Silvestrol

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Silvestrol 是一种来自 Aglaia foveolata 的潜在抗癌 rocaglate 衍生物，通过线粒体/凋亡体途径诱导癌细胞凋亡。

Silvestrol is a potential anticancer rocaglate derivative from Aglaia foveolata, induces apoptosis in cancer cells through the mitochondrial/apoptosome pathway; effectively targets the cyclin/CDK/Rb pathway, and additionally induces cytotoxicity via intrinsic apoptosis, exhibits low nanomolar potency both in MCL cell lines and primary MCL tumor cells; demonstrates B-cell selective activity in chronic lymphocytic leukemia and acute lymphoblastic leukemia in vitro and in vivo.

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. 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.

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.

-)-Silvestrol

Apoptosis

Apoptosis

Apoptosis

Cancer

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697235-38-4

654.665

C34H38O13

>98% (HPLC)

DMSO; H2O: < 1 mg/mL

O=C([C@H]([C@H]1C2=CC=CC=C2)[C@@H](O)[C@]3(O)[C@@]1(C4=CC=C(OC)C=C4)OC5=C3C(OC)=CC(OC6O[C@@H]([C@H](O)CO)CO[C@H]6OC)=C5)OC

1H-Cyclopenta[b]benzofuran-2-carboxylic acid, 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-, methyl ester, (1R,2R,3S,3aR,8bS)-

(-20℃)

With Ice Pack

≥ 2 years