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A new isocoumarin, 3-acetyl-3,4-dihydro-5,6-dimethoxy-1H-2-benzopyran-1-one, was isolated from the cortex of Phellodendron chinense schneid. The structure was determined on the basis of spectroscopic evidences.
OBJECTIVE: To Study the granulation of processed Cortex Phellodendri. METHOD: Take berberine, total alkaloids and dry extract as indexes to compare the semi-bionic extraction (SBE) with water extraction (WE). RESULT: In 5 kinds of phellodendron bark solution, berberine, total alkaloids and dry extract obtained by SBE are much better than those obtained by WE. CONCLUSION: In the preparation of oral granules from processed Cortex Phellodendri, SBE is superior to WE, when the pH value is adjusted by HCl solution to 1.0 in the first decoction, adjusted by saturated Ca(OH)2 solution to 7.0 in the second decoction and to 10.0 in the third decoction respectively.
Alcoholic liver disease (ALD) is one of the most common liver diseases in the world. Increased levels of proinflammatory cytokines, including interleukin-1beta (IL-1beta) and tumor necrosis factor-alpha (TNF-alpha), have been correlated with the patients affected by ALD. However, the direct effect of alcohol in the induction of IL-1beta and TNF-alpha has not been clarified. In this study, we demonstrated that acetaldehyde, the metabolic product of ethanol, was able to induce IL-1beta and TNF-alpha production in HepG2 cells. Nuclear factor-kappaB (NF-kappaB), the transcription factor involved in the regulation of cytokine production, was also activated by acetaldehyde through inhibitory kappaB-alpha (IkappaB-alpha) phosphorylation and degradation. However, the NF-kappaB inhibitors, such as aspirin, cyclosporin A and dexamethasone, inhibited both the acetaldehyde-induced NF-kappaB activity and the induced cytokine production. Therefore, these data suggested that acetaldehyde stimulated IL-1beta and TNF-alpha production via the regulation of NF-kappaB signaling pathway. By screening 297 controlled Chinese medicinal herbs supervised by Committee on Chinese Medicine and Pharmacy at Taiwan, we found that Coptis chinensis (Huang-Lien) and Phellodendron amurense (Huang-Po) were capable of inhibiting acetaldehyde-induced NF-kappaB activity. Berberine, the major ingredient of these herbs, abolished acetaldehyde-induced NF-kappaB activity and cytokine production in a dose-dependent manner. Moreover, its inhibitory ability was through the inhibition of induced IkappaB-alpha phosphorylation and degradation. In conclusion, we first linked the acetaldehyde-induced NF-kappaB activity to the induced proinflammatory cytokine production in HepG2 cells. Our findings also suggested the potential role of berberine in the treatment of ALD.
The topical anti-inflammatory activity of extracts from Cassia angustifolia, Rheum palmatum, Coptis chinensis, Phellodendron amurense and Scutellaria baicalensis, plants used in traditional East Asian medicine against different skin disorders, was studied. Though in different degree, all the extracts significantly inhibited the edema induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), in both single or multiple application, oxazolone, and arachidonic acid (AA). None of the extracts inhibited in vitro the activity of phospholipase A(2) (PLA(2)) from Naja naja.
This study describes the screening of extracts obtained from 18 plants and two fungi used in the Chinese and Mediterranean traditional medicines on epimastigote forms of Trypanosoma cruzi. The extracts were tested against epimastigote of T. cruzi Bra C15C2 clone in vitro at 27 degrees C and at a concentration of 250 microg/ml in axenic culture. Angelica dahurica, A. pubescens, A. sinensis, Astragalus membranaceus, Coptis chinensis, Haplophyllum hispanicum, Phellodendron amurense, Poria cocos, Ranunculus sceleratus and Scutellaria baicalensis showed significant effects against the parasite with a percentage of growth inhibition between 20 and 100%. C. chinensis and R. sceleratus showed the greatest activity with IC(50) values of 1.7 microg/ml for C. chinensis and 10.7 microg/ml for R. sceleratus. These activities are greater than that of allopurinol. C. chinesis and R. sceleratus extracts did not show cytotoxic effects on rat polimorphonuclear cells using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide and lactic dehydrogenase assays. These results allowed us to suggest that R. sceleratus and C. chinensis could be a source of new compounds clinically active against T. cruzi.
