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Sun J.,Peking Union Medical College | Wu Y.-Z.,Nanjing Medical University | Wang S.,Xian Institute for Food and Drug Control | Wang J.,Peking Union Medical College | And 2 more authors.
Chinese Traditional and Herbal Drugs | Year: 2013

Objective: To study the dissolving yield and ratio fluctuation of Sparganii Rhizoma effective composition groups, including total flavonoids, total alkaloid, and active Al3+, when processed with different vinegar processing technologies. Methods: L9(34) orthogonal test design was used with acetic acid content (A), vinegar ratio (B), soaking time (C), and frying temperature (D) as influencing factors. The differences of dissolving yield and ratio of 80% methanol extract, total flavonoids, total alkaloid, and active Al3+ of processed Sparganii Rhizoma under different vinegar processing technologies were compared. Results: Compared with crude Sparganii Rhizoma, the processed products with a little acetic acid had enhanced the dissolving yield of 80% methanol extract. Moreover, the processed Sparganii Rhizoma with vinegar had effectively enhanced the dissolving yield and ratio of total flavonoids, total alkaloid, and active Al3+. The dissolving yield and ratio of total flavonoids were greatly impacted by frying temperature. Meanwhile, the alkaloid dissolving yield and ratio were most influenced by acetic acid content. The products processed with abundant acetic acid had obviously reduced the dissolving yield of 80% methanol extract, but had increased the alkaloid and active Al3+ dissolving ratio in the extract. Conclusion: The processed Sparganii Rhizoma with vinegar could obviously affect the dissolving yield and ratio of different pharmacodynamic compositions in Sparganii Rhizoma. Suitable processed products should be adopted when Sparganii Rhizoma is used in the different treatments.


Du H.,Xi'an Jiaotong University | Du H.,Xian Institute for Food and Drug Control | Lv N.,Xi'an Jiaotong University | Wang S.,Xi'an Jiaotong University | He L.,Xi'an Jiaotong University
Combinatorial Chemistry and High Throughput Screening | Year: 2013

A new high-expression endothelial growth factor receptor (EGFR) cell membrane chromatography (CMC) method was applied to recognize the ligands acting on EGFR specifically, and investigate the affinity of gefitinib/HMQ1611 to EGFR. In the self and direct competitive assay, gefitinib/HMQ1611 was used as a competitor in the mobile phase to evaluate the effect of the competitor's concentrations on the retention of the ligands, respectively, and the competition between gefitinib and HMQ1611 binding to EGFR was also been examined. The retention behavior indicated that gefitinib had one type of binding sites on the EGFR, and the equilibrium dissociation constant (K D) was (9.11 ± 1.89) × 10-6 M; HMQ1611 had two major binding regions on the EGFR, and the KD values obtained from the model were (2.39 ± 0.33) × 10-7 and (3.87 ± 0.93) × 10-5 M for HMQ1611 at the high- and low-affinity sites, respectively. The competition between gefitinib and HMQ1611 occurred at the low-affinity sites on the EGFR. The low-affinity sites were of higher concentrations and contributed to a much larger part of retention of HMQ1611. The results suggested that gefitinib and HMQ1611 competed for the common binding sites on the EGFR, no matter the ligand was used as an analyte or a competitor. © 2013 Bentham Science Publishers.


Chen D.-M.,Xian Institute for Food and Drug Control | Chen D.-M.,Xi'an Jiaotong University | Fu Q.,Xian Institute for Food and Drug Control | Du W.,Xian Institute for Food and Drug Control | And 3 more authors.
Journal of Pharmaceutical Analysis | Year: 2011

An S-naproxen (S-NAP) molecularly imprinted monolithic stationary phase (MIMSP) with specific recognition for S-NAP and naproxen (NAP) was prepared by in situ technique, utilizing 4-vinylpridine (4-VP) as a function monomer, ethylene glycol dimethacrylate (EDMA) as a cross-linking agent, and low-polar solvents (toluene and dodecanol) as porogenic solvents. The selectivity of the polymers for S-NAP and NAP was evaluated by high performance liquid chromatography (HPLC). The binding characteristics were tested by Scatchard analysis. Racemic NAP could be specifically separated to some extent. At the same time, NAP could be separated from ibuprofen under optimized conditions. Scatchard analysis showed that two classes of binding sites existed in the S-NAP-imprinted polymers, with their dissociation constants estimated to be 1.045 and 5.496 μM, respectively. The results demonstrate that S-NAP and NAP can be recognized specifically on the obtained MIMSP.


Wang H.,Nanjing Agricultural University | Shu R.,Xian Institute for Food and Drug Control | Zhao Y.,Nanjing Agricultural University | Zhang Q.,Nanjing Agricultural University | And 2 more authors.
European Food Research and Technology | Year: 2014

The chicken slaughter line is a source of cross-contamination of Salmonella. In this study, ERIC-PCR was applied to analyse the ERIC-PCR genomic polymorphism of Salmonella isolates from a commercial chicken slaughter line and to trace the route of contamination. Samples were collected from carcasses and contact surfaces at the points of post-evisceration, post-chilling and post-grading. The prevalence of Salmonella at the evisceration point was high but significantly decreased along the slaughter line. The ERIC-PCR fingerprints indicated that a total of seven groups were clustered, and the genotypic diversity of isolates progressively decreased along the slaughter line. By tracing the genotypic diversity, contact surfaces at post-evisceration were found to be the major contamination sources of Salmonella during chicken processing, since the genotype diversity of isolates from the post-evisceration point could be exactly matched to that from the post-chilling and post-grading points. Interestingly, three Salmonella strains were still detected after decontamination and washing; these three isolates having a strong capacity for attachment were able to produce biofilm on polystyrene surfaces. This study suggests that the evisceration point is the source of cross-contamination, with Salmonella isolates still present after washing procedure. Therefore, more effective measures must be undertaken to control the spread of Salmonella in such processing lines. © 2014 Springer-Verlag Berlin Heidelberg.


