Coptis Rhizome Research Articles

Antimicrobial efficacies of plant extracts and sodium nitrite against Clostridium botulinum

This study was conducted to evaluate the antibotulinal activities of some plant extracts, alone or in combination with nitrite (NaNO 2). Water- and 99.5% ethanol-soluble extracts (1:9 plant material weight-by-solvent volume, 25 °C, 48 h) of 90 kinds of fresh and dehydrated herbs and spices were tested. The aqueous extract of clove and alcohol extracts of lemon eucalyptus, mace and licorice exhibited greater antibotulinal activities in TPGY medium with MIC ranging from 0.05% to 0.2%. However in TPGY, only the aqueous extract of Coptis rhizome exhibited synergistic antibotulinal activity with NaNO 2, reducing the individual MIC of NaNO 2 from 6–8 ppm to 2 ppm with 0.05% Coptis extract. In a model meat food, the alcohol-soluble extracts of nutmeg (0.05%) and sage (0.02%), and the aqueous fraction of clove extract (0.05%) exhibited antibotulinal activities in combination with 10 ppm NaNO 2. The observed synergy between plant extracts and NaNO 2 that resulted in lower MIC of both additives have significant repercussion in the control of botulism in minimally processed meat products without compromising organoleptic properties.

HPTLC for Quality Control of Traditional Chinese Medicines: Identification and Detection of Adulteration

For cGMP compliance of dietary supplements and quality control of herbal medicinal products, proper identification of herbal raw material is of great importance. In this respect Traditional Chinese Medicines (TCM) can present challenging tasks because pharmacopoeial drug monographs may include multiple species and often don't provide sufficient analytical methods. High Performance Thin-Layer Chromatography (HPTLC) is a very suitable tool for direct comparison of fingerprints from multiple samples side by side and allows determining similarities and differences of related species. Using “BEIMU” (Fritillaria spp.) and “CANGZHU” (Atractylodes spp.) as examples, the development and use of validated methods for this purpose is illustrated. The traditional approach of associating the quality of an herbal medicine with the quantity of a marker becomes questionable, if the product contains more than one plant material. CANGZHU XIANGLIAN SAN a TCM for veterinary use contains Coptis rhizome, Aucklandia root, and Atractylodes root but the Chinese Veterinary Pharmacopoeia only relies on identification and quantitation of berberin as principal marker. Berberin is present in Coptis only. This creates the possibility for adulterated products, missing either of the other two plants to enter the market. We propose an HPTLC method that allows a more complete monitoring of quality by ensuring the presence of all species in the appropriate quantity.

Relationship Between San-Huang-Xie-Xin-Tang and Its Herbal Components on the Gene Expression Profiles in HepG2 Cells

Traditional Chinese medicine (TCM) has been used for thousands of years. Most Chinese herbal formulae consist of several herbal components and have been used to treat various diseases. However, the mechanisms of most formulae and the relationship between formulae and their components remain to be elucidated. Here we analyzed the putative mechanism of San-Huang-Xie-Xin-Tang (SHXXT) and defined the relationship between SHXXT and its herbal components by microarray technique. HepG2 cells were treated with SHXXT or its components and the gene expression profiles were analyzed by DNA microarray. Gene set enrichment analysis indicated that SHXXT and its components displayed a unique anti-proliferation pattern via p53 signaling, p53 activated, and DNA damage signaling pathways in HepG2 cells. Network analysis showed that most genes were regulated by one molecule, p53. In addition, hierarchical clustering analysis showed that Rhizoma Coptis shared a similar gene expression profile with SHXXT. These findings may explain why Rhizoma Coptis is the principle herb that exerts the major effect in the herbal formula, SHXXT. Moreover, this is the first report to reveal the relationship between formulae and their herbal components in TCM by microarray and bioinformatics tools.

Selective inhibition of vascular smooth muscle cell proliferation by coptisine isolated from Coptis rhizoma, one of the crude drugs composing Kampo medicines Unsei-in

Acceleration of vascular smooth muscle cell (VSMC) proliferation is closely linked to the pathogenesis of vascular diseases. We, therefore, focused on traditional Japanese herbal medicines (Kampo medicines) used to ameliorate the impairment of microcirculation or blood stasis and screened them for their ability to inhibit rat VSMC proliferation. Among them, Unsei-in was found to effectively suppress VSMC proliferation, and Coptis rhizome was the responsible constituent crude drug. The extract of Coptis rhizome inhibited VSMC proliferation with the GI(50) value of 4.4 microg/ml, which was much lower than those against the proliferation of 3Y1, dRLh-84, B16, and HeLa cells. The Coptis rhizome extract inhibited the progression of VSMC arrested at G(0)/G(1) phase from G(0)/G(1) to S phase, but not that of 3Y1 cells. Biological assay-guided fractionation revealed that an alkaloid of Coptis rhizome, coptisine, was the active ingredient in selectively preventing VSMC proliferation with GI(50) of 3.3 microM (1.2 microg/ml). When the structurally-related isoquinoline alkaloids of protoberberine class were studied for their inhibitory activities, berberine decreased the VSMC proliferation with GI(50) of 95.1 microM (35.4 microg/ml), about 30 times higher concentration than coptisine, while palmatine failed to show any activity. This study provides evidence that coptisine, an ingredient of Unsei-in, prevents VSMC proliferation selectively at lower concentrations compared with various cells or other structurally related alkaloids.

