A Novel Potent Cell Cycle Inhibitor Dehydrophenylahistin

Enzymatic Synthesis and Inhibitory Activity toward Sea Urchin Embryo

Abstract

A novel dehydrogenated cyclic dipeptide named as dehydrophenylahistin (ΔPLH) was effectively prepared from a fungal metabolite (-)-phenylahistin by the enzymatic conversion catalyzed by the cell-free extract of Streptomyces albulus KO-23, an albonoursin-producing actinomycete. ΔPLH exhibited more than 1, 000 times as high potent inhibitory activity toward the first cleavage of sea urchin embryos as (-)-phenylahisitn which has been reported to be cell cycle inhibitor and more than 10, 000 as high as albonoursin, indicating that ΔPLH is a promising leading compound for anticancer drugs.