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Sesquiterpene lactones from Mikania micrantha and Mikaniacordifolia and their cytotoxic and anti-inflammatory evaluation.

机译:薇甘菊和薇甘菊的倍半萜内酯及其细胞毒性和抗炎性评价。

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摘要

The guaianolide 8-epi-mikanokryptin (1) and the melampolide 11H beta -11,13-dihydromicrantholide (2) along with known sesquiterpene lactones (3-13) and other constituents were isolated from the aerial parts of different populations of Mikania micrantha and Mikania cordifolia collected in several states of Mexico. The relative and absolute configurations of 1 were determined by X-ray diffraction and CD analysis, respectively. Considering the 1H and 13C NMR chemical shift similarities and the H-H coupling constant values, a [1D14, 15D5] conformation was established for micrantholides (2, 8-13). We tested nearly all the sesquiterpene lactones for antiproliferative activity in human cancer cell lines, and they exhibited moderate activity. Additionally, in a mouse ear model of edema induced by TPA, the anti-inflammatory activities were marginal.
机译:从薇甘菊(Mikania micrantha)和薇甘菊(Mikania micrantha)不同种群的地上部分离了愈创木酚8-表甘氨酸(1)和丙酰胺11Hβ-11,13-二氢麦甾醇(2)以及倍半萜内酯(3-13)和其他成分。 Mikania cordifolia在墨西哥几个州收集。 1的相对和绝对构型分别通过X射线衍射和CD分析确定。考虑到 1 H和 13 C NMR化学位移的相似性以及HH偶联常数,[ 1 D 14 ,确定了micrantholides(2,8-13)的 15 D 5 ]构象。我们测试了几乎所有倍半萜内酯在人类癌细胞系中的抗增殖活性,并且它们均显示出中等活性。另外,在由TPA诱导的水肿的小鼠耳朵模型中,抗炎活性是微不足道的。

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