The antiangiogenic activity of Kushecarpin D, a novel flavonoid isolated from Sophora flavescens Ait.

The antiangiogenic activity of Kushecarpin D, a novel flavonoid isolated from Sophora flavescens Ait.
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Kushecarpin D(一种从苦参中分离出来的新型黄酮类化合物)的抗血管生成活性。

DOI:
10.1016/j.lfs.2013.09.025
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发表时间:
2013-11
期刊:
影响因子:
6.1
通讯作者:
Wang, Chun-Ming
Wang, Chun-Ming
中科院分区:
医学2区
文献类型:
--
作者:
Pu, Li-Ping;Chen, He-Ping;Cao, Mei-Ai;Zhang, Xiu-Li;Gao, Qing-Xiang;Yuan, Cheng-Shan;Wang, Chun-Ming

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Kushecarpin D(KD)是从传统中草药苦参(Sophora flavescens Ait)中分离得到的一种新的黄酮类化合物。本研究以人脐静脉内皮细胞(ECV 304)为实验对象,采用SRB法和台盼蓝拒染法,观察KD对ECV 304细胞增殖的影响。KD的抗血管生成活性通过细胞迁移、细胞粘附和管形成的研究来评价。DCFH-DA和DHE荧光法检测活性氧(ROS)水平。过氧化氢酶活性测定采用比色法。用流式细胞仪和Hoechst 33258染色法检测细胞周期和凋亡。结果表明KD通过抑制细胞增殖、细胞迁移、细胞粘附和管腔形成而显示出抗血管生成活性。KD处理后,ROS水平下调,过氧化氢酶活性上调。细胞周期停滞在G2/M期,而使用Hoechst 33258染色法或亚G1比例流式细胞术分析后未观察到细胞凋亡。重要性KD的抗血管生成特性,结合其抗增殖作用和诱导细胞周期停滞而不诱导细胞凋亡的能力,使其成为开发抗肿瘤药物的良好候选药物。然而,进一步的研究是必要的,以阐明其作用机制。
AimsKushecarpin D (KD) is a novel flavonoid isolated from the traditional Chinese herbal medicineKushen(the dried root of Sophora flavescens Ait). As part of our continuous effort to explore Chinese traditional medicinal herbs and to identify novel natural anticancer products, the antiangiogenic properties of KD were examined in vitro using a human umbilical vein endothelial cell line (ECV304).Main methodsThe SRB and Trypan Blue exclusion assays were used to evaluate the effect of KD on cell proliferation. The antiangiogenic activities of KD were evaluated through studies of cell migration, cell adhesion, and tube formation. DCFH-DA and DHE fluorescent assays were used to detect the reactive oxygen species (ROS) levels. Catalase activity was detected using the colorimetric ammonium molybdate method. Cell cycle and apoptosis were measured using flow cytometry and the Hoechst 33258 staining assay.Key findingsThe results indicated that KD showed antiangiogenic activity via inhibitory effects on cell proliferation, cell migration, cell adhesion, and tube formation. ROS levels were down-regulated and catalase activity was up-regulated after treatment with KD. The cell cycle was arrested at the G2/M phase, while no apoptosis was observed using the Hoechst 33258 staining assay or following the flow cytometric analysis of the sub-G1 proportion.SignificanceThe antiangiogenic properties of KD, in combination with its anti-proliferative effect and ability to induce cell cycle arrest without inducing apoptosis, make it a good candidate for development as antitumor agent. However, further studies are essential to elucidate its mechanism of action.
DOI: 10.1016/j.tetlet.2004.09.176
发表时间: 2004-11
影响因子: 1.8
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