Fructus Psoraleae contains natural compounds with potent inhibitory effects towards human carboxylesterase 2

被引：76

作者：

Li, Yao-Guang ^{[1
,2
]}

Hou, Jie ^{[3
]}

Li, Shi-Yang ^{[1
]}

Lv, Xia ^{[1
]}

Ning, Jing ^{[1
,3
]}

Wang, Ping ^{[1
]}

Liu, Zhao-Ming ^{[1
]}

Ge, Guang-Bo ^{[1
]}

Ren, Jia-Yan ^{[2
]}

Yang, Ling ^{[1
]}

机构：

[1] Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China

[2] Shanxi Agr Univ, Coll Anim Sci & Vet Med, Taigu 030801, Peoples R China

[3] Dalian Med Univ, Dalian 116044, Peoples R China

来源：

FITOTERAPIA | 2015年 / 101卷

关键词：

Fructus Psoraleae; Human carboxylesterase 2; Inhibitory effects; LC-DAD-ESI-MS/MS; CATALYTIC-PROPERTIES; FLUORESCENT-PROBE; BAKUCHIOL; IRINOTECAN; CONSTITUENTS; ACTIVATION; COMPONENTS; INTESTINE; ISOZYMES; CES2;

D O I：

10.1016/j.fitote.2015.01.004

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

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 0.62 mu M to 3.89 mu M. This is the first report of the chemical constitutes in FP as potent inhibitors of hCE2. (C) 2015 Elsevier B.V. All rights reserved.

引用

页码：99 / 106

页数：8

共 41 条

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