Process for preparing purified S-BEL and R-BEL and compositions thereof
AssigneeWashington University in St. Louis
InventorRichard W. Gross
Life of this patent
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Abstract
A process for resolution of racemic BEL into its individual enantiomeric constituents by chiral HPLC. A method for determining the role of specific isoforms of iPLA2 in biologic processes.
Claims6
A method of identifying whether a lipase enzyme is metabolically active within a cellular environment, said method comprising contacting said cellular environment with at least one of S-isomer bromoenal lactone (S-BEL) and R-isomer bromoenal lactone (R-BEL) and determining the identity of the lipase enzyme based on the interaction of the lipase enzyme with at least one of S-BEL and R-BEL, wherein the S-BEL selectively inhibits β phospholipase and the R-BEL selectively γ phospholipase.
A diagnostic kit for determining the metabolic activity of a lipase within a cellular environment, wherein said kit comprises a lipase for which it is desired to determine the metabolic activity, contacting said cellular environment with at least one of S-isomer bromoenal lactone (S-BEL) and R-isomer bromoenal lactone (R-BEL) and determining at least one of an identify and an activity of the lipase based on the interaction of said lipase with at least one of S-BEL and R-BEL, wherein the S-BEL selectively inhibits β phospholipase and the R-BEL selectively inhibits γ phospholipase.
A method of differentially inhibiting at least one of iPLA2β and iPLA2γ by contacting the same with S-isomer bromoenal lactone (S-BEL), observing a selectivity of S-BEL toward one of iPLA2β or iPLA2γ and determining that one of iPLA2β or iPLA2γ has been inhibited.
A method for pharmacologically distinguishing iPLA2β from iPLA2γ, said method comprising contacting a candidate iPLA2 with S-BEL and if the S-isomer bromoenal lactone (S-BEL) is selective to the candidate iPLA2, then determining that the iPLA2 is iPLA2β.
Dependencies are inferred from the claim text.