4.4 Article

Rottlerin Exhibits Antiangiogenic Effects In vitro

期刊

CHEMICAL BIOLOGY & DRUG DESIGN
卷 77, 期 6, 页码 460-470

出版社

WILEY-BLACKWELL
DOI: 10.1111/j.1747-0285.2011.01121.x

关键词

cyclin D-1; endothelin converting enzyme-1; endothelial cells; endothelin-1; NF kappa B; nitric oxide; Rottlerin

资金

  1. Fondazione Monte dei Paschi di Siena
  2. Actelion

向作者/读者索取更多资源

Rottlerin, a natural product purified from Mallotus philippinensis, has a number of target molecules and biological effects. We recently found that Rottlerin caused growth arrest in MCF-7 breast cancer cells and human immortalized keratinocytes, through inhibition of NF kappa B and downregulation of cyclin D-1. To evaluate whether this effect could be generalized to primary cells, human microvascular endothelial cells were treated with Rottlerin. In this study, we demonstrated that Rottlerin prevents basal and TNF alpha-stimulated NF kappa B nuclear migration and DNA binding also in human microvascular endothelial cell, where NF kappa B inhibition was accompanied by the downregulation of NF kappa B target gene products, such as cyclin D-1 and endothelin-1, which are essential molecules for endothelial cell proliferation and survival. Rottlerin, indeed, inhibited human microvascular endothelial cells proliferation and tube formation on Matrigel. Rottlerin also increases cytoplasmic free calcium and nitric oxide levels and downregulates endothelin converting enzyme-1 expression, thus contributing to the drop in endothelin-1 and growth arrest. These results suggest that Rottlerin may prove useful in the development of therapeutic agents against angiogenesis.

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