College of Food and Bioengineering, South China University of Technology, Guangzhou 510640, China.
Food Chem. 2012 Dec 15;135(4):2175-81. doi: 10.1016/j.foodchem.2012.07.018. Epub 2012 Jul 15.
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.
甜橙 var. amara Engl，芸香科柑橘属植物，在中国广泛分布，民间用于消食、化痰、肠炎、胃病等疾病的治疗。本研究采用硅胶柱层析、Sephadex LH-20、质谱（MS）和核磁共振（NMR）等方法对甜橙 var. amara 的花进行化学成分分离鉴定，采用多种生物活性测定方法评价其抗氧化、抗炎、抗病毒和抗肿瘤活性。首次从甜橙 var. amara 中分离鉴定出两种主要化合物，5-羟基-6,7,3',4'-四甲氧基黄酮（HTF）和柠檬烯酸（LA）。生物活性测定结果表明，HTF 和 LA 在 6.25-50μg/ml 浓度范围内对 B16 细胞系和 12.5-200μg/ml 浓度范围内对 SMCC-7721 细胞系表现出显著的抗氧化活性，对 2.2.15 细胞的抗肿瘤作用、抗炎活性和 HBsAg、HBeAg 的抑制表达均呈现出浓度依赖性趋势。这两种来自甜橙 var. amara 的化合物可能具有作为药物开发中一种有前途的天然药物的潜力。
