Diaporthichalasin, a novel CYP3A4 inhibitor from an endophytic Diaporthe sp

A novel CYP3A4 inhibitor, diaporthichalasin, together with pycnidione were isolated from an endophytic fungus, Diaporthe sp. Their structures were elucidated on the basis of spectral data and the structure of diaporthichalasin was confirmed by X-ray crystallographic analysis. Diaporthichalasin exhib...

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Bibliographic Details
Published in:Tetrahedron letters 2007-01, Vol.48 (4), p.651-655
Main Authors: Pornpakakul, Surachai, Roengsumran, Sophon, Deechangvipart, Suchon, Petsom, Amorn, Muangsin, Nongnuch, Ngamrojnavanich, Nattaya, Sriubolmas, Nongluksna, Chaichit, Narongsak, Ohta, Tomihisa
Format: Article
Language:English
Subjects:
CYP3A4 inhibitor
Cytochalasin
Diaporthe
Endophytic fungi
Phomopsichalasin
Secondary metabolite
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Summary:A novel CYP3A4 inhibitor, diaporthichalasin, together with pycnidione were isolated from an endophytic fungus, Diaporthe sp. Their structures were elucidated on the basis of spectral data and the structure of diaporthichalasin was confirmed by X-ray crystallographic analysis. Diaporthichalasin exhibited significantly potent inhibition of CYP3A4 with an IC 50 value of 0.626 μM, while the IC 50 value of pycnidione was 465 μM.
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2006.11.102