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Relaxation effect of a novel Danshensu/tetramethylpyrazine derivative on rat mesenteric arteries
Li R.W.-S.1; Yang C.2; Shan L.3; Zhang Z.3; Wang Y.3; Kwan Y.W.4; Lee S.M.Y.5; Hoi M.P.M.5; Chan S.W.6; Cheung A.C.1; Cheung K.H.7; Leung G.P.H.1
2015-08-15
Source PublicationEuropean Journal of Pharmacology
ISSN18790712 00142999
Volume761Pages:153-160
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.

KeywordCalcium Channel Danshensu Tetramethylpyrazine Mesenteric Artery Relaxation
DOI10.1016/j.ejphar.2015.04.041
URLView the original
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000359227300020
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Cited Times [WOS]:12   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorLeung G.P.H.
Affiliation1.Department of Pharmacology and Pharmacy, The University of Hong Kong, Hong Kong
2.Ethnic Drug Screening & Pharmacology Center, Key Laboratory of Chemistry in Ethnic Medicinal Resources, State Ethnic Affairs Commission & Ministry of Education, Yunnan Minzu University, Kunming 650500, China
3.Institute of New Drug Research and Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine, Jinan University College of Pharmacy, Guangzhou 510632, China
4.School of Biomedical Sciences, The Chinese University of Hong Kong, Hong Kong
5.Institute of Chinese Medical Sciences, University of Macau, Macau, China
6.Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong
7.Department of Physiology, The University of Hong Kong, Hong Kong
Recommended Citation
GB/T 7714
Li R.W.-S.,Yang C.,Shan L.,et al. Relaxation effect of a novel Danshensu/tetramethylpyrazine derivative on rat mesenteric arteries[J]. European Journal of Pharmacology,2015,761:153-160.
APA Li R.W.-S..,Yang C..,Shan L..,Zhang Z..,Wang Y..,...&Leung G.P.H..(2015).Relaxation effect of a novel Danshensu/tetramethylpyrazine derivative on rat mesenteric arteries.European Journal of Pharmacology,761,153-160.
MLA Li R.W.-S.,et al."Relaxation effect of a novel Danshensu/tetramethylpyrazine derivative on rat mesenteric arteries".European Journal of Pharmacology 761(2015):153-160.
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