Heilpflanzen-Welt - Die Welt der Heilpflanzen!
Heilpflanzen-Welt - Natürlich natürlich!
December 2024

Planta Med. 2002 Oct; 68(10): 930-2.

Triterpenes and phytosterols as human leucocyte elastase inhibitors.

Mitaine-Offer AC, Hornebeck W, Sauvain M, Zèches-Hanrot M.

Laboratoire de Pharmacognosie, Faculté de Pharmacie, Université de Reims Champagne-Ardenne, Reims, France. [email protected]

Ten triterpenes and phytosterols beta-amyrin, lupeol, lupeol acetate, ursolic acid, friedelin, canophyllol, 29-hydroxy-friedelan-3-one, beta-sitosterol, 3- O-beta- D-glucopyranosyl-beta-sitosterol, 3-O-(6'- O-palmitoyl)-beta-D-glucopyranosyl-beta-sitosterol, were evaluated as potential inhibitors of human leucocyte elastase (HLE). In this series, lupeol, ursolic acid and canophyllol showed marked HLE inhibitory activity with IC(50) values at 1.9 microM, 4.4 microM, and 2.5 microM, respectively. It appeared that HLE inhibition depended on the presence and the orientation of two reactive groups in the tested molecules, distant from 10-12 A, reacting with Arg-217 in S(4) -S(5) subsites of the extended substrate-binding domain of HLE, and S(3), respectively.


Search only the database: 

© Top Fit Gesund, 1992-2024. Alle Rechte vorbehalten – ImpressumDatenschutzerklärung