| NO供体型大黄酸衍生物的合成及抗肿瘤活性 |
| |
| 引用本文： | 柏志伟,尚飞扬,戴卫国,何黎琴.NO供体型大黄酸衍生物的合成及抗肿瘤活性[J].中国药科大学学报,2021,52(1):38-43. |
| |
| 作者姓名： | 柏志伟 尚飞扬 戴卫国 何黎琴 |
| |
| 作者单位： | 安徽中医药大学药学院,合肥 230031,安徽中医药大学药学院,合肥 230031,安徽中医药大学药学院,合肥 230031,安徽中医药大学药学院,合肥 230031 |
| |
| 基金项目： | 安徽省自然科学基金资助项目（No.KJ2017A292） |
| |
| 摘 要： | 以大黄酸为原料,利用其羧基通过不同的连接臂与呋咱氮氧化合物偶联,得到7个NO供体型大黄酸衍生物,其结构经红外光谱、核磁共振氢谱和质谱确证.采用MTT法测试了目标化合物对人肝癌细胞HepG2、Bel-7402,人结肠癌细胞HCT116,人骨肉瘤细胞U2OS,耐药细胞Bel-7402/5-FU及正常肝细胞LO2的体外抗细胞...
|
| 关 键 词： | 大黄酸 衍生物 呋咱氮氧化合物 合成 抗肿瘤活性 |
| 收稿时间： | 2020/9/8 0:00:00 |
| 修稿时间： | 2020/12/29 0:00:00 |
Synthesis and antitumor activities of NO-donating rhein derivatives |
| |
| BAI Zhiwei,SHANG Feiyang,DAI Weiguo and HE Liqin.Synthesis and antitumor activities of NO-donating rhein derivatives[J].Journal of China Pharmaceutical University,2021,52(1):38-43. |
| |
| Authors: | BAI Zhiwei SHANG Feiyang DAI Weiguo and HE Liqin |
| |
| Institution: | College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China,College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China,College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China,College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China |
| |
| Abstract: | Seven target compounds coupled by rhein and furoxan were synthesized and their chemical structures were confirmed by 1H NMR, IR, and MS. All target compounds were evaluated for anti-proliferative activity against human hepatoma cells HepG2 and Bel-7402, human colon cancer cells HCT116, human osteosarcoma cells U2OS, drug-resistant cells Bel-7402/5-FU and normal hepatocytes cells LO2 in vitro by thiazolyl blue(MTT) colorimetry. The results indicated that all target compounds had more potent anti-proliferative activity than their parent compound rhein. Additionally, compound 4g had stronger proliferation inhibitory activity on HepG2, Bel-7402, U2OS and Bel-7402/5-FU,with little effect on the proliferation of normal cells, exhibiting selective inhibitory activity. Griess assay was used to measure the release of nitric oxide in vitro. Results showed that compound 4g could increase the releases NO in HepG2 cells, which may be associated with its antitumor effects. Furthermore, the antitumor activity of compound 4g was attenuated by NO scavenger (hemoglobin), which indicates that the antitumor activity of compound 4g may be partly related to the release of NO. |
| |
| Keywords: | rhein derivatives furoxan synthesis anti-tumor activity |
|
| 点击此处可从《中国药科大学学报》浏览原始摘要信息 |
| 点击此处可从《中国药科大学学报》下载免费的PDF全文 |
|
