• Asian Pacific Journal of Cancer Prevention
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• v.15 no.1
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• pp.495-499
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• 2014

Estrogens are considered the major breast cancer risk factor, and the carcinogenic potential of estrogens might be attributed to DNA modification caused by derivatives formed during metabolism. $17{\beta}$-estradiol ($E_2$), the main steroidal estrogen present in women, is metabolized via two major pathways: formation of 2-hydroxyestradiol (2-OH $E_2$) and 4-hydroxyestradiol ($4-OH\;E_2$) through the action of cytochrome P450 (CYP) 1A1 and 1B1, respectively. Previous reports suggested that $2-OH\;E_2$ has putative protective effects, while $4-OH\;E_2$ is genotoxic and has potent carcinogenic activity. Thus, the ratio of $2-OH\;E_2/4-OH\;E_2$ is a critical determinant of the toxicity of $E_2$ in mammary cells. In the present study, we investigated the effects of berberine on the expression profile of the estrogen metabolizing enzymes CYP1A1 and CYP1B1 in breast cancer MCF-7 cells. Berberine treatment produced significant induction of both forms at the level of mRNA expression, but with increased doses produced 16~ to 52~fold greater induction of CYP1A1 mRNA over CYP1B1 mRNA. Furthermore, berberine dramatically increased CYP1A1 protein levels but did not influence CYP1B1 protein levels in MCF-7 cells. In conclusion, we present the first report to show that berberine may provide protection against breast cancer by altering the ratio of CYP1A1/CYP1B1, could redirect $E_2$ metabolism in a more protective pathway in breast cancer MCF-7 cells.

• Biomolecules & Therapeutics
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• v.17 no.1
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• pp.70-78
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• 2009

Coptis japonica (C. japonica) is a perennial medicinal plant that has anti-inflammatory activity. C. japonica contains numerous biologically active alkaloids including berberine, palmatine, epi-berberine, and coptisine. The most well-known anti-inflammatory principal in C. japonica is berberine. For example, berberine has been implicated in the inhibition of iNOS induction by cytokines in microglial cells. However, the efficacies of other alkaloids components on microglial activation were not investigated yet. In this study, we investigated the effects of three alkaloids (palmatine, epi-berberine and coptisine) from C. japonica on lipopolysaccharide (LPS)-induced microglial activation. BV2 microglial cells were immunostimulated with LPS and then the production of several inflammatory mediators such as nitric oxide (NO), reactive oxygen species (ROS) and matrix metalloproteinase-9 (MMP-9) were examined as well as the phosphorylation status of Erk1/2 mitogen activated protein kinase (MAPK). Palmatine and to a lesser extent epi-berberine and coptisine, significantly reduced the release of NO, which was mediated by the inhibition of LPS-stimulated mRNA and protein induction of inducible nitric oxide synthase (iNOS) from BV2 microglia. In addition to NO, palmatine inhibited MMP-9 enzymatic activity and mRNA induction by LPS. Palmatine also inhibited the increase in the LPS-induced MMP-9 promoter activity determined by MMP-9 promoter luciferase reporter assay. LPS stimulation increased Erk1/2 phosphorylation in BV2 cells and these alkaloids inhibited the LPS-induced phosphorylation of Erk1/2. The anti-inflammatory effect of palmatine in LPS-stimulated microglia may suggest the potential use of the alkaloids in the modulation of neuroinflammatory responses, which might be important in the pathophysiological events of several neurological diseases including Alzheimer's disease (AD), multiple sclerosis (MS), Parkinson's disease (PD) and stroke.

• The Korean Journal of Food And Nutrition
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• v.27 no.3
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• pp.532-537
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• 2014

Cortex Phellodendri (CP) is derived from the dried bark of Phellodendron amurense. It has been widely used as a drug in traditional Korea medicine for treating diarrhea, jaundice, swelling pains in the knees and feet, urinary tract infections, and infections of the body surface. Many analytical methods have been used to study oriental herbal medicines, such as thin-layer chromatography, column liquid chromatography, and high performance liquid chromatography (HPLC). In this study, preparative centrifugal partition chromatography (CPC) was successfully carried out in order to separate pure compounds from a CP methanol extract. The optimum two-phase CPC solvent system was composed of n-butanol: acetic acid: water (4:1:5 v/v/v). The flow rate of the mobile phase was 3 mL/min in ascending mode with rotation at 1,000 rpm. The CPC-separated fraction and purification procedures were carried out by preparatory HPLC. The $^1H$ NMR spectrum revealed that the resonances at ${\delta}$ 4.10 and 4.20 ppm corresponded to three protons ($-OCH_3$), whereas those at ${\delta}$ 6.10 ppm corresponded to two protons ($-OCH_2O-$). Further, two aromatic protons (H-11 and H-12) conveys a doublet-doublet pattern. The H-11 doublet and H-12 doublet appear at ${\delta}$ 7.98 and 8.11, respectively. The $^{13}C$ NMR. spectrum showed a tetrasubstituted with a methylenedioxy group at C2 and C3, and two methoxy groups at C9 and C10. The chemical structure of the berberine was identified by $^1H$, $^{13}C$-nuclear magnetic resonance and electrospray ionization-mass spectroscopy spectral data analysis.

