Discovery of a Novel ERp57 Inhibitor as Antiplatelet Agent from Danshen (Salvia miltiorrhiza)

Evidence-based Complementary and Alternative Medicine : ECAM
Jia ZouGuozhen Cui

Abstract

Danshen (Salvia miltiorrhiza) is a well-known herb in Traditional Chinese Medicine (TCM) for treating cardiovascular diseases, but the underlying mechanism remains to be fully elucidated. Here, we showed that Danshen and its active ingredient rosmarinic acid exhibited antiplatelet effects through the inhibition of ERp57, a member of protein disulfide isomerase (PDI) with potential roles in platelet aggregation. Danshen extract (DSE) exhibited potent inhibitory effects on the platelet aggregation induced by arachidonic acid- (AA-) induced platelet aggregation and the enzymatic activity of ERp57. Rosmarinic acid was identified by virtual screening and molecular docking as one of the hit compounds for ERp57. In line with this, rosmarinic acid displayed significant inhibitory effect on ERp57 activity and inhibited AA-induced platelet aggregation. Taken together, we demonstrated for the first time that DSE and rosmarinic acid displayed inhibitory effects on the catalytic activity of ERp57, providing evidence of the regulatory role of ERp57 underlying the antiplatelet effects of Danshen.

References

Jun 28, 2003·BMJ : British Medical Journal·N J Wald, M R Law
Jan 19, 2007·Biochemical Pharmacology·Hwa Jung LeeYeong-Min Park
Mar 17, 2007·International Journal of Cardiology·Tsung O Cheng
May 7, 2008·The American Journal of Chinese Medicine·Yan YaoDe-An Guo
May 30, 2009·Antioxidants & Redox Signaling·Feras Hatahet, Lloyd W Ruddock
Feb 2, 2010·Nature Reviews. Drug Discovery·Alan D Michelson
Dec 16, 2011·Journal of Thrombosis and Haemostasis : JTH·L-M HolbrookJ M Gibbins
May 9, 2012·The Journal of Clinical Investigation·Reema JasujaRobert Flaumenhaft
Oct 3, 2012·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Xuelin ZhouJohn H K Yeung
Jan 8, 2013·International Journal of Cardiology·Guozhen CuiSimon Mingyuen Lee
Apr 2, 2013·Trends in Cardiovascular Medicine·Robert Flaumenhaft
Mar 29, 2014·Circulation Research·Bruce Furie, Robert Flaumenhaft
Feb 5, 2016·Planta medica·Solomon K S AmoahMaique W Biavatti
Nov 5, 2016·The American Journal of Chinese Medicine·Guozhen CuiSimon Ming-Yuen Lee

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Citations

Jun 12, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jian CuiQing-Wen Zhang
Apr 25, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Wantida ChaiyanaPimporn Leelapornpisid
Jun 21, 2021·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Qiuyang HuangLi Ma
May 5, 2021·Antioxidants & Redox Signaling·Renato Simões Gaspar, Jonathan M Gibbins
Nov 7, 2021·Purinergic Signalling·Gilnei Bruno da SilvaMargarete Dulce Bagatini

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Methods Mentioned

BETA
protein folding
Assay
X-ray

Software Mentioned

MOE
SPSS

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