Synthesis and bioevaluation of novel arylnaphthalene lignans as anticancer agents

• DOI: 10.1007/s00044-012-0245-1
• Publication Date: 2012-09-24T10:58:55Z
• Authors: Yu Zhao; Jie Hui; Li Zhu
• Keywords: 01 natural sciences; 0104 chemical sciences; 3. Good health

Novel arylnaphthalene lignans were synthesized and their structures were established by 1H NMR, 13C NMR, and HRMS. These compounds were evaluated for their in vitro cytotoxicity against cancer cell lines by MTT assay. Compound 5d possessed the highest cytotoxicity against KB cells. Apoptosis of KB cells treated with 5d was observed by acridine orange and ethidium bromide double staining assay. Western blot analysis disclosed that 5d induced apoptosis via mitochondrial pathway accompanied by an increased expression of Bax and a decreased expression of Bcl-2.