Herboxidiene is a polyketide originally isolated from S.
CAS：142861-00-5
分子式：C5H42O6
分子量：438.6
纯度：98%
存储：Store at -20°C

Background:

Herboxidiene is a polyketide originally isolated from S. chromofuscus that has diverse biological activities.[1],[2,][3],[4],[5] It inhibits growth of HeLa S3, SK-MEL-2, PC3, A549, and EBC-1 cells with GI50 values ranging from 7.4 to 62 nM.3 Herboxidiene is cytostatic against human umbilical vein endothelial cells (HUVECs; (IC50 = 26 nM)) and inhibits VEGF-induced invasion and tube formation of serum-starved HUVECs in a concentration-dependent manner, indicating antiangiogenic activity.[4] Herboxidiene (0.05 μM) inhibits HIF-1α mRNA splicing and reduces HIF-1α protein levels in HepG2 cells grown under hypoxic conditions. It also inhibits splicing of p27Kip mRNA in HeLa cells in a concentration-dependent manner via interaction with the SAP155 subunit of the SF3b complex.[2] Herboxidiene (0.1 and 1 μM) increases LDL receptor promoter-driven transcription in a cell-based reporter assay.[5] It also exhibits herbicidal activity against wild buckwheat, morning glory, maize, hemp sesbania, and rapeseed when applied at 0.069 kg/hectare.[1]

Reference:
[1]. Miller-Wideman, M., Makkar, N., tran, M.G.B., et al. Herboxidiene, a new herbicidal substance from Streptomyces chromofuscus A7847. Taxonomy, fermentation, isolation, physico-chemical and biological properties. J. Antibiot. (Tokyo) 45(6), 914-921 (1992).
[2]. Hasegawa, M., Miura, T., Kuzuya, K., et al. Identification of SAP155 as the target of GEX1A (Herboxidiene), an antitumor natural product. ACS Chem Biol. 6(3), 229-233 (2011).
[3]. Imaizumi, T., Nakagawa, H., Hori, R., et al. The synthesis and evaluation of the antiproliferative activity of deacidified GEX1A analogues. J Antibiot (Tokyo) 70(5), 675-679 (2017).
[4]. Jung, H.J., Kim, Y., Shin, J.Y., et al. Antiangiogenic activity of herboxidiene via downregulation of vascular endothelial growth factor receptor-2 and hypoxia-inducible factor-1α. Arch. Pharm. Res. 38(9), 1728-1735 (2015).
[5.] Koguchi, Y., Nishio, M., Kotera, J., et al. Trichostatin A and herboxidiene up-regulate the gene expression of low density lipoprotein receptor. J. Antibiot. (Tokyo). 50(11), 970-971 (1997).