C-P compounds, biological activities and medical uses.

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Since Horiguchi and Kandatsu first isolated natural C-P compound, 2-aminoethyl-phosphonate, much work has been carried out in Japan. Theme of the present 2-years project were (1) isolation and identification, (2) tissue distribution, (3) biological activities, (4) biosynthesis and (5) chemical synthesis of the C-P compounds.Following results were obtaied : (Theme 1) Several new C-P sphingoglycolipids were isolated from protostomia. Their carbohydrate and oligosaccharide structures were different from those of deuterostomia. A glycolipid had one mole each of 2-aminoethylphosphonate (C-P) and phosphoethanolamine (C-O-P) which suggests a way of molecular evolution of sphingoglycolipid species. (Theme 2) antiphosphonoglycocerebroside antisera specifically stain nervous tissues of crustacea. (Theme 3) C-P sphingoglycolipids isorated from Aplysia activated cAMP-dependent protein kinase by binding to the catalytic subunit of the enzyme. (theme 4) Genes of phosphoenolpyruvic acid (PnPy) phosphomutase and PnPy decarboxylase which were key enzymes for the synthesis of fosfomycin were cloned and a gene of p-methylating enzyme for the synthesis of C-P-C bond of bialaphos was cloned. (Theme 5) Oxygen of hemiacetal ring of sugar was replaced by phosphorus by sophisticated methods and many novel C-P compounds were chemically synthesized. Some of them were biologically active.