• Korean Journal of Oriental Medicine
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• v.13 no.2 s.20
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• pp.157-164
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• 2007

An imbalance in bone remodeling that is caused by increased bone resorption over bone formation leads to most adult skeletal diseases including osteoporosis. Since the development of anti-resorptive agents from natural substances has recently gained more interest in the treatment of osteoporosis, we evaluated the effects of 222 natural compounds on receptor activator of $NF-{\kappa}B$ ligand (RANKL)-induced of tartrate-resistance acid phosphatase (TRAP) activity in RAW264.7 murine macrophage cell, and found that berberine chloride is one of compounds inhibiting RANKL-induced TRAP activity. Berberine chloride significantly inhibited the RANKL-induced TRAP activity and the formation of multinucleated osteoclasts in a dose-dependent manner. In addition, berberine chloride prevented the RANKL-induced mRNA expression of TRAP, matrix metalloproteinase 9 and c-Src, which have been known to be highly expressed in the process of osteoclastogenesis. Interestingly, berberine chloride prevented the RANKL-induced activation of extracellular signal-regulated kinase (ERK) which is one of mitogen-activated protein (MAP) kinases. In conclusion, berberine chloride could inhibit the osteoclastogenesis via preventing the activation of ERK/MAP kinase signaling pathway.

• Journal of Microbiology and Biotechnology
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• v.13 no.4
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• pp.522-528
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• 2003

The growth responses of Phellodendron amurense root-derived materials against seven intestinal bacteria were examined, using an impregnated paper disk agar diffusion method and spectrometric method under $O_2$-free condition. The biologically active constituent of the P. amurense root extract was characterized as berberine chloride ($C_{20}H_{18}NO_{41}Cl$) using various spectroscopic analyses. The growth responses varied depending on the bacterial strain, chemicals, and dose tested. At 1 mg/disk, berberine chloride strongly inhibited the growth of Clostridium perfringens, and moderately inhibited the growth of Escherichia coli and Streptococcus mutans without any adverse effects on the growth of three lactic acid-bacteria (Bifidobacterium bifidum, B. longum, and Lactobacillus acidophilus). The structure-activity relationship revealed that berberine chloride exhibited more growth-inhibiting activity against C. perfringens, E. coli, and S. mutans than berberine iodide and berberine sulfate. These results, therefore, indicate that the growth-inhibiting activity of the three berberines was much more pronounced as chloridated analogue than iodided and sulphated analogues. As for the morphological effect caused by 1 mg/disk of berberine chloride, most strains of C. perfringens were damaged and killed, indicating that berberine chloride showed a strong inhibition against C. perfringens. As naturally occurring growth-inhibiting agents, the P. amurense root-derived materials described could be useful as a preventive agent against diseases caused by harmful intestinal bacteria such as clostridia.

• YAKHAK HOEJI
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• v.45 no.1
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• pp.34-38
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• 2001

The Phellodendri Cortex of Phellodendron amurense (Rutaceae) is known to contain a number of isoquinoline alkaloid, and berberine, palmatine, jateorrhizine, phellodendrine and magnoflorine are the major constituents of protoberberine alkaloids. For the determination of protoberberine alkaloids from Phellodendri Cortex and berberine chloride from the preparation, the new spectrophotometric method was developed with a simple and selective sample clean-up using thiocyanatocobaltate[II] complex ion. Samples were extracted with 0.1 mM hydrochloric acid, potassium biphthalate reagent, thiocyanatocobaltate reagent and 1.2-dichloroethane for 60 min. The absorbance of protoberberine alkaloid complexes in 1.2-dichloroethane solution was measured at 625 nm. Calibration curve for berberine was linear over the concentration range of 0.05~0.30 mg/ml 1.2-dichloroethane. The method proved to be rapid, simple and reliable for the determination of protoberberine alkaloids from Phellodendri Cortex and berberine chloride from the preparation.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.13
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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.

• Journal of the Korean Society of Clothing and Textiles
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• v.36 no.12
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• pp.1257-1269
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• 2012

The dyeing behaviors of berberine chloride, palmatine chloride hydrate, and Phellodendron bark extract on silk fabric were investigated to evaluate palmatine as another chromophoric substance of Phellodendron bark. The dyeing conditions were composed of combinations of pH (3, 5, 7, 9), temperature (10, 30, 55, $80^{\circ}C$), and time (10, 30, 60 min). The results indicate that palmatine was comparable to berberine in the dyeing behaviors tested for this study and the results were statistically significant. The dye exhaustion and dye uptake of palmatine-CH were slightly lower than berberine-C, which however were not statistically significant. Similar to berberine-C, palmatine-CH favored a pH 7 condition for both dye exhaustion and dye uptake. However, palmatine-CH favors a higher dyeing temperature and longer dyeing time than berberine-C for superior dyeing results.

