2',5,6',7-Tetrahydroxyflavone
2',5,6',7-Tetrahydroxyflavone inhibited hepatic testosterone 6beta-hydroxylation (CYP3A4) activity with a IC50 of 7.8 microM.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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Planta Med. 2005 Sep;71(9):885-7.
Skullcapflavone I from Scutellaria baicalensis induces apoptosis in activated rat hepatic stellate cells.[Pubmed:
16206047 ]
The therapeutic goal in liver fibrosis is the reversal of fibrosis and the selective clearance by apoptosis of hepatic stellate cells (HSCs), which play a central role in liver fibrogenesis.
METHODS AND RESULTS:
In this study, the apoptotic effect of wogonin, oroxylin A,
2',5,6',7-Tetrahydroxyflavone, skullcapflavone I, and baicalein, isolated from the dried root of Scutellaria baicalensis, was investigated in activated rat HSCs, T-HSC/Cl-6 cells transformed with the Simian virus 40. Among the isolated compounds, skullcapflavone I (20 microM for 24 h) significantly induced apoptosis in activated rat HSCs while there was no change in the cell viability of hepatocytes. Skullcapflavone I increased caspase-3 and -9 activities accompanied by the proteolytic cleavage of poly(ADP-ribose) polymerase. Specific inhibitors of caspase-3 and caspase-9 prevented the apoptotic process induced by skullcapflavone I.
CONCLUSIONS:
From these results, skullcapflavone I from S. baicalensis selectively induced apoptosis in T-HSC/Cl-6 cells via caspase-3 and caspase-9 activation.
J Toxicol Environ Health A. 2002 Mar;65(5-6):373-81.
Effects of flavonoids isolated from Scutellariae radix on cytochrome P-450 activities in human liver microsomes.[Pubmed:
11936218 ]
A series of flavonoids isolated from Scutellariae radix were evaluated for their effects on cytochrome P-450 (CYP) activities in human liver microsomes.
METHODS AND RESULTS:
All flavonoids did not substantially inhibit pentoxyresorufin O-deethylation (CYP2B 1), mephenytoin 4-hydroxylation (CYP2C19), dextromethorphan O-demethylation (CYP2D6), and chlorzoxazone 6-hydroxylation (CYP2E1) activities (IC50: >50 microM). Baicalein and
2',5,6',7-Tetrahydroxyflavone inhibited hepatic testosterone 6beta-hydroxylation (CYP3A4) activity with a IC50 of 17.4 and 7.8 microM, respectively. Oroxylin A inhibited diclofenac 4-hydroxylation (CYP2C9) activity with a IC50 of 6.7 microM. In contrast, all flavonoids tested inhibited hepatic caffeine N'-demethylation (CYP1A2) with IC50 values ranging from 0.7 to 51.3 microM. Kinetic analysis revealed that the mechanism of inhibition varied according to the flavonoids.
CONCLUSIONS:
These results suggest that flavonoids tested are inhibitors of hepatic CYP1A2 and that the extracts of Scutellariae radix, widely used as a hepatoprotective agent, may protect the liver through the prevention of CYPIA2-induced metabolic activation of protoxicants.
