• 대한한의학방제학회지
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• 제12권1호
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• pp.209-223
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• 2004

Objective: This study was conducted to investigate the effects of Coptidis Rhizoma on the plasma IL-6 and $TNF-{\alpha}$ level in mice by intracerebroventricular(I.C.V.) injection of Lipopolysaccharide (LPS). Method: 6 mice were assigned to each of the Normal group, the Control group, and the individual Experimental groups. In the Normal group only saline was administered intragastrically, and in the Control group LPS was injected intracerebroventricularly 1 hr after intragastric administration of saline. In the Experimental groups Coptidis Rhizoma(0.5g/kg, 1.0g/kg, 3.0g/kg) was administered intragastrically to mice 1 hr prior to LPS (100ng/mouse) I.C.V. Injection. To measure the plasma IL-6 and $TNF-{\alpha}$ level of mice, their blood samples were collected from retro-orbital venous plexus, immediately centrifuged at $4^{\circ}C$, and plasma was removed and stored frozen at $-83^{\circ}C$ for later determination of plasma IL-6 and $TNF-{\alpha}$. Result: 1. LPS I.C.V. Injection increased plasma IL-6 level significantly in a dose-dependent manner compared with Normal group. (P<0.01) The plasma IL-6 concentration reached a significant maximal level about 1 hr after LPS(100ng/mouse) I.C.V. Injection.(P<0.001) 2. Both the 0.5g/kg(Sample A) and 1.0g/kg(Sample B) groups to which Coptidis Rhizoma was administered intragastrically 1 hr prior to LPS(100ng/mouse) I.C.V. Injection showed insignificant lower plama IL-6 level in 1 hr than Control group(P>0.05), and 3.0g/kg group(Sample C) conversely showed higher plama IL-6 level than Control group. 3. LPS I.C.V. Injection increased plasma $TNF-{\alpha}$ level significantly in a dose-dependent manner compared with Normal group.(P<0.05) The plasma $TNF-{\alpha}$ concentration reached a significant maximal level about 1 hr after LPS(100ng/mouse) I.C.V. Injection.(P<0.001) 4. All Sample groups(0.5g/kg, 1.0g/kg, and 3.0g/kg) to which Coptidis Rhizoma was administered intragastrically with each constituent-dose 1 hr prior to LPS(100ng/mouse) I.C.V. Injection showed significant lower $TNF-{\alpha}$ plama level in 1 hr than Control group.(P<0.001) These data revealed that Coptidis Rhizoma might have anti inflammatory effect by reducing the plasma $TNF-{\alpha}$ level in a dose dependent manner in mice LPS I.C.V. Injection.

• Korean Journal of Acupuncture
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• 제21권2호
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• pp.95-110
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• 2004

Objectives : Ulcerative colitis and Crohn's diseases are chronic inflammatory disease of the gastrointestinal tract identified mainly for diarrhea, stomachache, hemafecia. The source and pathologic mechanism about ulcerative colitis and Crohn's disease are still unknown but stress, infection, a genetic factor, environmental factors etc. may be the cause of chronic inflammatory disease of the gastrointestinal tract recently. Methods : Because ulcerative colitis and Crohn's disease is recognized as Ha-ri(下痢) or Jang-Byok(腸?) in Oriental Medicine, Rhizoma Coptidis Herbal acupunctures were injected in hapgok $(LI_4)$ which is used to treat intestinal disease in clinic. All animals were subjected to the injection of saline $(300\;{\mu}l,\;500\;{\mu}l)$ for a study control and TNBS $(300\;{\mu}l,\;500\;{\mu}l)$ into the lumen of the colon, 8cm proximal to the anus through the intestine. Rhizoma Coptidis Herbal (20 mg/ml, 0.4 ml) acupuncture solution was injected to the $LI_4$ (both hands) at the secondary injection time of TNBS in rats. And body weight, RBC count, WBC count, total protein, Paw edema rate, rate of protein leakage into CMC-pouch fluid, IgG levels and IgM levels were observed to study the effects of Rhizoma Coptidis Herbal acupuncture in hapgok $(LI_4)$. Results : In results, Rhizoma Coptidis Herbal acupuncture in hapgok $(LI_4)$ on TNBS-induced colitis reduced the rate of weight loss but had no effect on RBC and WBC count. And it reduced total protein concentration, paw edema, rate of protein leakage into CMC-pouch fluid, IgG levels and IgM levels. Conclusion : Data suggest that injection of Rhizoma Coptidis herbal acupuncture solution into hapgok has significant therapeutic effect on the colitis.

