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Interaction of chelerythrine Choloride in Acid Buffer with Calf-thymus DNA

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Chinese Chemical Letters 2006年第5期17卷 691-694页

作者： Yah Jing SU Xiong Hui WEI Department of Applied Chemistry College of Chemistry and Molecular Engineering Peking University Beijing 100871

The binding of chelerythrine （CHE） iminium to calf-thymus （CT） DNA is characterized by hypochromism and bathochromism in the absorption band, enhancement of fluorescence intensity, increase in fluorescence polarization, and the perturbation of the CD spectra of DNA. These changes are characteristic of intercalation. Scatchard plots constructed from fluorescence titration data gave a binding constant of 5.77×10^5 and a binding site size of 3,4 base pairs at 25 ℃. The intercalative interaction is exothermic with a Van＇t Hoff enthalpy of -33.7 kJ/mol. In addition, △G =-32.9 kJ/mol, and △S =-2.9 J/mol/K. The intercalation of CHE into the DNA helix is enthalpy-driven.

关键词： chelerythrine CT-DNA intercalation thermodynamic.

Simultaneous Quantitative Determination of Nitidine, chelerythrine and Sanguinarine Using HPTLC from Callus Extract of <i>Zanthoxylum rhetsa</i>

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American Journal of Analytical Chemistry 2018年第8期9卷 386-396页

作者： Kavitha Perala Veeresham Ciddi University College of Pharmaceutical Sciences Kakatiya University Warangal India

Nitidine, chelerythrine and Sanguinarine, all these three alkaloids are benzophenanthridine alkaloids. Nitidine was used as an anti-HIV, anti-malarial and anti-cancer. chelerythrine had anti-cancer and anti-inflammatory activities. Sanguinarine was widely used as an anti-plaquestic and anti-cancer. High performance thin layer chromatography (HPTLC) method was used for simultaneous quantification of Nitidine, chelerythrine and Sanguinarine in callus extract of Zanthoxylum rhetsa by using Silica gel 60 F254 as stationary phase and ethyl acetate:methanol:water:diethylamine (30:5:2:0.5 v/v) as mobile phase at 280 nm. The linearity concentration range was 5 - 160 μg/band of each alkaloid. The Rf values of Nitidine, chelerythrine and Sanguinarine were found to be 0.28, 0.49 and 0.73. The limit of detection and limit of quantification were found to be 0.026, 0.088 μg/spot and 0.010 and 0.033 μg/spot, 0.0104 and 0.035 μg/spot respectively for Nitidine, chelerythrine and Sanguinarine. HPTLC method was developed and validated according to ICH guidelines for simultaneous estimation of Nitidine, chelerythrine and Sanguinarine and proved to be simple, specific, accurate, robust and rapid.

关键词： Nitidine chelerythrine Sanguinarine HPTLC

Stability of Sanguinarine and chelerythrine in Macleaya cordata (Willd.) R. Br.

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Medicinal Plant 2019年第6期10卷 20-23页

作者： Chunmei LI Xu CHEN Wenlan LI Bingmei LIU Li WANG Yubin JI School of Pharmacy Harbin University of CommerceHarbin 150070China Engineering Research Center of Natural Anti-tumor Drugs Ministry of EducationHarbin 150070China Post-doctoral Research Center of Drugs Research Institute Harbin 150070China Nangang Branch Hospital Heilongjiang Provincial HospitalHarbin 150001China

[Objectives]To explore the stability of sanguinarine and chelerythrine in Macleaya cordata(Willd.)***.[Methods]The solubility and stability of sanguinarine and chelerythrine in seven solvents were measured by ***,the effects of water quality,light source,oxidant,temperature,and pH on stability were investigated.[Results]The solubility and stability of sanguinarine and chelerythrine in methanol and ethanol are good;the stability of sanguinarine and chelerythrine in distilled water and rainwater is not affected by light and is very stable,but they are unstable in tap water whether they are protected from light or not;oxidants have a great influence on the stability of sanguinarine and chelerythrine;sanguinarine and chelerythrine are stable at room temperature lower than 54℃;sanguinarine is stable in pH 2.5-7.0,while chelerythrine is stable in pH 2.5-8.0.[Conclusions]The good stability of sanguinarine and chelerythrine under specific conditions shows that they have broad development prospects and value.

