中文名 | Silvestrol |
英文名 | Silvestrol |
别名 | 化合物 T16884 (1R,2R,3S,3AR,8BS)-6-[[(2S,3R,6R)-6-[(1R)-1,2-二羟基乙基]-3-甲氧基-1,4-二氧己环-2-基]氧基]-2,3,3A,8B-四氢-1,8B-二羟基-8-甲氧基-3A-(4-甲氧基苯基)-3-苯基-1H-环戊烯并[B]苯并呋喃-2-羧酸甲酯 |
英文别名 | Silvestrol (-)-Silvestrol (1R,2R,3S,3aR,8bS)-6-[[(2S,3R,6R)-6-[(1R)-1,2-Dihydroxyethyl]-3-methoxy-1,4-dioxan-2-yl]oxy]-2,3,3a,8b-tetrahydro-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-1H-cyclopenta[b]benzofuran-2-carboxylic acid methyl ester 1H-Cyclopenta[b]benzofuran-2-carboxylic acid, 6-[[(2S,3R,6R)-6-[(1R)-1,2-dihydroxyethyl]-3-Methoxy-1,4-dioxan-2-yl]o xy]-2,3,3a,8b-tetrahydro-1,8b-dihydroxy-8-Methoxy-3a-(4-Methoxypheny l)-3-phenyl-, Methyl ester, (1R,2R,3S,3aR,8bS)- |
CAS | 697235-38-4 |
化学式 | C34H38O13 |
分子量 | 654.66 |
密度 | 1.45 |
熔点 | 120-122℃ |
沸点 | 800.8±65.0 °C(Predicted) |
酸度系数 | 11.57±0.70(Predicted) |
存储条件 | -20℃ |
体外研究 | 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 IC 50 values ranging from 1 to 7 nM. 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. 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. 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. |
体内研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.528 ml | 7.638 ml | 15.275 ml |
5 mM | 0.306 ml | 1.528 ml | 3.055 ml |
10 mM | 0.153 ml | 0.764 ml | 1.528 ml |
5 mM | 0.031 ml | 0.153 ml | 0.306 ml |
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