piperidines and sophocarpine

The dry root of Sophora flavescens Ait. (SF) has long been used in a variety of Chinese herbal formulations to treat patients with cancer. Alkaloids are commonly known to present in SF as main active constituents. Here, we report that among the six characterized SF-derived quinolizidine alkaloids including sophoridine, aloperine, sophocarpine, matrine, oxymatrine and cytisine, aloperine exerted the most potent in vitro cytotoxic activity against the human cancer cell lines and oxymatrine exhibited selective anti-cancer activity against hepatocellular carcinoma HepG2 cells. Analysis of DNA fragmentation and PARP cleavage revealed that aloperine treatment for 48 hr induced apoptosis in HL-60 cells. In addition, autophagic formation of acidic vacuole was also observed in HL-60 cells exposed to aloperine. These results suggest that aloperine may be a novel contributor to the anti-cancer properties of SF.

Topics: Alkaloids; Antineoplastic Agents; Apoptosis; Azocines; Drugs, Chinese Herbal; Electrophoresis, Capillary; HL-60 Cells; Humans; Inhibitory Concentration 50; K562 Cells; Matrines; Phytotherapy; Piperidines; Plant Preparations; Plant Roots; Quinolizidines; Quinolizines; Sophora

To study the chemical constituents of the alkaloid fraction of Kushen decoction.. Constituents were isolated by different kinds of column chromatography and their structures were elucidated with spectral methods.. Eight compounds were isolated and identified as matrine (I), sophoridine (II), sophocarpine (III), sophoramine (IV), oxymatrine (V), oxysophocarpine (VI), aloperine (VII) and sparteine (VIII).. All these compounds were isolated from Kushen decoction for the first time. Aloperine was found firstly in Sophora flavescens, or Scutellaria baicalensis, or Rehmannia glutinosa which constituted Kushen decoction.

Topics: Alkaloids; Drug Combinations; Drugs, Chinese Herbal; Matrines; Piperidines; Plants, Medicinal; Quinolizidines; Quinolizines; Rehmannia; Scutellaria baicalensis; Sophora