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Rapid discovery and identification of multiple absorbed chemical constituents and metabolites in rat cerebrospinal fluid after oral administration of Jitai tablets by a LC-MS based metabolomics approach

An integrative strategy using LC-Q/TOF-MS and LC-QqQ-MS/MS coupled with multi-variate statistical analysis of principal component analysis (PCA) and orthogonal partial least squares discriminant analysis (OPLS-DA) was developed to screen and identify the constituents transported into the rat cerebrospinal fluid (CSF) after oral administration of Jitai tablets (JTTs). CSF samples were pretreated with cold methanol prior to liquid chromatography, and the separation was carried out on a HSS T3 column with a linear gradient elution. Mass spectra were acquired in positive ion mode for analyte identification and targeted MS/MS mode for quantification. In the S-plot of OPLS-DA, twenty-six interested ions were extracted, among which, sixteen absorbed prototype components of JTT and seven metabolites were identified in vivo. Cysteine conjugation, demethylation and glucuronidation were the major metabolic reaction types of the identified constituents. An LC-MS/MS method with targeted multiple-reaction monitoring of scopolamine, tetrahydrocoptisine, tetrahydroberineper, protopine, tetrahydropulmatine and corydaline in rat CSF was developed to validate the identification results. The concentration of the six compounds in rat CSF was in the range of 0.014-1.678 ng mL-1. In conclusion, a LC-MS based metabolomics approach can provide a rapid and sensitive method for characterizing bioactive components of JTT at micro concentration on pathological biopsy, which benefits further pharmacology and mechanism research of JTT.

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Enhancement of gamma-aminobutyric acid receptor binding by protopine-type alkaloids

Protopine, cryptopine and allocryptopine were demonstrated to enhance 3H-gamma-aminobutyric acid (3H-GABA) binding to rat brain synaptic membrane receptors. The above finding might be indicative of benzodiazepine-like activity of these alkaloids.

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Lead finding for acetyl cholinesterase inhibitors from natural origin: Structure activity relationship and scope

Acetylcholinesterase (AChE) inhibitors are considered as promising therapeutic agents for the treatment of several neurological disorders such as Alzheimer’s disease (AD), senile dementia, ataxia and myasthenia gravis. There are only few synthetic medicines with adverse effects, available for treatment of cognitive dysfunction and memory loss associated with these diseases. A variety of plants has been reported to possess AChE inhibitory activity and so may be relevant to the treatment of neurodegenerative disorders such as AD. Hence, developing potential AChE inhibitors from botanicals is the need of the day. This review will cover some of the promising acetylcholinesterase inhibitors isolated from plants with proven in vitro and in vivo activities with concern to their structure activity relationship.

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Applicability of a Monolithic Column for Separation of Isoquinoline Alkalodis from Chelidonium majus Extract

Isoquinoline alkaloids are the main group of secondary metabolites present in Chelidonium majus extracts, and they are still the object of interest of many researchers. Therefore, the development of methods for the investigation and separation of the alkaloids is still an important task. In this work, the application potential of a silica-based monolithic column for the separation of alkaloids was assessed. The influence of the organic modifier, temperature, salt concentration, and pH of the eluent on basic chromatographic parameters such as retention, resolution between neighboring peaks, chromatographic plate numbers, and peak asymmetry were investigated. Based on the obtained results, a gradient elution program was developed and used to separate and quantitatively determine the main alkaloids in a Chelidonium majus root extract.

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1081-17-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1081-17-0, Name is 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione, molecular formula is C11H9NO3. In a Article, authors is Rueffer, M.£¬once mentioned of 1081-17-0

ENZYMATIC FORMATION OF PROTOPINES BY A MICROSOMAL CYTOCHROME P-450 SYSTEM OF CORYDALIS VAGINANS

A microsomal cytochrome P-450-NADPH dependent enzyme which hydroxylates stereo- and regiospecifically carbon atom 14 of (S)-cis-N-methyltetrahydroprotoberberines has been discovered in a number of plant cell cultures originating from species containing protopine alkaloids; the monooxygenase was solubilized, partially purified (100-fold) and characterized.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. 1081-17-0, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 1081-17-0, name is 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione. In an article£¬Which mentioned a new discovery about 1081-17-0

Study on antitumor molecular mechanism of Chelidonium majus based on network pharmacology

Objective Chelidonium majus is applied to tumor therapy with good clinical effect and weak adverse effect. To explain the molecular mechanism of antitumor effect scientifically, the network pharmacology method was used to screen effective parts and major active components of C. majus and to construct the active compounds-targets network. Methods ADME calculation method was used to filtrate the active components of C. majus, and then the targets of the main active ingredients were collected by literature mining and multiple databases, and the targets of the compound were screened using the SysDT model. Besides, the compounds-targets network was constructed by Cytoscape software and network topology analysis was carried out. Biological information annotation databases (DAVID) was used to analyze the molecular function and biological pathway of the action targets. Results Alkaloids were the major active components of C. majus, 21 alkaloid components were screened out by ADME calculation method with 168 related targets, and 60 closely cancer-related pathways. Those pathways were integrated, with which a comprehensive C. majus antitumor pathway was constructed. According to the results of network topology analysis and ingredient correction results, it was speculated that chelerythrine, berberine and sanguinarine were the main active ingredients in C. majus, acting on the targets of PTGS2, SCN5A, F10, NCOA2, CHRM3, AR, TP5, CASP1/3/9, DRD1, MAPT, MAPK1, BLM, etc. Conclusion The antitumor activities of C. majus were mainly by inducing cell apoptosis and inhibiting cell proliferation, metastasis and invasion as phenotype intervention mode in network, thereby to exert antitumor activities and a certain central analgesic effect.

