生物活性 | |||
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描述 | Digitonin, a glycoside obtained from Digitalis purpurea, could increase cell permeability by binding to cholesterol molecules and reduce tumor growth. Digitonin enhanced the tumour-growth-retarding effect of CBDCA (carboplatin) given intra-arterially at 5 mg/kg but not at 25 mg/kg. Pretreatment with digitonin increases the tumour uptake of CBDCA and potentiates the cytotoxic effect of CBDCA[1]. Digitonin is thus useful both for selectively permeabilizing the plasma membrane and for intensifying the appearance of intracellular structures such as microfilaments that are normally difficult to observe in cells such as hepatocytes[2]. Perfusing a rat liver with digitonin in the concentration range 2-20 mg/ml results in complete decolorization of the organ within 45-250s[3]. The activity of rat liver microsomal squalene epoxidase is inhibited effectively by digitonin. The inhibition of squalene epoxidase by digitonin is concentration-dependent and takes place rapidly within 5 min of exposure of the microsomes to digitonin. Only 40% inhibition of cyclase activity is observed at 1 mg/ml of digitonin[4]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
0.81mL 0.16mL 0.08mL |
4.07mL 0.81mL 0.41mL |
8.13mL 1.63mL 0.81mL |
参考文献 |
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