Jiangsu Zeukov Pharmaceutical SandT. Inc

Nanjing, China

Jiangsu Zeukov Pharmaceutical SandT. Inc

Nanjing, China
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Meng Z.,Jiangsu Zeukov Pharmaceutical S and T Inc. | Meng Z.,Jiangsu Kanion Parmaceutical Co. | Meng Z.,State Key Laboratory of Pharmaceutical New Technology for Chinese Medicine | Ding G.,Jiangsu Zeukov Pharmaceutical S and T Inc. | And 14 more authors.
Zhongguo Zhongyao Zazhi | Year: 2011

Objective: To study on the purification of strictosamide from Nauclea officinalis by macroporous resin to provide reference for production. Method: The best macroporous resin was selected among 10 kinds of resins according to adsorption and desorption of the static adsorption experiments. The adsorption quantity, elution volume of water, concentration and elution volume of alcohol were determined according to the single factor experiment. Result: HPD400 was the best resin, and the best adsorption quantity was 20.23 mg·g -1, the elution volume of water and 30% alcohol was 6 BV, and the elution volume of 70% alcohol was 4 BV. Conclusion: This technology is simple, feasible, and it can provide reference for the industrialized production.

Xie D.,Jiangsu Zeukov Pharmaceutical S. and T. Inc. | Xie D.,State Key Laboratory of Pharmaceutical New Technology for Chinese Medicine | Li Y.,Jiangsu Zeukov Pharmaceutical S. and T. Inc. | Li Y.,State Key Laboratory of Pharmaceutical New Technology for Chinese Medicine | And 13 more authors.
Zhongguo Zhongyao Zazhi | Year: 2011

Objective: To study the chemical constituents of the leaves of Naudea officinalis. Method: The chemical constituents were separated by column chromatography and semi-preparative HPLC techniques, and their structures were determined by spectral analysis. Result: Five compounds were isolated and identified as strictosamide(1), 10-hydroxy strictosamide(2), kaempferol-3-O-rutinoside(3), rutin (4), pumiloside(5). Conclusion: Among these compounds, 2, 3, 4 are isolated from the leaves of Naudea officinalis for the first time.

Zheng H.,Southern Medical University | Liu A.,Southern Medical University | Liu B.,Sun Yat Sen University | Li M.,Jiangsu Zeukov Pharmaceutical S and T Inc. | And 2 more authors.
Cancer Letters | Year: 2010

The purpose of this work is to study mechanisms underlying anti-tumor effects of farnesyltransferase inhibitors (FTIs) in non-small cell lung cancer (NSCLC). We demonstrate that mRNA and protein levels of Ras homologue enriched in brain (Rheb) are highly expressed both in NSCLC tissues and in NSCLC cell lines. Rheb expression levels correlate with phosphorylation of its downstream target S6 and the sensitivity of NSCLC cells to FTIs (R115777 and SCH66336)-induced growth inhibition and apoptosis. FTIs effectively and preferentially inhibited Rheb downstream signaling in NSCLC cells. Moreover, inhibition of Rheb functions by FTIs or dominant-negative Rheb mutants enhance the effects of cisplatin on NSCLC cells. Rheb-CSVL, a FTIs-resistant mutant, reduces the effects of FTIs on NSCLC cells. Our results suggest that Rheb is a critical target for FTIs therapy in NSCLC. © 2010 Elsevier Ireland Ltd.

Li Z.,China Pharmaceutical University | Li Z.,Jiangsu Zeukov Pharmaceutical SandT. Inc | Li Z.,State Key Laboratory of New Technology for Chinese Medicine Pharmaceutical Process | Lin Y.,China Pharmaceutical University | And 14 more authors.
Chemical Biology and Drug Design | Year: 2015

A series of novel derivatives of strictosamide were synthesized and biologically evaluated. Most of the new compounds exhibited improved activities than the parent compound strictosamide. Among them, compounds Ib and If possessed antiviral activities against influenza A virus (A/Jinan/15/90) with IC50 values of 4.12 and 12.35 μg/mL, respectively. Compound Ie possessed antiviral activity against respiratory syncytial virus (RSV) with an IC50 value of 9.58 μg/mL. Both compounds IIc and IId had moderate antiproliferative effects against five human cancer cell lines. The preliminary structure-activity relationships were also concluded. This study provides a promising new template with potential antiviral activity. © 2015 John Wiley & Sons A/S.

Li N.,Jiangsu Zeukov Pharmaceutical S.andT. Inc. | Li N.,Jiangsu Kanion Pharmaceutical Co. | Cao L.,Jiangsu Zeukov Pharmaceutical S.andT. Inc. | Cao L.,Jiangsu Kanion Pharmaceutical Co. | And 11 more authors.
Pharmaceutical Biology | Year: 2014

