New derivatives of tenvermectins through biotransformation as potential insecticides

Abstract

Tenvermectins (TVMs) belongs to the 16-membered macrolactone family antibiotics with attractive insecticidal properties. In order to discover more potent TVM derivatives, microbial transformation of TVM-A and TVM-B by Penicilium griseofulvum CICC 40293 and Bacillus subtilis ATCC 6633 were investigated and offered us six new metabolites ( 1-5 , 7 ) with regioselectivity, especially rare glycosuccinylated products, in addition to two known compounds ( 6 , 8 ). Their chemical structures were well characterized via HR-ESI-MS and 1D/2D NMR spectra. All these metabolites exhibited good acaricidal and nematicidal activities against Tetranychus cinnabarinus and Bursaphelenchus xylophilus . These results indicated that the metabolites 1 - 8 can serve as potential leads for future development of new insecticides. • Six new tenvermectin derivatives and two known compounds were obtained through biotransformation. • All the metabolites exhibited good acaricidal and nematicidal activities. • The conversion products can serve as potential leads for future development of new insecticides.