Isolation of naturally occurring isoflavonone and some clinical uses thereof

摘要

The compound of formula (II), designated as "PMZ-1", was isolated from Bolusanthus speciosus (Bolus Harms). PMZ-1 is active against HIV-1RF (EC50 = 0.1 mu M) and HIV-1IIIB (EC50 = 0.2 mu M) with cytotoxic concentrations (IC50) of 30 to 50 mu M respectively. PMZ-1 has a broad therapeutic index (TI 300). The compound shows good activity when tested in the fresh human peripheral blood mononuclear cells (PBMC's, EC50 1 mu M) and monocytes/macrophages (Mono/MAC's, EC50 1 mu M) assays. It inhibited protease enzymatic activity (ID50 = 3.8 mu M) and integrase enzymatic activity (ID50 = 40 mu M). It shows activity against breast cancer.