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Comprehensive study of rutaecarpine on vascular constriction relative to RhoA/MLCP-MLC signaling

Xiukun Wang, Yugang Wang, Yushuang Chai, Jun Hu, Honglei Zhan, Dongming Xing, Xuefu You, Zhimin Wang, Xiuwei Yang, Fan Lei, Lijun Du*   

  1. 1. Protein Science Laboratory of the Ministry of Education, Laboratory of Pharmaceutical Sciences, School of Life Sciences and School of Medicine, Tsinghua University, Beijing 100084, China
    2. Institute of Medicinal Biotechnology, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China
    3. Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China
    4. School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2011-11-20 Revised:2012-05-20 Online:2012-09-15 Published:2012-09-15
  • Contact: Lijun Du*

Abstract: The aims of the present study are to investigate the effect of vasoconstriction and to explore the mechanism of rutaecarpine. The research findings showed that rutaecarpine could induce contractions of the rat thoracic aorta in vitro. The inhibitors of Rho-kinase and inositol 1,4,5-triphosphate receptor (IP3R) could suppress the effect of rutaecarpine-induced vasoconstriction. In the study of A7r5 cells (a line of smooth muscle cells), 300 μg/L rutaecarpine promoted the concentration of intracellular Ca2+ and enhanced the IP3R expression, which connects with 1,4,5-triphosphate to evoke the release of Ca2+ from the intracellular stores. Rutaecarpine increased the RhoA mRNA expression when the cells were pretreated with inhibitor H-1152, and improved the levels of phosphorylation of myosin light chain phosphatase (MLCP) and myosin light chain (MLC). These results suggest that rutaecarpine plays a role in vasoconstriction relative to the RhoA/MLCP-MLC signaling pathway, which denotes a new field of rutaecarpine in pharmacology.

Key words: Rutaecarpine, Blood vessel, Myosin light chain

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