Home
Resources
Publications
Biflavones From Ginkgo Biloba as Inhibitors of Human Thrombin

Biflavones From Ginkgo Biloba as Inhibitors of Human Thrombin

Tian-Ran Chen, Ling-Hua Wei, Xiao-Qing Guan, Chao Huang, Zhe-Yi Liu, Fang-Jun Wang, Jie Hou, Qiang Jin, Yi-Fan Liu, Pei-Hao Wen, Shui-Jun Zhang, Guang-Bo Ge, Wen-Zhi Guo

Bioorg Chem. 2019 Nov;92:103199.

PMID: 31446241

Abstract:

Ginkgo Biloba leaf extract has been widely used for the prevention and treatment of thrombosis and cardiovascular disease in both eastern and western countries, but the bioactive constituents and the underlying mechanism of anti-thrombosis have not been fully characterized. The purpose of this study was to investigate the inhibitory effects of major constituents in Ginkgo biloba on human thrombin, a key serine protease regulating the blood coagulation cascade and the processes of thrombosis. To this end, a fluorescence-based biochemical assay was used to assay the inhibitory effects of sixteen major constituents from Ginkgo biloba on human thrombin. Among all tested natural compounds, four biflavones (ginkgetin, isoginkgetin, bilobetin and amentoflavone), and five flavonoids (luteolin, apigenin, quercetin, kaempferol and isorhamnetin) were found with thrombin inhibition activity, with the IC50 values ranging from 8.05 μM to 82.08 μM. Inhibition kinetic analyses demonstrated that four biflavones were mixed inhibitors against thrombin-mediated Z-GGRAMC acetate hydrolysis, with the Ki values ranging from 4.12 μM to 11.01 μM. Molecular docking method showed that the four biflavones could occupy the active cavity with strong interactions of salt bridges and hydrogen bonds. In addition, mass spectrometry-based lysine labeling reactivity assay suggested that the biflavones could bind on human thrombin at exosite I rather than exosite II. All these findings suggested that the biflavones in Ginkgo biloba were naturally occurring inhibitors of human thrombin, and these compounds could be used as lead compounds for the development of novel thrombin inhibitors with improved efficacy and high safety profiles.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP521324	Bilobetin		521-32-4	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: