Currently, natural products are one of the priceless options for finding novel chemical pharmaceutical entities. Ellipticine is a naturally occurring alkaloid isolated from the leaves of Ochrosia elliptica Labill. Ellipticine and its derivatives are characterized by multiple biological activities. The purpose of this review was to provide a critical and systematic assessment of ellipticine and its derivatives as bioactive molecules over the last 60 years. Publications focused mainly on the total synthesis of alkaloids of this type without any evaluation of bioactivity have been excluded. We have reviewed papers dealing with the synthesis, bioactivity evaluation and mechanism of action of ellipticine and its derivatives. It was found that ellipticine and its derivatives showed cytotoxicity, antimicrobial ability, and anti-inflammatory activity, among which cytotoxicity toward cancer cell lines was the most investigated aspect. The inhibition of DNA topoisomerase II was the most relevant mechanism for cytotoxicity. The PI3K/AKT pathway, p53 pathway, and MAPK pathway were also closely related to the antiproliferative ability of these compounds. In addition, the structure-activity relationship was deduced, and future prospects were outlined. We are confident that these findings will lay a scientific foundation for ellipticine-based drug development, especially for anticancer agents.

中文翻译：

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2023年之前报道的玫瑰树碱衍生物的生物活性和作用机制


目前，天然产物是寻找新型化学药物实体的无价选择之一。玫瑰树碱 (Ellipticine) 是一种从 Ochrosia elliptica Labill 叶子中分离出来的天然生物碱。玫瑰树碱及其衍生物具有多种生物活性。本次综述的目的是对过去 60 年来作为生物活性分子的玫瑰树碱及其衍生物进行批判性和系统性的评估。主要关注此类生物碱的全合成而未对生物活性进行任何评估的出版物已被排除。我们综述了有关玫瑰树碱及其衍生物的合成、生物活性评价和作用机制的论文。研究发现，玫瑰树碱及其衍生物表现出细胞毒性、抗菌能力和抗炎活性，其中对癌细胞系的细胞毒性是研究最多的方面。 DNA 拓扑异构酶 II 的抑制是与细胞毒性最相关的机制。 PI3K/AKT通路、p53通路、MAPK通路也与这些化合物的抗增殖能力密切相关。此外，还推导了构效关系，并展望了未来的前景。我们相信，这些发现将为基于玫瑰树碱的药物开发，特别是抗癌药物的开发奠定科学基础。