α-Methylene-γ-lactones as a Novel Class of Anti-leukemic Agents
α-Methylene-γ-lactones as a Novel Class of Anti-leukemic Agents
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DOI：
10.2174/1871520614666140313095010
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发表时间：
2014-06-01
影响因子：
2.8
通讯作者：
Janecka, Anna
中科院分区：
文献类型：
--
作者：
Gach, Katarzyna;Janecka, Anna
天然产物是药物发现的重要线索。近年来，从植物中分离的含有α-亚甲基-γ-内酯骨架的天然化合物的抗白血病特性引起了广泛的关注。已经进行了广泛的研究，以表征其作用的分子机制和在不同类型的癌症（包括白血病）中的潜在化疗应用。倍半萜内酯是一组α-亚甲基-γ-内酯，是植物来源的化合物，主要是菊科植物，用于传统医学，特别是用于治疗炎症。然而，它们表现出广泛的其他生物学效应，包括细胞毒性、抗菌、抗蠕虫和抗肿瘤活性。最近，倍半萜内酯，小白菊，和其他几种含有α-亚甲基-γ-内酯骨架的化合物已成为潜在的抗白血病药物的感兴趣的话题。最近的研究强调了它们对白血病细胞的选择性活性，而正常造血细胞不受影响。在这篇综述中，我们简要描述了从植物中分离的天然α-亚甲基-γ-内酯及其经过微小化学修饰具有抗白血病活性的衍生物。我们还讨论了这些化合物的分子作用机制，特别是它们对白血病细胞的选择性。
Natural products are important leads in drug discovery. In recent years, the anti-leukemic properties of natural compounds isolated from plants, containing an alpha-methylene-gamma-lactone skeleton, have attracted a lot of attention. Extensive research has been carried out to characterize their molecular mechanisms of action and potential chemotherapeutic application in different types of cancer, including leukemias. Sesquiterpene lactones, a group of alpha-methylene-gamma-lactones, are plant-derived compounds, mostly of the Compositae family, used in traditional medicine especially for the treatment of inflammation. However, they exhibit a broad spectrum of other biological effects, including cytotoxic, anti-bacterial, anti-helminthic, and anti-tumor activity. Recently, a sesquiterpene lactone, parthenolide, and several other compounds containing an alpha-methylene-gamma-lactone skeleton have become topics of interest as potential anti-leukemic agents. The recent research emphasizes their selective activity against leukemia cells while the normal hematopoietic cells remain unaffected. In this review, we give a brief description of natural alpha-methylene-gamma-lactones isolated from plants and their derivates with minor chemical modifications that possess anti-leukemic activity. We also discuss molecular mechanisms of action of these compounds, in particular, their selectivity against leukemia cells.