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The contribution of plukenetione A to the anti-tumoral activity of Cuban propolis.

机译:uke烯酮A对古巴蜂胶的抗肿瘤活性的贡献。

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摘要

Increasing efforts are directed toward finding applications for natural products and their derivatives in the treatment of human diseases. Among such products, propolis, a resinous substance produced by honey bees from various plant sources, has been found to be a promising source of potential therapeutics. In the present work, we aimed at studying the perspective of Cuban propolis as a source of possible anti-cancer agents. We found an anti-metastatic effect in mice and considerable cytotoxicity without cross-resistance in both wild-type and chemoresistant human tumor cell lines. Plukenetione A--identified for the first time in Cuban propolis--induced G0/G1 arrest and DNA fragmentation in colon carcinoma cells. Furthermore, the activities of both topoisomerase I and DNA polymerase were inhibited, while the expression of topoisomerase II-beta, EGF receptor, and multidrug resistance-related protein genes was found repressed. We assume that plukenetione A contributes to the anti-tumoral effect of Cuban propolis mainly by targeting topoisomerase I as well as DNA polymerase.
机译:加大力度致力于寻找天然产物及其衍生物在人类疾病治疗中的应用。在这些产品中,蜂胶是蜜蜂从各种植物来源生产的一种树脂物质,已被发现是潜在疗法的有前途的来源。在当前的工作中,我们旨在研究古巴蜂胶作为可能的抗癌药来源的前景。我们在小鼠中发现了抗转移作用,并且在野生型和化学耐药性人类肿瘤细胞系中都没有交叉耐药性,并且具有相当的细胞毒性。 Plukenetione A-在古巴蜂胶中首次发现-诱导结肠癌细胞中的G0 / G1阻滞和DNA片段化。此外,拓扑异构酶I和DNA聚合酶的活性均受到抑制,而拓扑异构酶II-β,EGF受体和多药耐药相关蛋白基因的表达被抑制。我们假设plukenetione A主要通过靶向拓扑异构酶I和DNA聚合酶来促进古巴蜂胶的抗肿瘤作用。

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