The monoclonal antibody (MAb) against berberine, a bioactive constituent of Coptis japonica M., Phellodendron amurense R. and Hydrastis canadensis L., was produced and characterized. As immunogen, the derivative of berberine, 9-O-carboxymethyl berberrubine was synthesized and conjugated to carrier protein, bovine serum albumin (BSA). In order to confirm its immunogenicity, the ratio of hapten in berberine-BSA conjugate was determined by matrix-assisted laser desorption/ionization time of flight mass spectrometry (MALDI-TOF MS). After immunization, hybridomas secreting MAbs against berberine were produced by fusing splenocytes with mouse myeloma cell line, P3-X63-Ag8-653. After the screening, anti-berberine MAb 1D5-3B-7 was obtained. Subsequently, a quantitative ELISA system for berberine and its related compounds using the MAb was established and evaluated comparing with HPLC method. The ELISA method described in this study can be available as an analytical tool for quality control and standardization of medicinal plants and its prescriptions containing berberine and its related compounds.
The pharmacological effects of Oren-gedoku-to (OGT), a Japanese-Chinese traditional herbal medicinal mixture on lipid biosynthesis were investigated in cultured human hepatocyte HepG2 cells. The addition of OGT (0.5 and 4.2 mg/ml), which had no effect on cell proliferation and cellular protein content, caused a marked decrease in the cellular cholesterol content, particularly cholesteryl ester content following 24 h incubation. The incorporation of 14C-oleate into cellular cholesteryl ester fraction was also reduced remarkably during incubation for 6 and 24 h. The effects of OGT, its components and its main active chemicals on acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity were studied in vitro to explore the mechanism by which OGT inhibits cholesteryl ester formation. The data confirmed that OGT, in a dose-dependent manner, and its components (Scutellaria baicalensis, Coptis japonica, Gardenia jasminoides and Phellodendron amurense) remarkably inhibit ACAT activity. Among the main active chemicals of OGT, baicalein, a kind of flavonoid, decreased ACAT activity in a dose-dependent fashion from the level of 10(-6)M. These results strongly suggest that OGT reduces the cholesteryl ester formation in human hepatocytes by inhibiting ACAT, and that baicalein may, in part, be responsible for ACAT inhibition.
Methicillin-resistant Staphylococcus aureus (MRSA) bacteria have been responsible for substantial morbidity and mortality in hospitals because they usually have multidrug resistance. Some natural products are candidates as new antibiotic substances. In the present study, we investigated the antimicrobial activity of berberine, the main antibacterial substance of Coptidis rhizoma (Coptis chinensis Franch) and Phellodendri cortex (Phellodendron amurense Ruprecht), against clinical isolates of MRSA, and the effects of berberine on the adhesion to MRSA and intracellular invasion into human gingival fibroblasts (HGFs). Berberine showed antimicrobial activity against all tested strains of MRSA. Minimum inhibition concentrations (MICs) of berberine against MRSA ranged from 32 to 128 microg/mL. Ninety percent inhibition of MRSA was obtained with 64 microg/mL or less of berberine. In the checkerboard dilution test, berberine markedly lowered the MICs of ampicillin and oxacillin against MRSA. An additive effect was found between berberine and ampicillin, and a synergistic effect was found between berberine and oxacillin against MRSA. In the presence of 1-50 microg/mL berberine, MRSA adhesion and intracellular invasion were notably decreased compared with the vehicle-treated control group. These results suggest that berberine may have antimicrobial activity and the potential to restore the effectiveness of beta-lactam antibiotics against MRSA, and inhibit the MRSA adhesion and intracellular invasion in HGFs.
The anti-Candida potentials of 12 Korean medicinal plants were explored: methanol extracts from Coptis rhizoma and Phellodendron amurense caused significant inhibition of growth of Candida albicans, Candida glabrata, Candida krusei and Candida parapsilosis. The predominant active components of the extracts were the protoberberines berberine and palmatine; the most potent inhibition of growth was exhibited by berberine on C. krusei (MIC <4 mg/L) and palmatine on C. parapsilosis (MIC 16 mg/L). Both berberine and palmatine inhibited the in-vivo rate of incorporation of L-[methyl-14C]methionine into C-24 of ergosterol in C. albicans (50% inhibition concentration (IC50 values), 25 microM and 300 microM, respectively); this result suggests that sterol 24-methyl transferase (24-SMT) is one of the cellular targets for the antifungal activity of the protoberberines. In-vitro 24-SMT activity in microsomes from the yeast growth form of C. albicans was inhibited by both berberine (inhibition constant (Ki) 232 microM) and palmatine (Ki 257 microM) in a non-competitive manner; inhibition of 24-SMT was more marked for the mycelial form than for the yeast growth form of this organism. Palmatine inhibited chitin synthase from both the yeast and mycelial growth phases of C. albicans in a non-competitive manner (Ki 780 microM). The effects of protoberberines, extracted from established medicinal plants, on both sterol and cell wall biosyntheses in pathogenic fungi indicate that the potential of these compounds, or their semi-synthetic derivatives, as a novel class of antifungal agents should be investigated more fully.
