Chang Yan-Xu, Ge Ai-Hua, Jiang Yan, Teye Azietaku John, Li Jin, Gao Xiu-Mei
Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China; Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
Evid Based Complement Alternat Med. 2016;2016:5965067. doi: 10.1155/2016/5965067. Epub 2016 Jan 26.
Traditional Chinese medicine (TCM) has been used for the treatment of many complex diseases. However, the bioactive components are always undefined. In this study, a bioactivity-based method was developed and validated to screen lipase inhibitors and evaluate the effects of processing on the lipase inhibitory activity of TCM by ultrahigh performance liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry and fraction collector (UHPLC/Q-TOF-MS-FC). The results showed that both Polygonum multiflorum and processed P. multiflorum extracts had inhibitory effect against lipase with IC50 values of 38.84 μg/mL and 190.6 μg/mL, respectively. Stilbenes, phenolic acid, flavonoids, and anthraquinones were considered to be the potential lipase inhibitors. Eleven potential lipase inhibitors were simultaneously determined by UHPLC. Principal component analysis (PCA) was employed in exploring the effects of processing time on lipase inhibitory activity of P. multiflorum. Compared with conventional methods, a bioactivity-based method could quantitatively analyze lipase inhibitory activity of individual constituent and provide the total lipase inhibitory activity of the samples. The results demonstrated that the activity integrated UHPLC/Q-TOF-MS-FC method was an effective and powerful tool for screening and identifying lipase inhibitors from traditional Chinese medicines.
中药已被用于治疗多种复杂疾病。然而，其生物活性成分一直不明确。在本研究中，开发并验证了一种基于生物活性的方法，通过超高效液相色谱-四极杆-飞行时间质谱联用仪和馏分收集器（UHPLC/Q-TOF-MS-FC）筛选脂肪酶抑制剂并评估炮制对中药脂肪酶抑制活性的影响。结果表明，何首乌及其炮制品提取物均对脂肪酶有抑制作用，IC50值分别为38.84μg/mL和190.6μg/mL。二苯乙烯类、酚酸类、黄酮类和蒽醌类被认为是潜在的脂肪酶抑制剂。通过UHPLC同时测定了11种潜在的脂肪酶抑制剂。采用主成分分析（PCA）探究炮制时间对何首乌脂肪酶抑制活性的影响。与传统方法相比，基于生物活性的方法能够定量分析单个成分的脂肪酶抑制活性，并提供样品的总脂肪酶抑制活性。结果表明，活性整合UHPLC/Q-TOF-MS-FC方法是从中药中筛选和鉴定脂肪酶抑制剂的有效且强大的工具。
