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Isolation and characterization of compounds from Zanthoxylum setulosum in the development of novel structures for chemotherapeutic drugs.

机译：从花椒中的化合物的分离和表征开发化学治疗药物的新结构。

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摘要

Breast cancer is one of the leading causes of cancer death in American women and unfortunately, current chemotherapy protocols still have limitations: (1) most chemotherapy destroys not only cancer cells, but also many rapidly dividing normal cells and (2) cancer cells can develop resistance to chemotherapeutic agents through mutation. Thus, there is a crucial need to find new chemical agents which (1) exploit differences between normal cells and breast cancer cells in order to selectively kill the breast cancer cells and (2) provide new, complementary chemotherapeutic techniques to be used in conjunction with other breast cancer treatments or in combination with other anticancer drugs. Tropical rainforest plants have evolved chemical defensive mechanisms to avoid herbivory and resist pathogens. Zanthoxylum is a genus of about 250 species in Rutaceae that contain a rich source of lignans, alkaloids, coumarins, amides, flavonoids, terpenes and other metabolites with pharmacological properties. Therefore, there are beneficial novel chemical agents present in Zanthoxylum that can be studied for human maladies, such as cancer. In this work, the fractionation of active materials, screening of cytotoxicity, determination of isolated chemical structures, and binding energies of human DNA topoisomerase I of Zanthoxylum setulosum were evaluated. Zanthoxylum setulosum was notably cytotoxic (100% kill at 100 microg/ml) on MCF-7, MDA-MB-231, and MDA-MB-468 cells in vitro. The cytotoxic effects of isolated compounds from Zanthoxylum setulosum were tested against MCF-7 and MDA-MB-231 breast cancer cell lines. Chemical structures of cytotoxic compounds were determined through NMR, HPLC, and X-ray crystallography spectroscopic techniques. Lupeol, sesamin, lichexanthone, and sesquichamaenol were isolated from Zanthoxylum setulosum. Lupeol exhibited high cyctotoxic killing against MCF-7 and MDA-MB-231 cells at 100% kill at 100 mg/ml, with a LC50 value of 85.3 microM and 453.9 microM, respectively. Molecular docking studies for binding energies of lichexanthone with five DNA structures, PDB: 1k4t, 1z3f, 1al9, 1t8i, and 1sc7 were calculated using ArgusLab and Molegro Virtual Docker. The primary objective was to isolate fractions from Zanthoxylum setulosum and identify the active components and mechanism for new potential chemotherapeutic drugs.
机译：乳腺癌是美国女性癌症死亡的主要原因之一，不幸的是，当前的化学治疗方案仍然存在局限性：（1）大多数化学治疗不仅破坏癌细胞，而且破坏许多快速分裂的正常细胞，（2）癌细胞会发展通过突变对化学治疗剂的抗性。因此，迫切需要找到新的化学试剂，其（1）利用正常细胞和乳腺癌细胞之间的差异以选择性地杀死乳腺癌细胞，和（2）提供新的，互补的化学治疗技术，以结合使用其他乳腺癌治疗方法或与其他抗癌药物联合使用。热带雨林植物已经进化出化学防御机制来避免草食和抵抗病原体。花椒属（Zanthoxylum）是芸香科（Rutaceae）的大约250种，其包含丰富的木脂素，生物碱，香豆素，酰胺，类黄酮，萜烯和其他具有药理学性质的代谢物。因此，花椒中存在有益的新型化学试剂，可用于人类疾病（例如癌症）的研究。在这项工作中，评估了活性物质的分离，细胞毒性的筛选，确定的化学结构的确定以及花椒的人类DNA拓扑异构酶I的结合能。体外花椒对MCF-7，MDA-MB-231和MDA-MB-468细胞具有细胞毒性（100微克/毫升时100％杀死）。测试了来自花椒的分离的化合物对MCF-7和MDA-MB-231乳腺癌细胞系的细胞毒性作用。细胞毒性化合物的化学结构是通过NMR，HPLC和X射线晶体学光谱技术确定的。狼毒，芝麻素，利己酮和倍半茶烯酚是从花椒中分离得到的。羽扇豆酚对MCF-7和MDA-MB-231细胞具有100毫克/毫升的100％杀死率，对细胞毒性高，其LC50值分别为85.3 microM和453.9 microM。使用ArgusLab和Molegro Virtual Docker计算了具有六种DNA结构PDB：1k4t，1z3f，1al9、1t8i和1sc7的六己酮的结合能的分子对接研究。主要目的是从花椒中分离出级分，并确定新的潜在化学治疗药物的活性成分和机理。

著录项

  • 作者

    Walker, Tameka M.;

  • 作者单位

    The University of Alabama in Huntsville.;

  • 授予单位 The University of Alabama in Huntsville.;
  • 学科 Biology Botany.;Chemistry Pharmaceutical.;Chemistry Analytical.
  • 学位 Ph.D.
  • 年度 2011
  • 页码 113 p.
  • 总页数 113
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 TS97-4;
  • 关键词

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