Selective inhibition of vascular smooth muscle cell proliferation by coptisine isolated from Coptis rhizoma, one of the crude drugs composing Kampo medicines Unsei-in

Phytomedicine : International Journal of Phytotherapy and Phytopharmacology
H TanabeM Inoue

Abstract

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), abou...Continue Reading

References

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Citations

Mar 16, 2012·The American Journal of Chinese Medicine·Li-Li GongGuan-Hua Du
Jun 10, 2004·Biological & Pharmaceutical Bulletin·Makoto InoueHajime Mizukami
Feb 2, 2008·Chemical & Pharmaceutical Bulletin·Kazuo KojimaAkito Nagatsu
Feb 23, 2019·Journal of Separation Science·Jiahui WangNing Zhang
May 16, 2019·Journal of Nanobiotechnology·Sisi LaiYang Yu
Nov 9, 2018·Evidence-based Complementary and Alternative Medicine : ECAM·Kang XuXuefeng Qiu

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