关键词： Macleaya cordata(Willd.)R.Br. Sanguinarine chelerythrine Stability

Metabolomics Analysis of the Effects of chelerythrine on Ustilaginoidea virens

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Metabolomics Analysis of the Effects of Chelerythrine on Ust...

CRYSTAL AND MOLECULAR STRUCTURE OF 6-METHOXY-5, 6-DIHYDROchelerythrine

中国植物病理学会2024年学术年会

作者： WEI Qinghui ZHAI Xihai SONG Weifeng LI Zhiyong PAN Yaqing LI Baoying JIAO Zhanli SHI Zhenghao YU Jiangtao Institute of Plant Protection Heilongjiang Academy of Agricultural Sciences Yongyuan Town People's Government of Daowai District

Rice false smut(RFS),caused by Ustilaginoidea virens,is widely distributed in major rice-producing *** studies showed that treating RFS with chelerythrine can decrease fungus spore germination by 86.7% and induce fungal cell *** the present study,the effects of chelerythrine on the metabolism of *** were explored using metabolomics,and analysing differentially expressed genes and altered metabolic pathways.A total of 1 153 features(740 in positive ion mode,401 upregulated,339 downregulated;413 in negative ionisation mode,190 upregulated,223 downregulated).The top 15 metabolites in Random Forest analysis were significantly different between *** positive ion mode,purine metabolism(map00230),phenylalanine metabolism(map00360),phenylalanine,tyrosine and tryptophan biosynthesis(map00400),pyrimidine metabolism(map00240) and nitrogen metabolism(map00910) were ***,aspartate and glutamate metabolism(map00250) and phenylalanine metabolism(map00360) were enriched in negative ion *** expressed genes and altered metabolic pathways of *** were effected by *** findings support future research on the prevention and treatment of RFS by chelerythrine,and provide a theoretical basis for targeted drug delivery.

关键词： rice false smut chelerythrine Ustilaginoidea virens metabolomics UPLC-MS/MS

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Chinese Science Bulletin 1989年第14期34卷 1182-1185页

作者：陈元柱徐本杰杨丽丽黄治勋 Fujian Institute of Research on the Structure of Matter Academia Sinica Fuzhou Guangxi Research Center of Natural Materia Medica Nanning

Ⅰ. INTRODUCTION Seven alkaloids were isolated from the roots of Zanthoxylum nitidum by HUANG Zhi-xun et al. The compound C22H21O5N, named 6-methoxy-5, 6-dihydrochelerythrine, was one of the alkaloids. It exhibits medium antitumor *** carry out the X-ray structural analysis of the drug in order to study the relation between the molecular structure and its antitumor activities.

关键词： alkaloids chelerythrine antitumor

应对可转移多黏菌素耐药性--饲料添加剂来源的白屈菜红碱具有双重效应

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Engineering 2024年第1期32卷 163-173页

作者： Huangwei Song Xueyang Wang Muchen Zhang Zhiyu Zou Siyuan Yang Tian Yi Jianfeng Wang Dejun Liu Yingbo Shen Chongshan Dai Zhihai Liu Timothy R.Walsh Jianzhong Shen Congming Wu Yang Wang National Key Laboratory of Veterinary Public Health and Safety College ofVeterinary MedicineChina Agricultural UniversityBeijing 100193China Guangdong Laboratory for Lingnan Modern Agriculture Guangzhou 510642China State Key Laboratory for Zoonotic Diseases Key Laboratory of Zoonosis ResearchMinistry of EducationInstitute of ZoonosisCollege of Veterinary MedicineJilin UniversityChangchun 130015China College of Chemistry and Pharmaceutical Sciences Qingdao Agricultural University.Qingdao 266109China Ineos-Oxford Institute of Antimicrobial Research Department of BiologyUniversity of OxfordOxford OX13SZUK

