In:
Proceedings of the National Academy of Sciences, Proceedings of the National Academy of Sciences, Vol. 98, No. 1 ( 2001-01-02), p. 60-62
Kurzfassung:
Infections with parasitic helminths are important causes of morbidity and mortality worldwide. New drugs that are parasite specific
and minimally toxic to the host are needed to counter these infections effectively. Here we report the finding of a previously unidentified
compound, nafuredin, from Aspergillus niger . Nafuredin
inhibits NADH-fumarate reductase (complexes I + II) activity, a unique anaerobic electron transport system in helminth mitochondria, at nM
order. It competes for the quinone-binding site in complex I and shows high selective toxicity to the helminth enzyme. Moreover, nafuredin
exerts anthelmintic activity against Haemonchus
contortus in in vivo trials with sheep. Thus,
our study indicates that mitochondrial complex I is a promising target for chemotherapy, and nafuredin is a potential lead compound as an
anthelmintic isolated from microorganisms.
Materialart:
Online-Ressource
ISSN:
0027-8424
,
1091-6490
DOI:
10.1073/pnas.98.1.60
Sprache:
Englisch
Verlag:
Proceedings of the National Academy of Sciences
Publikationsdatum:
2001
ZDB Id:
209104-5
ZDB Id:
1461794-8
SSG:
11
SSG:
12
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