State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, People's Republic of China.
State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, People's Republic of China.
Fitoterapia. 2022 Oct;162:105289. doi: 10.1016/j.fitote.2022.105289. Epub 2022 Sep 1.
The chemical investigation on Corydalis balansae resulted in the isolation of three previous undescribed compounds (1, 10, and 11) and 17 known compounds. Compound 1 and 2 were obtained as two lignanamide dimers, and compound 11 had a spiro [benzofuranone-benzazepine] skeleton, which was found in Corydalis for the first time. The structures of new compound were determined by the detailed analysis of 1D/2D NMR, UV, and IR data. Absolute configurations of compounds 10 and 11 were defined by their crystal X-ray diffraction data and calculations of electronic circular dichroism (ECD). The CCK-8 method was used to assay the inhibition effect of all the compounds on the growth of Hela, MGC-803, A549, and HepG2 cancer cells. Compound 2, 13, and 14 showed moderate inhibitory activity against the tested cell lines. Compound 2 exhibited potential antitumor activity against MGC-803 cells with an IC value of 20.8 μM, while the positive control etoposide was 17.3 μM. Furthermore, results from the cellular-mechanism investigation indicated that compound 2 could induce S-phase cell-cycle arrest and MGC-803 cells apoptosis, which was triggered by the up-regulation of PARP1, caspase-3 and -9, Bax, and down-regulation of Bcl-2. The 2-induced strong apoptosis indicated that compound 2 had good potential as an antitumor lead compound.
对蓝堇的化学成分研究分离得到了三个以前未描述的化合物（1、10 和 11）和 17 个已知化合物。化合物 1 和 2 为两个木质素酰胺二聚体，化合物 11 具有螺 [苯并呋喃酮-苯并氮杂卓] 骨架，这是在紫堇属中首次发现的。新化合物的结构通过 1D/2D NMR、UV 和 IR 数据的详细分析来确定。通过化合物 10 和 11 的晶体 X 射线衍射数据和电子圆二色性（ECD）计算确定了它们的绝对构型。CCK-8 法测定了所有化合物对 Hela、MGC-803、A549 和 HepG2 癌细胞生长的抑制作用。化合物 2、13 和 14 对测试的细胞系表现出中等抑制活性。化合物 2 对 MGC-803 细胞表现出潜在的抗肿瘤活性，IC 值为 20.8 μM，而阳性对照依托泊苷为 17.3 μM。此外，细胞机制研究结果表明，化合物 2 可通过上调 PARP1、caspase-3 和 -9、Bax 和下调 Bcl-2 诱导 S 期细胞周期停滞和 MGC-803 细胞凋亡。2 诱导的强烈凋亡表明化合物 2 具有作为抗肿瘤先导化合物的良好潜力。
