Category: 1081-17-0

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Acetylcholinesterase inhibitors from the aerial parts of Corydalis speciosa.

In a bioassay-guided search for acetylcholinesterase inhibitors from Korean natural resources, four isoquinoline alkaloids, corynoxidine (1), protopine (2), palmatine (3), and berberine (4) have been isolated from the methanolic extract of the aerial parts of Corydalis speciosa. Structures of these compounds were elucidated on the basis of spectroscopic techniques. These compounds inhibited acetylcholinesterase activity in a dose-dependent manner, and the IC50 values of compounds 1-4 were 89.0, 16.1, 5.8, and 3.3 microM, respectively.

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Electric Literature of 1081-17-0, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 1081-17-0, molcular formula is C11H9NO3, introducing its new discovery.

Cholinesterase and prolyl oligopeptidase inhibitory activities of alkaloids from argemone platyceras (Papaveraceae)

Alzheimer’s disease is an age-related, neurodegenerative disorder, characterized by cognitive impairment and restrictions in activities of daily living. This disease is the most common form of dementia with complex multifactorial pathological mechanisms. Many therapeutic approaches have been proposed. Among them, inhibition of acetylcholinesterase, butyrylcholinesterase, and prolyl oligopeptidase can be beneficial targets in the treatment of Alzheimer’s disease. Roots, along with aerial parts of Argemone platyceras, were extracted with ethanol and fractionated on an alumina column using light petrol, chloroform and ethanol. Subsequently, repeated preparative thin-layer chromatography led to the isolation of (+)-laudanosine, protopine, (-)-argemonine, allocryptopine, (-)-platycerine, (-)-munitagine, and (-)-norargemonine belonging to pavine, protopine and benzyltetrahydroisoquinoline structural types. Chemical structures of the isolated alkaloids were elucidated by optical rotation, spectroscopic and spectrometric analysis (NMR, MS), and comparison with literature data. (+)-Laudanosine was isolated from A. platyceras for the first time. Isolated compounds were tested for human blood acetylcholinesterase, human plasma butyrylcholinesterase and recombinant prolyl oligopeptidase inhibitory activity. The alkaloids inhibited the enzymes in a dose-dependent manner. The most active compound (-)-munitagine, a pavine alkaloid, inhibited both acetylcholinesterase and prolyl oligopeptidase with IC50 values of 62.3 ¡À 5.8 muM and 277.0 ¡À 31.3 muM, respectively.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Application In Synthesis of 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione, 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

Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in vitro

A 70% ethanol extract of California poppy (Eschscholzia californica) was able to bind to 5-HT1A and 5-HT7 receptors at 100 mug/mL. The subsequent isolation procedure yielded the known alkaloids californidine (1), escholtzine (2), N-methyllaurotetanine (3), caryachine (4), and O-methylcaryachine (5), along with a new pavine alkaloid, 6S,12S-neocaryachine-7-O-methyl ether N-metho salt (7). The structure of 7 was determined by spectroscopic data interpretation, while the absolute stereochemistry was determined by means of circular dichroism. From the results obtained from the radioligand-binding assay of the pure compounds, including the commercially available protopine (6), it was evident that the activity on the 5-HT1A receptor was at least partly due to the presence of the aporphine alkaloid 3, which showed the highest inhibition of [3H]8-hydroxy-2-(di-N-propylamino)tetralin ([3H]8-OH-DPAT) binding with an EC50 value of 155 nM and a Ki of 85 nM.

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ALKALOIDS FROM THE ROOTS OF Papaver pseudo-orientale (FEDDE) MEDW.

Two new alkaloids, pseudorine (Ia) (quaternary benzyltetrahydroisoquinoline type) and pseudoronine (II) (benzil type), were isolated from the roots of Papaver pseudo-orientale (FEDDE) MEDW.This is a first occurence of this type of alkaloids in Papaveraceae.The main component of the tertiary alkaloid fraction was isothebaine accompanied by smaller amounts of orientalidine, mecambridine, bracteoline, nuciferine, protopine, and allocryptopine.The presence of salutaridine and papaverrubine D was established.Traces of coptisine and palmatine were also found in some samples.Strongly polar portion of the extract was converted to iodides.N-Methylisothebainium iodide (IIIa) (major component), pseudorine iodide (Ia), and corytuberine hydriodide (IV) (significant amounts), a minor alkaloids such as alborine iodide (alkaloid PO-5), pseudoronine (II), and magnoflorine iodide (IIIb) were isolated from this source.Structure of pseudorine was determined by UV, IR, 1H, and 13C NMR spectroscopy and using the correlation with laudanosine and codamine.Proposed structure of pseudoronine is based on the mass spectra comparison.

