Digitonin|11024-24-1|安捷凯

Background

Digitonin is a steroidal saponin used extensively as a mild non-ionic detergent ^[1]. Digitonin finds application as a cholesterol precipitating agent ^[2]. Digitonin increases cell permeability by binding specifically to cholesterol in the cell membrane ^[4].

Digitonin had high exhibition against Caco-2, MCF-7 with IC50 of 15.72 ± 0.16 and 5.23 ± 0.61μM, respectively. Combinations of the panel of SM with a non-toxic concentration of digitonin (2 or 5 μM) generally enhanced the cytotoxicity in Caco-2, MCF-7 cells ^[3]. Pretreatment with digitonin increases the tumour uptake of carboplatin and potentiates the cytotoxic effect of carboplatin ^[4].

参考文献:
[1]. Bridges C D. A method for preparing stable digitonin solutions for visual pigment extraction[J]. Vision Research, 1977, 17(2): 301-302.
[2]. Haust H L, Kuksis A, Beveridge J M R. Quantitative precipitation of various 3β-hydroxysterols with digitonin[J]. Canadian Journal of Biochemistry, 1966, 44(1): 119-128.
[3]. Eid S Y, El-Readi M Z, Wink M. Digitonin synergistically enhances the cytotoxicity of plant secondary metabolites in cancer cells[J]. Phytomedicine, 2012, 19(14): 1307-1314.
[4]. Lindnér P G, Heath D, Howell S B, et al. Digitonin enhances the efficacy of carboplatin in liver tumour after intra-arterial administration[J]. Cancer chemotherapy and pharmacology, 1997, 40(5): 444-448.

洋地黄皂苷是一种甾体皂苷，广泛用作温和的非离子洗涤剂^[1]。洋地黄皂苷可用作胆固醇沉淀剂^[2]。洋地黄皂苷通过特异性结合细胞膜中的胆固醇来增加细胞通透性^[4]。

Digitonin 对 Caco-2、MCF-7 具有很强的抑制作用，IC50 分别为 15.72 ± 0.16 和 5.23 ± 0.61μM。 SM 组与无毒浓度的洋地黄皂苷（2 或 5 μM）的组合通常增强 Caco-2、MCF-7 细胞的细胞毒性^[3]。毛地黄皂苷预处理可增加卡铂的肿瘤摄取并增强卡铂的细胞毒作用^[4]。

Protocol

Cell experiment [1]:

Cell lines

Caco-2 and MCF-7 cells

Preparation Method

The cells were incubated with 100 μl of medium containing different concentrations of digitonin and other secondary metabolites for 24 hours.

Reaction Conditions

0-500μM for 24 hours.

Applications

Digitonin showed the high exhibition to Caco-2, MCF-7 with IC50 of 15.72 ± 0.16 and 5.23 ± 0.61μM, respectively.

Animal experiment [2]:

Animal models

Inbred rats of both sexes of the Lister-Hooded (LH) strain

Preparation Method

Digitonin was dissolved in dimethylsulfoxide (DMSO) and diluted with saline to yield a solution that contained 400 μM digitonin and 40 μM DMSO; 0.2 ml of the solution was infused into the hepatic artery.

Dosage form

400 μM 0.2 ml of Digitonin solution, a catheter (PE 10, inner diameter 0.28 mm, outer diameter 0.61 mm) was inserted into the hepatic artery proper via the gastroduodenal artery

Applications

After pretreatment with digitonin the platinum content in the tumour as measured at 1 h after CBDCA infusion was 66±19 ng/mg. This was more than 5 times higher than the values obtained after pretreatment with saline alone (12±4 ng/mg) or with DMSO-saline (10±2 ng/mg)

参考文献:

[1]: Eid S Y, El-Readi M Z, Wink M. Digitonin synergistically enhances the cytotoxicity of plant secondary metabolites in cancer cells[J]. Phytomedicine, 2012, 19(14): 1307-1314.
[2]: Lindnér P G, Heath D, Howell S B, et al. Digitonin enhances the efficacy of carboplatin in liver tumour after intra-arterial administration[J]. Cancer chemotherapy and pharmacology, 1997, 40(5): 444-448.

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Digitonin

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Background

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