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In vitro: Fumagillin selectively inhibits the growth of a Δmap1 strain but not a wild-type or a Δmap2 S. cerevisiae strain missing MetAP-2. In budding yeast cells, as a potent inhibitor of angiogenesis, Fumagillin not only reverses the growth inhibitory activity of Vpr, but also inhibits Vpr-dependent viral gene expression upon the infection of human macrophages. Though the toxicity of fumagillin has limited its use for human applications, the analogues using structure-activity relationships relating to its angiogenesis properties may be further explored in the treatment of angiogenesis-dependent diseases. In vivo: In DEN-treated rats, fumagillin (30 mg/kg, i.p.) inhibits both progression of HCC in the liver itself and systemic metastasis.
| Cell Experiment | |
|---|---|
| Cell lines | lymphoma cell lines |
| Preparation method | The transcript and protein product of replication transcriptional activator (RTA) were induced by 1-10 μM fumagillin at 24 and 48 h, respectively. Western blot analysis demonstrated that 10 μM fumagillin induced not only RTA expression but also other KSHV-encoded lytic proteins. A real-time PCR array detecting KSHV gene expression demonstrated that the expression profiles of KSHV induced by fumagillin were similar to those induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), but the amounts of each transcript were lower than those induced by TPA. Finally, real-time PCR demonstrated an increase in that viral DNA copy number per cell in fumagillin-stimulated primary effusion lymphoma cell lines, indicating replication of KSHV. |
| Concentrations | 1-10 μM |
| Incubation time | 48h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 458.54 |
| Formula | C26H34O7 |
| CAS Number | 23110-15-8 |
| Solubility (25°C) | 72 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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