Actinoallolides A-E, new anti-trypanosomal macrolides, produced by an endophytic actinomycete, actinoallomurus fulvus MK10-036
Date Issued
2015-01-01
Author(s)
Inahashi, Yuki
Iwatsuki, Masato
Ishiyama, Aki
Matsumoto, Atsuko
Hirose, Tomoyasu
Oshita, Jun
Sunazuka, Toshiaki
Panbangred, Watanalai
Takahashi, Yoko
Otoguro, Kazuhiko
Ōmura, Satoshi
DOI
10.1021/ol5037216
Abstract
Five new anti-trypanosomal macrolides, actinoallolides A-E (1-5), were discovered from the cultured broth of Actinoallomurus fulvus MK10-036. The structures of the actinoallolides, including absolute stereochemistry, were elucidated by a combination of spectroscopic analyses and a series of chemical derivatization studies. Actinoallolide A showed the most potent and selective in vitro anti-trypanosomal activity without cytotoxicity. A new class of promising lead compounds was identified for the development of drugs for both sleeping sickness and Chagas disease.