• Journal of the Korean Chemical Society
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• v.41 no.2
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• pp.98-104
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• 1997

A simple, accurate and reproducible capillary electrophoresis(CE) assay has been developed for the determination of berberine, cinnamic acid, and glycyrrhizin which are used in traditional Korean medicinal preparations. Separation of these compounds was performed in 20 mM phosphate buffer(pH 7.5) and acetonitrile(75:25, v/v) using a bare fused silica capillary($57 cm{\times}75 {\mu}m$ i.d.) at 25$^{\circ}C$. With the electric field of 350 V/cm, the time needed for the separation of berberine, cinnamic acid and glycyrrhizin was within 13 min. Calibration curves were linear for 1∼100 ${\mu}g/mL$ berberine, 0.3∼100 ${\mu}g/mL$ cinnamic acid and 2.5∼100 ${\mu}g/mL$ glycyrrhizin. The ranges of relative standard deviations(n=5) for those samples were between 0.96∼2.35%. The limits of detection(S/N=3) for berberine, cinnamic acid and glycyrrhizin were 0.5, 0.1 and 2.0 ${\mu}g/mL$, respectively. The numbers of theoretical plates were 181,000(berberine), 88,000(cinnamic acid) and 169,000(glycyrrhizin), while they were 3,100∼4,800 in HPLC.

• Korean Journal of Pharmacognosy
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• v.29 no.2
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• pp.125-128
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• 1998

Sporadic diarrhea occurring predominantly in infants and young children is a significant illness of worldwide importance. Rotaviruses are the etiologic agents for 47% of the cases of infantile diarrhea in Seoul, Korea. This research was undertaken to investigate the inhibitory effect of traditional herbal medicines on rotatvirus infection. Among tested 50 kinds of herbal medicines, Coptidis Rhizoma was best on inhibitory activity of rotavirus infection, followed by Astragali Radix and Anthrisci Radix. The active component of Coptidis Rhizoma was berberine.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2008.04a
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• pp.165-165
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• 2008

• Proceedings of the PSK Conference
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• 2003.10a
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• pp.112-112
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• 2003

Morphine is a potent analgesic and addictive substance. Morphine produces neurotoxicity such as rewarding effect, analgesic tolerance and physical dependence. It has been restricted to the use of morphine in patients because of these problems. The present study was investigated the effect of berberine on the neurotoxicity of morphine. Repeated administration of morphine produced conditioned place prefernece (CPP) and behavioral sensitization in mice. (omitted)

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.270.1-270.1
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• 2003

Enzyme-linked immunoassay system using monoclonal antibody (MAb) has become an important methodology for the quantitative and qualitative analysis of drugs and phytochemical compounds having small molecular weight. In this study, monoclonal antibodies against berberine, one of main constituent of Phellodendron amurense, Coptis japonica and Corydalis turtschaninovii, were produced. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.197.2-197.2
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• 2003

One of the consequences of hyperglycemia is the excessive nonenzymatic glycation of proteins known as Millard reaction. Under hyperglycemia the irreversibly formed advanced glycation endproducts(AGEs) do not return to normal when hyperglycemia is corrected and continue to accumulate over the lifetime of protein. AGEs are largely involved in the pathogenesis of diabetic complications. To find possible AGEs inhibitor, BSA was added to a mixture of sugars and unprocessed-, processed Coptidis Rhizoma, Berberine, its standard compound or AG(Aminoguanidine HCl: positive control). (omitted)

• Biomolecules & Therapeutics
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• v.15 no.3
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• pp.162-168
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• 2007

It is well known that oxidized low-density lipoprotein (oxLDL) is the most characterized humoral factor that plays an important role in the pathogenesis of atherosclerosis. The water extract of the Korean herbal remedy, ZoaGumHwan (ZGH), which is composed of roots of Coptis chinensis Franch and fruits of Evodia officinalis Dode with the ratio of 6 to 1, reduced the in vitro oxidation of low density lipoproteins (LDL). Also, the ZGH extract and berberine, one of the major components of ZGH, significantly prevented oxLDL-induced adhesion of monocytes to human umbilical vein endothelial cells (HUVEC). Furthermore, the ZGH water extract and berberine decreased oxLDL-induced expression of CC chemokine receptor 2 (CCR2), a dominant monocyte chemotaxis receptor, in U937 human monocytic cells. The protective effects of the ZGH water extract and berberine were similar to those of simvastatin, an effective lipid-lowering drug. The results suggest that Korean herbal remedy, ZGH, seems to have protective effect against oxLDL-induced monocyte chemoattractant protein (MCP)-1/CCR2-dependent monocyte recruitment onto endothelial cells.