Toth, I., Hughes, R.A., Munday, M., Murphy, M.R., Mascagni, C.A. and Gibbons, W.A. (1991) Lipidic peptides. II. Synthesis, activity and transport of anti-inflammatory benzoquinolizine-lipidic peptide conjugates. International Journal of Pharmaceutics, 68 (1-3). pp. 191-198. 10.1016/0378-5173(91)90141-A.
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Two series of lipidic peptide conjugates 1c-1i and 2c-2e of the anti-inflammatory benzoquinolizine alkaloids 1b and 2b were synthesised. The biological activities 1c, 1d and 1f were assessed by determining their ability to inhibit the release of histamine from rat mast cells in vitro. Conjugates 1d and 1f, their parent alkaloid 1b and its methyl ester 1a, gave 40-50% inhibition, whereas conjugate 1c showd 2-fold greater activity. The radiolabelled compounds 2a* and 2c* were produced by reduction of 1a and 1f with NaB3H4. Following their oral administration to rats, peak serum levels of the conjugate 2c* were 5 times greater than that observed for the parent compound 2a*. The results suggest that conjugation of lipidic amino acids and peptides can be a useful aproach to improving the oral absorption of poorly absorbed drugs.
|Uncontrolled Keywords:||Anti-inflammatory drug; Histamine release; Lipidic amino acid; Lipidic peptide; Oral absorption; Transmembrane drug delivery|
|Departments, units and centres:||Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry|
|Journal or Publication Title:||International Journal of Pharmaceutics|
|Deposited By:||Library Staff|
|Deposited On:||22 Mar 2012 14:18|
|Last Modified:||22 Mar 2012 14:18|
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