title: Investigations of ibuprofen and paracetamol binding to lens proteins to explore their protective role against cataract.
abstract: There is evidence that ibuprofen and paracetamol can act as anti-cataract drugs. [14C]-Ibuprofen labelled at the methyl group of the propanoic acid moiety was synthesized. The labelled ibuprofen was found to bind non-covalently to alpha-crystallin but not to beta- and gamma-crystallin of the bovine lens. Labelled paracetamol binds to total lens soluble proteins. Both drugs penetrate into the lens cortex and nucleus within 24 hr. Affinity chromatographic studies suggest that the lipophilic isobutyl group of ibuprofen hinders binding to the lens proteins. Hence, in the light of weak binding of ibuprofen and paracetamol and strong binding of the ibuprofen analogue used in the affinity chromatography, it is suggested, in this paper, that the protection against cataract by these analgesics is possibly due to their metabolites interacting with the lens proteins.
authors.affiliation: Nuffield Laboratory of Ophthalmology, Oxford University, U.K.
authors.forename: A Z
authors.initials: AZ
authors.lastname: Shyadehi
authors.forename: J J
authors.initials: JJ
authors.lastname: Harding
mesh_terms: D000082:Acetaminophen / Q000378:metabolism* / Q000493:pharmacokinetics / Q000627:therapeutic use; D000818:Animals; D002386:Cataract / Q000517:prevention & control*; D002417:Cattle; D002846:Chromatography, Affinity; D003459:Crystallins / Q000378:metabolism*; D007052:Ibuprofen / Q000378:metabolism* / Q000493:pharmacokinetics / Q000627:therapeutic use; D007700:Kinetics; D007908:Lens, Crystalline / Q000378:metabolism
chemical_list: D003459:Crystallins; D000082:Acetaminophen; D007052:Ibuprofen