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Simultaneous determination of fifteen constituents of Jitai tablet using ultra high-performance liquid chromatography coupled with triple quadrupole electrospray tandem mass spectrometry

An ultra-high-performance liquid chromatography-electrospray ionization tandem mass spectrometry (UHPLC-ESI-MS/MS) method was developed for simultaneous determination of fifteen constituents in Jitai tablet (JTT), a complex Traditional Chinese Medicine prescription (TCMP) used in treating opiate addiction. Benefitting from a small particle size (1.8 mum) C18 column, accelerated analysis with satisfactory resolution, sensitivity and selectivity were achieved in a single run within 7 min with linear gradient elution of acetonitrile-0.1% (v/v) formic acid in water. The analytical signal was obtained by multiple reaction monitoring transitions via electrospray ionization source operating in both positive and negative ionization mode. The approach was validated for linearity, sensitivity, precision, repeatability, stability and recovery. All analytes showed good linearity over a wide concentration range (r > 0.99). The method limits ranged from 0.03 ng/mL to 19.35 ng/mL which are sensitive enough for quality control studies. The developed method was successfully applied to the simultaneous determination of fifteen constituents in JTT. In conclusion, our experimental results demonstrate that UHPLC-ESIMS/MS is a useful approach for the overall quality assessment of complex TCMPs.

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Alkaloids induce programmed cell death in bloodstream forms of trypanosomes (Trypanosoma b. brucei)

The potential induction of a programmed cell death (PCD) in Trypanosoma b. brucei by 55 alkaloids of the quinoline, quinolizidine, isoquinoline, indole, terpene, tropane, steroid, and piperidine type was studied by measuring DNA fragmentation and changes in mitochondrial membrane potential. For comparison, the induction of apoptosis by the same alkaloids in human leukemia cells (Jurkat APO-S) was tested. Several alkaloids of the isoquinoline, quinoline, indole and steroidal type (berberine, chelerythrine, emetine, sanguinarine, quinine, ajmalicine, ergotamine, harmine, vinblastine, vincristine, colchicine, chaconine, demissidine and veratridine) induced programmed cell death, whereas quinolizidine, tropane, terpene and piperidine alkaloids were mostly inactive. Effective PCD induction (EC50 below 10 muM) was caused in T. brucei by chelerythrine, emetine, sanguinarine, and chaconine. The active alkaloids can be characterized by their general property to inhibit protein biosynthesis, to intercalate DNA, to disturb membrane fluidity or to inhibit microtubule formation.

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STEM ALKALOIDS OF FUMARIA INDICA

Narlumicine, a seco-phthalide isoquinoline alkaloid, has been isolated from the stems of Fumaria indica together with protopine, protopine nitrate, DL-tetrahydrocoptisine and narlumidine.Its structure has been established by spectroscopic methods.Key Word Index – Fumaria indica; Fumariaceae; stem; alkaloids; protopine; DL-tetrahydrocoptisine; narlumidine; protopine nitrate; narlumicine.

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Alkaloids with acetylcholinesterase inhibitory activity from Corydalis racemosa (Thunb.) Pers

Two new isoquinoline alkaloids (1 and 2) along with fourteen known alkaloids (3?16) were isolated from Corydalis racemosa (Thunb.) Pers. Their structures were elucidated by analyzing spectroscopic and spectrometric data (NMR, UV, IR, and MS) and comparing their spectroscopic, spectrometric and physicochemical data with the values archived in the literature. The absolute configurations of new compounds were determined via X-ray crystallographic assay and electronic circular dichroism calculations. Acetylcholinesterase (AChE) inhibitory activity of all compounds was evaluated. Compounds 5, 6, 9, 11, and 12 exhibited inhibitory activity against AChE with IC50 values ranged from 10.2 to 63.4 muM.

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Effects of protopine on proliferation of cultured rabbit aortic vascular smooth muscle cells

AIM To study the effect of protopine (Pro) on proliferation of cultured rabbit aortic vascular smooth muscle cells (VSMC) induced by endothelin-1(ET) or without ET. METHODS The method of celluar culture, the number of VSMC, [3H]-TdR incorporation into DNA assay, MTT method and electronic microscopy were performed for the effect of Pro on proliferation of cultured rat vascular smooth muscle cell. RESULTS It was observed that exposure of VSMC to ET could markedly stimulate the proliferation of VSMC and increased respectively in MTT OD values and the DNA synthesis of VSMC. The concentration 1 mumol¡¤L-1, 10 mumol¡¤L-1, 100 mumol¡¤L-1 of Pro significantly decreased the number of VSMC, the absorbance (A) of MTT and [3H]-TdR incorporation induced by ET-1 (P < 0.01 or P < 0.05). While the proliferation of normal VSMC was decreased only by the concentration 10 mumol¡¤L-1, 100 mumol¡¤L-1 of Pro, and the inhibition rate is lower than ET group's. Furthermore, Pro could antagonize morphological changes of VSMC. CONCLUSION Pro has an effective inhibition on VSMC proliferation induced by ET-1 or without ET-1, and the inhibition rate increased by Pro concentration rising and time passing by. Furthermore, the inhibition of Pro to the proliferation of VSMC is more significantly induced by ET than treated without ET. This suggests that Pro could be of interest to prevent and cure arteriosclerosis clinically. Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Product Details of 1081-17-0, you can also check out more blogs about1081-17-0

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QUATERNARY ALKALOIDS FROM Glaucium oxylobum BOISS. et BUSHE

From the fraction of quaternary alkaloids of the aerial part of Glaucium oxylobum BOISS. et BUHSE (-)-trans-N-methylcanadinium iodide was isolated as the main alkaloid after conversion to iodides, and, in a smaller amount, (+)-N-methylcorydinium iodide, detected for the first time in Papaveraceae, further (-)-trans-N-methylstylopinium iodide, magnoflorine iodide and a new quaternary alkaloid, N-methyldomesticinium iodide, isolated for the first time as a natural substance.In the roots, magnoflorine iodide accompanied by (+)-N-methylcorydinium iodide represented the main component of the quaternary fraction.From both plant parts corytuberine was also isolated for the first time.In the tertiary fraction of alkaloids (+)-corydine, protopine and allocryptopine were the major components, accompanied by smaller amounts of sanguinarine, chelerythrine, chelirubine, domesticine, isoboldine and scoulerine.In the fraction of quaternary protoberberines coptisine, berberine and traces of corysamine were detected.