Study of total alkaloids from Rhizoma Coptis Chinensis on experimental gastric ulcers

To study the effects of total alkaloids (TA) extracted from Rhizoma Coptis Chinensis on experimental gastric ulcer models. Four kinds of experimental ulcer models were established respectively by water-immersion stress, intragastric ethanol, acetic acid erosion, and pylorus ligation. The anti-ulcer effects of TA were evaluated, and compared with that of berberine (Ber) and cimetidine (Cim). TA showed significant inhibitory effects on ulcerative formation induced by water-immersion stress, intragastric ethanol, and pylorus ligation in dose-dependent manner, and showed therapeutic effect on acetic acid erosion-inducing ulcer, in comparison with the control group. The anti-ulcer activity of Ber was less than TA containing equal content of Ber. TA significantly reduced the free acidity, total acidity and total acid output, but didn't affect the gastric juice volume, gastric pepsin activity, adherent mucus quantity of stomach wall and free mucus dissolving in gastric juice. The suppressive activities of TA on gastric acid secretion didn't occur when it was administered into dodecadactylon at a dose of 360 mg/kg wt. Moreover, when compared with Cim, the inhibitory effect of TA on gastric acid secretion isn't proportional to the inhibitory effects on the formation of the 4 kinds of experimental ulcers. TA is a potent candidate in therapeutic drugs for treating gastric ulcer. Its anti-ulcer effective components and mechanism is not only related to Ber and inhibition of gastric acid, but also to other ingredients of TA and mechanism so far unknown.

The mechanism of alteration of monoamine metabolism in brain regions in marble burying behavior-isolated housing mice and effect of oren-gedoku-to on this alteration

The mechanism of the alteration in marble burying behavior-isolated housing (MBB-IH) mice was investigated. The determination of hypothalamus monoamine and serum corticosterone contents indicated that MBB-IH mice readily responded to the stress stimuli in conditioned fear stress. Six drugs, such as buspirone (10 mg/kg, p.o.), zimelidine (10 mg/kg, p.o.), clomipramin (10 mg/kg, p.o.), yohimbine (5 mg/kg, p.o.), ethyl beta-carboline-3-carboxylate (beta-CCE, 5 mg/kg, p.o.) and flumazenil (15 mg/kg, p.o.) were singly and/or three times administered to MBB-IH mice. Their inhibitory activity on the MBB-IH mice was considered by the use of activity profiles consisting of spontaneous locomotor activity, marble burying behavior and hypothalamus monoamine content. Using these profiles, we calculated the activities as vector in three-dimensional space, and compared the distance from the control point (DCP). DCPDOPAC and DCP5-HIAA were shortened by single administration of beta-CCE and flumazenil. Oren-gedoku-to (30 and 300 mg/kg, p.o.) shortened the DCPDOPAC and DCP5-HIAA similarly to beta-CCE. The blended crude drugs in Oren-gedoku-to, Coptis rhizome (636.0 mg/kg, p.o.), Scutellaria root (644.4 mg/kg, p.o.) and Gardenia fruit (894.8 mg/kg, p.o.) shortened the DCPDOPAC. Coptis rhizome and Scutellaria root also shortened the DCP5-HIAA. These results suggest that GABA neuron function intensely affects the alteration of MBB-IH and Oren-gedoku-to has the intrinsic benzodiazepine-like activity.

Differential inhibitory effects of protoberberines on sterol and chitin biosyntheses in Candida albicans.

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.

New Developments in Capillary Electrophoresis. Application of Capillary Electrophoresis to Quantitative Analysis and Characterization. Determination of berberine-type alkaloids in Coptis Rhizoma and Phellodendri Cortex by capillary electrophoresis.

New Developments in Capillary Electrophoresis. Application of Capillary Electrophoresis to Quantitative Analysis and Characterization. Determination of berberine-type alkaloids in Coptis Rhizoma and Phellodendri Cortex by capillary electrophoresis.

Inhibitors of DNA topoisomerase I and II isolated from the Coptis rhizomes.