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Effect of isoquinoline alkaloids of different structural types on antiplatelet aggregation in vitro

Forty-one isoquinoline alkaloids were tested for antiplatelet aggregation effects. Among them, (-)-discretamine (6), protopine (7), ochotensimine (18), O-methylarmepavinemethine (23), lindoldhamine (25), isotetrandrine (26), thalicarpine (27), papaverine (28), and D-(+)-N-norarmepavine (32) exhibited significant inhibitory activity towards adenosine 5?-diphosphate (ADP)-, arachidonic acid (AA)-, collagen-, and/or platelet-activating factor (PAF)-induced platelet aggregation. The results are discussed on the basis of structure-activity relationships. Georg Thieme Verlag KG Stuttgart.

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1081-17-0, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, the author is Georgieva, Lidiya and a compound is mentioned, 1081-17-0, 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione, introducing its new discovery.

Protopine Production by Fumaria Cell Suspension Cultures: Effect of Light

Protopine biosynthesis in Fumaria rostellata and Fumaria officinalis cell suspensions was investigated. For the first time, we reported for calli and cell suspensions obtained from F. rostellata and F. officinalis. Callus induction was initiated on a Murashige and Skoog medium, supplemented with sucrose and various concentrations of plant growth regulators: 2,4-dichlorophenoxyacetic acid (2,4-D) and 6-benzylaminopurine (BAP). The best morphological characteristics, growth behavior, and protopine biosynthesis were observed for two callus lines (5FRL14 and 12FOL1) cultivated under submerged conditions, at low concentration of 2,4-D (0.2 and 0.5 mg/L) and higher concentration of BAP (2.0 and 3.0 mg/L). The maximal yield of protopine was accumulated from cell suspension of F. rostellata (line 5FRL14) cultivated under illumination49.6 mg/L. Time courses of utilization of sucrose, ammonium, nitrate, and phosphate ions in cultural liquid and acetylcholinesterase inhibitory activity of alkaloid extracts of studied suspensions are also presented.

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Discovery of 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 1081-17-0 is helpful to your research. 1081-17-0

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. 1081-17-0, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 1081-17-0, name is 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione. In an article£¬Which mentioned a new discovery about 1081-17-0

Protopine protects mice against LPS-Induced acute kidney injury by inhibiting apoptosis and inflammation via the TLR4 signaling pathway

Corydalis humosa Migo is a traditional Chinese medicine that clears away damp heat, relieves sore. Protopine (PRO) is an alkaloid component isolated from C. humosa Migo. However, the role of protopine in acute kidney injury (AKI) has not yet been reported. This study aims to investigate the effect and mechanism of protopine isolated from C. humosa Migo on lipopolysaccharide (LPS)-induced AKI in mice. Inflammation accumulation was assessed by small animal living imaging. The blood urea nitrogen (BUN), and serum creatinine (Scr) were measured to assess the effects of protopine on renal function in LPS-induced AKI. The levels of tumor necrosis factor (TNF), interleukin-2 (IL-2), interferon- (IFN-), and (interleukin-10) IL-10 in serum were detected by cytometric bead array. Flow cytometry was used to detect the levels of reactive oxygen species (ROS) in primary kidney cells. The proportions of granulocytes, neutrophils, and macrophages in peripheral blood were examined to evaluate the effect of protopine on immune cells in mice with AKI. Toll-like receptor (TLR4) and apoptotic signaling pathway were detected byWestern blot analysis. The results showed that protopine markedly improved the renal function, relieve inflammation, reversed inflammatory cytokines, transformed apoptosis markers, and regulated the TLR4 signaling pathway in mice with AKI induced by LPS. The protopine isolated from C. humosa Migo protected mice against LPS-induced AKI by inhibiting apoptosis and inflammation via the TLR4 signaling pathway, thus providing a molecular basis for a novel medical treatment of AKI.

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More research is needed about

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1081-17-0, Name is 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione, molecular formula is C11H9NO3, 1081-17-0. In a Article, authors is Tang, Huaqi£¬once mentioned of 1081-17-0

Xuan Hu Suo San (XHSS) is a traditional Chinese medicine that has been extensively applied in the treatment of osteoarthritis for many years, however, its chemical composition has not yet been elucidated. Thus, a rapid, efficient, and precise method based on ultra high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry was applied in both positive- and negative-ion modes to rapidly separate and identify the main chemical ingredients in XHSS for the first time. Finally, with the optimised separation and detection method, a total of 57 compounds were simultaneously separated within 13?min, among which 14 compounds were confirmed by comparing retention time and MS data with reference standards and others were tentatively identified by comparing with reference literatures. This rapid and sensitive approach is highly useful for the identification and characterisation of chemical constituents, and provides fundamental and extensive information supporting further metabolic and pharmacokinetic studies of XHSS.

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