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首页> 外文期刊>Journal of natural products >Amaryllidaceae alkaloids belonging to different structural subgroups display activity against apoptosis-resistant cancer cells.
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Amaryllidaceae alkaloids belonging to different structural subgroups display activity against apoptosis-resistant cancer cells.

机译:属于不同结构亚组的金石科生物碱显示出抗凋亡抗性癌细胞的活性。

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摘要

Fifteen Amaryllidaceae alkaloids (1-15) were evaluated for their antiproliferative activities against six distinct cancer cell lines. Several of these natural products were found to have low micromolar antiproliferative potencies. The log P values of these compounds did not influence their observed activity. When active, the compounds displayed cytostatic, not cytotoxic activity, with the exception of pseudolycorine (3), which exhibited cytotoxic profiles. The active compounds showed similar efficacies toward cancer cells irrespective of whether the cell lines were responsive or resistant to proapoptotic stimuli. Altogether, the data from the present study revealed that lycorine (1), amarbellisine (6), haemanthamine (14), and haemanthidine (15) are potentially useful chemical scaffolds to generate further compounds to combat cancers associated with poor prognoses, especially those naturally resistant to apoptosis, such as glioblastoma, melanoma, non-small-cell lung, and metastatic cancers.
机译:评价了十五种金莲花科生物碱(1-15)对六种不同癌细胞系的抗增殖活性。发现这些天然产物中的几种具有低微摩尔抗增殖能力。这些化合物的log P值不影响其观察到的活性。当具有活性时,这些化合物显示出细胞抑制活性,而不是细胞毒性活性,但假丝氨酸(3)除外,后者具有细胞毒性谱。不管细胞系对促凋亡刺激是响应还是抗性,活性化合物对癌细胞都显示出相似的功效。总体而言,本研究的数据表明,赖氨酸(1),a菜碱(6),甘露胺(14)和甘露定(15)可能是有用的化学支架,可以产生进一步的化合物来对抗与不良预后有关的癌症,尤其是天然癌症对凋亡具有抵抗力,例如胶质母细胞瘤,黑色素瘤,非小细胞肺癌和转移性癌症。

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