Chen Guilin, Li Xun, Saleri Flora, Guo Mingquan
Key Laboratory of Plant Germplasm Enhancement and Specialty Agriculture, Wuhan Botanical Garden, Chinese Academy of Sciences, Wuhan 430074, China.
Graduate University of Chinese Academy of Sciences, Beijing 100049, China.
Molecules. 2016 Sep 23;21(10):1275. doi: 10.3390/molecules21101275.
Rhamnus davurica Pall. (R. davurica) has been used as a traditional medicinal herb for many years in China and abroad. It has been well documented as a rich source of flavonoids with diversified structures, which in turn results in far-ranging biological activities, such as anti-inflammation, anticancer, antibacterial and antioxidant activities. In order to further correlate their anticancer potentials with the phytochemical components, the fingerprint profile of R. davurica herb from Dongbei was firstly investigated using HPLC-ESI-MS/MS. Thirty two peaks were detected and identified, 14 of which were found in R. davurica for the first time in this work. Furthermore, a total of 23 peaks were resolved as flavonoids, which are the major components found in R. davurica. Meanwhile, the antiproliferative activities against human cancer cells of HT-29 and SGC-7901 in vitro exhibited distinct inhibitory effects with IC50 values at 24.96 ± 0.74 and 89.53 ± 4.11 μg/mL, respectively. Finally, the general toxicity against L-O2 cells displayed a much higher IC50 at 229.19 ± 8.52 μg/mL, which suggested very low or no toxicity on hepatic cell viability. The current study revealed for the first time the correlations between the flavonoids of R. davurica with their antiproliferative activities, which indicated that the fingerprint profile of flavonoids and their anticancer activities could provide valuable information on the quality control for herbal medicines and their derived natural remedies from this valuable medicinal plant.
鼠李在中国和国外已被用作传统草药多年。它作为多种结构黄酮类化合物的丰富来源已有充分记载，这些黄酮类化合物又具有广泛的生物活性，如抗炎、抗癌、抗菌和抗氧化活性。为了进一步将其抗癌潜力与植物化学成分联系起来，首先采用HPLC-ESI-MS/MS对东北鼠李草的指纹图谱进行了研究。检测并鉴定出32个峰，其中14个峰是本研究首次在鼠李中发现的。此外，共解析出23个黄酮类化合物峰，它们是鼠李中的主要成分。同时，其对人癌细胞HT-29和SGC-7901的体外增殖抑制活性表现出明显的抑制作用，IC50值分别为24.96±0.74和89.53±4.11μg/mL。最后，其对L-O2细胞的一般毒性显示出更高的IC50，为229.19±8.52μg/mL，这表明对肝细胞活力的毒性非常低或无毒性。本研究首次揭示了鼠李黄酮类化合物与其增殖抑制活性之间的相关性，这表明黄酮类化合物的指纹图谱及其抗癌活性可为这种珍贵药用植物的草药及其衍生天然药物的质量控制提供有价值的信息。
