Herboxidiene (142861-00-5) is a novel polyketide fermentation product produced by Streptomyces chromofuscus, originally discovered by screening for herbicidal activity. Potent and selective inhibitor of spliceosome subunit SF3b.2?Specifically targets SAP155, a subunit of SF3b responsible for pre-mRNA splicing.3?Displays anti-angiogenic activity via down-regulation of VEGFR-2 and HIF-1α.4?Spliceosome inhibitors have attracted enormous attention due to their potential use in cancer treatment.5
Herboxidiene is an anticancer agent. Herboxidiene is used in the lowering of plasma cholesterol, pre-mRNA splicing-modulatory action and in anti-tumor activity in numerous cell lines. It also exhibits herbicidal properties.
1) Miller-Wideman?et al.?(1992),?Herboxidiene, a new herbicidal substance from Streptomyces chromofuscus A7847. Taxonomy, fermentation, isolation, physio-chemical and biological properties; J. Antibiot. (Tokyo),?45?914
2) Gao?et al.?(2013),?Comparison of splicing factor 3b inhibitors in human cells; Chembiochem,?14?49
3) Hasegawa?et al.?(2011),?Identification of SAP155 as the target of GEX1A (Herboxidiene), an antitumor natural product; ACS Chem. Biol.,?6?229
4) Jung?et al.?(2015),?Antiangiogenic activity of herboxidiene via downregulation of vascular endothelial growth factor receptor-2 and hypoxia-inducible factor-1α; Arch. Pharm. Res.,?38?1728
5) Martinez-Montiel?et al.?(2016),?Microbial and Natural Metabolites That Inhibit Splicing: A Powerful Alternative for Cancer Treatment;?Biomed. Res. Int.,?2016?3681094