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Thromb Haemost 1999; 81(03): 423-427
DOI: 10.1055/s-0037-1614489
Review Article
Schattauer GmbH

The Activation of Plasminogen Activator Inhibitor-1 Expression by IL-1β Is Attenuated by Estrogen in Hepatoblastoma HepG2 Cells Expressing Estrogen Receptor α

Edward J. Kilbourne
1   From the Women’s Health Research Institute, Wyeth-Ayerst Research, Radnor, PA, USA
,
Marshall S. Scicchitano
1   From the Women’s Health Research Institute, Wyeth-Ayerst Research, Radnor, PA, USA
› Author Affiliations
Further Information

Publication History

Received10 July 1998

Accepted after revision04 December 1998

Publication Date:
09 December 2017 (online)

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Summary

A low estrogen status in postmenopausal women is associated with elevated plasma levels of plasminogen activator inhibitor-1 (PAI-1). In this study, the ability of estrogen compounds to regulate PAI-1 expression was determined in a hepatocyte HepG2 cell line made to stably express estrogen receptor α (ERα). In both the wild type and ER expressing HepG2 cells, estrogen had no effect on basal PAI-1 expression. However, in the ER expressing cells the ability of IL-1β to increase PAI-1 mRNA and protein levels was attenuated by 17β-estradiol, tamoxifen and twelve estrogen components of Premarin. In contrast, the mixed agonist/antagonist raloxifene had weak agonist activity and like the pure antagonist ICI 182780, it dose dependently blocked the effect of 17β-estradiol on IL-1β stimulated PAI-1 levels. These results suggest that estrogen agonists may lower PAI-1 levels in vivo by inhibiting cytokine activated PAI-1 expression by an ER dependent mechanism.

 

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