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Corynoline Isolated from Corydalis bungeana Turcz. Exhibits Anti-Inflammatory Effects via Modulation of Nfr2 and MAPKs

Corydalis bungeana Turcz. is an anti-inflammatory medicinal herb used widely in traditional Chinese medicine for upper respiratory tract infections. It is demonstrated that corynoline is its active anti-inflammatory component. The nuclear factor-erythroid-2-related factor 2 (Nrf2)/antioxidant response element (ARE) pathway and the mitogen-activated protein kinase (MAPK) pathway play important roles in the regulation of inflammation. In this study, we investigated the potential anti-inflammatory mechanism of corynoline through modulation of Nfr2 and MAPKs. Lipopolysaccharide (LPS)-activated RAW264.7 cells were used to explore modulatory role of NO production and the activation of signaling proteins and transcription factors using nitrite assay, Western bloting and qPCR. Treatment with corynoline reduced production of nitric oxide (NO) and the protein and mRNA levels of inducible nitric oxide (iNOS) and cyclooxygenase-2 (COX-2)Treatment also significantly increased the expression of Nrf2, quinone oxidoreductase 1 (NQO1) and hemeoxygenase-1 (HO-1) at the mRNA and protein levels, which demonstrated that corynoline may protect cells from inflammation through the Nrf2/ARE pathway In addition, corynoline suppressed the expression of inflammatory cytokines, such as tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta), at the mRNA and protein levels. Furthermore, molecular data revealed that corynoline inhibited lipopolysaccharide-stimulated phosphorylation of c-jun NH2-terminal kinase (JNK) and p38. Taken together, these results suggest that corynoline reduces the levels of pro-inflammatory mediators, such as iNOS, COX-2, TNF-alpha and IL-1beta, by suppressing extracellular signal-regulated kinase 1/2 (ERK) and p38 phosphorylation in RAW264.7 cells, which is regulated by the Nrf2/ARE pathway. These findings reveal part of the molecular basis for the anti-inflammatory properties of corynoline.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Electric Literature of 1081-17-0. In my other articles, you can also check out more blogs about 1081-17-0

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The alkaloids of Corydalis meifolia

Six tetrahydroprotoberberines, (+)-sinactine, apocavidine, stylopine, (+)- cavidine, cheilanthifoline, and dehydrocavidine; two spirobenzylisoquinolines, yenhusomine and yenhusomidine; one phthalideisoquinoline; corlumine; one benzophenanthridine, dihydrosanguinarine and protopine, have been isolated from the leaves and stems of Corydalis meifolia Wall. Of these alkaloids, dehydrocavidine was a new base. The remaining alkaloids, although known, were isolated for the first time for this plant. (+)-Cavidine, protopine, corlumine, yenhusomine, and dehydrocavidine exhibited spasmolytic activity.

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Pyrroline – Wikipedia,
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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 1081-17-0, name is 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione, introducing its new discovery. Recommanded Product: 1081-17-0

Protopine attenuates inflammation stimulated by carrageenan and LPS via the MAPK/NF-kappaB pathway

We investigated the anti-inflammatory activity of protopine (PTP) and sought to determine its mechanism of action in LPS-stimulated BV2 cells and a carrageenan (CA)-induced mouse model. Treatment with PTP (5, 10, and 20 muM) significantly suppresses the secretion of NO and PGE2 in a concentration-dependent manner without affecting cell viability by downregulating iNOS and COX-2 expression in LPS-induced BV2 cells. PTP also attenuates the production of pro-inflammatory chemokines, such as MCP-1, and cytokines, including TNF-alpha, IL-1beta and IL-6, and augments the expression of the anti-inflammatory cytokine IL-10. In addition, PTP suppresses the nuclear translocation of NF-kappaB by hindering the degradation of IkappaB and downregulating the expression of mitogen-activated protein kinases (MAPKs), including p38, ERK1/2 and JNK protein. Furthermore, PTP treatment significantly suppresses CA-induced paw oedema in mice compared to that seen in untreated mice. Expression of iNOS and COX-2 proteins is also abrogated by PTP (50 mg/kg) treatment in CA-induced mice. PTP treatment also abolishes IkappaB phosphorylation, which hinders the activation of NF-kappaB. Collectively, these results suggest PTP has potential for attenuating CA- and LPS-induced inflammatory symptoms through modulation of MAPKs/NF-kappaB signaling cascades.

