Screening of selected basidiomycetes for inhibitory activity on neutral endopeptidase (NEP) and angiotensin-converting enzyme (ACE).
Aqueous extracts of 27 basidiomycetes were investigated for their ability to inhibit the activity of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP). The extracts of 5 fungi inhibited both, ACE and NEP activity, another 18 extracts showed inhibition of the NEP activity whereas only 1 basidiomycete inhibited the ACE activity exclusively. The IC50 values for the ACE inhibition are rather high (between 200 and 1500 micrograms/ml) in comparison to the IC50 of the NEP inhibition (between 40 and 2000 micrograms/ml). These results indicate that the basidiomycetes investigated seem to have a higher potential for the inhibition of the activity of NEP than of ACE. In general, basidiomycetes are a new source for inhibitors of metalloendopeptidases. Resulting from the isolation and characterization of these compounds new leading structures are expectable.
Melzig
M F
MF
Institute for Molecular Pharmacology, Ernst-Moritz-Arndt-University, Greifswald, Germany.
Pieper
S
S
Siems
W E
WE
Heder
G
G
Bóttger
A
A
Liberra
K
K
Lindequist
U
U
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D001487:Basidiomycota / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D015260:Neprilysin / Q000037:antagonists & inhibitors*; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology
D000806:Angiotensin-Converting Enzyme Inhibitors; D004791:Enzyme Inhibitors; D011480:Protease Inhibitors; D015260:Neprilysin