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Short Paper | Special issue | Vol 84, No. 2, 2012, pp.1245-1250
Published online, 22nd June, 2011
DOI: 10.3987/COM-11-S(P)18
Nonactin and Related Compounds Found in a Screening Program for Wnt Signal Inhibitory Activity

Yuuya Tamai, Kazufumi Toume, Midori A. Arai, Akinori Hayashida, Hikaru Kato, Yoshikazu Shizuri, Sachiko Tsukamoto, and Masami Ishibashi*

*Department of Natural Products Chemistry, Graduate School of Pharmaceutical Science, Chiba University, 1-33 Yayoi-cho, Inage-ku, Chiba 263-8522, Japan


A screening study using a luciferase assay to identify natural products with inhibitory activity against Wnt signaling was carried out. Fractionation of the culture extract of an actinomycete, strain CKK179, led to the identification of nonactin (1), monactin (2), and dinactin (3) as active compounds. We examined the effects of dimeric dinactin (4), isolated from another actinomycete, Streptomyces sp. (YM09-028), on Wnt signaling activity and found that 1 - 4 inhibited TCF/β-catenin transcriptional activity with IC50 values of 0.6 - 7.4 nM.