Leucinostatin A

BeschreibungLeucinostatin A is a fungal metabolite originally isolated from P. lilacinus with diverse biological activities. It is active against P. oryzae, B. cinera, P. chrysogenum, X. oryzae, S. cerevisiae, and C. albicans fungi and B. subtilis, S. aureus, S. lutea, and M. phlei bacteria in a disc assay. Leucinostatin A (0.1-1 μg/ml) reduces T cell activation induced by phorbol 12-myristate 13-acetate (TPA; ) or an anti-CD3 antibody in a concentration-dependent manner. It inhibits proliferation of DU145 prostate cancer cells co-cultured with PrSC stromal cells in vitro (IC50 = 0.045 μg/ml).

VerwendenLeucinostatin A is the major component of an atypical nonapeptide complex produced by Paecilomyces lilacinus, first reported in 1973. Leucinostatins display broad bioactivity against Gram positive bacteria, fungi, plants and tumour cell lines. Leucinostatin A inhibits respiration by uncoupling oxidative phosphorylation and is potentiated by inhibitors such as venturicidin and oligomycin. More recently, interest in leucinostatin has focused on understanding its activity as an insulin-like growth factor I regulator, an ionophore, inhibitor of cell surface expression of viral glycoproteins and its anti-trypanosomal activity.