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Zhi K.,Lanzhou University of Technology | Yang Z.,Lanzhou University of Technology | Sheng J.,Lanzhou University of Technology | Shu Z.,Lanzhou University of Technology | And 3 more authors.
Iranian Journal of Pharmaceutical Research | Year: 2016

To develop a new more accurate spectrophotometric method for detecting monoamine oxidase inhibitors from plant extracts, a series of amine substrates were selected and their ability to be oxidized by monoamine oxidase was evaluated by the HPLC method and a new substrate was used to develop a peroxidase-linked spectrophotometric assay. 4-(Trifluoromethyl) benzylamine (11) was proved to be an excellent substrate for peroxidase-linked spectrophotometric assay. Therefore, a new peroxidase-linked spectrophotometric assay was set up. The principle of the method is that the MAO converts 11 into aldehyde, ammonia and hydrogen peroxide. In the presence of peroxidase, the hydrogen peroxide will oxidize 4-aminoantipyrine into oxidised 4-aminoantipyrine which can condense with vanillic acid to give a red quinoneimine dye. The production of the quinoneimine dye was detected at 490 nm by a microplate reader. The ⊿OD value between the blank group and blank negative control group in this new method is twice as much as that in Holt’s method, which enables the procedure to be more accurate and avoids the produce of false positive results. The new method will be helpful for researchers to screening monoamine oxidase inhibitors from deep-color plant extracts. © 2016 by School of Pharmacy Shaheed Beheshti University of Medical Sciences and Health Services. Source


Jin G.,Lanzhou University of Technology | Yang Z.,Lanzhou University of Technology | Xue W.,Lanzhou University | Sheng J.,Lanzhou University of Technology | And 4 more authors.
Chinese Journal of Chemistry | Year: 2013

New isoconessimine derivatives were synthesized from conessine (1) and evaluated as acetylcholinesterase (AChE) inhibitors. The derivatives were prepared via two reaction steps, N-demethylation and nucleophilic substitution. All of the synthesized derivatives exhibited more potential anti- acetylcholinesterase activities than conessine (1) (IC50=16 μmol·L-1) and isoconessimine (2) (IC50>300 μmol·L-1). Compound 7b (3β-[methyl-[2-(4-nitrophenoxy) ethyl]amino]con-5-enine) showed the most potent inhibitory activity with an IC50 of 110 nmol/L which is close to that of reference compound huperzine A (IC50=70 nmol/L). The mode of AChE inhibition by 7b was reversible and non-competitive. In addition, molecular modeling was performed to explore the binding mode of inhibitor 7b at the active site of AChE and the results showed that 7b could be docked into the acetylcholinesterase active site and compound 7b had hydrophobic interactions with Trp279 and Leu282. A series of 3-N-aryloxyethyl substitutional isoconessimine derivatives were synthesized and evaluated as acetylcholinesterase (AChE) inhibitors. All of the synthesized derivatives exhibited potential anti-acetylcholinesterase activities with IC50 values at micromolar to sub-micromolar range. 7b showed the most potent inhibitory activity with an IC50of 110 nmol/L. The molecular docking results showed that 7b can be well docked into the active site of acetylcholinesterase. Copyright © 2013 SIOC, CAS, Shanghai & WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. Source


Shang R.,Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS | Shang R.,Key Laboratory of Veterinary Pharmaceutical Development | Yi Y.,Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS | Yi Y.,Key Laboratory of Veterinary Pharmaceutical Development | And 2 more authors.
Zeitschrift fur Kristallographie - New Crystal Structures | Year: 2016

C34H49NO6S, monoclinic, P21 (no. 4), a = 11.7112(8) Å, b = 10.0135(5) Å, c = 14.6411(10) Å, V = 1664.4 Å3, Z = 2, Rgt(F) = 0.0659, wRref(F2) = 0.1269, T = 293 K. © 2016 Ruofeng Shang et al., published by De Gruyter. Source


Li B.,Key Laboratory of Veterinary Pharmaceutical Development | Li B.,Key Laboratory of New Animal Drug Project of Gansu Province | Li B.,Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS | Zhang J.,Fulin Animal Science and Veterinary Medicine Officer | And 24 more authors.
Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences | Year: 2015

A rapid and sensitive high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated to simultaneous quantify artesunate and its metabolite in sheep plasma. The plasma samples were prepared by liquid-liquid extraction. Chromatographic separation was achieved on a C18 column (250×4.6mm, 5μm) using methanol: water (60:40, v/v) (the water included 1mM ammonium acetate, 0.1% formic acid, and 0.02% acetic acid) as the mobile phase. Mass detection was carried out using positive electrospray ionization in multiple reaction monitoring mode. The calibration curve was linear from 1ng/mL to 400ng/mL (r2=0.9992 for artesunate, r2=0.9993 for its metabolite). The intra- and inter-day accuracy and precision were within the acceptable limits of ±10% at all concentrations for both artesunate and its metabolite. The recoveries ranged from 92% to 98% at the three concentrations for both. In summary, the LC-MS/MS metho described herein was fully successfully applied to pharmacokinetic studies of artesunate nanoemulsion after intramuscular delivery to sheep. © 2015. Source


Li B.,Key Laboratory of Veterinary Pharmaceutical Development | Li B.,Key Laboratory of New Animal Drug Project of Gansu Province | Li B.,Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS | Zhou X.-Z.,Key Laboratory of Veterinary Pharmaceutical Development | And 23 more authors.
Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences | Year: 2014

A rapid and sensitive high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the determination of arecoline concentration in dog plasma. Plasma sample was prepared by protein precipitation using n-hexane (containing 1% isoamyl alcohol) with β-pinene as an internal standard. Chromatographic separation was achieved on an Agilent C18 column (4.6 × 75. mm, 3.5. μm) using methanol: 5. mM ammonium acetate as the mobile phase with isocratic elution. Mass detection was carried out using positive electrospray ionization in multiple reaction monitoring mode. The calibration curve for arecoline was linear over a concentration range of 2-500. ng/mL. The intra-day and inter-day accuracy and precision were within the acceptable limits of ±10% at all concentrations. In summary, the LC-MS/MS method described herein was fully validated and successfully applied to the pharmacokinetic study of arecoline hydrobromide tablets in dogs after oral administration. © 2014. Source

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