• 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.

• The Korean Journal of Physiology and Pharmacology
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• 제20권4호
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• pp.415-424
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• 2016

Berberine is an isoquinoline alkaloid found in Rhizoma coptidis, and elicits anti-inflammatory effects through diverse mechanisms. Based on previous reports that activating transcription factor-3 (ATF-3) acts as a negative regulator of LPS signaling, the authors investigated the possible involvement of ATF-3 in the anti-inflammatory effects of berberine. It was found berberine concentration-dependently induced the expressions of ATF-3 at the mRNA and protein levels and concomitantly suppressed the LPS-induced productions of proinflammatory cytokines ($TNF-{\alpha}$, IL-6, and $IL-1{\beta}$). In addition, ATF-3 knockdown abolished the inhibitory effects of berberine on LPS-induced proinflammatory cytokine production, and prevented the berberine-induced suppression of MAPK phosphorylation, but had little effect on AMPK phosphorylation. On the other hand, the effects of berberine, that is, ATF-3 induction, proinflammatory cytokine inhibition, and MAPK inactivation, were prevented by AMPK knockdown, suggesting ATF-3 induction occurs downstream of AMPK activation. The in vivo administration of berberine to mice with LPS-induced endotoxemia increased ATF-3 expression and AMPK phosphorylation in spleen and lung tissues, and concomitantly reduced the plasma and tissue levels of proinflammatory cytokines. These results suggest berberine has an anti-inflammatory effect on macrophages and that this effect is attributable, at least in part, to pathways involving AMPK activation and ATF-3 induction.

• 한국의류학회지
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• 제35권12호
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• pp.1507-1517
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• 2011

Berberine, palmatine, and Phellodendron bark dye was prepared in methanol for HPLC-DAD-MS analysis of liquid dye. Silk was dyed using berberine, palmatine, and Phellodendron bark dye prepared in water. The dye was extracted from the dyed silk using the HCl/methanol/water (2:1:1 v/v/v) solvent system with a slight modification. The liquid dyes and the dye extracted from the silk samples dyed with the three dye sources were examined using the HPLC-DAD-MS analysis to simultaneously detect berberine and palmatine from the plant dye and the dyeings. Colorimetric measurement was carried out using a spectrophotometer to examine the color and the intensities of berberine, palmatine, and Phellodendron bark dyed silk samples. From the liquid dyes, berberine eluted at 5.21 min with the molecular cation m/z=336 and the UV spectrum confirming that the product was berberine. Palmatine eluted at 5.12 min with the molecular cation m/z=352 and the UV spectrum confirming that the product was palmatine. From the silk dyed with berberine and palmatine dye, berberine and palmatine species eluted at 5.35 min and 5.24 min, respectively. From the silk dyed with Phellodendron bark, berberine and palmatine were detected simultaneously at 5.35 min and 5.26 min, respectively. All three dyes had yellow hue while palmatine dyed silk showed the highest hue and chroma. Palmatine dyed silk showed the highest K/S value that indicated the strongest color intensity and the highest dye uptake.

• 약학회지
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• 제38권2호
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• pp.174-178
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• 1994

Isoguanosine and berberine 1:1 mixture[l:[1(mole:mole)] has been prepared and evaluated by measuring antitumor effects against various tumor cell lines in culture and in mice. We reported that the synergistic effect of isoguanosine and berberine mixture has been revealed compared with each of isoguanosine and berberine increased by $3{\sim}8$ times than that of each components in various tumor cell lines in vitro. The most effective dose of isoguanosine and berberine mixture was 60 mg/kg/day in mice bearing S-180 solid tumor, the %(1-T/C) values were 70%. Against the P-388 leukemia, isoguanosine-berberine mixture was the most effective at the dose of 60 mg/kg/day, the %T/C values were 163%.

• 생약학회지
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• 제17권2호
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• pp.123-128
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• 1986

The determination of berberine in Berberis koreana was examined by the high performance liquid chromatography using ${\mu}-Bondapak$ $C_{18}$ column and $CH_3CN/phosphate$ buffer (pH 5.2) (60/40) as a mobile phase. The seasonal variations of berberine contents in Berberis koreana were as follows; 1) In roots, the average berberine content was 0.94% with the highest level of 1.32% in October. 2) In stems, their average berberine content was about 0.1% and in March, April, October and November, the contents were relatively high. 3) In leaves, however, the content was as low as 0.005%. According to the experimental results obtained, we found that Berberis koreana roots can serve as the useful natural plant resources for the berberine and October is the optimal season for the collection.

• KSBB Journal
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• 제7권3호
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• pp.222-228
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• 1992

Thalictrum rugosum세포배양에서 세포증식 및 berberine생산에 미치는 자당 수용액의 영향을 연구하였다. 순수한 자당 수용액내에서는 무시할만한 세포증식에도 불구하고 상당한 berberine생성의 증가가 있었다. 자당의 농도가 높은 경우 세포의 수분 함유량이 매우 낮아졌으며 세포당 berberine생성량은 4배나 증가되었다. 최적 자당 농도는 8%로 확인되었다. 8%자당 수용액상에서의 회분배양 결과, 이 방법의 장점을 최대한 효과적으로 이용하기 위해서는 접종후 최소 5일 이상은 지나야 함을 알 수 있었다. 비타민, 생장조절제, 무기염류 등의 첨가는 생산성 향상에 도움이 되지 않았다.