A water extract of Coptis chinensis was found to have the ability to stabilize the cleavable complex with mammalian DNA topoisomerase I. As the result of bioassay-guided fractionation, two protoberberine alkaloids, epiberberine and groenlandicine, were identified as active principles with topoisomerase I-mediated DNA cleavage activity in vitro. These two alkaloids did not induce topoisomerase II-mediated DNA cleavage. During further examination of the structurally related protoberberine alkaloids, berberrubine which is produced during the processing of Coptis rhizome as traditional medicine, was identified as a specific inducer of topoisomerase II-mediated DNA cleavage in vitro. These results indicated that protoberberine alkaloids are a chemical family which can induce cleavable complexes with topoisomerases I and II.

076 Effect of coptis rhizome and its fractions on the lipogenesis of organ cultured sebaceous glands of hamster pinna

076 Effect of coptis rhizome and its fractions on the lipogenesis of organ cultured sebaceous glands of hamster pinna

Determination of quaternary alkaloids from Coptidis Rhizoma by capillary electrophoresis

A simple and rapid method for the simultaneous determination of eight quaternary alkaloids (coptisine, berberine, epiberberine, palmarine, columbamine, berberastine, jatrorrhizine and magnoflorine) in coptis rhizome by capillary electrophoresis was developed. A buffer solution composed of 85% 0.1 M sodium acetate solution and 15% methanol was found to be the most suitable electrolyte for this separation, whereby the levels of the eight quaternary alkaloids in the crude drug Coptidis Rhizoma could be easily determined.

Alkaloids of Coptis Rhizome

Alkaloids of Coptis Rhizome

Studies on the pharmaceutical quality evaluation of crude drug preparations used in orient medicine "Kampoo". III. Precipitation reaction of glycyrrhizin with alkaloids or alkaloidal crude drugs in aqueous solution.

Precipitation reaction of glycyrrhizin (I) with 32 kinds of alkaloids including synthetic bases and 10 kinds of crude drugs which contain various types of alkaloids in aqueous solution was investigated and following results were obtained. 1) Tertiary alkaloids which had heterocyclic aromatic rings or nitrogen atoms neighbouring to aromatic ring or conjugated olefine systems in the structure, namely, papaverine, noscapine, emetine, O-methyl domesticine, domesticine, nornuciferine, dl-tetrahydroberberine, l-corydaline, quinine, reserpine and sinoactine gave precipitate, while other types of alkaloids, namely, l-ephedrine, N-methylephedrine, l-phenylalaninol, atropine, l-scopolamine, cocaine, morphine, ethylmorphine, codeine, hydrocodeine, thebaine, sinomenine, aconitine, physostigmine, caffeine, pethidine did not. 2) Tertiary alkaloids which had pKa values smaller than 7.5 were likely to precipitate with I, while those which had pKa values larger than 7.5 did not. 3) Among quaternary alkaloids, berberine and coptisine produced precipitate, while menisperine, N-methyl scopolamine and neostigmine did not. 4) Among crude drugs which contained various alkaloids, coptis rhizome, corydalis roots, phellodendron cortex and evodia fruits gave precipitate with I in aqueous solution, while aconite roots, areca seeds, ephedra herb, magnolia cortex, nupharis rhizome and sinomenium roots did not.

High-speed liquid chromatographic analysis of drugs. II. Rapid estimation of berberine in crude drugs (author's transl)

A rapid estimation procedure using a high-speed liquid chromatography is described for determination of berberine in crude drugs (phellodendron cortex, coptis rhizome, and phellodendron extract). Separation can be achieved within 10 min employing a 1 m column packed with Zipax SCX, using 0.1 M NaClO4 (CH3CN-H2O 6 : 4), and 0.2M H3BO3-0.002 M NaClO4 (pH 8.5) (7 : 3) solution as an eluant in a Du Pont LC 830 liquid chromatograph. Berberine in crude drugs was extracted with citric acid-methanol solution and injected into the column. Accuracy in this method was found to be less than ±1% with the relation Y=13.806X+0.0025, where X=quantity of berberine (μg) and Y=peak height of berberine (cm), and a relative coefficient of 0.999.

Studies on anti-inflammatory agents. Anti-inflammatory screening by fertile egg method (author's transl)

The fertile egg method of D'arcy, et al. was found to be suitable for anti-inflammatory screening of extracts of natural sources. The suitable primary incubation period and implantation period were 9 and 4 days, respectively. Certain dose of steroidal anti-inflammatory drugs, e.g., 6.3 μg/disc of dexamethazone, significantly inhibited the granulation tissue formation of chorio-allantoic membrane in the established method. Non-steroidal drugs, such as phenylbutazone, showed inhibitory action at 500 μg/disc. This screening method was applied to aqueous methanolic (1 : 1) extracts from more than a thousand crude drugs and plants and 62 extracts were found to be active at 800 μg/disc. It was found that berberine-containing plants, e.g., coptis rhizome, were strongly active even in a dose of 400 μg/disc.