Antiprotease effect of anti-inflammatory lupeol esters

Macrides, T, Kweifio-Okai, G and Hodges, L 2003, 'Antiprotease effect of anti-inflammatory lupeol esters', Molecular and Cellular Biochemistry, vol. 252, no. 1, pp. 97-101.

Document type: Journal Article
Collection: Journal Articles

Title Antiprotease effect of anti-inflammatory lupeol esters
Author(s) Macrides, T
Kweifio-Okai, G
Hodges, L
Year 2003
Journal name Molecular and Cellular Biochemistry
Volume number 252
Issue number 1
Start page 97
End page 101
Total pages 4
Publisher Kluwer Academic Publishers
Abstract Lupeol-3-palmitate (LP) and lupeol-3-linoleate (LL), two synthetic long chain fatty acid ester analogues of the plant-derived anti-inflammatory pentacyclic triterpenoid lupeol (L), were studied in vitro as potential inhibitors of serine protease activity. With respect to the natural protein substrate bovine serum albumin (BSA), lupeol palmitate and lupeol linoleate inhibited trypsin activity in a manner consistent with mixed inhibition (KIC values of 103 and 52 M respectively; KIU values of 30 and 14 M respectively). However, the lupeol esters showed no inhibitory effect on the catalytic activity of porcine pancreatic elastase (PPE) with respect to the synthetic tetrapeptide substrate succinyl-(alanyl)3-p-nitroanilide (SAAANA). The present paper shows the lupeol triterpenes to be selective protease inhibitors.
Subject Basic Pharmacology
DOI - identifier 10.1023/A:1025569805468
Copyright notice © 2003 Kluwer Academic Publishers. Printed in the Netherlands.
ISSN 0300-8177
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