• Journal of Life Science
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• v.20 no.7
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• pp.1143-1150
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• 2010

The antibacterial activity of methanol extracts from 70 kinds of oriental medicinal herbs on four strains of Staphylococcus aureus and S. epidermidis was investigated. The results showed that C. japonica, C. sappan, R. javanica, R. tanguticum, and S. miltiorrhiza had an antibacterial activity on all the strains used. Among these, C. japonica and R. javanica, which showed excellent antibacterial activity, were extracted with water, ethanol, methanol, and ethyl acetate for further study of antibacterial activities. The results showed that the boiled water extract of C. japonica had the best antibacterial activity. Assuming that the antibacterial activity of C. japonica originated from berberine, which has been reported many times, the berberine content of the boiled water extract of C. japonica was analyzed and the result was 13.88%. To compare the antibacterial activity of berberine with that of other antibiotics, berberine chloride and three other kinds of antibiotics were investigated, which showed that berberine chloride had an antibacterial activity on KCCM 35494 S. epidermidis only when the concentration was higher than 600 mg/l, and it did not show antibacterial activity in the other strains. Based on these results, it was concluded that the antibacterial activity of the boiled water extract of C. japonica on the strains used in this study originated from high concentration of berberine or substances other than berberine. Therefore, identification of the substance will be necessary.

• Textile Coloration and Finishing
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• v.26 no.4
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• pp.311-321
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• 2014

In this study, Aftertreatment properties of PCM/Nylon sheath/core fabrics have been determined. Especially, the relationship between finishing property and content including of PCM ratio. Samples of PCM/Nylon fabrics were monitored, separately, with 2% o.w.f solutions of each of the berberine chloride, cetylpyridinium chloride(CPC), benzyldimethylhexadecyl ammonium chloride(BDHAC) and dodecyltrimetyl ammonium bromide(DTAB). Various temperatures and liquor ratio and pH conditions were also studied to optimize aftertreatment properties. Berberine chloride finished sample showed the good color fastness. Cetylpyridinium chloride(CPC) finished sample showed very effective antibacterial properties against Staphylococcus aureus and Klebsiella pneumoniae.

• Journal of the Korean Society of Clothing and Textiles
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• v.33 no.12
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• pp.2002-2010
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• 2009

The degradation behavior of berberine is examined using GC-MS to select the fingerprint products that can be used to identify berberine dye in badly faded archaeological textiles. A total of $100^{\circ}C$ thermal and $H_2O_2/UV/O_2$ degradation systems were used to degrade berberine chloride 0.1% solution up to 408 hours. The samples were analyzed using the GC-MS. Dihydroberberine, 2-pteridinamine, 6,7-dimethyl-N-[(trimethylsilyl) oxy]-, and 8-methoxy-11-[3-methylbutyl]-11H-indolo[3,2-c]-quinoline, 5-oxide were detected as the major products of thermal degradation and identified as the fingerprint products for berberine dye at the early stage of degradation. Isobenzofuran-1,3-dione,4,5-dimethoxy-, 9H-fluorene,3,6-bis(2-hydroxyethyl)-,1,3-dioxolo[4,5-g]isoquinolin-5(6H)-one,7,8-dihydro-, and 3-tert-butyl-4-hydroxyanisole were detected as the major products generated by the $H_2O_2/UV/O_2$ degradation and identified as the fingerprint products for berberine dye under severe degradation conditions.

• Journal of Microbiology and Biotechnology
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• v.15 no.6
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• pp.1402-1407
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• 2005

The fungicidal activities of Coptis japonica (Makino) extracts and their active principles were determined against Botrytis cineria, Erysiphe graminis, Phytophthora infestans, Puccinia recondita, Pyricularia grisea, and Rhizoctonia solani using a whole plant method in vivo, and compared with natural fungicides. The responses varied according to the plant pathogen tested. At 2,000 mg/l, the chloroform and butanol fractions obtained from methanolic extracts of C. japonica exhibited strong/moderate fungicidal activities against B. cinerea, E. graminis, P. recondita, and Py. grisea. Two active constituents from the chloroform fractions and one active constituent from the butanol fractions were characterized as isoquinoline alkaloids, berberine chloride, palmatine iodide, and coptisine chloride, respectively, using spectral analysis. Berberine chloride had an apparent $LC_{50}$ value of approximately 190, 80, and 50 mg/l against B. cinerea, E. graminis, and P. recondita, respectively; coptisine chloride had an $LC_{50}$ value of 210,20, 180, and 290 mg/l against B. cinerea, E. graminis, P. recondita, and Py. grisea, respectively; and palmatine iodide had an $LC_{50}$ value of 160 mg/l against Py. grisea. The isoquinoline alkaloids were also found to be more potent than the natural fungicides, curcumin and emodin. Therefore, these compounds isolated from C. japonica may be useful leads for the development of new types of natural fungicides for controlling B. cinerea, E. graminis, P. recondita, and Py. grisea in crops.

• Textile Coloration and Finishing
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• v.18 no.1
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• pp.28-32
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• 2006

A multi-layer of the dye, natural colorant Berberine, was successfully developed by the self-assembly deposition from water-soluble cationic dye(Berberine chloride) and anionic polyelectrolyte PSS(Polysodium 4-styrenesulfonate) in aqueous solution via electrostatic attraction. The corresponding results on multi-layer were characterized by UV-Vis absorbance measurements. The growth of multi-layer formed by the sequential interaction was also determined. The findings measured by UV-Vis spectrophotometer showed that the bilayer deposition characteristic was linear and highly reproducible from layer to layer.