Skullcapflavone I from Scutellaria baicalensis induces apoptosis in activated rat hepatic stellate cells.
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. 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. From these results, skullcapflavone I from S. baicalensis selectively induced apoptosis in T-HSC/Cl-6 cells via caspase-3 and caspase-9 activation.
Park
Eun-Jeon
EJ
Department of Pharmacy, Wonkwang University, Iksan, Jeonbuk, Republic of Korea.
Zhao
Yu-Zhe
YZ
Lian
Lihua
L
Kim
Youn-Chul
YC
Sohn
Dong Hwan
DH
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D017209:Apoptosis / Q000187:drug effects*; D020169:Caspases / Q000378:metabolism; D002478:Cells, Cultured; D047309:Flavones / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D005434:Flow Cytometry; D008099:Liver / Q000166:cytology / Q000187:drug effects* / Q000201:enzymology; D008103:Liver Cirrhosis / Q000188:drug therapy; D008297:Male; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D018517:Plant Roots; D051381:Rats; D017207:Rats, Sprague-Dawley; D031364:Scutellaria baicalensis
D000972:Antineoplastic Agents, Phytogenic; D047309:Flavones; D010936:Plant Extracts; C506426:skullcapflavone I; D020169:Caspases