• 대한본초학회지
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• 제22권4호
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• pp.109-116
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• 2007

Objectives : In the present study, we investigated anti-inflammatory effects of chloroform fraction of Coptidis rhizoma (CR-C) on the production of inflammatory mediators such as nitric oxide (NO) and proinflammatory cytokines, tumor necrosis factor-alpha (TNF-${\alpha}$) and interleukin-1beta (IL-1${\beta}$) in LPS-stimulated BV2 microglial cells. Methods : Copriditis rhizoma was extracted with 80% methanol, and then extracted with chloroform. BV2 cells were pre-treated with CR-C, and stimulated with LPS. The cytotoxicity was determined by MTT assay. The production of NO and cytokines was measured by Griess assay and ELISA. The mRNA expression of inducible nirtic oxide synthase (iNOS) and cytokines were determined by RT-PCR. Results : CR-C significantly inhibited the production of NO. TNF-${\alpha}$ and IL-1${\beta}$ in a dose-dependent manner in LPS-stimulated BV2 cells. In addition, CR-C suppressed the mRNA expressions of iNOS and inflammatory cytokines induced by LPS stimulation. These results indicate that CR-C was involved in anti-inflammatory effects in activated microglia. Conclusion : The present study suggests that chloroform extract of Coptidis rhizoma can be useful as a potential anti-inflammatory agent for treatment of various neurodegenerative diseases.

• Journal of Pharmaceutical Investigation
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• 제24권4호
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• pp.233-243
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• 1994

Precipitation was formed during the preparation of decoction from a mixture of Scutellariae Radix and Coptidis Rhizoma or Phellodendri Cortex according to the prescription of Hwang-ryean-hae-dog-tang. Baicalin and berberine were identified in coprecipitated product and these components were the active ingredients of two herbal medicine. The coprecipitated product was very slightly soluble in water and sparingly soluble in ethanol. The stoichiometric ratio of baicalin and berberine was found to be 1:1. The lipid-water partition coefficients of coprecipitated product were increased more than baicalin and berberine in chloroform, but were decreased in other organic solvents. The content of baicalin and berberine in coprecipitated product, determined by HPLC, were 23.08% and 26.75%, but the content of active ingredients in supernatant were 0.66% and 0.26%, respectively. The dissolution profile of baicalin of coprecipitated product was increased more than extract of Scutellariae Radix in artificial gastric juice, but was decreased in artificial intestinal juice. The dissolution rate of berberine of coprecipitated product was lower than extract of Coptidis Rhizoma in artificial gastric juice and intestinal juice commonly.

• 한국자원식물학회지
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• 제30권6호
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• pp.693-698
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• 2017

The quality control of natural products is principal key to guarantee the Good Manufacturing Practices (GMP) and Good Clinical Practices (GCP) for the functional food, pharmaceuticals and cosmeceuticals in the industry. In this study, we examined the quantitative analysis of berberine as marker substance of Coptidis Rhizoma by high performance liquid chromatography-photodiode array detector (HPLC-DAD). The HPLC method was validated and met all the requirements for the quality control analysis recommended by FDA and ICH. The berberine was separated on a Xterra $C_{18}$ column ($5{\mu}m$, $4.6{\times}250mm$) using mobile phase consisting of distilled water and acetonitrile with $KH_2PO_4$ (3.4 g) and $Na_2SO_4$ (1.7 g). Calibration curve of berberine has been estimated (y = 42293.47x-41589 with the correlation coefficient 0.9999). The amount of berberine was calculated as 4.25%. And berberastine, palmatine, columbamine, jatrorrhizine, epiberberine, berberine and coptisine in the Coptidis Rhizoma were identified by high performance liquid chromatography - electrospray ionization-mass spectrometer (HPLC-ESI-MS) method.

• Journal of Pharmaceutical Investigation
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• 제25권3호
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• pp.185-192
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• 1995

Precipitation reaction occured between berberine in Coptidis Rhizoma and glycyrrhizin in Glycyrrhizae Radix when they were boiled together in aqueous solution and the supernatant solution thus obtained did not show any antibacterial activity which was derived from berberine. The content of berberine in BG and CGP by HPLC analysis were 41.1%, 8.3% respectively. BG was occured mostly at pH 5.0. The solubility of berberine was 0.15%, while that of BG and CGP was 0.07%, 0.12%, respectively. CGP shown more increased antibacterial activity to gram positive bacteria, S. dysenteriae and K. pneumoniae than berberine. The absorption rates of CGP in stomach, duodenum and jejunum of rats were compared with those of Coptidis Rhizoma water extracts (CR), which were increased more than CR. The time required for the maximum serum concentration of berberine from CGP in mice was 90 minutes after oral administration. The maximum serum concentration of berberine from CGP was higher than that from CR. The dissolution of CGP was increased more than berberine and BG in both artificial gastric and intestinal fluids. The dissolution of CGP pill made from gelatin was 63.4% in artificial gastric fluids and that made from CMC was 76.0% in artificial intestinal fluids.

