期刊
MOLECULES
卷 25, 期 5, 页码 -出版社
MDPI
DOI: 10.3390/molecules25051168
关键词
sophora alkaloid; hybrid; cinnamic acid; antitumor; apoptosis
资金
- National Natural Science Foundation of China [81502929]
- Drug Innovation Major Project [2018ZX09711-001-005-008]
- CAMSInnovation Fund for Medical Sciences [2016-I2M-3-015]
- Beijing Natural Science Foundation [7192129]
Twenty-five sophora alkaloids-cinnamic acid hybrids (including matrine-cinnamic acid hybrids, sophoridine-cinnamic acid hybrids, and sophocarpine-cinnamic acid hybrids) were designed, synthesized, and evaluated in vitro against three human tumor cell lines (HeLa, HepG2 and A549) with cisplatin as a positive control. Some matrine-cinnamic acid and sophoridine-cinnamic acid compounds exhibited potent effect against all three cancer cell lines, such as compounds 5b, 5e, 5g, and 6d. The structure-activity relationship study of the synthesized compounds was also performed. Preliminary mechanistic studies indicated that compounds 5e and 6d could induce apoptosis in HepG2 cell line. Further, compounds 5e and 6d altered mitochondrial membrane potential and produced ROS leading to cell apoptosis of HepG2 cells. Overall, our findings suggested that these compounds may provide promising lead compounds for further development as antitumor agents by structural modification.
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