Design, synthesis and biological evaluation of novel sesquiterpene mustards as potential anticancer agents.

Several novel series of sesquiterpene mustards (SMs) bearing nitrogen mustard and glutathione (GSH)-reactive α-methylene-γ-butyrolactone groups were successfully prepared for the first time and showed excellent antiproliferative activities in vitro. Among them, compounds 2e and 2g displayed the highest antiproliferative properties with IC50 values ranging from 2.5 to 8.7 µM. The selectivity of these two compounds was evaluated by SRB method against human cancer and normal hepatic cells (HepG2 and L02). The induction of apoptosis and effects on the cell cycle distribution with compounds 2e and 2g were investigated by Hoechst 33,258 staining and flow cytometry, which exhibited that they could induce selective cell apoptosis and cell cycle arrest in HepG2 and L02 cells. In addition, further investigation showed that compounds 2e and 2g could obviously inhibit the proliferation of HepG2 cells by inducing significant DNA cross-linking and depleting GSH in cell media. The good cytotoxicity and selectivity of compounds 2e and 2g pointed them as promising leads for anticancer drug design.

New lignans from the roots of Schisandra sphenanthera.

Nine new lignans (1-8, 13) and five known ones (9-12, 14) have been isolated from the roots of Schisandra sphenanthera and were tested for their capacity to scavenge 2,2-diphenyl-1-Picryl-hydrazyl (DPPH). Of these lignans tested, compounds 1, 7, 8 and 13 exhibited noteworthy antioxidant activity with IC50 values of 92, 115, 35 and 48 µg/mL, respectively. The anti-oxidative haemolysis of human red blood cells (RBCs) activity of the most active compound 8, which is similar to that of vitamin C, was evaluated.