Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.8 (cholinesterase)
 12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The major compound responsible for toxicity to Artemia salina of some Fusarium tricinctum strains has been isolated, and its structure has been elucidated by spectroscopical methods, i.e. UV, IR, MS, 1H-NMR and 13C-NMR. The novel compound, trivially named visoltricin, is the first imidazole derivative produced by Fusarium spp., and its structure has been established as the methyl ester of 3-[1-methyl-4-(3-methyl-2-butenyl)-imidazol-5yl]-2-propenoic acid (molecular formula C13H18N2O2; MW = 234.297). Visoltricin was toxic to A. salina larvae (LD50 = 8.5 x 10(-7) M), and inhibited the growth of six human tumour cell lines (out of 60 lines tested) at concentrations lower than 10(-5) M. Tested on rabbit eye it showed an interesting miotic activity similar to that of pilocarpine, a miotic agent largely used in the therapy of glaucoma. This biological activity could be explained in part by the anticholinesterase properties shown by visoltricin towards both human serum and pure enzymes (EC 3.1.1.7 and EC 3.1.1.8). Kinetics studies showed for visoltricin a mixed-type and reversible inhibition of the EC 3.1.1.7 enzyme with the competitive inhibition constant (Ki) = 1.9 x 10(-4) M.
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PMID:Visoltricin, a novel biologically active compound produced by Fusarium tricinctum. 766 51