期刊
MOLECULES
卷 25, 期 5, 页码 -出版社
MDPI
DOI: 10.3390/molecules25051209
关键词
ergosterol peroxide; semicarbazone; thiosemicarbazone; anti-tumor activity; apoptosis; HepG2 cells
资金
- Qiqihar Academy of Medical Sciences Project [QMSI2017B-09]
- Administration of Traditional Chinese Medicine of Heilongjiang Province [ZHY18-164]
- Central Government Support Fund for the Reform and Development of Local Universities-Talent Training Support Program Project [ZYZX2019]
A series of novel steroidal 5 alpha ,8 alpha -endoperoxide derivatives bearing semicarbazone (7a-g) or thiosemicarbazone (7h-k) side chain were designed, synthesized and evaluated for their cytotoxicities in four human cancer cell lines (HepG2, HCT-116, MCF-7, and A549) using the MTT assay in vitro. The results showed that compound 7j exhibited significant cytotoxic activity against HepG2 cells (IC50 = 3.52 mu M), being more potent than ergosterol peroxide. Further cellular mechanism studies in HepG2 cells indicated that compound 7j triggered the mitochondrial-mediated apoptosis by decreasing mitochondrial membrane potential (MMP), which was associated with up-regulation of Bax, down-regulation of Bcl-2, activation levels of the caspase cascade, and formation of reactive oxygen species (ROS). The above findings indicated that compound 7j may be used as a promising skeleton for antitumor agents with improved efficacy.
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