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多聚异戊烯基多环酰基间苯三酚:来自藤黄属植物的血管生成抑制剂。

Polyprenylated polycyclic acylphloroglucinol: Angiogenesis inhibitor from Garcinia multiflora.

机构信息

School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan.

Department of Biological Sciences, National Sun Yat-Sen University, Kaohsiung 804, Taiwan.

出版信息

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1860-1863. doi: 10.1016/j.bmcl.2018.04.006. Epub 2018 Apr 6.

Abstract

A new polyprenylated polycyclic acylphloroglucinol, garcimultiflorone K (1), has been isolated from the stems of Garcinia multiflora, together with two known compounds, garcimultiflorone A (2) and garcimultiflorone B (3). The structure of new compound 1 was determined through spectroscopic methods including 1D and 2D NMR and MS analyses. The anti-angiogenic and anti-cancer effects of compounds 1-3 were evaluated in human endothelial progenitor cells (EPCs) and cancer cells. Of these, garcimultiflorone K (1) displayed the most potent anti-angiogenic property by suppressing cell growth and tube formation of EPCs. Compound 1 also exhibited growth-inhibitory activities against human hepatocellular carcinoma cell line SK-Hep-1 and hormone refractory prostate cancer cell line PC-3 with GI values of 4.3 ± 1.6 and 6.6 ± 0.4 μM, respectively.

摘要

从密花藤茎部分离得到一个新的多聚异戊二烯多环酰基间苯三酚,garcimultiflorone K(1),与两个已知化合物,garcimultiflorone A(2)和 garcimultiflorone B(3)一起。新化合物 1 的结构通过包括 1D 和 2D NMR 和 MS 分析在内的光谱方法确定。化合物 1-3 的抗血管生成和抗癌作用在人内皮祖细胞(EPCs)和癌细胞中进行了评估。其中,garcimultiflorone K(1)通过抑制 EPCs 的细胞生长和管形成显示出最强的抗血管生成特性。化合物 1 对人肝癌细胞系 SK-Hep-1 和激素难治性前列腺癌细胞系 PC-3 的生长抑制活性分别为 GI 值 4.3±1.6 和 6.6±0.4 μM。

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