SML0172
Cercosporamide from Cercosporidium henningsii
≥98% (HPLC)
别名:
4-Dibenzofurancarboxamide
InChI
1S/C16H13NO7/c1-5(18)10-7(20)4-9-16(2,14(10)22)12-8(21)3-6(19)11(15(17)23)13(12)24-9/h3-4,19-21H,1-2H3,(H2,17,23)/t16-/m1/s1
InChI key
GEWLYFZWVLXQME-MRXNPFEDSA-N
assay
≥98% (HPLC)
solubility
chloroform: 1 mg/mL, ethyl acetate: 1 mg/mL, DMSO: 5 mg/mL (Solution in DMSO is unstable and thus should be freshly prepared.)
storage temp.
−20°C
Quality Level
Application
Cercosporamide from Cercosporidium henningsii has been used as a mitogen-activated protein (MAP) kinase-interacting kinase (MNK) inhibitor in glioblastoma (GBM)-derived BS287 spheres. It has also been used as an inhibitor of bone morphogenetic protein receptor (BMPR) type I kinase in HepG2 cells and zebrafish embryos in particular to test its rescue potential against developmental defects.
Biochem/physiol Actions
Cercosporamide was initially identified as a phytotoxin with broad-spectrum anti-fungal activity. Studies have shown that cercosporamide is a specific, highly potent fungal inhibitor of the cell wall integrity-signaling pathway mediator, protein kinase (Pkc1) inhibitor. Semisynthetic cercosporamide analogues demonstrated hypoglycemic activity and therefore, serve as candidates for potential new anti diabetic drugs. Cercosporamide was found to block eIF4E (Eukaryotic Initiation Factor) phosphorylation in cultured cancer cells, inducing apoptosis, suppressing proliferation, and reducing soft agar colonization. Its eIF4E phosphorylation inhibitory effect was also shown when administrated orally on xenograft human tissue and mouse liver tissue. Cercosporamide is a potent and selective Mnk inhibitor. It reduces tumor growth in xenografted HCT116 tumor and suppresses the outgrowth of B16 melanoma lung metastases. Hence, blocking Mnk function and eIF4E phosphorylation may be an attractive anticancer strategy.
Phytotoxin with broad-spectrum anti-fungal activity.
Preparation Note
DMSO solution (1 mg/ml), kept at -20 °C, is stable for at least three months.
Li-Wei Wang et al.
Applied microbiology and biotechnology, 93(3), 1231-1239 (2011-08-05)
Through bioassay-guided fractionation, the EtOAc extract of a culture broth of the endophytic fungus Phoma species ZJWCF006 in Arisaema erubescens afforded a new α-tetralone derivative, (3S)-3,6,7-trihydroxy-α-tetralone (1), together with cercosporamide (2), β-sitosterol (3), and trichodermin (4). The structures of compounds
Kenji Wakabayashi et al.
Biological & pharmaceutical bulletin, 34(7), 1094-1104 (2011-07-02)
Peroxisome proliferator-activated receptor γ (PPARγ; NR1C3) is known as a key regulator of adipocytogenesis and the molecular target of thiazolidinediones (TZDs), also known as antidiabetic agents. Despite the clinical benefits of TZDs, their use is often associated with adverse effects
Akihiro Furukawa et al.
Bioorganic & medicinal chemistry letters, 20(7), 2095-2098 (2010-03-12)
In an investigation of (-)-Cercosporamide derivatives with a plasma glucose-lowering effect, we found that N-benzylcarboxamide derivative 4 was a partial agonist of PPARgamma. A SAR study of the substituents on carboxamide nitrogen afforded the N-(1-naphthyl)methylcarboxamide derivative 23 as the most
Z Hong et al.
Molecular and cellular biology, 14(2), 1017-1025 (1994-02-01)
k9 killer toxin from Hansenula mrakii was used to select a number of resistant mutants from Saccharomyces cerevisiae. Preliminary biochemical and genetic studies showed that some of them acquired structural defects in the cell wall. One of these mutants, the
Maya P Singh et al.
Journal of industrial microbiology & biotechnology, 37(4), 335-340 (2009-12-25)
Fungi are well known for their vast diversity of secondary metabolites that include many life-saving drugs and highly toxic mycotoxins. In general, fungal cultures producing such metabolites are immune to their toxic effects. However, some are known to produce self-toxic
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