Abstract

Rhizoma Coptidis (RC) is a widely used traditional Chinese medicine. Although modern research has found that some alkaloids from RC are the pharmacologically active constituents, the differences in their biological effects are not completely clear. This study analyzed the differences in the typical alkaloids in RC at a systematic level and provided comprehensive information on the pharmaceutical mechanisms of the different alkaloids. The ethanol RC extract (RCE) was characterized using HPLC assay. HepG2, 3T3-L1, and RAW264.7 cells were used to detect the cytotoxicity of alkaloids. Transcriptome analyses were performed to elucidate the cellular pathways affected by RCE and alkaloids. HPLC analysis revealed that the typical alkaloids of RCE were berberine, coptisine, and palmatine. Coptisine and berberine displayed a stronger inhibitory effect on cell proliferation than palmatine. The overlapping ratios of differentially expressed genes between RCE and berberine, coptisine, and palmatine were 70.8%, 52.6%, and 42.1%, respectively. Pathway clustering analysis indicated that berberine and coptisine possessed a certain similarity to RCE, and both compounds affected the cell cycle pathway; moreover, some pathways were uniquely enriched by berberine or coptisine. Berberine and coptisine had different regulatory effects on genes involved in lipid metabolism. These results provide comprehensive information on the pharmaceutical mechanisms of the different RC alkaloids and insights into their better combinatory use for the treatment of diseases.

Highlights

  • IntroductionRhizoma Coptidis (RC) is a widely used traditional Chinese medicine

  • National Engineering Research Center for Beijing Biochip Technology, Beijing 102206, China; Department of Pathophysiology, Fenyang College, Shanxi Medical University, Fenyang 032200, China; These authors contributed to this work

  • Considering our previous studies on the regulatory effect of RC extract (RCE) on lipid metabolism, we explored the roles of berberine, coptisine, and palmatine on genes involved in cholesterol biosynthesis and LDL-c uptake, i.e., low-density lipoprotein receptor (LDLR)

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Summary

Introduction

Rhizoma Coptidis (RC) is a widely used traditional Chinese medicine. HPLC analysis revealed that the typical alkaloids of RCE were berberine, coptisine, and palmatine. Coptisine and berberine displayed a stronger inhibitory effect on cell proliferation than palmatine. The overlapping ratios of differentially expressed genes between RCE and berberine, coptisine, and palmatine were 70.8%, 52.6%, and 42.1%, respectively. Berberine and coptisine had different regulatory effects on genes involved in lipid metabolism. These results provide comprehensive information on the pharmaceutical mechanisms of the different RC alkaloids and insights into their better combinatory use for the treatment of diseases. In the Chinese Pharmacopoeia, berberine, coptisine, palmatine, and epiberberine are designated as quality markers for RC

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