Dual inhibition of metallopeptidases ACE and NEP by extracts, and iridoids from Ligustrum vulgare L.
OBJECTIVE
In order to confirm the traditional use of Ligustrum vulgare L. (common privet, Oleaceae) we investigated the inhibitory activity of different extracts from leaves (LlE), flowers (LflE) and fruits (LfrE) on metallopeptidases ACE and NEP.


METHODS
Powdered plant materials were first extracted with water and then with ethyl acetate and n-butanol saturated with water. The metallopeptidases activity was determined using in vitro fluorimetric assays.


RESULTS
At a concentration of 100microg/ml the ethyl acetate extracts showed the highest activity. The bio-guided fractionation of the leaves extract led to the isolation of two iridoids which were identified by (1)H, (13)C and HETCOR NMR spectroscopy as oleuropein and ligstroside aglycones. Both compounds are dual ACE/NEP inhibitors with IC(50) of 20 and 25microM for ACE and IC(50) of 35 and 75microM for NEP, respectively. Secoirydoids glycosides, tyrozol and hydroxytyrozol, as well as, flavonoids present in the ethyl acetate extracts showed little or no inhibitory activity.


CONCLUSIONS
Our results partially support the diuretic and hypotensive activities of common privet.
Kiss
A K
AK
Department of Pharmacognosy and Molecular Basis of Phytotherapy, Medical University of Warsaw, Banacha 1, 02-098 Warsaw, Poland. akiss@wum.edu.pl
Mańk
M
M
Melzig
M F
MF
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D035264:Flowers; D005470:Fluorometry; D005638:Fruit; D005960:Glucosides / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D057888:Iridoid Glucosides; D039823:Iridoids / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D031659:Ligustrum / Q000737:chemistry*; D008297:Male; D008519:Medicine, Traditional; D015260:Neprilysin / Q000037:antagonists & inhibitors; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology*; D018515:Plant Leaves; D011714:Pyrans / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology; D013552:Swine
D000806:Angiotensin-Converting Enzyme Inhibitors; D005960:Glucosides; D057888:Iridoid Glucosides; D039823:Iridoids; D010936:Plant Extracts; D011714:Pyrans; C002769:oleuropein; C445380:ligstroside; D015260:Neprilysin