isobavachalcone and bavachalcone

A method for the simultaneous quantification of 13 bioactive compounds (psoralen, isopsoralen, isobavachin, bakuchalcone, neobabaisoflavone, bavachin, corylin, psoralidin, isobavachalcone, bavachinin, corylifol A, bavachalcone, and bakuchiol) by ultra-high-performance liquid chromatography coupled with triple quadrupole mass spectrometry has been developed and validated in rat plasma. Osthol was used as an internal standard and plasma samples were pretreated with one-step liquid-liquid extraction. These analytes were separated using a gradient mobile phase system of water and acetonitrile at a flow rate of 0.2 mL/min on a reverse-phase C18 column and analyzed in the selected multiple reactions monitoring mode. All calibration curves were linear (r > 0.9952) over the tested ranges. The intra- and interday accuracy and precisions of these analytes at three different concentration levels were within the acceptable limits of <15% at all concentrations. The mean recoveries of these analytes at three concentrations were more than 60.2% and the matrix effects were in the range of 85-115%. Stability studies proved that the analytes were stable under the tested conditions. The developed method was applied to evaluating the pharmacokinetic study of 13 bioactive compounds after oral administration of Psoraleae Fructus in rat of different genders. Some active compounds in Psoraleae Fructus had sex-related pharmacokinetics.

Topics: Animals; Benzofurans; Chalcones; Chromatography, High Pressure Liquid; Coumarins; Female; Ficusin; Flavones; Flavonoids; Furocoumarins; Male; Mass Spectrometry; Molecular Structure; Phenols; Psoralea; Rats; Rats, Sprague-Dawley

Pancreatic lipase (PL), a crucial enzyme in the digestive system of mammals, has been proven as a therapeutic target to prevent and treat obesity. The purpose of this study is to evaluate and characterize the PL inhibition activities of the major constituents from Fructus Psoraleae (FP), one of the most frequently used Chinese herbs with lipid-lowering activity. To this end, a total of eleven major constituents isolated from Fructus Psoraleae have been obtained and their inhibition potentials against PL have been assayed by a fluorescence-based assay. Among all tested compounds, isobavachalcone, bavachalcone and corylifol A displayed strong inhibition on PL (IC

Topics: Animals; Chalcones; Drugs, Chinese Herbal; Enzyme Inhibitors; Flavones; Fruit; Lipase; Pancrelipase; Psoralea; Swine

Cullen corylifolium is a plant widely used in traditional Chinese medicine for its stomachic, anthelmintic, and diuretic properties. Bavachalcone, which is known as a component of C. corylifolium has been reported to inhibit osteoclast differentiation. However, the anticancer efficacy and mechanism of C. corylifolium and bavachalcone have not been studied.. Our aim is to determine whether C. corylifolium has an anticancer effect and to identify the apoptosis and autophagy mechanism of bavachalcone.. The anti-proliferative activity of C. corylifolium and bavachalcone was measured with MTT assay. Apoptosis was analyzed using Annexin V and propidium iodide staining. The expression of apoptosis, cell cycle and autophagy related gene was evaluated by western blot. Cell cycle stage was investigated with Tali. C. corylifolium exhibited potent effect on apoptosis in HepG2 cells. To identify which compound in C. corylifolium is responsible for this effect, we determined the effects of psoralen, psoralidin, bavachalcone, and isobavachalcone on the activity of bid, caspase 3, and PARP. Of all the studied compounds, bavachalcone was the most potent inducer of apoptosis and acted via crosstalk between the intrinsic and extrinsic pathways. In addition, bavachalcone caused cell cycle arrest and decreased the levels of early cell cycle regulatory proteins such as CDK 4 and CDK 2, whereas p21 and p27 levels were increased. We also investigated the extent to which bavachalcone-induced autophagy and apoptosis were related. Phosphorylation and expression of Akt and mTOR were decreased, while the LC3 Ⅱ to LC3Ⅰ ratio was increased in bavachalcone-treated cells. These results suggest that bavachalcone has anticancer activity by promoting both autophagy and apoptosis in HepG2 cells.. C. corylifolium has an anticancer effect. Especially, bavachalcone has excellent anticancer ability among other components of C. corylifolium by inducing apoptosis and autophagy.

Topics: Antineoplastic Agents, Phytogenic; Apoptosis; Autophagy; Caspase 3; Cell Cycle; Cell Cycle Checkpoints; Chalcones; Fabaceae; Flavones; Hep G2 Cells; Humans; Proto-Oncogene Proteins c-akt; TOR Serine-Threonine Kinases