Triterpenes and phytosterols as human leucocyte elastase inhibitors.

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Mitaine-Offer AC, Hornebeck W, Sauvain M, Zeches-Hanrot M

Triterpenes and phytosterols as human leucocyte elastase inhibitors.

Planta Med. 2002 Oct;68(10):930-2. doi: 10.1055/s-2002-34929.

PubMed ID

12391559 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Lupeol	Neutrophil elastase	Protein	Humans	Unknown	Inhibitor	Details
Ursolic acid	Neutrophil elastase	Protein	Humans	Unknown	Inhibitor	Details