The emergence and spread of the mobile colistin-resistance gene,mcr-1,and its variants pose achallenge to the use of colistin,a last-resort antibiotic used to treat severe infections caused by extensively drug-resistant(XDR)Gram-negative *** adjuvants are a promising strategy to enhance the efficacy of colistin against colistin-resistant pathogens;however,few studies have considered the effects of adjuvants on limiting resistance-gene *** found that chelerythrine(4 mg·L^(-1))derived from Macleaya cordata extract,which is used as an animal feed additive,reduced the minimal inhibitory concentration(MIC)of colistin against an mcr-1 positive Escherichia coli(***)strain by 16-fold(from 2.000 to 0.125 mg·L^(-1)).eliminated approximately 10^(4) colony-forming units(CFUs)of an mcr-1-carrying strain in a murine intestinal infection model,and inhibited the conjugation of an mcr-1-bearing plasmid in vitro(by>100-fold)and in a mouse model(by up to 5-fold).A detailed analysis revealed that chelery-thrine binds to phospholipids on bacterial membranes and increases cytoplasmic membrane fluidity,thereby impairing respiration,disrupting proton motive force(PMF),generating reactive oxygen species(ROS),and decreasing intracellular adenosine triphosphate(ATP)levels,which subsequently downregu-lates mcr-1 and conjugation-associated *** dual effects of chelerythrine can expand the use of antibiotic adjuvants and may provide a new strategy for circumventing mobile colistin resistance.

关键词： chelerythrine Antibiotic adjuvant Conjugation inhibitor Colistin mcr-1 Dual effects

The Genome of Medicinal Plant Macleaya cordata Provides New Insights into Benzylisoquinoline Alkaloids Metabolism

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Molecular Plant 2017年第7期10卷 975-989页

作者： Xiubin Liu Yisong Liu Peng Huang Yongshuo Ma Zhixing Qing Qi Tang Huifen Cao Pi Cheng Yajie Zheng Zejun Yuan Yuan Zhou Jinfeng Liu Zhaoshan Tang Yixiu Zhuo Yancong Zhang Linlan Yu Jialu Huang Peng Yang Qiong Peng dinbo Zhang Wenkai Jiang Zhonghua Zhang Kui Lin Dae-Kyun Ro Xiaoya Chen Xingyao Xiong Yi Shang Sanwen Huang Jianguo Zeng National and Local Union Engineering Research Center of Veterinary Herbal Medicine Resource and Initiative Hunan Co-Innovation Center for Utilization of Botanical Functional Ingredients Horticulture and Landscape College Veterinary Medicine College Hunan Agricultural University Changsha 410128 China Institute of Vegetables and Flowers Chinese Academy of Agricultural Sciences Key Laboratory of Biology and Genetic Improvement of Horticultural Crops of the Ministry of Agriculture Sino-Dutch Joint Laboratory of Horticultural Genomics Beijing 100081 China Agricuitural Genome Institute at Shenzhen Chinese Academy of Agricultural Sciences Shenzhen 518124 China School of Pharmacy Hunan University of Chinese Medicine Changsha 410208 China MOE Key Laboratory for Biodiversity Science and Ecological Engineering and College of Life Sciences Beijing Normal University Beijing 100875 China Micolta Bioresource Inc. Changsha 410016 China Herbal Extract Engineering Research Center Changsha 410331 China Biotechnology Research Center Hunan Academy of Agricultural Sciences Changsha 410125 China Novogene Bioinformatics Institute Beijing 100083 China Department of Biological Sciences University of Calgary Calgary T2N1N4 Canada National Key Laboratory of Plant Molecular Genetics National Plant Gene Research Center Institute of Plant Physiology and Ecology Shanghai Institutes forBiological Sciences Chinese Academy of Sciences Shanghai 200032 China Plant Science Research Center Shanghai Chenshan Botanical Garden Shanghai 201602 China

