Discovery of diketopiperazine alkaloids from an endophytic Kitasatospora sp. by heterologous expression
Guiyang Wang1, Yuanjuan Wei1, Yan Li2
1Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.
Abstract:
Heterologous expression of a tRNA-dependent cyclodipeptide synthase (CDPS)-containing biosynthetic gene cluster from the endophytic Kitasatospora sp. CPCC204717 resulted in the discovery of two novel diastereoisomeric 3-hydroxy-2-oxindole diketopiperazine alkaloids (1-2) along with three known congeners cyclo-L-tryptophan-L-tryptophan (3), guanitrypmycin C3-2 (4), and guanitrypmycin C3-1 (5). Their structures were elucidated by extensive spectroscopic analyses combined with ECD calculations. Compound 2 exhibited antibacterial activities against Staphylococcus aureusa while 1-5 displayed binding affinities and inhibitory effects against CYP121.
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