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

Related Products of 1081-17-0, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 1081-17-0, molcular formula is C11H9NO3, introducing its new discovery.

ALKALOIDS FROM Papaver rhoeas var. chelidonioides O. KUNTZE, P. confine JORD., AND P. dubium L.

Papaver rhoeas var. chelidonioides O.KUNTZE (diploid, 2n=14) contains rhoeadine (0.027percent) and coptisine (0.004percent) as the dominant alkaloids, the latter being the yellow principle of the latex.As minor constituents were isolated protopine, papaverrubine A, rhoeagenine, (-)-stylopine, an unidentified alkaloid PCH 1 (m.p. 205 deg C), 2-methyl-1,2,3,4-tetrahydro-beta-carboline and (-)-trans-N-methylstylopinium hydroxide.Chromatographic analysis detected isorhoeadine, allocryptopine, cryptopine, papaverrubine C, D and E, scoulerine, isoboldine, berberine, corysamine, magnofloflorine and corytuberine.P. confine JORD. (tetraploid, 2n=28) was found todisplay a very low alkaloid content (0.003percent) and afforded corytuberine and berberine as principal alkaloids, along with minor amounts of protopine, rhoeadine, scoulerine and cryptopine.Chromatography identified isocorydine, corydine, allocryptopine, aporheine, stylopine, sinactine, thebaine, mecambrine, papaverrubines A, E, C and D, coptisine and corysamine.The tertiary alkaloid fraction from ripe capsules of P. dubium L. (hexaploid, 2n=42; 0,24percent of alkaloids) of domestic origin afforded (+)-roemerine (aporheine) as the main constituent (87percent of total bases); mecambrine, protopine, rhoeadine and papaverrubines D and C (traces of A and E) were detected.From strongly polar bases N-methylaporheinium hydroxide (as iodide) was isolated and corytuberine detected.

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Pyrroline – Wikipedia,
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Protopine from Corydalis ternata has anticholinesterase and antiamnesic activities

While screening extracts of natural products in search of anticholinesterase activity, we found that a total methanolic extract of the tuber of Corydalis ternata (Papaveraceae) showed significant inhibitory effects on acetylcholinesterase. Further fractionation of this extract using acetylcholinesterase inhibition as the parameter screened resulted in the isolation and purification of an alkaloid, protopine. Protopine inhibited acetylcholinesterase activity in a dose-dependent manner. The concentration required for 50% inhibition was 50 muM. The anti-acetylcholinesterase activity of protopine was specific, reversible and competitive in manner. Furthermore, when mice were pretreated with protopine, the alkaloid significantly alleviated scopolamine-induced memory impairment. In fact, protopine had an efficacy almost identical to that of velnacrine, a tacrine derivative developed by a major drug manufacturer to treat Alzheimer’s disease, at an identical therapeutic concentration. We suggest, therefore, that protopine has both anti-acetylcholinesterase and antiamnesic properties that may ultimately hold significant therapeutic value in alleviating certain memory impairments observed in dementia.

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Related Products of 1081-17-0, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.1081-17-0, Name is 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione, molecular formula is C11H9NO3. In a article£¬once mentioned of 1081-17-0

Two new isoquinoline alkaloids from the seeds of Nandina domestica

Two new isoquinoline alkaloids, 6 R,6aS-N-nantenine Nbeta-oxide (1), 6S,6aS-N-nantenine Nalpha-oxide (2), along with nine known alkaloids, nantenine (3), oxonantenine (4), protopine (5), nornantenine (6), N-methyl-laurotetanine (7), isocorydine (8), O-methyflavinantine (9), N-methyl-2,3,6-trimethoxymorphinan-dien-7-one Nbeta-oxide (10) and (+)-10-O-methylhernovine Nbeta-oxide (11) were isolated from the seeds of Nandina domestica. Their structures were elucidated by extensive analyses of spectroscopic data (IR, UV, HRESIMS, 1 D and 2 D NMR), ECD calculation and comparison with the related literatures. In addition, the cytotoxicity against A549 cells of these alkaloids was determined by the MTT assay.

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