Gymnochromes E and F, Cytotoxic Phenanthroperylenequinones from a Deep-Water Crinoid, Holopus rangii

详细信息    查看全文

• 作者：Hilaire V. Kemami Wangun ; Alexander Wood ; Catherine Fiorilla ; John K. Reed ; Peter J. McCarthy ; Amy E. Wright
• 刊名：Journal of Natural Products
• 出版年：2010
• 出版时间：April 23, 2010
• 年：2010
• 卷：73
• 期：4
• 页码：712-715
• 全文大小：133K
• 年卷期：v.73,no.4(April 23, 2010)
• ISSN：1520-6025

文摘

Bioactivity-guided fractionation of metabolites from the crinoid Holopus rangii led to the discovery of two new phenanthroperylenequinone derivatives, gymnochromes E (1) and F (2). Gymnochrome E showed cytotoxic activity toward the NCI/ADR-Res with an IC₅₀ of 3.5 μM. It also inhibited histone deacetylase-1 with an IC₅₀ of 3.3 μM. Gymnochrome F was a moderate inhibitor of myeloid cell leukemia sequence 1 (MCL-1) binding to Bak. Two anthraquinone metabolites, emodic acid (4) and its new bromo derivative (5), were also isolated from the crinoid and show remarkable similarity to the phenanthroperylenequinone core, suggesting that these metabolites share the same polyketide biosynthetic pathway.