烟曲霉毒素c
烟曲霉毒素c 性质
| 熔点 | 259.5-260.5℃ |
|---|---|
| 沸点 | 642.9±55.0 °C(Predicted) |
| 密度 | 1.34±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 乙腈：可溶5 mg/mL |
| 酸度系数(pKa) | 17.16±0.40(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至浅棕色 |
| InChIKey | DBEYVIGIPJSTOR-FHWLQOOXSA-N |
| SMILES | N1C2=C(C=CC(OC)=C2)C2C[C@@]3([H])C(=O)N4CCC[C@@]4([H])C(=O)N3[C@@H](/C=C(/C)\C)C1=2 |
烟曲霉毒素c 用途与合成方法
Multidrug resistance (MDR) is a major problem in cancer chemotherapy. Fumitremorgin C is extremely effective in reversing resistance to mitoxantrone, doxorubicin, and topotecan in multidrug-selected cell lines. In MCF-7/mtxR (a mitoxantroneselected cell line), fumitremorgin C reverses mitoxantrone resistance (114-fold) and doxorubicin resistance (3-fold). Fumitremorgin C (5/AM)significantly potentiates the toxicity of mitoxantrone (93-fold), doxorubicin (26-fold), and topotecan (24-fold) in S1M1-3.2 cells. Reversal of resistance is associated with an increase in drug accumulation. Fumitremorgin C does not reverse drug resistance in cells with elevated expression of Pgp or MRP. Fumitremorgin C almost completely reverses resistance mediated by BCRP in vitro and is a pharmacological probe for the expression and molecular action of this transporter. Fumitremorgin C also enhances the toxicity of mitoxantrone and topotecan in vector-transfected MCF-7 cells (2.5–5.6 fold). It reduces the IC 50 of topotecan in BCRP-overexpressing cells below that observed in the untreated vector-transfected cells. .
