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 on...

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Bibliographic Details
Published inPharmazie Vol. 51; no. 7; p. 501
Main Authors Melzig, M F, Pieper, S, Siems, W E, Heder, G, Bóttger, A, Liberra, K, Lindequist, U
Format Journal Article
LanguageEnglish
Published Germany 01.07.1996
Subjects
Angiotensin-Converting Enzyme Inhibitors - chemistry
Angiotensin-Converting Enzyme Inhibitors - pharmacology
Basidiomycota - chemistry
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Neprilysin - antagonists & inhibitors
Protease Inhibitors - chemistry
Protease Inhibitors - pharmacology
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Summary: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.
ISSN:0031-7144