摘要
背景:植物产生几种具有生物活性的次级代谢产物,其被用作治疗剂以治疗几种疾病,其中癌症。三萜类化合物是次生代谢产物,能够对抗多种细胞内和细胞外的目标,发挥抑制活性。这些靶标是参与细胞凋亡,细胞发育和分化,血管生成,转移和炎症过程的蛋白质。一些作者表明,它们功能的抑制导致细胞生长,分化和迁移减少,导致抗肿瘤活性。此外,近年来还开发了合成三萜类衍生物来实现起始化合物的效力和功效,从而获得具有有希望的抗癌活性的新剂。 _目的:在这篇综述中,我们报告了有关该领域研究最多的三萜类化合物及其半合成衍生物的抗癌活性的最新结果,目的是总结三萜类化合物作为分子导致发育的作用新类别的抗肿瘤剂。 方法:我们专注于关于三萜类化合物在癌症治疗中的最新文献,强调了从这些天然化合物开始开发新药物的潜力。 结论:几种“老”三萜类化合物如熊果酸,桦木酸和齐墩果酸最近被重新认为是开发创新型抗癌剂的模型化合物。它们对抗涉及肿瘤发展的蛋白质的活性提高了利用这些化合物作为新的多靶点治疗剂的机会。此外,从其天然存在的结构合成新化合物的可能性可以替代克服细胞对药物的抗性并可以改善其治疗效力。
关键词: 三萜类化合物,癌症,生物活性次级代谢产物,抗肿瘤活性,治疗剂,合成三萜类化合物
Current Medicinal Chemistry
Title:Known Triterpenes and their Derivatives as Scaffolds for the Development of New Therapeutic Agents for Cancer
Volume: 25 Issue: 10
关键词: 三萜类化合物,癌症,生物活性次级代谢产物,抗肿瘤活性,治疗剂,合成三萜类化合物
摘要: Background: Plants produce several bioactive secondary metabolites whose are used as therapeutic agents to treat several diseases, among whom cancer. Triterpenes are secondary metabolites that exert inhibitory activity against multiple intracellular and extracellular targets in euchariotic cells. These targets are proteins involved in apoptosis, cell development and differentiation, angiogenesis, metastasis and inflammatory processes. The inhibition of their functions leads to decreased cellular growth, differentiation and migration, resulting in antitumor activity, as shown by several authors. Furthermore, during recent years synthetic triterpenoid derivatives have also been developed to implement potency and efficacy of starting compounds, allowing the obtainment of new agents having promising anticancer activity.
Objective: In this review we report the latest results regarding anticancer activity of some of the most studied triterpenes in the field, as well as of their semi-synthetic derivatives, with the aim to summarize the role of triterpenes as molecular leads for the development of new classes of antitumor agents.
Methods: We focused on the most recent literature regarding triterpenes in cancer treatment, highlighting the potential of developing new drugs starting from these natural compounds.
Conclusion: Several “old” triterpenes as ursolic, betulinic and oleanolic acids were recently reconsidered as model compounds for the development of innovative anticancer agents. Their activity against proteins involved in tumor development enhances the opportunity to exploit these compounds as new multi-target therapeutic agents. Furthermore, the possibility to synthetize new compounds from their natural-occurring structures could be an alternative to overcome cellular resistance to drugs and could improve their therapeutic efficacy.
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Known Triterpenes and their Derivatives as Scaffolds for the Development of New Therapeutic Agents for Cancer, Current Medicinal Chemistry 2018; 25 (10) . https://dx.doi.org/10.2174/0929867324666170818111933
DOI https://dx.doi.org/10.2174/0929867324666170818111933 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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