• 대한한방소아과학회지
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• 제33권3호
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• pp.103-111
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• 2019

Objectives The purpose of this study is to understand the correlations between lung, large intestine, and skin of 3-week-old mice in which ulcerative colitis was induced, up on administration of Coptidis rhizome and Glycyrrhiza uralensis mixed extract. Methods Mice were divided into 4 groups as follows; no treatment group (Ctrl group), ulcerative colitis-induced mice group (UE group), ulcerative colitis-induced mice group after administering Pentasa (PT group), ulcerative colitis-induced mice group after administering Coptidis rhizoma and Glycyrrhiza uralensis mixed extract (CGT group). Mice were induced ulcerative colitis by Dextran sulfate sodium (DSS). After 5 days of administration, We obvserved anti-inflammatory effect, alveolar formation, and skin barrier control in the colon mucosa. Results The CGT group was observed arrangement of normal intestinal cells, Infiltration of less inflammatory cells. The CGT significantly decreased positive rseponse of $TNF-{\alpha}$, p-IkB, Caspase 3 in large intestine, and significantly increased positive rseponse of EGF, IGF, catalase, Filaggrin, involucrin, loricrin. Conclusions The results of this study show the correlation of Lung-Large intestine-Skin by administering Coptidis rhizoma and Glycyrrhiza uralensis mixed extract to ulcerative colitis-induced mice.

• 약학회지
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• 제49권4호
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• pp.323-329
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• 2005

Antimicrobial peptides are evolutionary ancient weapons for animal and plant species to depend themselves against infectious microbes. In the present study, we investigated if an antimicrobial peptide was produced from Coptidis Rhizoma. For the determination, protein substance from the medicinal plant was isolated by various preparations. Among the preparations, the protein portion dissolved in phosphate-buffered saline solution (CRP-DS) that contained the most amount of protein $(90\%)$ resulted in maximal inhibition of Candida albicans which causes local and systemic infections. Analyses by gel-electrophoresis and gel-permeation chromatography showed the CRP-DS formed a single band of approximately 11.8 KDa as molecular size. Antifungal activity of the CRP-DS was almost equivalent to antifungal activity by fluconazole, resulting in MIC (minimal inhibitory concentration) of approximately $50{\mu}g/ml$. The antifungal activity was a dose-dependent. The antifungal activity appeared to be inactivated by heat-treatment and ionic strength, respectively. In a murine model, the CRP-DS enhanced resistance of mice against disseminated candidiasis. The HPLC analysis demonstrated maximum $4\%$ of berberine as residual content in the CRP-DS preparation resulted in no influence on the antifungal activity. In addition, protein portion isolated from Phellodendri Cortex producing the alkaloid component like Coptidis Rhizoma had no such anticandidal effect. These results indicate that the protein substance from Coptidis Rhizoma was responsible for the antifungal activity.

• 생약학회지
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• 제45권2호
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• pp.168-173
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• 2014

The aim of this study was to evaluate the anti-helicobacter activity of the ethanol extract of Sohamhyoongtang (Coptidis Rhizoma, Pinelliae Tuber and Trichosanthis Semen) and Coptidis Rhizoma total alkaloids, which is one of the components of Sohamhyoongtang. Crude ethanol extract of Sohamhyoongtang (ESHHT) and Coptidis Rhizoma total alkaloids (CRTA) were used for this experiment. Five different types of H. pylori (including H. pylori 26695) were used as test strain. To determine anti-helicobacter activity, minimum inhibitory concentration (MIC) was determined by agar dilution method. The effect of ESHHT and CRTA on the gene expression of H. pylori was investigated by quantitative realtime-PCR (qRT-PCR). MICs of ESHHT against five H. pylori strains were $250{\sim}500{\mu}g/ml$ and MICs of CRTA against five H. pylori strains were $50{\sim}200{\mu}g/ml$. Four representative virulence genes of H. pylori, cagA, ureA, ureB and ureI were tested as target genes for qRT-PCR. According to the qRT-PCR results, both ESHHT and CRTA markedly repressed the expression of cagA gene of H. pylori 26695 (6.91 and 20 folds respecively). These results showed that the ESHHT and CRTA demonstrated antihelicobacter properties, suggesting their potential use in gastritis or duodenal ulcer.

• 생약학회지
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• 제51권4호
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• pp.349-359
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• 2020

Gastroesophageal reflux disease (GERD) is a disease that stomach contents continually refluxing, and is currently on the rise worldwide. The purpose of this study is to find natural materials that can reduce side effects and effectively treat chronic acid reflux esophagitis (CARE), one of GERD. First, the antioxidant activity was confirmed by varying the mixing ratio of Coptidis Rhizoma and Evodiae Fructus, which are effective against chronic reflux esophagitis. After, animal experiments were conducted using a 1:1 (CE) and 1:2 (CEE) combination ratio of Coptidis Rhizoma and Evodiae Fructus, which had the best antioxidant efficacy. Gross lesion of esophageal mucosa after CE or CEE treatment showed a superior enhancement compared with that of CARE control rats. Additionally, its inhibited MAPK phosphorylation and led NF-κB inactivation through the suppression of IκBα phosporylation by regulating Nrf2/Keap-1, and NF-κB inactivation induced reduced protein expressions including inflammatory mediators and cytokines. Moreover, its improved esophageal barrier function through upregulating protein expressions of tight junction protein, whereas downregulating protein expressions of MMPs. Taken together, a mixture of Coptidis Rhizoma and Evodiae Fructus can attenuate the esophageal mucosal ulcer by inhibiting MAPK and NF-κB pathway, and upregulating proteins associated with tight junction.