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首页> 外文学位 >PHYTOCHEMICAL AND MECHANISTIC STUDIES ON THE CONSTITUENTS OF WIKSTROEMIA ELLIPTICA AND STIZOPHYLLUM RIPARIUM.
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PHYTOCHEMICAL AND MECHANISTIC STUDIES ON THE CONSTITUENTS OF WIKSTROEMIA ELLIPTICA AND STIZOPHYLLUM RIPARIUM.

机译：椭圆形维克斯氏菌和裂殖藻的化学成分的理化和力学研究。

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摘要

The chloroform extract of the combined stem wood and stem bark of Wikstroemia elliptica Merrill (Thymelaeaceae) was found to have significant cytotoxic activity against the P-388 lymphocytic leukemia test system in cell culture. Bioactivity-directed fractionation of this extract has led to the isolation of five cytotoxic substances, namely the new lignan, ((+OR-))-5'-methoxylariciresinol, and the known compounds, ((+OR-))-lariciresinol, ((+OR-))-syringaresinol, daphnoretin and umbelliferone.;The most cytotoxic constituent of S. riparium, stizophyllin, exhibited an ED(,50) of 0.07 (mu)g/ml in the P-388 lymphocytic leukemia system in cell culture. Stizophyllin formed adducts with nucleophilic substances such as cysteine and (beta)-mercaptoethanol as judged by decreasing absorbance at its ultraviolet maximum at 241 nm. The adduct formed with (beta)-mercaptomethanol was isolated and structurally characterized. As compared to stizophyllin, the cytotoxic potential of the adduct was decreased 20-fold. When log phase P-388 cells were pulsed with radioactive thymidine, uridine or leucine in the presence of various concentration of stizophyllin, DNA, RNA and protein biosynthesis all appeared to be inhibited. Stizophyllin blocked P-388 cell cycle progression in the G(,2)+M phase. However, the substance did not modulate in vitro tubulin polymerization reactions, and did not affect the morphology of db cAMP-treated astrocytoma cells in culture. Since synchronous P-388 cells were most sensitive in the G(,2) phase, stizophyllin appears to function during this segment of the cycle-cycle. (Abstract shortened with permission of author.).;The chloroform extract of the entire plant of Stizophyllum riparium (H.B.K.) Sandw. was found to display significant activity against the P-388 lymphocytic leukemia system in cell culture. Bioactivity-guided fractionation has led to the isolation and characterization of two new cytotoxic triterpene esters, 3(beta)-hydroxy-24-trans-ferulyloxyurs-12-en-28-oic acid, and the isomeric, 3(beta)-hydroxy-24-cis-ferulyloxy-urs-12-en-28-oic acid, as well as a new cytotoxic pregnane derivative, 2(alpha),3(beta),12(beta)-trihydroxypregna-4,7,16-trien-20-one (stizophyllin). An additional four compounds were isolated in the course of this investigation that were devoid of cytotoxic activity, and the new compounds, 3(beta),19-dihydroxy-24-trans-ferulyloxy-12-en-28-oic acid, 2(alpha),3(beta),12(beta)-trihydroxypregna-4,7-dien-20 one, and 16-(alpha)-methoxy-2(alpha),3(beta),12(beta)-trihydroxypregna-4,7-dien-20 one.
机译：发现椭圆形美人蕉（Thymelaeaceae）茎木和茎皮的组合中的氯仿提取物对细胞培养中的P-388淋巴细胞白血病测试系统具有明显的细胞毒活性。该提取物的生物活性定向分馏已导致分离出五种细胞毒性物质，即新的木脂素（（+ OR-））-5'-甲氧基lariciresinol和已知的化合物（（+ OR-））-lariciresinol， （（+ OR-））-丁香脂素醇，达夫诺汀和伞形酮。; S.riparium的最强细胞毒性成分stizophyllin在P-388淋巴细胞性白血病系统中表现出ED（，50）为0.07（μ）g / ml。细胞培养。花青素与亲核物质如半胱氨酸和β-巯基乙醇形成加合物，这可通过降低其在241 nm紫外线最大吸收值来判断。与β-巯基乙醇形成的加合物被分离并进行结构表征。与stizophyllin相比，加合物的细胞毒性潜力降低了20倍。当对数期P-388细胞在不同浓度的促叶绿素存在下用放射性胸苷，尿苷或亮氨酸脉冲处理时，DNA，RNA和蛋白质的生物合成均受到抑制。 Stizophyllin阻止了G（，2）+ M期的P-388细胞周期进程。但是，该物质不会调节体外微管蛋白聚合反应，也不会影响经db cAMP处理的星形细胞瘤细胞的形态。由于同步的P-388细胞在G（，2）阶段最敏感，因此stizophyllin似乎在周期的这一阶段起作用。 （经作者许可，缩短摘要）.;整个花椒（Stizophyllum riparium（H.B.K.）Sandw）的氯仿提取物。已发现在细胞培养中对P-388淋巴细胞白血病系统显示出显着的活性。生物活性指导的分馏已导致分离和表征了两种新的细胞毒性三萜酯，即3β-羟基-24-反式-阿魏酰氧基脲-12-en-28-油酸和异构体3β-羟基-24-顺式阿魏酸-urs-12-en-28-油酸，以及一种新的具有细胞毒性的孕烷衍生物2α，3β，12β-三羟基孕烷4,7,16- Trien-20-一（stizophyllin）。在此研究过程中还分离了另外四种没有细胞毒活性的化合物，而新化合物3β，19-二羟基-24-反-阿魏酰氧基-12-en-28-油酸2（ alpha），3β，12β-trihydroxypregna-4,7-dien-20one和16-α-甲氧基-2α，3β，12β-trihydroxypregna- 4,7-dien-20一。

著录项

  • 作者

    DUH, CHANG-YIH.;

  • 作者单位

    University of Illinois at Chicago, Health Sciences Center.;

  • 授予单位 University of Illinois at Chicago, Health Sciences Center.;
  • 学科 Health Sciences Pharmacy.
  • 学位 Ph.D.
  • 年度 1986
  • 页码 234 p.
  • 总页数 234
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

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