Silvestrol(Synonyms: (-)-Silvestrol)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Silvestrol (Synonyms: (-)-Silvestrol) 纯度: 98.11%

Silvestrol 是从 Aglaia foveolata 的果实和枝条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。

Silvestrol(Synonyms: (-)-Silvestrol)

Silvestrol Chemical Structure

CAS No. : 697235-38-4

规格 价格 是否有货 数量
1 mg ¥9900 In-stock
2 mg ¥16500 In-stock
5 mg ¥32000 In-stock
10 mg ¥45000 In-stock
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100 mg   询价  

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Silvestrol 相关产品

相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus

生物活性

Silvestrol is a eukaryotic translation initiation factor 4A (eIF4A) inhibitor isolated from the fruits and twigs of Aglaia foveolata. Silvestrol induces autophagy and caspase-mediated apoptosis[1][2][3].

IC50 & Target

eIF4A[1]

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 IC50 values 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

654.66

Formula

C34H38O13

CAS 号

697235-38-4

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
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 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].

参考文献
  • [1]. Chambers JM, et al. Synthesis of biotinylated episilvestrol: highly selective targeting of the translation factors eIF4AI/II. Org Lett. 2013 Mar 15;15(6):1406-9.

    [2]. Kim S, et al. Silvestrol, a potential anticancer rocaglate derivative from Aglaia foveolata, induces apoptosis in LNCaP cells through the mitochondrial/apoptosome pathway without activation of executioner caspase-3 or -7. Anticancer Res. 2007 Jul-Aug;27(4B):2175-83.

    [3]. Chen WL, et al. Silvestrol induces early autophagy and apoptosis in human melanoma cells. BMC Cancer. 2016 Jan 13;16:17.

    [4]. Daker M, et al. Inhibition of nasopharyngeal carcinoma cell proliferation and synergism of CDDP with silvestrol and episilvestrol isolated from Aglaia stellatopilosa. Exp Ther Med. 2016 Jun;11(6):2117-2126.

    [5]. Patton JT, et al. The translation inhibitor silvestrol exhibits direct anti-tumor activity while preserving innate and adaptive immunity against EBV-driven lymphoproliferative disease. Oncotarget. 2015 Feb 20;6(5):2693-708.

    [6]. Wolfe AL, et al. RNA G-quadruplexes cause eIF4A-dependent oncogene translation in cancer. Nature. 2014 Sep 4;513(7516):65-70.

    [7]. Wiegering A, et al. Targeting Translation Initiation Bypasses Signaling Crosstalk Mechanisms That Maintain High MYC Levels in Colorectal Cancer. Cancer Discov. 2015 Jul;5(7):768-781.

    [8]. Todt D, et al. The natural compound silvestrol inhibits hepatitis E virus (HEV) replication in vitro and in vivo. Antiviral Res. 2018 Sep;157:151-158.

Cell Assay
[2]

The cells are seeded at a density of 7×104 cells/mL in 100-mm culture dishes and are treated with 30 nM or 120 nM concentrations of Silvestrol for 24 h[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[5]

Mice[5]
Peripheral blood mononuclear cells (PBMC) are injected intraperitoneally (IP) into SCID mice depleted of murine natural killer (NK) cells by pretreatment (plus weekly re-treatment) with anti-asialo (GM1). Engraftment is confirmed by hu-IgG ELISA. Treatments with vehicle (30% hydroxypropyl-β-cyclodextrin) or Silvestrol (1.5 mg/kg every 48 hr IP) begin 2 weeks post-engraftment[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Chambers JM, et al. Synthesis of biotinylated episilvestrol: highly selective targeting of the translation factors eIF4AI/II. Org Lett. 2013 Mar 15;15(6):1406-9.

    [2]. Kim S, et al. Silvestrol, a potential anticancer rocaglate derivative from Aglaia foveolata, induces apoptosis in LNCaP cells through the mitochondrial/apoptosome pathway without activation of executioner caspase-3 or -7. Anticancer Res. 2007 Jul-Aug;27(4B):2175-83.

    [3]. Chen WL, et al. Silvestrol induces early autophagy and apoptosis in human melanoma cells. BMC Cancer. 2016 Jan 13;16:17.

    [4]. Daker M, et al. Inhibition of nasopharyngeal carcinoma cell proliferation and synergism of CDDP with silvestrol and episilvestrol isolated from Aglaia stellatopilosa. Exp Ther Med. 2016 Jun;11(6):2117-2126.

    [5]. Patton JT, et al. The translation inhibitor silvestrol exhibits direct anti-tumor activity while preserving innate and adaptive immunity against EBV-driven lymphoproliferative disease. Oncotarget. 2015 Feb 20;6(5):2693-708.

    [6]. Wolfe AL, et al. RNA G-quadruplexes cause eIF4A-dependent oncogene translation in cancer. Nature. 2014 Sep 4;513(7516):65-70.

    [7]. Wiegering A, et al. Targeting Translation Initiation Bypasses Signaling Crosstalk Mechanisms That Maintain High MYC Levels in Colorectal Cancer. Cancer Discov. 2015 Jul;5(7):768-781.

    [8]. Todt D, et al. The natural compound silvestrol inhibits hepatitis E virus (HEV) replication in vitro and in vivo. Antiviral Res. 2018 Sep;157:151-158.

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