Liu Q.-C.,Northwest University, China | Guo T.-T.,Xian Institute for Food and Drug Control | Zhao C.,Northwest University, China | Sun J.,Northwest University, China | Li W.-H.,Northwest University, China
Helvetica Chimica Acta | Year: 2014

Chemical synthesis of a trisaccharide related to the cytotoxic triterpenoid saponins isolated from the bark of Albizia procera has been accomplished through a concise stepwise glycosylation strategy starting from commercially available D-xylose, 2-acetamido-2-deoxy-D-glucose and L-arabinose. The target trisaccharide was designed with a 4-methoxyphenyl (MP) aglycone to extend the scope of conversion to suitable glycoconjugates via selective removal of 4-methoxyphenyl (MP) group. An unexpected phenomenon, i.e., the arabinosyl residue assumed the 1C4 conformation instead of the typical 4C1 form, was observed. Deprotection could restore the normal conformation. Copyright © 2014 Verlag Helvetica Chimica Acta AG, Zürich.


Hou B.,Northwest University, China | Ai Y.,Northwest University, China | Ai Y.,Xian Institute for Food and Drug Control | Wang C.,Northwest University, China | And 4 more authors.
Chinese Journal of Organic Chemistry | Year: 2016

The isatin derivatives 4a~4f were prepared and underwent oxidative hydrolysis to give the anthranilic acid 5a~5d. A and/or D-ring substituted tryptanthrins were designed and synthesized from 4a~4f to 5a~5d. Then C-ring Schiff bases of tryptanthrin were synthesized by condensation of 6-carbonyl with hydrazine and hydroxylamine hydrochloride. Finally, the B-ring was replaced with piperazine to give 11H-indeno[1,2-b]quinoxalin-11-one. 20 compounds were synthesized and their structures were confirmed by 1H NMR, IR and elemental analysis. To best of our knowledge, 13 of them were unknown in the literature. The antitumor activities of synthesized compounds were evaluated against A549 cell line in vitro. The preliminary results indicated that 1b, 1c, 1i, 1j, 1p and 1q showed good antitumor activity with the IC50 of 3.58, 0.99, 1.03, 2.10, 0.51 and 0.43 μmol·L-1, respectively. Structure-activity relationship showed that halogen substitution located in the D-ring enhanced the anti-tumor activity, while the same substitution located in the A ring reduced the activity. The anti-tumor activity disappeared when B-ring was replaced by piperazine, while there was no significant difference for tryptanthrin and its C-ring Schiff base. © 2016 Chinese Chemical Society & SIOC, CAS.


Du H.,Xian Institute for Food and Drug Control | Zhou N.,Xian Institute for Food and Drug Control | Li J.,Xian Institute for Food and Drug Control | Fan F.,Xian Institute for Food and Drug Control
Chinese Journal of Chromatography (Se Pu) | Year: 2015

A rat striatum cell membrane chromatography (CMC) frontal analysis method was developed for the determination of the equilibrium dissociation constants ( KD ) for 5- hydroxytryptamine (5-HT) receptor 5-HT1D -ligustilide interactions. Rat striatum was used for preparation of the cell membrane stationary phase (CMSP). An enzyme-linked immunosorbent assay (ELISA) was applied to determine the 5-HT level of CMSP before and after the adsorption of cell membrane, and the value was (40.5±2.3) pg per gram of silica. The CMC-offline-HPLC system was applied to specifically recognize the mixed standard solution of sumatriptan and ligustilide. Sumatriptan, a 5-HT1D agonist of 24.2 to 242 nmol/L, was pumped through a CMC column continuously, and the breakthrough curves were recorded. For further competitive studies, the mobile phase that contained ligustilide (37.0-370 nmol/L) was pumped through the column to saturate the binding sites. Afterwards, sumatriptan was propelled towards the column. The breakthrough curves were recorded and compared with those obtained from the column without saturation. KD values obtained using frontal analysis were 389 nmol/L and 4.21 μmol/L for sumatriptan and ligustilide, respectively. The competitive binding study indicated that the CMC method could be a quick and efficient way for determining the KD values in drugreceptor interactions.


Zhang Y.-F.,Xian Institute for Food and Drug Control | Shu R.-H.,Xian Institute for Food and Drug Control | Wang Y.-T.,Xian Institute for Food and Drug Control | Li Z.,Xian Institute for Food and Drug Control
Chinese Traditional and Herbal Drugs | Year: 2014

Objective: To establish an HPLC-MS/MS method for determination of allantoin in Dioscoreae Rhizoma. Methods: Determination of LC system used Agilent Eclipse Plus C18 (100 mm × 4.6 mm, 3.5 μm) column and acetonitrile-water (90:10) as mobile phase in linear gradient condition. The flow rate was 0.3 mL/min. The mass spectrometer was operated under the negative ion mode with ESI source. MRM (precursor ion of m/z 156.9 and product ion of m/z 96.7) was used to qualify allantoin. Results: The linear range of the component was 0.12-6.0 μg/mL, r=0.998 5; The average recovery was 101%, and the RSD was 3.2%. Conclusion: The method is sensitive, reliable, and accurate, and can be applied in the quality control of Dioscoreae Rhizoma. ©, 2014, Editorial Office of Chinese Traditional and Herbal Drugs. All right reserved.

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