[Show abstract][Hide abstract] ABSTRACT: A series of 1-aryl, 5-(phenoxy-substituted)aryl-1,4-pentadien-3-one derivatives were synthesized and evaluated for anticancer activity. Amongst the synthesized ethers, 4A and 4Y exhibited substantial antiproliferative activity with IC(50) values ranging from 6.6-8.6 mu mol L(-1) against a variety of human cancer cell lines. Preliminarily mechanism of antitumor action of 4A by DNA Ladder, Annexin V/PI double staining and related studies indicated growth inhibition of PC3, BGC-823 and Bcap-37 cells by induction of tumor cells apoptosis.
Full-text · Article · Jul 2011 · Medicinal Chemistry Communication
[Show abstract][Hide abstract] ABSTRACT: Recently, interest in phytochemicals from traditional Chinese medicinal herbs with the capability to inhibit cancer cells growth and proliferation has been growing rapidly due to their nontoxic nature. Dysosma versipellis as Bereridaceae plants is an endemic species in China, which has been proved to be an important Chinese herbal medicine because of its biological activity. However, systematic and comprehensive studies on the phytochemicals from Dysosma versipellis and their bioactivity are limited.
Fifteen compounds were isolated and characterized from the roots of Dysosma versipellis, among which six compounds were isolated from this plant for the first time. The inhibitory activities of these compounds were investigated on tumor cells PC3, Bcap-37 and BGC-823 in vitro by MTT method, and the results showed that podophyllotoxone (PTO) and 4'-demethyldeoxypodophyllotoxin (DDPT) had potent inhibitory activities against the growth of human carcinoma cell lines. Subsequent fluorescence staining and flow cytometry analysis indicated that these two compounds could induce apoptosis in PC3 and Bcap-37 cells, and the apoptosis ratios reached the peak (12.0% and 14.1%) after 72 h of treatment at 20 μM, respectively.
This study suggests that most of the compounds from the roots of D. versipellis could inhibit the growth of human carcinoma cells. In addition, PTO and DDPT could induce apoptosis of tumor cells.