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 (APLH) 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 a cell cycle inhibitor and more than 10,000 as high as albonoursin, indicating that ΔPLH is a promising leading compound for anticancer drugs.