Qing-Luo-Yin (QLY), a traditional Chinese herbal medicine for the treatment of rheumatoid arthritis, is a combination of the extracts of Sophora flavescens Ait., Phellodendron amurense Rupr., Sinomenium acutum Rehd. et Wils. and Dioscorea hypoglauca Palib. The suppressive effect of QLY on the development of angiogenesis was investigated in a rat model of collagen-induced arthritis (CIA). QLY (0.3 g/kg) was orally administered daily for 27 days. Neo-angiogenesis, pannus and cartilage damage, the expression of metalloproteinases (MMP)-3 messenger RNA (mRNA) and the level of the tissue inhibitor of matrix metalloproteinase (TIMP)-1 in the synovium were examined by histology, in situ hybridization and immunohistochemiscal assays, respectively. It was observed that the articular morphological alterations, the over-expression of MMP-3 mRNA and the reduced production of TIMP-1 in CIA rats were significantly ameliorated by QLY. QLY performed about as effectively as tripterygium glycosidorum tablets (0.1 g/kg) extracted from Tripterygium wilfordii Hook. f.. These results indicate that QLY exerts a suppressive effect on the angiogenesis of CIA rats, and suggest that the therapeutic effect of QLY could be due to restoring the balance of MMP-3 and TIMP-1 in rheumatoid synovium.
In chinese medicine, Phellodendri Cortex (Phellodendron amurense Ruprecht) has been used to treat the patient who suffers from gastroenteritis, abdominal pain or diarrhea. Berberine has been identified as a major component in this plant, and it has biological activities, such as bactericidal activity, anti-cholera toxin effect, anti-inflammatory effect, stimulative effect of bile secretion or bilirubin discharge. In the previous study, we have shown the presence of anti-inflammatory activity in the berberine-free fraction of the extract from this plant. In the present study, we also found anti-ulcer activity in the fraction. The fraction significantly inhibited the formation of ethanol-induced ulcer, aspirin-induced ulcer (s.c., p.o.), pylorus-ligated ulcer (p.o., i.d.) in rats, as well as that of stress ulcer in restrained and water-immersed mice (p.o.). In addition, gastric acid secretion was significantly reduced in pylorus-ligated rats by subcutaneous or intraduodenal administration of the fraction, but not by oral administration. These findings suggest that the suppression of ulcer formation may be due to the additive effect of the cytoprotection effect and the reduction of gastric acid secretion by administration of the berberine-free fraction.
The potential responses of forest succession in the clear-cut site of mixed coniferous and broad-leaved Korean pine forest (MCBLKPF) in Yichun, Heilongjiang Province to global climate change and elevated CO2 after 50 years by BKPF model were simulated. The results indicated that the densities of Pinus koraiensis and hardwood species(Fraxinus mandshurica, Tilia amurensis, Juglans mandshurica and Phellodendron amurense) would increase, while the densities of Larix olgensis, Betula platyphylla and Populus davidiana would decrease after 50 years. The stand densities would be slightly lower than those at the same age under the current climate condition. The stand productivity, total aboveground biomass and leaf area index will increase by 7-28%, 15-24% and 5-8%, respectively. Climate change would be beneficial to the forest succession from the clear-cut site to MCBLKPF.
