Brefeldin A

BFA, Cyanein, Ascotoxin, Decumbin; NSC244390, Nectrolide, Synergisidin
Protein Synthesis and Transport Inhibitor
    Cat #: B-275
    Sizes: 1 mg, 5 x 1 mg
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Origin Isolated from Eupenicillium brefeldianum.
    Source: Natural
    MW: 280.4 Da.
    Purity >99%.
    Effective concentration 1-100 µM.
    Structure
    Chemical name γ-4-Dihdyroxy-2-(6-hydroxy-1- heptenyl)-4-cyclopentanecrotonic acid.
    Molecular formula C16H24O4.
    CAS number 20350-15-6.
    Activity Brefeldin A is an antiviral antibiotic and inhibits protein transport from the endoplasmic reticulum (ER) to the golgi by disassembling the golgi1,2. It can also induce apoptosis in some cell types3. Brefeldein A is widely used as an enhancer of intracellular cytokine accumulation and neurodegenerative disease inducer in cell culture models4,5.
    Storage before reconstitution Lyophilized powder can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Reconstitution DMSO, Ethanol, Methanol, Dichloromethane. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage after reconstitution Up to two weeks at 4°C or six months at -20°C.
    Our bioassay
    Alomone Labs Brefaldin A inhibits the assembly of the golgi complex in HeLa cells.
    Cells were treated with or without 40 µg Brefeldin A (#B-275) for 1 h. The upper and lower right panels show that Golgin (red), a golgi marker, is disassembled upon treatment. DAPI is used as the counterstain (blue).
    Alomone Labs Brefeldin A  inhibits the assembly of the Golgi complex in 3T3-L1 cells.
    Cells were treated without (A) or with (B) 40 µg/ml Brefeldin A (#B-275) for 1 h.  The figure represents superposition of triple labeling using anti-manosidase II - a Golgi apparatus marker (red), DAPI for nuclear staining (blue) and DIOC16 for cell membrane staining (green).
    References
    1. Herri, E. et al. (1963) Helv. Chim. Acta46, 1235.
    2. Handschin, U. et alHelv. Chim. Acta. (1968) 51, 1943.
    3. Tamura, G. et al. (1968) J. Antibiot. (Tokyo) 21, 160.
    4. Oda, K. et al. (1987) FEBS Lett214, 135.
    5. Takatsuki, A. et al. (1985) Agric. Biol. Chem49, 899.
    6. Fujiwara, T. (1988) J. Biol. Chem263, 18545.
    7. Lippincott-Schwartz, J. et al. (1989) Cell 56, 801.
    8. Klausner, R.D. et al. (1992) J. Cell. Biol116, 1071.
    9. Misumi, Y. et al. (1986) J. Biol. Chem261, 11398.
    10. Betina, V. (1992) Folia Microbiol. (Praha) 37, 3.
    11. Pommepuy, I. et al. (2003) Oncology 64, 459.
    12. Sales F.T. et al. (2004) Oral Oncol40, 585.
    13. Kikuchi, S. et al. (2004) J. Neurosci. Res71, 591.
    Scientific background

    Brefeldin A (BFA)1, is a macrocyclic lactone synthesized from palmitate (C16) by a variety of fungi. It was initially isolated and characterized in the 1960's as an antiviral antibiotic.2-3 In the late 1980's, it was found to act as a very powerful inhibitor of intracellular protein transport.4-6 BFA specifically and reversibly blocks protein transport from the endoplasmic reticulum (ER) to the Golgi apparatus in many cell types and species.7-8 These effects are generally accompanied by distinct structural changes expressed in apparent collapse of the Golgi stacks and its redistribution into the ER as well as into nuclear envelope,6-7 which leads to inhibition of protein secretion, vesicular assembly and antigen presentation.3-9 A large body of evidence demonstrates that BFA inhibits the whole cell membrane traffic by its ability to inhibit binding of regulatory coat proteins to their target organelles. In this way, BFA deregulates membrane traffic throughout the central vacuolar system of the cell.8

    BFA was also shown to act as a mitosis inhibitor in plant cells, and as a cancerostatic and apoptosis inducer in animal cells.6-10

    BFA is very effective for enhancing accumulation of intracellular cytokines and it has relatively low toxicity (LD50 in mice (intraperitoneal injection) >200 mg/kg).10 Due to its peculiar activity, BFA is used as an inducer of pathogenesis in models of neurodegenerative diseases.10-13

    Last update: 19/02/2018

    Alomone Labs is pleased to offer Brefeldin A (#B-275), isolated and purified from Eupenicillium brefeldianum.

    For research purposes only, not for human use