piperidines and oxymatrine

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 establish a method for determination of 7 alkaloid in Herba Sophorae Alopecuroidis by HPLC.. X-Brige C18 (4.6 mm x 200 mm, 5 microm) column was used with acetonitriles-0.05 mol x L(-1) KH2PO4 solution (2.0 mL x L(-1) triethylamine) with gradient elution as the mobile phase and 1.0 mL x min(-1) as the flow rate. The detection wavelength was 205 nm.. Aloperin curve was linear in the range from 20.66 to 103.32 microg (r = 0.998 8) and the average recovery was 97.12% (RSD 7. 3%); sophoridine curve was linear in the range from 22.82 to 114.12 microg (r = 0.999 7) and the average recovery was 97.47% (RSD 3.0%); oxymatrine curve was linear in the range from 25.10 to 125.52 microg (r = 0.999 1) and the average recovery was 96.21% (RSD 4.5%); oxysophocarpine curve was linear in the range from 23.88 to 119.40 microg (r = 0.997 5) and the average recovery was 94. 64% (RSD 5.2%); matrine curve was linear in the range from 5.00 to 24.99 microg (r = 0.998 6) and the average recovery was 98.04% (RSD 5.4%); sophocarping curve was linear in the range from 4.69 to 23.46 microg (r = 0.999 6) and the average recovery was 96.24 (RSD 5.8%); lehmannine curve was linear in the range from 4.60 to 23.01 microg (r = 0.997 8) and the average recovery was 101.31% (RSD 4.3%).. The method is accurate, simple and feasible. It can be used as a quality evaluation in Herba S. Alopecuroidis.

Topics: Alkaloids; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Matrines; Piperidines; Quality Control; Quinolizidines; Quinolizines; Sophora