Chang Yaqing, Zhang Dan, Yang Guiya, Zheng Yuguang, Guo Long
Traditional Chinese Medicine Processing Technology Innovation Center of Hebei Province, Hebei University of Chinese Medicine, Shijiazhuang, China.
Hebei Chemical and Pharmaceutical College, Shijiazhuang, China.
Front Pharmacol. 2021 May 7;12:675396. doi: 10.3389/fphar.2021.675396. eCollection 2021.
Pancreatic lipase is a key lipase for triacylglyceride digestion and absorption, which is recognized as a promising target for treatment of metabolic disorders. Natural phytochemicals are hopeful sources for pancreatic lipase inhibitors. The leaves of H.Lév. and Vaniot (AL) is commonly used as herbal medicine or food supplement in China and other Asian countries for hundreds of years. AL mainly contains essential oils, phenolic acids, flavonoids and terpenoids, which exhibit many pharmacological activities such as antioxidant, anti-inflammatory, antimicrobial, analgetic, anti-cancer, anti-diabetes and immunomodulatory effects. However, the anti-lipase activity of AL was lack of study and the investigation of anti-lipase ingredients from AL was also insufficient. In the present study, the anti-lipase activity of AL was evaluated and the potentially pancreatic lipase inhibitors of AL were investigated. High performance liquid chromatography was used to establish fingerprints of AL samples, and fifteen peaks were selected. The anti-lipase activities of AL samples were evaluated by a pancreatic lipase inhibition assay. Then, the spectrum-effect relationships between fingerprints and pancreatic lipase inhibitory activities were investigated to identify the anti-lipase constitutes in AL. As the results, four caffeoylquinic acids, which were identified as neochlorogenic acid, chlorogenic acid, isochlorogenic acid B, and isochlorogenic acid A by high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry, were selected as potential pancreatic lipase inhibitors in AL. Moreover, anti-lipase activity assessment and molecular docking study of the four compounds were performed to validate the potential lipase inhibitors in AL. The results revealed that the four caffeoylquinic acids in AL as bioactive compounds displayed with anti-lipase activity. The present research provided evidences for the anti-lipase activity of AL, and suggested that some bioactive compounds in AL could be used as lead compounds for discovering of new pancreatic lipase inhibitors.
胰腺脂肪酶是三酰甘油消化和吸收的关键脂肪酶，被认为是治疗代谢紊乱的一个有前景的靶点。天然植物化学物质是胰腺脂肪酶抑制剂的有望来源。亮叶桦（Betula luminifera H. Winkl.）和香桦（Betula insignis Franch.）的叶子（AL）在中国和其他亚洲国家数百年来一直被用作草药或食品补充剂。AL主要含有精油、酚酸、黄酮类化合物和萜类化合物，具有许多药理活性，如抗氧化、抗炎、抗菌、止痛、抗癌、抗糖尿病和免疫调节作用。然而，AL的抗脂肪酶活性缺乏研究，对其抗脂肪酶成分的研究也不足。在本研究中，评估了AL的抗脂肪酶活性，并研究了其潜在的胰腺脂肪酶抑制剂。采用高效液相色谱法建立AL样品的指纹图谱，共选择了15个峰。通过胰腺脂肪酶抑制试验评估AL样品的抗脂肪酶活性。然后，研究指纹图谱与胰腺脂肪酶抑制活性之间的谱效关系，以确定AL中的抗脂肪酶成分。结果，通过高效液相色谱-四极杆飞行时间质谱法鉴定为新绿原酸、绿原酸、异绿原酸B和异绿原酸A的四种咖啡酰奎尼酸被选为AL中潜在的胰腺脂肪酶抑制剂。此外，对这四种化合物进行了抗脂肪酶活性评估和分子对接研究，以验证AL中潜在的脂肪酶抑制剂。结果表明，AL中的四种咖啡酰奎尼酸作为生物活性化合物具有抗脂肪酶活性。本研究为AL的抗脂肪酶活性提供了证据，并表明AL中的一些生物活性化合物可作为发现新型胰腺脂肪酶抑制剂的先导化合物。
