ABSTRACT
Macleaya cordata, a perennial plant in the genus Macleaya, it mainly distributed in most provinces and regions south of the Yangtze river and north of Nanling mountains of China and has been used as a Chinese traditional medicine. It is bitter, cold, warm, poisonous. M. cordata has the functions of dispelling wind, analgesia, detoxification and detumescence. It mainly treats poisonous abscess, cachexia, ulcer, scabies, trichomonal vaginitis, etc. It also has insecticidal and anti-itching activities. The main chemical constituents of M. cordata are isoquinoline alkaloids, sanguinarine, chelerythrine, protoopioid and allocrine alkaloids are the higher ones. In addition, it also contains phenylpropanoids, steroids, organic acids, phenols and volatile oils. The pharmacological effects of M. cordata are mainly anti-bacterial, anti-inflammatory, anti-tumor and improving liver function. In agriculture, it can be used as botanical insecticides and bacteriostasis, and also as feed additives for animal husbandry. By reviewing and analyzing domestic and foreign researches that isoquinolines were the main active constituents and characteristic components of M. cordata. This paper provides theoretical basis for the development and utilization of M. cordata extract and its' monomer compounds.
ABSTRACT
G-quadruplex DNA has become an important target for tumor therapy and anti-tumor development. Modern pharmacology has proved that Macleaya cordata has anti-inflammatory, antibacterial, anti-tumor and other pharmacological effects. Affinity ultrafiltration method can screen active ingredients from compounds rapidly, but G-quadruplex DNA ligands are difficult to dissociate, which is a key step in conventional ultrafiltration method. In this paper, the filtrates after ultrafiltration were determined by HPLC-MS in substitution. The peaks with 20% reduction of MS response from the incubation vs control were considered to be ligand components to G-quadruplex. Two of the peaks with the relative abundance above 30% were identified as sanguinarine(SAN) and chelerine(CHE). Their circular dichroism conformations further proved that SAN and CHE are active ligands of HT4. In addition, another two gradients with high relative abundance were identified as protopine(PRO) and allpcryprotopine(ALL). The binding rate of SAN, CHE, PRO and ALL was calculated according to the HPLC-MS results, and the results showed a consistency with that of the molecular docking method. The proposed method can be used to screen active components from mixture.
Subject(s)
Chromatography, High Pressure Liquid , Chromatography, Liquid , G-Quadruplexes , Ligands , Mass Spectrometry , Molecular Docking Simulation , UltrafiltrationABSTRACT
OBJECTIVE： To establish the separation and purification technology of sanguinarine from the extract of Macleaya cordata with ion exchang resin. METHODS： The content of sanguinarine from the extract of M. cordata was determined by HPLC， with Cosmosil C18-R-Ⅱ column （250 mm×4.6 mm，5 μm）， mobile phase of acetonitrile-0.2％ acetic acid solution （25 ∶ 75，V/V）， the flow rate of 1 mL/min， detection wavelength of 270 nm， column temperature of 30 ℃， and sample size of 20 μL. Static adsorption and desorption tests were carried out to compare the adsorption and desorption properties of 8 ion exchange resins for sanguinarine. The optimum concentration of sample solution， pH value and volume of sample were investigated by optimum ion exchange resin. APPS 10D liquid phase preparation system was used to investigate the dynamic elution conditions and obtain M. cordata refined extract solution. The refined purified product of M. cordata was obtained by desalination， elution on a reversed-phase （RP） C18 column and drying. The purity of the purified product was analyzed by HPLC. The structure of the purified product was confirmed by HPLC， UV spectrophotometry， MS and NMR. RESULTS： CM-FF resin was screened for the separation and purification of sanguinarine from M. cordata extract. It was eluted with 20 mmol/L ammonium acetate solution 100 mL containing 20％ methanol and 0.25 mol/L sodium chloride. The optimal dynamic absorption condition included that the concentration of sample was 6.0 mg/mL at pH 5.0，and the loading amount was 25 mL； after desalination and refinement， for the eluted refined extract， the purified product with 97％ purity （purified yield of 71％） was obtained， and its structure was confirmed to be sanguinarine. CONCLUSIONS： The optimal separation and purification technology by ion exchange resin is green， safe， efficient and easy to operate， which can be used for the separation and purification of sanguinarine from M. cordata extract and is suitable for industrial production.
