Silvestrol 是从Agave americanaLinn.中分离的真核翻译起始因子 (eIF4A) 抑制剂。Silvestrol 诱导细胞自噬以及 caspase 介导的细胞凋亡。
| 生物活性 | Silvestrol is a eukaryotic translation initiation factor 4A (eIF4A) inhibitor isolated fromAgave americanaLinn.. Silvestrol inducesautophagyand caspase-mediatedapoptosis[1][2][3]. |
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体外研究
(In Vitro) | Silvestrol is a specific eIF4A-targeting translation inhibitor. Silvestrol exhibits significant cytotoxic activity against many human cancer cell lines, such as lung, prostate, and breast cancer with IC50values ranging from 1 to 7 nM[1].
Silvestrol significantly reduces the number of LNCaP cell colonies. Silvestrol (30 nM, 120 nM) induces apoptosis in LNCaP cells, through the mitochondrial pathway. Apaf-1, Caspase-2, caspase-9, and caspase-10 are involved in Silvestrol-induced apoptosis but caspase-3 and 7 are not[2].
Silvestrol induces caspase-3 activation and apoptotic cell death in a time- and dose-dependent manner. Silvestrol-mediated cell death is attenuated in ATG7-null mouse embryonic fibroblasts (MEFs) lacking a functional autophagy protein[3].
Silvestrol (50 nM) exerts an immediate inhibitory effect and causes near-static cell index compared with the control cells. Silvestrol (6.25 nM) enhances proliferation more than the vehicle control-treated cells, whereas a higher concentration of Silvestrol (50 nM) can inhibit cell proliferation. Silvestrol and episilvestrol display synergistic effects in combination with CDDP[4].
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体内研究
(In Vivo) | Silvestrol (1.5 mg/kg, i.p.) does not adversely affect production of human IgG by xenografted B-lymphocytes in mice. Silvestrol significantly prolongs survival compared to vehicle. There is no such lymphocyte infiltration detected in the spleens of any of the Silvestrol-treated mice, and nor do these animals exhibit any other obvious signs of lymphoma upon necropsy[5].
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| 来源 | - Plants
- Agavaceae
- Agave americanaLinn.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 6.6 mg/mL(10.08 mM) H2O :< 0.1 mg/mL(insoluble) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.5275 mL | 7.6376 mL | 15.2751 mL | | 5 mM | 0.3055 mL | 1.5275 mL | 3.0550 mL | | 10 mM | 0.1528 mL | 0.7638 mL | 1.5275 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 1. Silvestrol is prepared in 5.2% Tween 80 5.2% PEG 400[6]. 2. Silvestrol is dissolved in 20%(w/v) 2-hydroxyproply beta-cyclodextrin vehicle at a concentration of 125 μg/mL and injected into mice i.p.[7]. 3. Silvestrol is formulated in 30% 2-hydroxypropyl-β-cyclodextrin[8].
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