• 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.

• 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.

• 대한본초학회지
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• 제28권1호
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• pp.1-7
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• 2013

Objectives : Coptidis Rhizoma has been used for stomach disease. However, its property is so cold that it might be avoided to prescribe for the elderly and the infirm having indigestion or diarrhea. Accordingly, the present study was designed to investigate the protective effects of Coptidis Rhizoma herbal acupuncture extract against acute gastric mucosal lesions induced by compound 48/80 in rats. Methods : The Coptidis Rhizoma herbal acupuncture (CRHA) was injected in Choksamni and Chungwan 1 h before compound 48/80 treatment. The animals were sacrificed under anesthesia 3 h after compound 48/80 treatment. The stomachs were removed and the amount of gastric adherent mucus, gastric mucosal hexosamine, SOD, XO, TBARS and histological examination were performed. Results : The decline of gastric adherent mucus, gastric mucosal hexosamine and the histological defects of gastric mucus were significantly protected by CRHA treatment. Gastric adherent mucus in control group was reduced to $38.2{\pm}5.0%$. CRHA groups significantly protected the loss of mucus to $77.5{\pm}4.9%$. Mucosal hexosamine content showed similar patterns. Mucosal hexosamine content in control group was reduced to $45.2{\pm}6.2%$. CRHA groups significantly protected the loss of mucus to $83.0{\pm}7.0%$. The changes of gastric mucosal SOD and TBARS were recovered by CRHA treatment as well. Conclusions : CRHA showed the protective effects on the acute gastric mucosal lesions induced by compound 48/80 in rats. These results suggest that CRHA may have protective effects on the gastritis.

• Journal of Periodontal and Implant Science
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• 제26권3호
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• pp.641-654
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• 1996

In infectious disease, invasion of host tissue by bacteria or their products frequently induces a wide variety of inflammatory and immunopathologic reaction. Evidence indicates that cytokines are involved in the initiation and progression of chronic inflammatory diseases, such as periodontitis. Interleukin-6, which is a multifunctional cytokine, has important roles in acute and chronic inflammation and may also be implicated in bone resorption. Periodontal diseases are characterized by chronic inflammation of the periodontium with alveolar bone resoption. A principal driving force behind this response appears to lie in the immune system's response to bacteria. Many of the cell components which have been shown to function as virulence factors in gram-negative bacteria are associated with the bacterial surface. Of these, lipopolysaccharide has been characterized as one that mediates a number of biological activities which can lead to the destruction of host tissue. Non-steroidal antiinflammatory drug is used for reduce inflammation, and most of NSAIDs inhibit prostaglandine $E_2$ production, but it is shown that $PGE_2$ production is stimulated by IL-1 in recent study. So, the influence of other cytokines except $PGE_2$ on periodontium can not be avoided. Therefore, new antiinflammatory drug is needed. Rhizoma coptidis is used in oriental medicine for anti-inflammation and antiseptics. In this present study, we examined the IL-6 release in periodontal ligament cells treated with the lipopolysaccharide, and also the effect of rhizoma coptidis on cellular activity and IL-6 production of periodontal ligament cells. To evaluate the effect of rhizoma coptidis on cellular activity, the cells were seeded at a cell density of $1{\times}10^4$ cells/well in 24-well culture plates. After one day incubation, 1-6, 10-9 and 10-12 g/ml of rhizoma coptidis and 5, $10{\mu}g/ml$ of LPS were added to the each well and incubated for 1 and 2 days, respectively. Then, MTT assay were carried out. To evaluate the effect of rhizoma coptidis on IL-6 production, the cells were seeded at a cell density of $1.5{\times}10^4$ cells/well in 24-well culture plates. After one day incubation, 10-9 g/ml of rhizoma coptidis and 5, $10{\mu}g/ml$ of LPS were added to the each well and incubated for 3, 6, 12 and 24 hours. Then, amounts of IL-6 production is measured by IL-6 ELISA kit used. The results were as follows : 1. Rhizoma coptidisrbelow to ($10^{-6}g/ml$) significantly increaed cellular activity of periodontal ligament cells than control. 2. Rhizoma coptidist ($10^{-9}g/ml$) significantly increased cellular activity of LPS($5{\mu}g/ml$)-treated periodontal ligament cells than control. 3. LPS(5 and $10{\mu}g/ml$) significantly increased IL-6 production of periodontal ligament cells than control. 4. Rhizoma coptidis($10^{-9}g/ml$) decreased IL-6 production of LPS ($5{\mu}g/ml$)-treated periodontal.ligarnent cells than LPS only tested group. These findings suggest that stimulation of the IL-6 release of periodontal ligament cells by LPS may have a role in the progression of inflammation and alveolar bone resoption in periodontal disease, and that inhibition of the IL-6 release of cells and stimulation of cellular activity by rhizoma coptidis may help the periodontal regeneration.

• 대한한방내과학회지
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• 제19권2호
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• pp.261-277
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• 1998

The purpose of this research was to investigate cytotoxicity of DangkwiYonghoe-Hwan(DYH) and the constitutive crude drugs on several cancer cell-lines, thymocytes, splenocytes and 3T3 cells. The DYH consists of Coptidis Rhizoma, Scutellariae Radix, Phellodendri Cortex, Gardeniae Fructus, Gentianae scabrae Radix, Indigo pulverata Levis, Aloe, Rhei Rhizoma, Moschus, Saussureae Radix and Angelicae Gigantis Radix. The cytotoxicity was determined by MTT method. The DYH inhibited the proliferation of MOLT-4, K562, HL-60, Jurkat, L1210, P815, S180 and Yac-1, thymocyte, splenocyte and 3T3 cells. The cytotoxicity of Coptidis Rhizoma on the cancer cell-lines was the most potent in the constitutive crude drugs. The proliferation of cancer cell-lines was partly inhibition and partly increase by the treatment of Scutellariae Radix, Gardeniae Fructus, Gentianae scabrae Radix, Indigo pulverata Levis, Aloe, Rhei Rhizoma, Moschus and Angelicae Gigantis Radix. Phellodendri Cortex and Saussureae Radix had a poor cytotoxicity on cancer cell-lines. Coptidis Rhizoma and Phellodendri Cortex inhibited the proliferation of thymocyte, splenocyte and 3T3 cells.

• 한국치위생학회지
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• 제1권1호
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• pp.101-109
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• 2001

This study was conducted to investigate the effect of natural resources against growth of oral bacteria. The CHJ-5 strain was isolated from oral cavity of dental patients. Similarity index values of oral bacterium CHJ-5 was 0.876 to E. faecalis by cellular fatty acid analysis(Analytical Services Inc., USA). As a result of investigation about the growth inhibition of 32 kinds of natural resources on E. faecalis CHJ-5. This strain was inhibited by Schizamdrae fructus, Coptidis rhizoma and Caryophylli flos. Minimal inhibitory concentrations of Schizamdrae fructus, Coptidis rhizoma and Caryophylli flos were 0.1%, 02% and 0.1% on E. faecalis CHJ-5, respectively.