Skullcapflavone I

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.

Int Immunopharmacol. 2011 Jan;11(1):79-84.

In vitro modulation of LPS/calcimycin induced inflammatory and allergic mediators by pure compounds of Andrographis paniculata (King of bitters) extract.[Pubmed: 21034865]

METHODS AND RESULTS:
The aim of the current study is to probe the anti-inflammatory/anti-allergic potential of seven phytoconstituents (andrographolide, neoandrographolide, isoandrographolide, andrograpanin, 14-deoxy-11,12-didehydroandrographolide, 7-O-methylwogonin and Skullcapflavone I) isolated from Andrographis paniculata (King of bitters) on the production of key inflammatory/allergic mediators (NO, PGE(2), IL-1 beta, IL-6, LTB(4), TXB(2) and histamine). The results demonstrated that andrographolide, isoandrographolide, 7-O-methylwogonin and Skullcapflavone I significantly inhibited LPS stimulated NO and PGE(2) release in J774A.1 macrophages. Andrographolide, isoandrographolide and 7-O-methylwogonin showed considerable inhibition of IL-1 beta production in LPS elicited macrophages. LPS induced IL-6 production was significantly inhibited by andrographolide, isoandrographolide and Skullcapflavone I in a concentration dependent manner. The results revealed that andrographolide, isoandrographolide and Skullcapflavone I significantly decreased TXB(2) release in A23187 activated HL-60 promyelocytic cells. Furthermore, the anti-allergic properties of the phytoconstituents was investigated on A23187 induced LTB(4) production (HL-60 cells) and histamine release (RBL-2H3 basophilic cells). The results showed that only Skullcapflavone I and 7-O-methylwogonin showed marked inhibitory effect on LTB(4) production, however, only 7-O-methylwogonin exerted dose-dependent inhibition towards histamine release.
CONCLUSIONS:
Therefore, this study indicates that some of these phytoconstituents exhibit potent anti-inflammatory/anti-allergic effects by modulating different inflammatory/allergic mediators. Hence, these phytoconstituents might provide useful phytomedical treatment against variety of inflammatory and allergic disorders.