• 한국염색가공학회지
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• 제14권2호
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• pp.85-85
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• 2002

The interaction between berberine and tannin in aqueous solution was investigated spectrophotometerically. The dyeing mechanism of silk fabrics (control and tannin treated silk fabrics) with berberine was based on thermodynamic parameters obtained from equilibrium adsorption experiments. In adsorption spectra of aqueous solution of berberine and tannin mixture two isosbestic points (328nm, 357nm) were found and the mole fraction of reaction of components was 1:1. Initial dyeing rates were increased and the diffusion of dye was more effective by tannin treatment. Without regard to tannin treatment the adsorption isotherm of berberine was the langmuir type except high temperature, 80℃. By tannin treatment the saturation dye uptake was increased, the increase of dye uptake appeared to be a result of entropy change rather than enthalpy change. All these results can be interpreted by the hydrophobic interaction between berberine and silk treated with tannin and it is reasonable to conclude that not only the ionic force, but also the hydrophobic interaction contributes to the binding of berberine and tannin treated silk treated with tannin.

• 한국염색가공학회지
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• 제14권2호
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• pp.9-17
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• 2002

The interaction between berberine and tannin in aqueous solution was investigated spectrophotometerically. The dyeing mechanism of silk fabrics (control and tannin treated silk fabrics) with berberine was based on thermodynamic parameters obtained from equilibrium adsorption experiments. In adsorption spectra of aqueous solution of berberine and tannin mixture two isosbestic points (328nm, 357nm) were found and the mole fraction of reaction of components was 1:1. Initial dyeing rates were increased and the diffusion of dye was more effective by tannin treatment. Without regard to tannin treatment the adsorption isotherm of berberine was the langmuir type except high temperature, $80^\circ{C}$. By tannin treatment the saturation dye uptake was increased, the increase of dye uptake appeared to be a result of entropy change rather than enthalpy change. All these results can be interpreted by the hydrophobic interaction between berberine and silk treated with tannin and it is reasonable to conclude that not only the ionic force, but also the hydrophobic interaction contributes to the binding of berberine and tannin treated silk treated with tannin.

• KSBB Journal
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• 제8권4호
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• pp.390-396
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• 1993

Thalicrtrum rugosum 식물세포 현탁배양에 의한 berberine 생산에 미치는 여러 가지 종류의 elicitor들의 영향에 관해 연구 하였다. 효모 유래의 elicitor, 15가지의 서로 다른 종류의 무생물 종류 elicitor, 3가지 곰팡이로부터 얻은 elicitor 들을 처리하여 세포의 생장 및 berberine 생산에 미치는 영향을 비교 분석해 본 결과, 이들 elicitor들은 T. rugosum에 의한 berberine 생산을 크게 증대시키지 못함을 확인하였다.

• Asian Pacific Journal of Cancer Prevention
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• 제16권13호
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• pp.5371-5376
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• 2015

Berberine (B1), isolated from stems of Coscinium fenestratum (Goetgh.) Colebr, was used as a principle structure to synthesize three phenolic derivatives: berberrubine (B2) with a single phenolic group, berberrubine chloride (B3) as a chloride counter ion derivative, and 2,3,9,10-tetra-hydroxyberberine chloride (B4) with four phenolic groups, to investigate their direct and indirect antioxidant activities. For DPPH assay, compounds B4, B3, and B2 showed good direct antioxidant activity ($IC_{50}$ values=$10.7{\pm}1.76$, $55.2{\pm}2.24$, and $87.4{\pm}6.65{\mu}M$, respectively) whereas the $IC_{50}$ value of berberine was higher than $500{\mu}M$. Moreover, compound B4 exhibited a better DPPH scavenging activity than BHT as a standard antioxidant ($IC_{50}=72.7{\pm}7.22{\mu}M$) due to the ortho position of hydroxyl groups and its capacity to undergo intramolecular hydrogen bonding. For cytotoxicity assay against human fibrosarcoma cells (HT1080) using MTT reagent, the sequence of $IC_{50}$ value at 7-day treatment stated that B1 < B4 < B2 ($0.44{\pm}0.03$, $2.88{\pm}0.23$, and $6.05{\pm}0.64{\mu}M$, respectively). Berberine derivatives, B2 and B4, showed approximately the same level of CAT expression and significant up-regulation of SOD expression in a dose-dependent manner compared to berberine treatment for 7-day exposure using reverse transcription-polymerase chain reaction (RT-PCR) assays. Our findings show a better direct-antioxidant activity of the derivatives containing phenolic groups than berberine in a cell-free system. For cell-based system, berberine was able to exert better cytotoxic activity than its derivatives. Berberine derivatives containing a single and four phenolic groups showed improved up-regulation of SOD gene expression. Cytotoxic action might not be the main effect of berberine derivatives. Other pharmacological targets of these derivatives should be further investigated to confirm the medical benefit of phenolic groups introduced into the berberine molecule.