Title : Thiolation of polycarbophil enhances its inhibition of intestinal brush border membrane bound aminopeptidase N.

Pub. Date : 2001 Nov

PMID : 11745748






8 Functional Relationships(s)
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1 Thiolation of polycarbophil enhances its inhibition of intestinal brush border membrane bound aminopeptidase N. calcium polycarbophil alanyl aminopeptidase, membrane Sus scrofa
2 Aminopeptidase N activity was assayed spectrophotometrically using L-leucine p-nitroanilide (leu-pNA) as a synthetic substrate and against the model peptide drug leu-enkp, by high-performance liquid chromatography (HPLC). H-LEU-PNA alanyl aminopeptidase, membrane Sus scrofa
3 Aminopeptidase N activity was assayed spectrophotometrically using L-leucine p-nitroanilide (leu-pNA) as a synthetic substrate and against the model peptide drug leu-enkp, by high-performance liquid chromatography (HPLC). L-Leucine-p-nitroanilide alanyl aminopeptidase, membrane Sus scrofa
4 Free cysteine at 6.3 and 63 microM (pH 6) significantly (p < 0.05) inhibited aminopeptidase N activity, and PCP-Cys (0.25% w/v, pH 6) had a significantly (p < 0.05) greater inhibitory effect than PCP on the aminopeptidase N activity towards both substrates. Cysteine alanyl aminopeptidase, membrane Sus scrofa
5 Free cysteine at 6.3 and 63 microM (pH 6) significantly (p < 0.05) inhibited aminopeptidase N activity, and PCP-Cys (0.25% w/v, pH 6) had a significantly (p < 0.05) greater inhibitory effect than PCP on the aminopeptidase N activity towards both substrates. pcp-cys alanyl aminopeptidase, membrane Sus scrofa
6 PCP-Cys completely protected leu-enkp against aminopeptidase N activity over a 2-h incubation period, whereas 83 +/- 4 and 60 +/- 7% remained stable in the presence of PCP and buffer only, respectively. pcp-cys alanyl aminopeptidase, membrane Sus scrofa
7 PCP-Cys completely protected leu-enkp against aminopeptidase N activity over a 2-h incubation period, whereas 83 +/- 4 and 60 +/- 7% remained stable in the presence of PCP and buffer only, respectively. pcp alanyl aminopeptidase, membrane Sus scrofa
8 Thiolation of PCP increased the stability of leu-enkp against the enzymatic degradation by aminopeptidase N and the intact intestinal mucosa, identifying a promising new excipient for peroral delivery of peptides. pcp alanyl aminopeptidase, membrane Sus scrofa