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Danshen extract (Salvia miltiorrhiza Bunge) attenuate spinal cord injury in a rat model: A metabolomic approach for the mechanism study

Backgroud: Spinal cord injury (SCI) is a devastating neurological disorder caused by trauma. To date, SCI treatment is still a significant challenge in clinic and research around the world. Danshen (dried roots and rhizomes of Salvia miltiorrhiza), a commonly used Chinese medicinal herb, has been attracting attention in SCI treatment. Purpose: Aim of this study was to evaluate the potential beneficial effects of danshen extract in a SCI rat model, as well as investigate possible mechanism of action and potential biomarkers. Methods: Here, a rat SCI model was established with weight-drop method, and danshen extract was administered by oral gavage (12.5 g/kg). Recovery of motor function and histomorphological changes were evaluated by Basso, Beattie and Bresnahan score and hematoxylin-eosin staining, respectively. In addition, neurofilament 200 (NF-H), brain-derived neurotrophic factor (BDNF), glial fibrillary acidic protein (GFAP) and CD11b expressions were assayed by immunofluorescence and western blot analysis. Furthermore, a metabolomics analysis based on ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) approach was conducted. Results: The results demonstrated that danshen extract could significantly ameliorated histopathology changes and improved recovery of motor function after SCI. Moreover, NF-H, BDNF and CD11b expression were progressively increased until 4 weeks post-injury after administrated danshen extract. Furthermore, a good separation was observed among different groups using OPLS-DA. Trajectory analysis showed the gradual shift from position of model group toward normal group with increasing time after administration of danshen extract. Meanwhile, 51 significantly altered metabolites were identified, while metabolic pathway analysis suggested that 6 metabolic pathways were disturbed by the altered metabolites. Conclusion: In summary, this study provides an overview of neuroprotective effects and investigates possible mechanism of danshen extract in SCI treatment. However, further research is needed to uncover its regulatory mechanisms more clearly.

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Validated liquid chromatography-tandem mass spectrometry method for quantitative determination of dauricine in human plasma and its application to pharmacokinetic study

A highly sensitive and selective LC-MS/MS method was developed and validated for the determination of dauricine in human plasma, using protopine as internal standard (IS). The analyte and IS were extracted by liquid-liquid extraction and analyzed by LC-MS/MS. Chromatographic separation was performed on Agilent TC-C18 column with a mobile phase of methanol-water-glacial acetic acid (60:40:0.8, v/v/v) at a flow rate of 0.7 mL/min. Detection was performed on a triple quadrupole tandem mass spectrum by multiple reaction monitoring (MRM) mode using the electrospray ionization technique in positive mode. The method was linear over the concentration range of 1-200 ng/mL. The lower limit of quantification (LLOQ) was 1 ng/mL in human plasma with acceptable precision and accuracy. The intra- and inter-day precision was less than 5.9% determined from quality control (QC) samples at concentrations of 2.0, 20.0 and 160 ng/mL, and the accuracy was within ¡À9.9%. This method was successfully applied for the evaluation of pharmacokinetics of dauricine after oral doses of 100, 300 and 600 mg phenolic alkaloids of menispermum dauricum tablet (PAMDT) to 12 Chinese healthy volunteers.

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The Effect of isoquinoline alkaloids on opiate withdrawal

Our interest has been centered on isoquinoline alkaloids obtained from Argemone mexicana (Papaveraceae), Aristolochia constricta (Aristolochiaceae) and the opium alkaloid, papaverine. In this respect, the effect of these isoquinoline alkaloids was investigated on contractions induced by naloxone of isolated guinea pig ileum acutely exposed to morphine in vitro. The activity of these alkaloids was compared to the control compound, papaverine. Furthermore, the effect of these isoquinoline alkaloids was also determined on naloxone-precipitated withdrawal in isolated guinea pig ileum exposed to DAMGO (highly selective mu opioid receptor agonist) and U50-488H (highly selective kappa opioid receptor agonist) to test whether the possible interaction of isoquinoline alkaloids on opioid withdrawal involves mu- and/or kappa-opioid receptors. Isoquinoline alkaloids from A. mexicana (from 5¡Á10-6 to 1¡Á10-4 M), from A. constricta (1¡Á10-5-5¡Á10-5-1¡Á 10-4 M) as well as papaverine treatment (1¡Á10-7-5¡Á10-6-1¡Á10-6 M) before or after the opioid agonists were able of both preventing and reversing the naloxone-induced contraction after exposure to mu(morphine and DAMGO) or kappa (U50-488H) opiate receptor agonists in a concentration-dependent manner. Both acetylcholine response and electrical stimulation were also reduced by isoquinoline alkaloids and papaverine treatment as well as the final opiate withdrawal was still reduced. The results of the present study i ndicate that isoquinoline alkaloids as well as papaverine were able to produce significant influence on the opiate withdrawal in vitro and these compounds were able to exert their effects both at muand kappa opioid agonists.

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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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