Melzig M F, Pieper S, Siems W E, Heder G, Bóttger A, Liberra K, Lindequist U
Institute for Molecular Pharmacology, Ernst-Moritz-Arndt-University, Greifswald, Germany.
Pharmazie. 1996 Jul;51(7):501-3.
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.
对27种担子菌的水提取物进行了研究，以考察它们抑制血管紧张素转换酶（ACE）和中性内肽酶（NEP）活性的能力。5种真菌的提取物同时抑制了ACE和NEP的活性，另外18种提取物表现出对NEP活性的抑制，而只有1种担子菌仅抑制ACE的活性。与NEP抑制的IC50值（40至2000微克/毫升）相比，ACE抑制的IC50值相当高（200至1500微克/毫升）。这些结果表明，所研究的担子菌对NEP活性的抑制潜力似乎高于对ACE活性的抑制潜力。总体而言，担子菌是金属内肽酶抑制剂的新来源。通过这些化合物的分离和表征有望得到新的先导结构。
