Strongylophorines: Natural Product Inhibitors of Hypoxia-Inducible Factor-1 Transcriptional Pathway

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• 作者：Kaleem A. Mohammed ; Raquel C. Jadulco ; Tim S. Bugni ; Mary Kay Harper ; Megan Sturdy ; Chris M. Ireland
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：March 13, 2008
• 年：2008
• 卷：51
• 期：5
• 页码：1402 - 1405
• 全文大小：221K
• 年卷期：v.51,no.5(March 13, 2008)
• ISSN：1520-4804

文摘

Rapidly increasing experimental and clinical data provides evidence for the role of hypoxia inducible factor-1 (HIF-1) as a crucial mediator of tumor survival and progression. In our effort to identify inhibitors of the HIF-1 activation pathway, we screened fractions from marine invertebrates. Fractions from an extract of Petrosia (Strongylophora) strongylata potently inhibited the HIF-1 activation pathway. Strongylophorines 2, 3, and 8 isolated from the active fractions were found to be responsible for the HIF-1 inhibition with EC₅₀ values of 8, 13, and 6 µM, respectively.