Li Yao-Guang, Hou Jie, Li Shi-Yang, Lv Xia, Ning Jing, Wang Ping, Liu Zhao-Ming, Ge Guang-Bo, Ren Jia-Yan, Yang Ling
Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, China; College of Animal Science and Veterinary Medicine, Shanxi Agricultural University, Taigu 030801, China.
Dalian Medical University, Dalian 116044, China.
Fitoterapia. 2015 Mar;101:99-106. doi: 10.1016/j.fitote.2015.01.004. Epub 2015 Jan 13.
Fructus Psoraleae (FP) is an edible Chinese herbal which is widely used in Asia for the treatment of various diseases including asthma, diarrhea, and osteoporosis. This study aimed to investigate the inhibitory effects of the crude ethanol extract from FP on human carboxylesterase 2 (hCE2), as well as to identity and characterize the naturally occurring inhibitors of hCE2 in FP. Our results demonstrated that the ethanol extract of FP displayed potent inhibitory effects towards hCE2, while five major bioactive constitutes in FP were efficiently identified by LC-DAD-ESI-MS/MS, with the aid of LC-based activity profiling. The identified bioactive compounds including neobavaisoflavone, isobavachalcone, bavachinin, corylifol A and bakuchiol were found to be naturally occurring potent inhibitors of hCE2, with low Ki values ranging from 0.62μM to 3.89μM. This is the first report of the chemical constitutes in FP as potent inhibitors of hCE2.
补骨脂是一种可食用的中草药，在亚洲被广泛用于治疗包括哮喘、腹泻和骨质疏松症在内的各种疾病。本研究旨在研究补骨脂粗乙醇提取物对人羧酸酯酶2（hCE2）的抑制作用，并鉴定和表征补骨脂中天然存在的hCE2抑制剂。我们的结果表明，补骨脂乙醇提取物对hCE2具有显著的抑制作用，同时借助基于液相色谱的活性分析，通过LC-DAD-ESI-MS/MS有效地鉴定了补骨脂中的五种主要生物活性成分。所鉴定的生物活性化合物包括新补骨脂异黄酮、异补骨脂查尔酮、补骨脂宁、补骨脂酚A和补骨脂酚，它们是天然存在的hCE2有效抑制剂，Ki值较低，范围为0.62μM至3.89μM。这是关于补骨脂化学成分作为hCE2有效抑制剂的首次报道。
