PMID- 12391559
OWN - NLM
STAT- MEDLINE
DCOM- 20021217
LR  - 20041117
IS  - 0032-0943 (Print)
IS  - 0032-0943 (Linking)
VI  - 68
IP  - 10
DP  - 2002 Oct
TI  - Triterpenes and phytosterols as human leucocyte elastase inhibitors.
PG  - 930-2
AB  - 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.
FAU - Mitaine-Offer, Anne-Claire
AU  - Mitaine-Offer AC
AD  - Laboratoire de Pharmacognosie, Faculte de Pharmacie, Universite de Reims 
      Champagne-Ardenne, Reims, France. acoffer@u-bourgogne.fr
FAU - Hornebeck, William
AU  - Hornebeck W
FAU - Sauvain, Michel
AU  - Sauvain M
FAU - Zeches-Hanrot, Monique
AU  - Zeches-Hanrot M
LA  - eng
PT  - Journal Article
PL  - Germany
TA  - Planta Med
JT  - Planta medica
JID - 0066751
RN  - 0 (Phytosterols)
RN  - 0 (Triterpenes)
RN  - EC 3.4.21.37 (Leukocyte Elastase)
SB  - IM
MH  - Bignoniaceae
MH  - Caesalpinia
MH  - Humans
MH  - Inhibitory Concentration 50
MH  - Leukocyte Elastase/*antagonists & inhibitors/*drug effects
MH  - Moraceae
MH  - Phytosterols/administration & dosage/*pharmacology
MH  - *Phytotherapy
MH  - *Plants, Medicinal
MH  - Triterpenes/administration & dosage/*pharmacology
EDAT- 2002/10/23 04:00
MHDA- 2002/12/18 04:00
CRDT- 2002/10/23 04:00
PHST- 2002/10/23 04:00 [pubmed]
PHST- 2002/12/18 04:00 [medline]
PHST- 2002/10/23 04:00 [entrez]
AID - 10.1055/s-2002-34929 [doi]
PST - ppublish
SO  - Planta Med. 2002 Oct;68(10):930-2. doi: 10.1055/s-2002-34929.