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제110회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Induction of apoptosis by 2,4,6,8-tetrakis(2-methoxyphenyl)-3,7-diazabicyclo[3.3.1] nonan-9-one derivative

2012년 9월 5일 13시 57분 30초
BIO.P-778 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
10월 17일 (수요일) 16:00~19:00
저자 및
이명진, 황지영, XuYi1, 김동규2
인제대학교 화학과, Korea
1인제대학교 화학과, China
2인제대학교 의생명화학과, Korea
In previous study, we examined that 2,4,6,8-tetrakis(2-methoxyphenyl)-3,7-diazabicyclo[3.3.1] nonan-9-one has anticancer effect on HeLa cells. So, novel 9 compounds were derived from 2,4,6,8-tetrakis(2-methoxyphenyl)-3,7-diazabicyclo[3.3.1] nonan-9-one and they were prepared to evaluate their cytotoxicity in HeLa cell line by using WST-8 assay. Among those compounds, compound 6 had most significant so we choose compound 6 for examining as anticancer drug. Its IC50 value was about 25μM. In addition, compound 6 inhibited clearly the proliferation of HeLa cell. Though its mother compound had less IC50, compound 6 had radical scavenger function. We could compare their radical scavenger effect by using DPPH radical scavenger assay. Also, compound 6 led intracellular ROS to increase in time-dependent manner. Results from cell cycle arrest analysis showed that compound 6 induced G1 phase arrest of HeLa cell. We found that compound 6 induced apoptosis by Annexin V-FITC/PI double staining assay. Morphologic results showed compound 6 induced remarkable changes like cellular shrinkage and disruption. Moreover, compound 6 led intracellular △Ψm(mitochondrial membrane potential) at HeLa cell to decrease. Gathering those data, we could regard compound 6 as good candidate for anticancer drug and antioxidant.