School of Pharmacy, Zunyi Medical University, Zunyi, China.
Department of Clinical Pharmacy, Affiliated Hospital of Zunyi Medical University, Zunyi, China.
Nat Prod Res. 2024 Jan-Feb;38(2):311-319. doi: 10.1080/14786419.2022.2121828. Epub 2022 Sep 12.
Due to complexity of tumor diseases and resistance of targeted drug, targeted drug usually cannot meet the needs of cancer treatment. Therefore, the conjugate constructed by two anticancer agents maybe a better solution for the tumor diseases. As natural anticancer agents, icaritin and norcantharidin are selected for the construction of conjugate. In the condition of EDCI/DMAP, icaritin is reacted with norcantharidin esters to give the desired 7-esters selectively in a moderate yield. MTT method was used to test the cytotoxicity and intensity on Hep G2 and MCF-7 in vitro. Some of the compounds (, and ) show a better inhibition against Hep G2 and MCF-7 cell lines in vitro, and are deserved to be a potential drug candidate to develop in vivo.
由于肿瘤疾病的复杂性和靶向药物的耐药性，靶向药物通常无法满足癌症治疗的需求。因此，将两种抗癌药物构建成缀合物可能是解决肿瘤疾病的更好方法。作为天然抗癌药物，淫羊藿苷和去甲斑蝥素被选来构建缀合物。在 EDCI/DMAP 的条件下，淫羊藿苷与去甲斑蝥素酯反应，以中等收率选择性地得到所需的 7-酯。MTT 法用于测试体外对 Hep G2 和 MCF-7 的细胞毒性和强度。一些化合物（、和）对 Hep G2 和 MCF-7 细胞系表现出更好的体外抑制作用，值得进一步开发为体内潜在药物候选物。
