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阿克肖昔莫苷 P,2'-醋酸酯:一种来自头序拉拉藤的 Hedgehog 信号抑制成分。

Acoschimperoside P, 2'-acetate: a Hedgehog signaling inhibitory constituent from Vallaris glabra.

机构信息

Graduate School of Pharmaceutical Sciences, Chiba University, Chiba, Japan.

出版信息

J Nat Med. 2011 Jul;65(3-4):629-32. doi: 10.1007/s11418-011-0530-1. Epub 2011 Apr 6.

DOI:10.1007/s11418-011-0530-1
PMID:21625949
Abstract

Complete (1)H and (13)C NMR assignments of acoschimperoside P, 2'-acetate (1) and a new cardiac glycoside (2), isolated from the leaves of Vallaris glabra, are described. Compound 1 was active in the assay for Hedgehog signaling inhibition. In further experiments, this compound showed a strong cytotoxicity against human pancreatic (PANC1) and human prostate (DU145) cancer cells. The expression of GLI-related proteins (PTCH and BCL-2) in a dose-dependent manner was also inhibited by 1.

摘要

描述了从山黧豆属植物的叶子中分离得到的 acoschimperoside P 的(1)H 和(13)C NMR 全归属和 2'- 乙酸酯(1)和一种新的强心苷(2)。化合物 1 在 Hedgehog 信号抑制测定中具有活性。在进一步的实验中,该化合物对人胰腺(PANC1)和人前列腺(DU145)癌细胞表现出强烈的细胞毒性。1 还以剂量依赖的方式抑制 GLI 相关蛋白(PTCH 和 BCL-2)的表达。

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本文引用的文献

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Bioorg Med Chem Lett. 2011 Jan 15;21(2):718-22. doi: 10.1016/j.bmcl.2010.11.126. Epub 2010 Dec 5.
2
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J Nat Prod. 2010 May 28;73(5):995-7. doi: 10.1021/np1000818.
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Hedgehog/GLI-mediated transcriptional inhibitors from Zizyphus cambodiana.
从Lour.的根中获得的三种新强心苷及其细胞毒性和黑色素生成抑制活性。
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