4.5 Article

Spoxazomicins A-C, novel antitrypanosomal alkaloids produced by an endophytic actinomycete, Streptosporangium oxazolinicum K07-0460T

Journal

JOURNAL OF ANTIBIOTICS
Volume 64, Issue 4, Pages 303-307

Publisher

JAPAN ANTIBIOTICS RESEARCH ASSOC
DOI: 10.1038/ja.2011.16

Keywords

antitrypanosome; endophytic actinomycete; spoxazomicins; Streptosporangium oxazolinicum

Funding

  1. Drugs for Neglected Diseases initiative (DNDi)
  2. Quality Assurance Framework of Higher Education from the Ministry of Education, Culture, Sports, Science and Technology, Japan (MEXT)
  3. Institute for Fermentation, Osaka (IFO), Japan
  4. All Kitasato Project Study (AKPS)
  5. Grants-in-Aid for Scientific Research [21580129] Funding Source: KAKEN

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Three novel antitrypanosomal alkaloids, named spoxazomicins A-C, were isolated by silica gel column chromatography and HPLC from the culture broth of a new endophytic actinomycete species, Streptosporangium oxazolinicum K07-0460(T). The structures of the spoxazomicins were elucidated by NMR and X-ray crystal analyses and shown to be new types of pyochelin family antibiotic. Spoxazomicin A showed potent and selective antitrypanosomal activity with an IC50 value of 0.11 mu g ml(-1) in vitro without cytotoxicity against MRC-5 cells (IC50=27.8 mu g ml(-1)). The Journal of Antibiotics (2011) 64, 303-307; doi: 10.1038/ja.2011.16; published online 9 March 2011

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