OBJECTIVE: To screen some Chinese herbal medicines for their inhibitory activity on cariogenic bacteria, and investigate their active ingredients, and measure their minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC). METHODS: Active components were isolated from every tested Chinese herbal medicine by means of aqueous extraction and ethanolic extraction. Berberine was purified from Coptis chinensis Fra. Disk agar diffusion method was employed in screening herbs with inhibiting effect on cariogenic bacteria. MIC and MBC were determined by broth dilution method. RESULTS: Against Streptococcus mutans Ingbritt, MBCs of Magnolia officinalis ethanolic extract, Berberine, Coptis chinensis Fra aqueous extract and Coptis chinensis Fra ethanolic extract were 0.488, 0.625, 7.800 and 1.950 g/L respectively. Against Streptococcus sobrinus 6715, MBCs of Magnolia extract, Coptis chinensis Fra ethanolic extract, Rhus chinensis Mill ethanolic extract and Phellodendron chinen ethanolic extract were 0.488, 0.625, 1.950, 3.900, 3.900 and 3.900 g/L respectively. Against Actinomyces viscosus ATCC 19246, MBCs of Berberine, Coptis chinensis Fra aqueous extract, Coptis chinensis Fra ethanolic extract, Rheum palmatum L aqueous extract and Rheum palmatum L ethanolic extract were 1.250, 3.900, 3.900, 15.600 and 31.250 g/L respectively. CONCLUSIONS: Magnolia officinalis, Coptis chinensis Fran, Rheum palmatum L aqueous extracts exhibit strong inhibition on cariogenic bacteria. Magnolia officinalis ethanolic extract has the strongest bactericidal effects on Streptococcus mutans and Streptococcus sobrinus.
OBJECTIVE: To establish the quality standards for fuyanke(FYK) granule. METHODS: The phellodendron Chinese schneid, polygonum cuspidatum, sieb. et Zucc and glycyrrihza uralensis fisch in FYK granule were identified by thin-layer chromatography(TLC). The contents of berberine were determined by thin-layer chromatographic scanning(TLCs). RESULTS: The average recovery rate was 97.86%, and the relative standard deviation 1.96%. CONCLUSION: The method is simple, accurate and reliable.
Shangke Wangshui is a new Chinese traditional patent medicine. Its main ingredients Coptis Chinsis Franch, Phellodendron amurense Rupr. and Gardenia jasminoides Ellis. were identified by TLC and PC. The content of active component berberine in Shangke Wangshui was determined by TLC-scanner. This mothod is simple, quick and highly reproducible and can be as a quality control standards for this preparation.
The spatial features and attribute data of urban forests in Shenyang arboretum were acquired by using aerial photographs and field investigation. After systemic and quantitative analysis of the species composition and spatial distribution pattern of urban forest community based on geographic information system (GIS), the following results were achieved: 1) the vegetation in the arboretum was rich and in a good condition. Phellodendron amurense, Robinia pseudoacacia, and Ulmus punita were the main species according to their abundant individuals and relative dominance. The spatial distribution pattern of this vegetation indicated that it was in a growing level and in the best state for ecological benefits; 2) the tree species relative dominance based on vegetation quantity had no distinct relationship with the species abundance, and the species having abundant individuals might have a low relative dominance; and 3) the curve displayed in the relationship diagram between tree individuals and tree height showed ascending and protruding. With the increment of tree height class, the individuals were unchanged nearly at the beginning, but when the height was more than 12 m, the individuals reduced distinctly, and the curve displayed a quickly declined trend. The relationship between tree individuals and tree diameter at the breast height (DBH) showed the same result.
A description is given for the preparation of flow through sensor and of the incorporation of the sensor into a flow injection analysis system. The parameters affecting the measurement are discussed. An accurate, convenient and rapid method is proposed for the determination of berberine-type alkaloids in various Chinese patent medicines (Coptis chinensis Franch., Phellodendron chinesis Schneid., xianglian wan, zuojin wan, ermiao wan and sanmiao wan). The slope is 54-60 mV/decade over the concentration range of 10(-3)-3 x 10(-6) mol/L berberine at pH 2-9.5. Direct potentiometry determination of berberine in various samples showed an average recovery of 99.5-103.5% and a relative standard deviation of 1.3-3.5% at a sampling rate of 120/h.
In the paper systematic studies on quality standards for Qingwei Huanglian Pills are reported, along with the TLC identification of Gardenia jasminoides, Scutellaria baicalensis and Anemarrhena asphodeloides and the quantitative determination of berberine in Coptis chinensis and Phellodendron chinese by TLC densitometric method. To simplify the operation, the same solvent was used for both the identification and determination. The quantitative method is simple, sensitive, reproducible and accurate. The recovery of berberine is 99.48%. The coefficient of variation is 1.42%.