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Chlortetracycline (CTC), one kind of common antibiotic for prevention and treatment of various diseases, also exhibits good performance in accelerating the growth of livestock. Macleaya cordata, a traditional Chinese medicine, is usually used as a natural additive in livestock because of its anti-microbial, anti-fungal, anti-inflammatory, and pesticidal activity. In this work, we studied whether M. cordata helps regulate the growth-promoting effect of CTC on broiler chickens. It is demonstrated that M. cordata improves the growth-promoting effect of CTC on growth performance indices of broiler chickens, such as survival rate, daily weight, and feed to weight rate. M. cordata also delays the maximum of CTC residues in plasma. It may depend on the higher values of operational taxonomic unit (OTU) and the indices of α diversity driven by simultaneous use of CTC and M. cordata.
Subject(s)
Animals , Female , Male , Anti-Bacterial Agents/pharmacology , Chickens/growth & development , Chlortetracycline/pharmacology , Drugs, Chinese Herbal/pharmacology , Duodenum/pathology , Gastrointestinal Microbiome , Medicine, Chinese TraditionalABSTRACT
Objective To establish the fingerprint profiling of fruits of Macleaya cordata and study the method for its quality evaluation. Methods The fingerprint profiling of M. cordata fruits from different regions was established using high performance liquid chromatography (HPLC) based on the local standard which was the determination method of the content of protopine, allocryptopine, sanguinarine, and chelerythrine from Changsha of Hunan Province in 2009. The principal component analysis (PCA) and cluster analysis (CA) were performed to explore the correlation among the common fingerprint peaks, origins, and quality of M. cordata fruits. Results Eleven common fingerprint peaks were identified in the fingerprint profiling of chemical constituents of M. cordata fruits from different regions. M. cordata fruits produced from eight areas were classified into two classes by PCA and CA method, and there were five common peaks, including peak 5, 7, 8, 9, and 11 with significant contribution on the regional difference of the fingerprint. Also, common peak 6 was the right peak as the reference peak because of its less variation, appropriate retention time and intensity. Conclusion The fingerprint profiling of chemical constituents of M. cordata fruits established in this study has good precision, repeatability, and stability, which can be used to evaluate the quality of fruits of M. cordata from different producing areas.
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Objective:To study the alkaloids in Macleaya cordata. Methods:The compounds were isolated and purified by silica gel,recrystallization,and semi-preparative HPLC, and their strcuctures were confirmed by MS and NMR. Results: Nine alkaloids were obtained and identified as dihydrochelerythrine(1), 6-cyanodihydrosanguinarine(2), R-6-((R)-1-hydroxyethyl)dihydrochel-erythrine(3),8-demethyl-dihydrochelerythrine(4),cheilanthifoline(5),canadine(6),8-demethyl-chelerythrine(7),protopine(8) and allocryptopine(9). Conclusion:Compounds 4-6 are isolated from the genus of Macleaya for the first time.