The overuse of antibiotics in animal agriculture and medicine has caused a series of potential threats to public health. Macleaya cordata is a medicinal plant species from the Papaveraceae family, providing a safe resource for the manufacture of antimicrobial feed additive for livestock. The active constituents from M. cordata are known to include benzylisoquinoline alkaloids （BIAs） such as sanguinarine （SAN） and chelerythrine （CHE）, but their metabolic pathways have yet to be studied in this non-model plant. The active biosynthesis of SAN and CHE in M. cordata was first examined and confirmed by feeding ^13C-labeled tyrosine. To gain further insights, we de novo sequenced the whole genome of M. cordata, the first to be sequenced from the Papaveraceae family. The M. cordata genome covering 378 Mb encodes 22,328 predicted protein-coding genes with 43.5% being transposable elements. As a member of basal eudicot, M. cordata genome lacks the paleohexaploidy event that occurred in almost all eudicots. From the genomics data, a complete set of 16 metabolic genes for SAN and CHE biosynthesis was retrieved, and 14 of their biochemical activities were validated. These genomics and metabolic data show the conserved BIA metabolic pathways in M. cordata and provide the knowledge foundation for future productions of SAN and CHE by crop improvement or microbial pathway reconstruction.

关键词： Macleaya cordata genome Benzylisoquinoline alkaloids Secondary metabolism Sanguinarine chelerythrine Isotopic labeling

Remifentanil mimics cardioprotective effect of ischemic preconditioning via protein kinase C activation in open chest of rats

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Acta Pharmacologica Sinica 2005年第5期26卷 546-550页

作者： Michael G IRWIN Tak-ming WONG Department of Anesthesiology Department of Physiology the University of Hong Kong Hong Kong China

Aim:To examine whether the protective effect of remifentanil preconditioning（RPC）on postischemic hearts is mediated by protein kinase（PKC）activation incomparison with ischemic preconditioning（IPC）.Methods:Male Sprague-Dawleyrats were anesthetized and their chests were *** experiment was per-formed with chelerythrine（CHE,2mg/kg）,GF109203X（0.05 mg/kg）protein kinaseC（PKC）inhibitors administered before RPC(remifentanil 6μ***-1·min-1×3 cycle)orIPC,*** size（IS）,as a percentage of the area at risk（AAR）,wasdetermined by triphenyltetrazolium ***:In groups subjected to IPCand RPC the IS/AAR were significantly reduced（IS/AAR from 52.7%±5.5% to12.9%±3.4%,P0.05 vs CON）or IPC（CHE+IPC 53.7%±4.3%,GF+IPC54.1%±6.2%,P>0.05 vs CON）.The difference was not significant in any of thehemodynamic parameters between control and treatment groups during ischemiaand ***:Remifentanil confers myocardial protection againstischemic injury through a mechanism that is similar to IPC and involves PKCactivation.

关键词： remifentanil myocardial ischemia preconditioning myocardial reperfusion injury protein kinase C chelerythrine GF109203X

蒺藜皂苷对缺血心肌细胞内核转录因子-κB的作用

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中草药 2008年第6期39卷 889-892页

作者：孙巍李晶莹李红杨世杰吉林大学白求恩医学院药理教研室吉林长春130021

目的研究蒺藜皂苷对培养大鼠乳鼠心肌细胞H2O2损伤时心肌细胞内蛋白激酶C(PKCε)、细胞外信号调节激酶(ERK1/2)及核转录因子-κB(NF-κB)水平的影响。方法利用培养的Wistar大鼠乳鼠心肌细胞,采用H2O2建立心肌细胞损伤模型,应用PKCε抑制... 详细信息

目的研究蒺藜皂苷对培养大鼠乳鼠心肌细胞H2O2损伤时心肌细胞内蛋白激酶C(PKCε)、细胞外信号调节激酶(ERK1/2)及核转录因子-κB(NF-κB)水平的影响。方法利用培养的Wistar大鼠乳鼠心肌细胞,采用H2O2建立心肌细胞损伤模型,应用PKCε抑制剂chelerythrine干预后,观察细胞形态学改变,应用流式细胞仪定性检测细胞凋亡率,Western blotting定量检测各组PKCε、ERK1/2及NF-κB水平。结果蒺藜皂苷明显保护受损心肌细胞,降低细胞凋亡率,并且能够升高PKCε、ERK1/2及NF-κB水平;应用chelerythrine可部分阻断蒺藜皂苷的上述作用。结论蒺藜皂苷对H2O2损伤大鼠心肌细胞具有保护作用,其保护作用机制与PKCε、ERK1/2及NF-κB激活有关。

关键词：蒺藜皂苷 PKCε ERK1/2 核转录因子-kB(NF-kB) chelerythrine