Jack Babalwa U, Malherbe Christiaan J, Willenburg Elize L, de Beer Dalene, Huisamen Barbara, Joubert Elizabeth, Muller Christo J F, Louw Johan, Pheiffer Carmen
Biomedical Research and Innovation Platform, South African Medical Research Council, Tygerberg, South Africa.
Division of Medical Physiology, Faculty of Medicine and Health Sciences, University of Stellenbosch, Tygerberg, South Africa.
Planta Med. 2018 Jan;84(2):100-110. doi: 10.1055/s-0043-119463. Epub 2017 Sep 22.
species are increasingly investigated as sources of phenolic compounds with potential as therapeutic agents. Recently, we demonstrated that a crude polyphenol-enriched organic fraction (CPEF) of , currently forming the bulk of commercial production, decreased lipid content in 3T3-L1 adipocytes and inhibited body weight gain in obese db/db mice. The aim of the present study was to determine whether a more effective product and/or one with higher specificity could be obtained by fractionation of the CPEF by purposely increasing xanthone and benzophenone levels. Fractionation of the CPEF using high performance counter-current chromatography (HPCCC) resulted in four fractions (F1-F4), predominantly containing iriflophenone-3---D-glucoside-4---D-glucoside (benzophenone: F1), hesperidin (flavanone: F2), mangiferin (xanthone: F3), and neoponcirin (flavone: F4), as quantified by high-performance liquid chromatography with diode array detection (HPLC-DAD), and confirmed by LC-DAD with mass spectrometric (MS) and tandem MS (MS) detection. All fractions inhibited lipid accumulation in 3T3-L1 pre-adipocytes and decreased lipid content in mature 3T3-L1 adipocytes, although their effects were concentration-dependent. F1-F3 stimulated lipolysis in mature adipocytes. Treatment of mature adipocytes with F1 and F2 increased the messenger RNA expression of hormone sensitive lipase, while treatment with F1 and F4 increased uncoupling protein 3 expression. In conclusion, HPCCC resulted in fractions with different phenolic compounds and varying anti-obesity effects. The activities of fractions were lower than the CPEF; thus, fractionation did not enhance activity within a single fraction worthwhile for exploitation as a nutraceutical product, which illustrates the importance of considering synergistic effects in plant extracts.
越来越多的物种被作为具有治疗潜力的酚类化合物来源进行研究。最近，我们证明了目前构成商业生产主体的[物种名称]的粗制富含多酚有机组分（CPEF）可降低3T3-L1脂肪细胞中的脂质含量，并抑制肥胖db/db小鼠的体重增加。本研究的目的是确定通过有目的地提高氧杂蒽酮和二苯甲酮水平对CPEF进行分馏是否能够获得更有效的产品和/或具有更高特异性的产品。使用高效逆流色谱法（HPCCC）对CPEF进行分馏得到了四个组分（F1-F4），主要包含异戊二烯苯酮-3---D-葡萄糖苷-4---D-葡萄糖苷（二苯甲酮：F1）、橙皮苷（黄烷酮：F2）、芒果苷（氧杂蒽酮：F3）和新橙皮苷（黄酮：F4），通过配有二极管阵列检测的高效液相色谱法（HPLC-DAD）进行定量，并通过配有质谱（MS）和串联质谱（MS）检测的液相色谱-二极管阵列检测（LC-DAD）进行确认。所有组分均抑制3T3-L1前脂肪细胞中的脂质积累，并降低成熟3T3-L1脂肪细胞中的脂质含量，尽管它们的作用具有浓度依赖性。F1-F3刺激成熟脂肪细胞中的脂肪分解。用F1和F2处理成熟脂肪细胞可增加激素敏感性脂肪酶的信使核糖核酸表达，而用F1和F4处理可增加解偶联蛋白3的表达。总之，HPCCC得到了具有不同酚类化合物和不同抗肥胖作用的组分。各组分的活性低于CPEF；因此，分馏并未提高单一组分中值得作为营养保健品开发利用的活性，这说明了考虑植物提取物中协同效应的重要性。
