Synthesis and Characterization of Destruxins

In the August issue of J. Antibiotics (Tokyo) Yoshida and coworkers at the University of Tsukuba reviewed their excellent work on synthesis, SAR, biology and chemical biology of the Destruxins, fungal cyclodepsipeptides from Metarhizium sp. They developed a practical synthesis using a macrolactonization strategy allowing gram scale production; synthesized 64 analogs; carried out SAR studies; and prepared azide sidechain analogs for click chemistry-based target identification. Destruxins reversibly inhibit the bone resorption activity of osteoclasts by inducing morphological changes without affecting cell viability. It also blocks growth of hepatocellular carcinoma cells via modulation of the Wnt/β-catenin pathway.

Focus Biomolecules offers Destruxin A and Destruxin B for research applications.