PDF(Pubmed)
Abstract：
Edible berries such as the fruits of black chokeberry (Aronia melanocarpa (Michx.) Elliott) and bilberry (Vaccinium myrtillus L.) are considered to be rich in phenolic compounds, which are nowadays attracting great interest due to their promising health benefits. The main objective of our study was to investigate, for the first time, their inhibitory properties on Src tyrosine kinase activity, as this enzyme plays an important role in multiple cellular processes and is activated in both cancer and inflammatory cells. In hydroethanolic fruit extracts, 5.0-5.9% of total polyphenols were determined spectrophotometrically, including high amounts of hydroxycinnamic acid derivatives. HPLC analysis revealed that the black chokeberry and bilberry extracts contained 2.05 mg/g and 2.54 mg/g of chlorogenic acid, respectively. Using a time-resolved fluorescence resonance energy transfer (TR-FRET) assay, the extracts studied were found to have comparable inhibitory effects on Src tyrosine kinase, with IC50 values of 366 µg/mL and 369 µg/mL, respectively. The results also indicated that chlorogenic acid contributes significantly to the observed effect. In addition, both fruit extracts exhibited antioxidant activity by scavenging DPPH and NO radicals with SC50 values of 153-352 µg/mL. Our study suggested that black chokeberry and bilberry fruits may be beneficial in cancer and other inflammation-related diseases.
摘要：
食用浆果，例如黑苦莓的果实（Aroniamelanocarpa（Michx。）艾略特）和越橘（VacciniummyrtillusL.）被认为富含酚类化合物，由于它们有前途的健康益处，它们如今吸引了极大的兴趣。我们研究的主要目的是调查，第一次,它们对Src酪氨酸激酶活性的抑制特性，因为这种酶在多个细胞过程中起着重要作用，并且在癌症和炎症细胞中都被激活。在含水乙醇果实提取物中，分光光度法测定总多酚的5.0-5.9％，包括大量的羟基肉桂酸衍生物。HPLC分析表明，黑苦莓和越橘提取物含有2.05mg/g和2.54mg/g绿原酸，分别。使用时间分辨荧光共振能量转移（TR-FRET）测定，研究发现提取物对Src酪氨酸激酶具有相当的抑制作用，IC50值为366µg/mL和369µg/mL，分别。结果还表明绿原酸对观察到的效果有显著贡献。此外,两种水果提取物均通过清除DPPH和NO自由基而表现出抗氧化活性，SC50值为153-352µg/mL。我们的研究表明，黑苦莓和越橘果实可能对癌症和其他炎症相关疾病有益。
