A novel inositol mono-phosphatase inhibitor from Memnoniella echinata. Producing organism, fermentation, isolation, physicochemical and in vitro biological properties

  • J Antibiot (Tokyo). 1992 Sep;45(9):1397-403. doi: 10.7164/antibiotics.45.1397.
Y K Lam  1 ,  C F Wichmann ,  M S Meinz ,  L Guariglia ,  R A Giacobbe ,  S Mochales ,  L Kong ,  S S Honeycutt ,  D Zink ,  G F Bills
Affiliations
  • 1. Merck Research Laboratories, Rahway, New Jersey 07065.
PMID: 1331013 DOI: 10.7164/antibiotics.45.1397
Abstract

A novel inositol mono-phosphatase inhibitor, L-671,776 (1), was discovered from a culture of the hyphomycete, Memnoniella echinata (ATCC 20928). 1 has a molecular weight of 388 and a molecular formula of C23H32O5. The mode of inhibition is non-competitive, with a Ki of 450 microM. It shows no inhibition of myo-inositol 1,4-bisphosphate 1-phosphatase or myo-inositol 1,4,5-triphosphate 5-phosphatase, although it weakly inhibits myo-inositol 1,4,5-triphosphate 3-kinase (IC50 = 3 mM). It elevates inositol monophosphates in rat parotid slices (EC50 approximately 3 mM), but abolishes agonist effects. It also produces short-lived contraction of guinea pig trachea at 300 microM.

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