School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai, 264005, PR China.
Shandong Shenxiangchuanqi Biotechnology Co., Ltd., Weihai, 264400, PRChina.
Anticancer Agents Med Chem. 2023;23(15):1731-1739. doi: 10.2174/1871520623666230412095428.
20()-PD, a tetracyclic triterpenoid, is a non-natural saponin present in the form of protopanaxadiol. Because of its essential biological activities, especially anti-tumor activity, structural modification of 20()-PD and the development of innovative and novel 20()-PD derivatives with better anti-tumor activity are increasingly relevant.
20()-Panaxadiol (20()-PD) can inhibit tumor proliferation. Three series of novel 20(-PD derivatives were synthesized by modifying the A-ring.
The objective of this work was to synthesize and evaluate the anti-proliferative activities of 20()- PD derivatives in LNCaP, LS180, and MKN45 cancer cells. Structural modifications were performed at the C-3 position and A-ring.
The anti-proliferative activities of novel derivatives in LNCaP, LS180, and MKN45 cells were evaluated by the MTT assay. The effects of compounds 5 and C9 on apoptosis were determined by flow cytometry.
Compounds 5, B2, C2, C4, C7, C8, C9, C10, and C11 exhibited good anti-proliferative activities in LNCaP, LS180, and MKN45 cells . The best anti-proliferative activity was observed for the C-series derivatives with the introduction of amino acids at the C-3 position. C9 exhibited good potent activity with an IC of 2.89 μM.
Compound C9 is a potential candidate with potent anti-proliferative activity.
20-（-PD 是一种四环三萜类化合物，以原人参二醇的形式存在，是一种非天然皂苷。由于其重要的生物学活性，特别是抗肿瘤活性，对 20-（-PD 的结构修饰以及开发具有更好抗肿瘤活性的创新新型 20-（-PD 衍生物越来越重要。
20-（-PD 可抑制肿瘤增殖。通过修饰 A 环，合成了三系列新型 20-（-PD 衍生物。
本工作的目的是合成并评价 20-（-PD 衍生物在 LNCaP、LS180 和 MKN45 癌细胞中的抗增殖活性。在 C-3 位和 A 环进行结构修饰。
通过 MTT 法评价新型衍生物在 LNCaP、LS180 和 MKN45 细胞中的抗增殖活性。用流式细胞术测定化合物 5 和 C9 对细胞凋亡的影响。
化合物 5、B2、C2、C4、C7、C8、C9、C10 和 C11 在 LNCaP、LS180 和 MKN45 细胞中均表现出良好的抗增殖活性。在 C-3 位引入氨基酸的 C 系列衍生物表现出最好的抗增殖活性。C9 的 IC 为 2.89 μM，表现出良好的活性。
化合物 C9 是一种具有潜在抗增殖活性的候选药物。
