Dryocrassin ABBA

The rhizome of Dryopteris crassirhizoma Nakai.

Dryocrassin ABBA Induces Apoptosis in Human Hepatocellular Carcinoma HepG2 Cells Through a Caspase-Dependent Mitochondrial Pathway.[Pubmed:27221859]

Asian Pac J Cancer Prev. 2016;17(4):1823-8.

BACKGROUND: Biological and pharmacological activities of Dryocrassin ABBA, a phloroglucinol derivative extracted from Dryopteris crassirhizoma, have attracted attention. In this study, the apoptotic effect of Dryocrassin ABBA on human hepatocellular carcinoma HepG2 cells was investigated. MATERIALS AND METHODS: We tested the effects of Dryocrassin ABBA on HepG2 in vitro by MTT, flow cytometry, real-time PCR, and Western blotting. KM male mice were used to detect the effect of Dryocrassin ABBA on H22 cells in vivo. RESULTS: Dryocrassin ABBA inhibited the growth of HepG2 cells in a concentration-dependent manner. After treatment with 25, 50, and 75 mug/mL Dryocrassin ABBA, the cell viability was 68%, 60% and 49%, respectively. Dryocrassin ABBA was able to induce apoptosis, measured by propidium iodide (PI)/annexin V-FITC double staining. The results of real-time PCR and Western ting showed that Dryocrassin ABBA up-regulated p53 and Bax expression and inhibited Bcl-2 expression which led to an activation of caspase-3 and caspase-7 in the cytosol, and then induction of cell apoptosis. In vivo experiments also showed that Dryocrassin ABBA treatment significantly suppressed tumor growth, without major side effects. CONCLUSIONS: Overall, these findings provide evidence that Dryocrassin ABBA may induce apoptosis in human hepatocellular carcinoma cells through a caspase-mediated mitochondrial pathway.

Application of a sensitive and accurate LC-MS/MS method for determination of dryocrassin ABBA in rat plasma for a bioavailability study.[Pubmed:24497015]

Biomed Chromatogr. 2014 Sep;28(9):1205-11.

A sensitive and accurate liquid chromatography-tandem mass spectrometry method was developed and validated for the determination of Dryocrassin ABBA, a potential active component isolated from Dryopteris crassirhizoma, in rat plasma. Chromatographic separation was achieved on a Zorbax SB-C18 column (50 x 2.1 mm, 1.8 microm), with elution consisting of eluent (A) 10 mm ammonium acetate in methanol containing 0.1% formic acid and (B) 10 mm ammonium acetate in water containing 0.1% formic acid (A:B = 99:1, v/v) at a flow rate of 0.3 mL/min. Multiple reaction monitoring mode was used to monitor the precursor-product ion transitions of m/z 819.3 --> 403.4 for Dryocrassin ABBA and m/z 426.2 --> 409.2 for internal standard. This assay exhibited a good linearity with a correlation coefficient >0.99 and showed no endogenous interference with the analyte and internal standard. The lower limit of quantification of Dryocrassin ABBA was 4 ng/mL in 50 muL of rat plasma. The method was successfully applied in the pharmacokinetic study of Dryocrassin ABBA in rats after intravenous (2.35 mg/kg) and oral (23.5 mg/kg) doses of Dryocrassin ABBA. The oral bioavailability (F) of Dryocrassin ABBA was estimated to be 50.1%. Our study is the first to clarify the pharmacokinetic behaviors of Dryocrassin ABBA in animals.

Dryocrassin ABBA (Dryocrassin) is a flavonoid natural product derived from Dryopteris crassirhizoma, with antiviral and antibacterial activities. Dryocrassin ABBA exhibits antiviral activity against H5N1 avian influenza virus. Dryocrassin ABBA inhibits the coagulase activity of Staphylococcus aureus vWbp. Dryocrassin ABBA suppresses immunostimulatory function of dendritic cells and prolongs skin allograft survival.

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