Bruceantin
Bruceantin has antiviral activity, it can inhibit pepper mottle virus in pepper; it also shows high antimalarial activity. Bruceantin is an effective agent in controlling the proliferation, viability and migration of multiple myeloma cancer stem cells (CSCs) as well as angiogenesis in vitro. Bruceantin exhibits NF-κB p65 inhibition, and cytotoxic potential against HT-29, HeLa, and HL-60 cells .
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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Virus Res. 2017 Jan 2;227:49-56.
Quassinoids isolated from Brucea javanica inhibit pepper mottle virus in pepper.[Pubmed:
27686478 ]
METHODS AND RESULTS:
A green fluorescent protein (GFP)-tagged pepper mottle virus (PepMoV) based leaf-disc method and systemic host method were developed to identify antiviral agents. Preliminary experiments using a PepMoV-GFP based leaf-disc method led to the isolation of five quassinoids, including brusatol (1), Bruceantin (2), brucein A (3), Bruceantinol (4), and brucein B (5), from the CH3OH extract of Brucea javanica.
CONCLUSIONS:
All isolated compounds exhibited inactivation effects in systemic host plants, and compounds 3 and 4 were potent, with a minimum inhibitory concentration of 10μM. Furthermore, compound 3 was found to have a protective effect at the tested concentration of 40μM.
Cancer Biol Ther. 2016 Sep;17(9):966-75.
Bruceantin inhibits multiple myeloma cancer stem cell proliferation.[Pubmed:
27434731 ]
Multiple myeloma (MM) continues to claim the lives of a majority of patients. MM cancer stem cells (CSCs) have been demonstrated to sustain tumor growth. Due to their ability to self-renew and to express detoxifying enzymes and efflux transporters, MM-CSCs are rendered highly resistant to conventional therapies. Therefore, managing MM-CSCs characteristics could have profound clinical implications. Bruceantin (BCT) is a natural product previously demonstrated to inhibit the growth of MM in RPMI 8226 cells-inoculated mouse xenograft models, and to cause regression in already established tumors.
METHODS AND RESULTS:
The objectives of the present study were to test the inhibitory effects of BCT on MM-CSCs growth derived from a human primary tumor, and to explore a mechanism of action underlying these effects. BCT exhibited potent antiproliferative activity in MM-CSCs starting at 25 nM. BCT induced cell cycle arrest, cell death and apoptosis in MM-CSCs as well as inhibited cell migration and angiogenesis in vitro. Using a qPCR screen, it was found that the gene expression of a number of Notch pathway members was altered. Pretreatment of MM-CSCs with the γ-secretase inhibitor RO4929097, a Notch pathway inhibitor, reversed BCT-induced effects on MM-CSCs proliferation.
CONCLUSIONS:
In this study, BCT was shown to be an effective agent in controlling the proliferation, viability and migration of MM-CSCs as well as angiogenesis in vitro. The effect on MM-CSCs proliferation may be mediated by the Notch pathway. These results warrant further investigation of BCT in a broader set of human-derived MM-CSCs and with in vivo models representative of MM.
Anticancer Res. 2010 Sep;30(9):3295-300.
NF-kappaB inhibitors from Brucea javanica exhibiting intracellular effects on reactive oxygen species.[Pubmed:
20944100 ]
Brucea javanica was studied to identify nuclear factor kappaB (NF-κB) inhibitors exhibiting reactive oxygen species (ROS) intracellular amplification.
METHODS AND RESULTS:
Eight compounds were evaluated for selective cytotoxicity using HT-29, HeLa, and HL-60 cells, and in a NF-κB assay. Active compounds were then tested using ROS and mitochondria transmembrane potential (MTP) assays. NF-κB and nuclear factor activated T-cell (NFAT) translocation were also assessed using their respective whole cell assays.
Bruceajavanone B, Bruceantin, bruceine A, (-)-hydnocarpin, and chrysoeriol exhibited cytotoxic potential and NF-κB p65 inhibition. Chrysoeriol exhibited selective cytotoxicity against leukemia cells with greater potency and also showed an ability to up-regulate NFAT transcriptional pathways through the amplification of intracellular ROS, in the presence of H2O2, to a greater degree than Bruceantin and bruceine.
CONCLUSIONS:
Chrysoeriol selectively kills leukemic cells and potentiates the amplification of ROS levels. Therefore, chrysoeriol could serve as a potential chemotherapeutic modifier for leukemia chemotherapy since leukemia cells have a higher susceptibility to elevated ROS levels.
Med Chem. 2005 Jan;1(1):3-11.
Synthesis of A/B-ring partial analogs of bruceantin as potential antimalarial agents.[Pubmed:
16789880]
METHODS AND RESULTS:
Bruceantin (1), a classical quassinoid with the highest reported antimalarial activity among the quassinoids examined thus far, was selected as a natural product lead for the design of a series of A/B-ring analogs. A viable strategy for the synthesis of the series was developed.
CONCLUSIONS:
The functionalized A-ring and the C-15 ester moiety in Bruceantin are incorporated in all designed compounds. The preliminary bioassay results will be discussed in detail.
