• Asian Pacific Journal of Cancer Prevention
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• 제15권1호
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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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• 제17권1호
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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.

• 한국식품영양학회지
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• 제27권3호
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• pp.532-537
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• 2014

황백(Cortex Phellodendri: CP)은 황벽나무(Phellodendron amurense)의 건조된 수피로부터 얻어진다. 이 수피는 한국의 전통 한약제로서 설사, 황달, 무릎과 발의 통증, 요도관 및 피부 감염증에 폭넓게 사용되어 왔다. 이들 기능성 성분의 분리 및 정제는 박층 크로마토크래피, 컬럼 액체 크로마토크래피 및 HPLC와 같은 여러 분석법들이 동양의 약초연구에 이용되어 왔다. 본 연구는 CP로부터 berberine을 분리하기 위해 향류분배 크로마토크래피법(CPC)으로 효과적으로 수행하였다. 두 용매의 CPC 최적조성은 n-butanol: acetic acid: water(4:1:5 v/v/v)이었다. 이동상의 유속은 1,000 rpm 회전력에서 상승법으로 분당 3 mL 속도로 전개시켰다. CPC에서 분리된 분획분은 prep-HPLC로 정제하였다. $^1H$-NMR 스펙트럼은 4.10과 4.20 ppm에서 $3H(-OCH_3)$, 6.10 ppm에서 2H의 ($-OCH_2O-$) proton signal의 공명이 관찰되었다. 2개의 방향족 proton은 이중결합 패턴을 보였다. H-11과 H-12 doublet은 각각 7.98과 8.11에서 나타났다. $^{13}C$-NMR 스펙트럼에서는 C2와 C3의 methylenedioxy group($-OCH_2O-$), C9과 C10에 methoxy group($-OCH_3$)이 4개의 치환된 형태로 보였다. 분리 정제된 berberine의 화학구조는 $^1H$, $^{13}C$-NMR, ESI-MS 데이터 분석으로 확인하였다.

• 대한화학회지
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• 제41권2호
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• pp.98-104
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• 1997

한국에서 전통적으로 사용되고 있는 생약제제 중 베르베린, 계피산 및 글리시리진의 정량을 위한 간단하고, 정확하고, 재현성 있는 모세관 전기이동법을 개발하였다. 이 성분들의 분리는 25$^{\circ}C$, 20 mM 인산완충액(pH 7.5)에서 실리카 캐필러리($57 cm{\times}75 {\mu}m$ i.d.)를 사용하여 수행하였다. 350 V/cm의 전기장으로 베르베린, 계피산 및 글리시리진의 동시 정량을 13분내에 할 수 있었다. 검정곡선은 베르베린에 대해서는 1~100 ${\mu}g/mL$, 계피산은 0.3~100 ${\mu}g/mL$, 글리시리진은 2.5~100 ${\mu}g/mL$의 농도 범위 안에서 좋은 직선성을 보여 주었다. 이 성분들에 대한 상대 표준편차(n=5)의 범위는 0.96∼2.35%이었다. 베르베린, 계피산 및 글리시리진에 대한 검출한계(S/N=3)는 각각 0.5, 0.1 및 2.0 ${\mu}g/mL$이었다. 이론단수는 181,000(베르베린), 88,000(계피산) 및 169,000(글리시리진)이었다. HPLC에서는 3,100~4,800이었다.

• 생약학회지
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• 제29권2호
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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.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 2008년도 Proceedings of the Convention
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• pp.165-165
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• 2008

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-1
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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)

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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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)

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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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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• 제15권3호
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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.