Citrus aurantium L. var. amara Engl, a member of genus Citrus (Rutaceae), widespread in China, is used as folk medicine for the treatment of helping digest, phlegm, enteritidis, stomachic and other deceases. In the present research, silica gel column, Sephadex LH-20, mass spectrometer (MS) and nuclear magnetic resonance (NMR) were used to separate and identify the chemical compounds from the flowers of C. aurantium var. amara , and several bioactivity assays were used to evaluate their antioxidant, anti-inflammatory, anti-virus and antitumour activities. Two major compounds, 5-hydroxy-6,7,3′,4′-tetramethoxyflavone (HTF) and limonexic acid (LA), were isolated and identified from C. aurantium var. amara for the first time. The results of the bioactivity assays showed that HTF and LA displayed significant antioxidant activities and showed significant inhibition effects on the B16 cell lines at a concentration range from 6.25 to 50 μg/ml, and on the SMCC-7721 cell lines from 12.5 to 200 μg/ml. The antitumour effect, anti-inflammatory activity and the inhibiting expression of HBsAg and HBeAg of 2.2.15 cells displayed the tendency in a concentration-dependent manner. These two compounds from C. aurantium var. amara could potentially be used as a promising natural agent in the pharmaceutical industries.
Kaihui Zhang,Meiqi Wang,Yufeng Yao,Tao Huang,Fangle Liu,Chenchen Zhu,Chaozhan Lin
A rapid, sensitive, and reliable ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method has been developed to simultaneously determine the major bioactive components of Xiaoyan Lidan Formula (XYLDF) in rat plasma, using sulfamethoxazole as the internal standard (IS). The seven major bioactive components are andrographolide, dehydroandrographolide, enmein, 1-methoxicabony-β-carboline, 4,5-dimethoxy-canthin-6-one, 4-methoxy-5-hydroxy-canthin-6-one, and 1-hydroxymethyl-β-carboline. After pretreating by protein precipitation with methanol, separation was performed on a UPLC C18 column using gradient elution with a mobile phase consisting of acetonitrile and 0.1% formic acid at a flowing rate of 0.7 mL/min. Detection was performed on TSQ Quantum mass spectrometry set at the positive/negative ionization and multiple reaction monitoring (MRM) mode. The intra- and inter-day precision were less than 9.8%, whereas the intra- and inter-day accuracy were within ± 13.4%. The method was validated and applied to compare the pharmacokinetic profiles of the analytes in serum of Alpha-naphthylisothiocyanate (ANIT)-induced cholestasis and control rats after oral administration of XYLDF. The results showed remarkable differences in pharmacokinetic properties of the analytes between cholestatic (model) and control groups, thereby providing essential scientific information for better understanding of mechanism of XYLDF and a reference for its clinical applications.
危险品化学品经营许可证（带存储）