• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文学位 >Anti-proliferative withanolides from Vassobia breviflora and Withania somnifera.
【24h】

Anti-proliferative withanolides from Vassobia breviflora and Withania somnifera.

机译：来自短叶紫花苜蓿和Withania somnifera的抗增殖性山梨醇。

获取原文
获取原文并翻译 | 示例
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

In order to identify anti-proliferative compounds from selected Latin American plants, approximately 200 plant extracts were screened by the MTS assay (3-[4,5-dimethylthiazol-2yl]-5-[3-carboxymethoxyphenyl]-2-[4-sulfophenyl]-2 H tetrazolium). Vassobia breviflora (Solanaceae), was identified as the most active of the species tested in this study. Following a bioassay-guided approach, withaferin A was isolated and characterized. This withanolide-type steroidal lactone showed anti-proliferative activities with IC50 values from 0.5 to 2.2 muM against head and neck squamous cell carcinoma (HNSCC) MDA1986, JMAR, UM-SCC-2 and JHU011. A mechanistic study showed that withaferin A induced apoptosis and cell death in HNSCC cells as well as a shift from G0/G1 to G2/M arrest in cell cycle studies. Western data demonstrated that the anti-proliferative action of withaferin A could be in part explained through degradation of total Akt levels as well as decrease in activation of Akt levels. In order to establish anticancer structure activity relationships, three analogues were semi-synthesized from withaferin A, and ten related withanolides, including a new chlorinated withanolide 6&agr;-chloro-5beta,17&agr;-dihydroxywithaferin, were isolated from Withania somnifera (Solanaceae). All structures were elucidated on the basis of spectroscopic methods (IR, MS, and 1D/2D NMR). X-ray crystallography confirmed the absolute configuration of the new withanolide. A method for large-scale isolation of withaferin A from W. somnifera was also developed and presented.
机译：为了从所选的拉丁美洲植物中鉴定抗增殖化合物，通过MTS分析（​​3- [4,5-二甲基噻唑-2基] -5- [3-羧基甲氧基苯基] -2- [4-磺苯基] -2 H四唑鎓）。在本研究中，Vassobia breviflora（茄科）被认为是最活跃的物种。在生物测定指导的方法之后，分离并鉴定了withferinA。该withanolide型甾体内酯对头颈部鳞状细胞癌（HNSCC）MDA1986，JMAR，UM-SCC-2和JHU011表现出抗增殖活性，IC50值为0.5至2.2μM。一项机理研究表明，在细胞周期研究中，用Aferin A诱导HNSCC细胞凋亡和细胞死亡，以及从G0 / G1转变为G2 / M阻滞。西方数据表明，Withferin A的抗增殖作用可以部分通过总Akt水平的降解以及Akt水平活化的降低来解释。为了建立抗癌结构活性关系，从枯草杆菌素A半合成了三个类似物，并从茄子（Withania somnifera）（茄科）中分离了十个相关的枯草苷，包括新的氯化枯草苷6-agr-氯-5beta，17＆agr-二羟基枯草杆菌素。根据光谱方法（IR，MS和1D / 2D NMR）阐明了所有结构。 X射线晶体学证实了新的withanolide的绝对构型。还开发并提出了一种从W. somnifera大规模分离大黄素A的方法。

著录项

  • 作者

    Tong, Xiaoqin.;

  • 作者单位

    University of Kansas.;

  • 授予单位 University of Kansas.;
  • 学科 Chemistry Organic.;Health Sciences Pharmacy.
  • 学位 M.S.
  • 年度 2011
  • 页码 94 p.
  • 总页数 94
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号