Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/30839
Title: Relaxation effect of a novel Danshensu/tetramethylpyrazine derivative on rat mesenteric arteries
Authors: Li, RWS
Yang, C
Shan, L
Zhang, Z
Wang, Y
Kwan, YW
Lee, SMY
Hoi, MPM
Chan, SW
Cheung, AC
Cheung, KH
Leung, GPH
Keywords: Calcium channel
Danshensu tetramethylpyrazine
Mesenteric artery
Relaxation
Issue Date: 2015
Publisher: Elsevier
Source: European journal of pharmacology, 2015, v. 761, p. 153-160 How to cite?
Journal: European journal of pharmacology 
Abstract: Danshen (Radix Salviae miltiorrhizae) and ChuanXiong (Ligusticum wallichii) are two traditional herbal medicines commonly used in China for the treatment of cardiovascular diseases. The active components in Danshen and ChuanXiong are Danshensu (DSS, (R)-3, 4-dihydroxyphenyllactic acid) and tetramethylpyrazine (TMP), respectively. In the present study, a new compound named ADTM, which is a conjugation of DSS and TMP, was synthesized and its effect on the contractility of rat mesenteric arteries was examined. The relaxation effect of ADTM on rat mesenteric arteries was studied using myography. The effects of ADTM on Ca2+ channels were measured by Ca2+ imaging and patch-clamp techniques. The results showed that ADTM caused a concentration-dependent relaxation of rat mesenteric arteries. This relaxation effect was not affected by the removal of endothelium or inhibitors of nitric oxide synthase, cyclooxygenase, guanylyl cyclase and adenylyl cyclase. Potassium channel blockers including tetraethylammonium, iberiotoxin, apamin, 4-aminopyridine, BaCl2 and glibenclamide also failed to inhibit the relaxation response to ADTM. ADTM inhibited CaCl2-induced contractions and reduced the Ca2+ influx in isolated mesenteric arterial muscle cells. Our results suggest that ADTM may be a novel relaxing agent. Its mechanism of action involves the direct blockade of voltage-gated Ca2+ channels in vascular smooth muscle cells, resulting in a decrease in Ca2+ influx into the cells.
URI: http://hdl.handle.net/10397/30839
ISSN: 0014-2999
DOI: 10.1016/j.ejphar.2015.04.041
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