Automated evaluation of protein binding affinity of anti-inflammatory choline based ionic liquids

Talanta
Rosa RibeiroM Lúcia M F S Saraiva

Abstract

In this work, an automated system for the study of the interaction of drugs with human serum albumin (HSA) was developed. The methodology was based on the quenching of the intrinsic fluorescence of HSA by binding of the drug to one of its binding sites. The fluorescence quenching assay was implemented in a sequential injection analysis (SIA) system and the optimized assay was applied to ionic liquids based on the association of non-steroidal anti-inflammatory drugs with choline (IL-API). In each cycle, 100 µL of HSA and 100 µL of IL-API (variable concentration) were aspirated at a flow rate of 1 mL min(-1) and then sent through the reaction coil to the detector where the fluorescence intensity was measured. In the optimized conditions the effect of increasing concentrations of choline ketoprofenate and choline naproxenate (and respective starting materials: ketoprofen and naproxen) on the intrinsic fluorescence of HSA was studied and the dissociation constants (Kd) were calculated by means of models of drug-protein binding in the equilibrium. The calculated Kd showed that all the compounds bind strongly to HSA (Kd<100 µmol L(-1)) and that the use of the drugs in the IL format does not affect or can even improve their HSA bindin...Continue Reading

References

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Citations

Jan 27, 2017·Chemical Reviews·Ksenia S EgorovaValentine P Ananikov
Dec 29, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Paula OssowiczIvan Angelov
Aug 7, 2021·International Journal of Pharmaceutics·Anita UmerskaLidia Tajber

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