Fungal strain NR6356, Fusarium merismoides Corda, was discovered as the source of the protein kinase C (PKC) inhibitor, azepinostatin.The strain was identified based on its growth on potato sucrose agar, slender conidial shape, characteristic polyphialide and production of abundant chlamydospores. Fusarium aquaeductuum Lagh. IMI 103658 and Fusarium sp. NR7222 were also found to produce the same inhibitor. After single colony isolation and mediumoptimization trials, a more than 30-fold increase in the production of azepinostatin over the original culture was achieved.Azepinostatin selectively and potently inhibited rat brain PKCwith an IC50 value of 70 nM. Other enzymes utilizing ATP, including hexokinase, were not affected. The Ki of azepinostatin for PKCwas 0.5 nM. The inhibition of PKCwas competitive with ATPand uncompetitive with histone.
Panclicins A, B, C, D, and E are novel pancreatic lipase inhibitors isolated from Streptomyces sp. NR0619. Structurally, panclicins A, B, C, D, and E are analogues of tetrahydrolipstatin (THL), which contains a /Mactone and a 7V-formyl leucine ester, and the IC5Os of panclicins A, B, C, D, and E for porcine pancreatic lipase are 2.9, 2.6, 0.62, 0.66, and 0.89/m, respectively. The potency of the inhibitory activity of each compoundis attributed to the aminoacid moiety of each structure. The panclicins are either glycine-type compounds such as panclicins C, D, E, which are two to
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