Document Detail

Selective inhibition of vascular smooth muscle cell proliferation by coptisine isolated from Coptis rhizoma, one of the crude drugs composing Kampo medicines Unsei-in.
MedLine Citation:
PMID:  16635741     Owner:  NLM     Status:  MEDLINE    
Acceleration of vascular smooth muscle cell (VSMC) proliferation is closely linked to the pathogenesis of vascular diseases. We, therefore, focused on traditional Japanese herbal medicines (Kampo medicines) used to ameliorate the impairment of microcirculation or blood stasis and screened them for their ability to inhibit rat VSMC proliferation. Among them, Unsei-in was found to effectively suppress VSMC proliferation, and Coptis rhizome was the responsible constituent crude drug. The extract of Coptis rhizome inhibited VSMC proliferation with the GI(50) value of 4.4 microg/ml, which was much lower than those against the proliferation of 3Y1, dRLh-84, B16, and HeLa cells. The Coptis rhizome extract inhibited the progression of VSMC arrested at G(0)/G(1) phase from G(0)/G(1) to S phase, but not that of 3Y1 cells. Biological assay-guided fractionation revealed that an alkaloid of Coptis rhizome, coptisine, was the active ingredient in selectively preventing VSMC proliferation with GI(50) of 3.3 microM (1.2 microg/ml). When the structurally-related isoquinoline alkaloids of protoberberine class were studied for their inhibitory activities, berberine decreased the VSMC proliferation with GI(50) of 95.1 microM (35.4 microg/ml), about 30 times higher concentration than coptisine, while palmatine failed to show any activity. This study provides evidence that coptisine, an ingredient of Unsei-in, prevents VSMC proliferation selectively at lower concentrations compared with various cells or other structurally related alkaloids.
H Tanabe; H Suzuki; A Nagatsu; H Mizukami; Y Ogihara; M Inoue
Publication Detail:
Type:  Comparative Study; Journal Article     Date:  2005-09-23
Journal Detail:
Title:  Phytomedicine : international journal of phytotherapy and phytopharmacology     Volume:  13     ISSN:  0944-7113     ISO Abbreviation:  Phytomedicine     Publication Date:  2006 May 
Date Detail:
Created Date:  2006-04-25     Completed Date:  2006-08-16     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9438794     Medline TA:  Phytomedicine     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  334-42     Citation Subset:  IM    
Laboratory of Pharmacognosy, Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya 467-8603, Japan.
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MeSH Terms
Berberine / analogs & derivatives*,  pharmacology
Cell Cycle / drug effects
Cell Proliferation / drug effects*
Chromatography, High Pressure Liquid / methods
Coptis / chemistry*
Drugs, Chinese Herbal / chemistry,  pharmacology
Hela Cells
Inhibitory Concentration 50
Medicine, Kampo*
Melanoma, Experimental
Muscle, Smooth, Vascular / cytology,  drug effects*
Rats, Sprague-Dawley
Rhizome / chemistry
Reg. No./Substance:
0/Drugs, Chinese Herbal; 0/unsei in; 2086-83-1/Berberine; 3486-66-6/coptisine

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