Pharmacokinetics of diphenylboroxazolidones of L-α-amino acids with activity on the CNS: Quantification in rat DBS by UPLC-MS/MS

Alberto Garcáa González, Leticia Contreras Zavala, Alionka P.Angeles Moreno, Eduardo Ramárez San Juan, José G.Trujillo Ferrara, Liliana Rivera Espinosa, Gabriel Marcelán Jiméez

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10 Scopus citations


Background: A growing number of boron-containing compounds exhibit many important biological activities; of particular interest are the αamino acid borinic derivatives with activity in the CNS. A validated, sensitive and specific UPLC-MS/MS technique for quantification of the diphenylboroxazolidones of glycine (DBPX-gly), L-aspartate (DPBX-L-asp) and L-glutamate (DPBX-L-glu) in dried blood spots (DBSs) is presented. Results: The most intense signal corresponds to compounds with11B. The extraction procedure was liquid elution of 3.2-mm punched DBSs with acetonitrile:aqueous formic acid 0.1% (80:20 v/v). Assays proved to be linear, falling accurately and precisely within the range of 0.3-50 μg/ml for DPBX-L-asp and DPBX-L-glu and 0.1-5 μg/ml for DBPX-gly. Chromatograms exhibit clean 2.0-min running time peaks and S/N ratios for the LLOQ were approximately 15:1. The technique was used to evaluate the pharmacokinetics of the molecules and to correlate these with timecourse toxic effects. Conclusion: DBSs represent an advantage for the collection of small volumes of samples, and also in terms of processing and storage. UPLC-MS/MS allow us not only to identify the isotopic pattern of boron in DBPX, but also to quantify them with accuracy and specificity. Pharmacokinetics of these molecules exhibit a high apparent volume of distribution; it suggests a preference of DPBX-amino acids for fatty tissues such as the CNS. © 2011 Future Science Ltd.
Original languageAmerican English
Pages (from-to)439-448
Number of pages10
StatePublished - 1 Feb 2011

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