NO供体型硝酸酯类甘草次酸衍生物的合成及抗肿瘤活性

Synthesis and antitumor activity of nitric oxide-donating glycyrrhetinic acid derivatives coupled with nitrate moiety

摘要: 甘草次酸的3位羟基和30位羧基通过脂肪链连接基团引入硝酸酯结构片段，合成了9个新的NO供体型硝酸酯类甘草次酸衍生物 (4a~4f,8a~8c) 。目标化合物的结构均经红外光谱、质谱、磁共振氢谱确证。体外采用MTT法测定了目标化合物对4种人肿瘤细胞株增殖的抑制活性，结果表明部分目标化合物对人肝癌细胞(HepG2和BEL-7402)、人乳腺癌细胞MCF-7和人早幼粒细胞白血病细胞HL-60的增殖具有较好的抑制活性。
- 甘草次酸 /
- NO供体 /
- 硝酸酯 /
- 合成 /
- 抗肿瘤活性
Abstract: Nine new nitric oxide-donating derivatives of glycyrrhetinic acid coupled with nitrate moieties were designed,synthesized,and evaluated for their in vitro cytotoxicity against four cancer cell lines by MTT assay.Nitrate moieties were conjugated with C3-OH or/and C30-COOH of glycyrrhetinic acid via a variety of aliphatic linkers,affording the target compounds 4a-4f and 8a-8c ,respectively,and their structures were confirmed by MS,IR and ¹H NMR.The MTT assay demonstrated that some of the target compounds exhibited potential cytotoxicity against human hepatocellular carcinoma cells(HepG2 and BEL-7402),human breast cancer MCF-7 cells and human promyelocytic leukemia HL-60 cells.
- glycyrrhetinic acid /
- NO donor /
- nitrate /
- synthesis /
- antitumor activity