Polyphyllin VI induces apoptosis and autophagy in human osteosarcoma cells by modulation of ROS/JNK activation.

Purpose: Polyphyllin VI, a main active saponin isolated from traditional medicinal plant , has exhibited antitumor activities in several cancer cell lines. In the present study, we investigated the antitumor effect of Polyphyllin VI against human osteosarcoma cells (U2OS) and the underlying molecular mechanisms.

Methods: The U2OS cell lines were used to determine the antiproliferative effect of Polyphyllin VI by CCK8 assay.

Synthesis and biological evaluation of novel HIV-1 protease inhibitors using tertiary amine as P2-ligands.

A series of tertiary amine derivatives exhibiting potent HIV-1 protease inhibiting properties were identified. These novel inhibitors were designed based on the structure of Darunavir with modification on the P2 and P2' position. This effort led to discovery of 35e and 38e, which exhibited excellent HIV-1 protease inhibition with IC50 values of 15 nM and 64 nM, respectively.

Quinoline-3-carboxamide derivatives as potential cholesteryl ester transfer protein inhibitors.

A series of novel quinoline-3-carboxamide derivatives 10-17 and 23-27 were designed and synthesized as cholesteryl ester transfer protein (CETP) inhibitors. All of them exhibited activity against CETP. Particularly, compounds 24 and 26 displayed the best activity against CETP with the same inhibitory rate of 80.