MilbemycinA3 is a member of a complex family of macrocyclic lactones that contain a characteristic spiroketal group produced from the fermentation of soil bacterium S. hygroscopicus subsp. aureolacrimosus. As a compound that potentiates glutamate and GABA-gated chloride-channel opening, milbemycinA3 is used as a nematocide and insecticide. The acaricidal and nematocidal activity of a mixture of milbemycinA3 and milbemycin A4 against adult spider mites, spider mite eggs, and C. elegans are reported at IC50 values of 5.3, 41.1, and 9.5 μg/ml.
Milbemectin is composed of 30% milbemycinA3 and 70% milbemycin A4, exhibiting acaricidal and nematocidal properties effective against adult spider mites, their eggs, and C. elegans, with IC50 values of 5.3, 41.1, and 9.5 µg ml, respectively. It functions as an allosteric agonist of the Drosophila RDL GABA receptor, and demonstrates efficacy against the pinewood nematode, B. xylophilus, with an LC20 of 0.0781 mg liter.