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Objective: To develop the quantitative analysis method combined with laser microdissection and LC-MS/MS technique for determinating sanguinarine, protopin, allocryptopine, chelerythrine, dihydrochelerythrine, and dihydrosanguinarine in the roots of Macleaya cordata, and performe the histochemical study on M. cordata roots. Methods: The technology of laser-microdissection was used to dissect the cork, cortex, phloem, xylem vascular bundles, and xylem rays from 2-year-old M. cordata roots at different growth stages, the technique of LC-MS/MS was applied to detecting the contents of targeted alkaloids in the microdissected tissues. Results: The six kinds of alkaloids possesed a wide linear ranges and a good linear relationship (r2 > 0.996 6); The RSD of intra- and inter-day precision was all less than 2.4%; The highest limits of detection and quantification were respectively 0.29 and 0.57 ng/mL; The repeatability RSD was below 13.2%. The recovery varied from 85.1% to 133.9%, and its RSD ranged from 9.4% to 20.7%. The total amounts of six kinds of alkaloids in the above five tissues were respectively 0.14, 0.10, 0.07, 0.16 and 0.11 μg/mm2 for seedling stage root; 0.38, 0.22, 0.15, 0.41 and 0.26 μg/mm2 for flowering stage root; 0.46, 0.29, 0.27, 0.55 and 0.22 μg/mm2 for fruit stage root, and 0.52, 0.29, 0.24, 0.41 and 0.23 μg/mm2 for latering fruit stage root. Conclusion: The integrated method is high-resolution, specific, sensitive, and reliable for the quantitative analysis of alkaloid in tissues; The six kinds of alkaloids are mainly located in corks and xylem vascular bundles from the roots of M. cordata.
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A new alkaloid was isolated from the leaves of Macleaya cordata with 95% ethanol extracted and its isolation was by column chromatography and preparation HPLC. The new structure was elucidated as 6'-hydroxy-2',3'-dimethoxyarnottianamide on the basis of its spectroscopic date.
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Objective: To study the antitumor molecular mechanism started on sanguinarine (San) and chelerythrine (Che) from Macleaya cordata. Methods: Determining the IC50 values of San and Che against A-549, HCT-8, and Bel-7402 cell lines by using MTT to clarify whether these two alkaloids are the active components in M. cordata; studying the interaction between human telomeric DNA and two alkaloids respectively by using UV-Vis, FL, and CD methods. Results: San and Che are the active antitumor components of M. cordata; San could induce HT4 to form antiparallel G-quadruplex completely with Ka of 5×108 and Che could induce HT4 to form antiparallel G-quadruplex partially with Ka of 930. Conclusion: One of the antitumor molecular mechanisms of M. cordata is that the two active components could induce human telomeric DNA to form G-quadruplex.
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Objective To find out the main target organs, their main pathological changes and to explore the toxic mechanism of the macleaya cordata. Method SD rats were intoxicated by oral administration with extracts of macleaya cordata followed by pathological and electromicroscopic examination of main organs. Results The LD50 was 19.5% when 1.5g/ml macleaya cordata extract was oral administrated. All pocsoned rat's serum GPT, Cr, BUN, CK, CK-MB increased markedly. The EKG were abnormal. The weight of brain, liver, spleen, and kidneys decreased significantly. There were extensive congestion and hemorrhage in heart, brain, liver and kidneys. The mitochondria, endoplasmic reticulum and nuclear membrane of the rat's heart, brain, liver, and kidney were destroyed. Conclusion The results indicated that the toxic target organs of macleaya cordata were the heart, brain, liver and kidneys mainly. The toxic mechanism of macleaya cordata poisoning was the damage of the mitochondrial, endoplasmic reticulum and nuclear membrane directly causd by the macleaya cordata.
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Objective To study the mechanism of the rat’s myocardium induced by macleaya cordata. Methods36 SD rats were randomly assigned to 2 experimental groups treated by macleaya cordata decoction with a dose of 1/6 LD50, 1/3 LD50 respectively and a control group treated with distilled water by oral administration. The rats were killed 6 hours after the administration for taking the cardiac muscle to examine the Ca2+.Mg2+-ATPase, SDH while observing the structures. ResoultsIn the group treated by macleaya cordata with dose of 1/6 LD50, the activity of Ca2+.Mg2+-ATPase and SDH were increased significantly.However, the groups treated by macleaya cordata with dose of 1/3 LD50 and distilled water, the activity of Ca2+.Mg2+-ATPase,SDH showed no significant change. The apoptosise in myocardium cells of rat’s can be observed in the experimental groups,while the changes were not seen in control group. ConclusionThe results indicate that the macleaye cordata can induce and improve the apoptosis of myocardium cells in low dose, and these effects may be induced by stimulating the activity of Ca2+.Mg2+-ATPase,SDH in myocardium cells.