chem Pharm Bull (Tokyo). 2007 May;55(5):757-61. | | New constituent from Podocarpus macrophyllus var. macrophyllus shows anti-tyrosinase effect and regulates tyrosinase-related proteins and mRNA in human epidermal melanocytes.[Pubmed: 17473463] | A new biflavonoid, 2,3-dihydro-4',4'''-di-O-methylamentoflavone (5), and five known compounds, (-)-catechin (1), quercetin (2), 2,3-dihydrosciadopitysin (3), sciadopitysin (4), and isoginkgetin (6), were isolated from Podocarpus macrophyllus var. macrophyllus (Podocarpaceae). These compounds were evaluated their ability to inhibit cellular tyrosinase activity and for their melanin inhibitory activity in human epidermal melanocytes (HEMn).
METHODS AND RESULTS:
In the melanin synthesis assay, 2,3-dihydro-4',4'''-di-O-methylamentoflavone (5) showed a potent anti-tyrosinase effect with IC(50)=0.098 mM in HEMn. It also significantly decreased both protein and mRNA levels of the tyrosinase-related protein-2 (TRP-2) by Western blot and quantitative real-time PCR (qRT-PCR) analysis.
CONCLUSIONS:
These findings suggest that the new compound, 2,3-dihydro-4',4'''-di-O-methylamentoflavone (5), is the most active component of P. macrophyllus var. macrophyllus in inhibiting pigmentation and that this inhibition is exerted through inhibition of transcription of the genes encoding TRP2. | | Z Naturforsch C. 2003 Jan-Feb;58(1-2):65-9. | | Antifungal activity of biflavones from Taxus baccata and Ginkgo biloba.[Pubmed: 12622229] | Bilobetin and 4'''-O-methylamentoflavone were isolated and identified in the needles of Taxus baccata, for the first time in this species.
METHODS AND RESULTS:
The antifungal activity of biflavones from T. baccata and Ginkgo biloba, namely amentoflavone, 7-O-methylamentoflavone, bilobetin, ginkgetin, sciadopitysin and 2,3-dihydrosciadopitysin towards the fungi Alternaria alternata, Fusarium culmorum, Cladosporium oxysporum was determined employing computer-aided image analysis couplet to a microscope.
CONCLUSIONS:
Bilobetin exhibited a significant antifungal activity with values of ED50 14, 11 and 17 microM respectively. This compound completely inhibited the growth of germinating tubes of Cladosporium oxysporum and Fusarium culmorum at a concentration 100 microM. Activity of ginkgetin and 7-O-methylamentoflavone towards Alternaria alternata was stronger than that of bilobetin. Moreover, slight structural changes in the cell wall of Alternaria alternata exposed to ginkgetin at concentration of 200 microM were observed. |
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