Context: Strictosamide is the main representative constituent of Nauclea officinalis Pierre ex Pitard (Rubiaceae), which has been used for a long time in China to treat diseases related to infection and inflammation, but its pharmacological activities are not well studied.Objective: This work evaluates the anti-inflammatory and analgesic activities of strictosamide by in vivo experiments.Materials and methods: The anti-inflammatory activity was assessed in mice by models of 12-O-tetradecanoylphorbol-13-Acetate (TPA)-induced ear edema, acetic acid-elevated vascular permeability, and carboxymethylcellulose sodium (CMC-Na)-induced leukocyte migration. The analgesic activity was estimated in mice using acetic acid-induced writhing and hot-plate tests. Compound was injected to mice twice a day for 3d at doses of 10, 20, and 40mg/kg.Results: At 20 and 40mg/kg, strictosamide obviously decreased the TPA-induced mice ear edema (24.7 and 28.1% inhibition, respectively), and significantly inhibited acetic acid-stimulated peritoneal vascular permeability in mice (23.3 and 33.4% inhibition, respectively). It also significantly decreased the leukocytes in the mice peritoneal cavity induced by CMC-Na at all the tested doses (46.0, 49.1, and 58.7% inhibition, respectively). To acetic acid-induced writhing test in mice, strictosamide markedly prolonged the pain latency at 20 and 40mg/kg and decreased the writhing counts at 40mg/kg (49.7% inhibition). However, it did not obviously improve the pain threshold of mice in hot-plate test.Discussion and conclusion: Strictosamide may have important effects on inflammation and inflammatory pain. The results provide scientific support for the role of strictosamide in the use of N. officinalis to treat inflammatory diseases. © 2014 Informa Healthcare USA, Inc. All rights reserved.

Xie D.-W.,Jiangsu Zeukov Pharmaceutical S. and T. Inc. | Li Y.-H.,Jiangsu Zeukov Pharmaceutical S. and T. Inc. | Li Y.-H.,Jiangsu Kanion Pharmaceutical Co. | Li Y.-H.,State Key Laboratory of New Technology for Chinese Medicine | And 12 more authors.
Journal of Food and Drug Analysis | Year: 2012

A simple, rapid and validated method was developed for the simultaneous determination of five characteristic components, including three alkaloids (pumiloside, 10-hydroxy strictosamide, and strictosamide), and two flavonoids (rutin and kaempferol-3-O-rutinoside), in the Nauclea officinalis leaves. The chromatographic separation was achieved with a lichrospher C-18 analytical column by gradient elution with (A) 0.1% aqueous phosphoric acid and (B) acetonitrile as mobile phase, with a flow rate of 1.0 mL/min. The column temperature was set at 30°C. Detection was carried out on a photodiode array detector at 226 nm. The method was validated for system suitability, precision, accuracy and linearity. The average recovery of the method was 98.00-100.44% and linearity (r) was>0.9993. Furthermore, the method was successfully applied to the simultaneous determination of five analytes in 10 samples of N. officinalis leaves from different harvesting time of the herb. The results suggested that the method could be efficiently employed to evaluate the quality of N. officinalis leaves from various sources, which would benefit its quality control.

Dai C.,China Pharmaceutical University | Dai C.,Jiangsu Zeukov Pharmaceutical S. and T. Inc. | Xiao W.,China Pharmaceutical University | Liang Y.,China Pharmaceutical University | And 21 more authors.
Biomedical Chromatography | Year: 2011

A simple, sensitive and specific high-performance liquid chromatography mass spectrometry (LC-MS) method was developed and validated for the quantification of strictosamide in dog plasma. Strictosamide and internal standard (IS, ranolazine) extracted by liquid-liquid extraction with ethyl acetate were separated on a C18 column using a gradient elution program. The detection was performed by selected ion monitoring mode via a positive electrospray ionization interface. The LLOQ was 1.0ng/mL and the method exhibited acceptable precision, extraction efficiency and matrix effect. Finally, this proposed method was successfully applied to dog pharmacokinetic study and yielded the most comprehensive data on systemic exposure of strictosamide to date. © 2011 John Wiley & Sons, Ltd.

Liang Y.,China Pharmaceutical University | Xiao W.,Jiangsu Kanion Pharmaceutical Co. | Dai C.,China Pharmaceutical University | Xie L.,China Pharmaceutical University | And 17 more authors.
Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences | Year: 2011

We report herein, a facile metabolite identification workflow on the antimicrobial strictosamide, which is derived from accurate mass measurement by a hybrid ion trap-TOF mass spectrometer. In step 1, the parent drug and metabolites in rat bile were separated on an HPLC column followed by ion trap-TOF mass spectrometer analysis after a single oral dose of 50. mg/kg strictosamide. In step 2, mass defect filter technique, which enables high-resolution mass spectrometers to be utilized for detecting drug metabolites based on well-defined mass defect ranges, was used to find metabolites in the mass spectrum. In step 3, the differences of accurate masses and their mass fragmentation pattern among the parent drug and metabolites used to assign structures for the metabolites successfully. As a result, five metabolites of strictosamide were found in rat bile, and all the metabolites were reported for the first time. © 2011 Elsevier B.V.

Meng Z.-Q.,Jiangsu Zeukov Pharmaceutical S and T. Inc | Meng Z.-Q.,State Key Laboratory of New Technology for Chinese Medicine Pharmaceutical Process | Meng Z.-Q.,China Pharmaceutical University | Liu W.-J.,Jiangsu Zeukov Pharmaceutical S and T. Inc | And 13 more authors.
Chinese Journal of Natural Medicines | Year: 2013

Aim: To identify the structure of the acid-catalyzed product of strictosamide and explore the reaction mechanism. Methods: The acid-catalyzed reaction process of strictosamide was monitored by HPLC, and a macroporous resin was used to purify the reaction solution. The structure of the product was confirmed by MS, NMR, and ROESY spectra. Results: The acid-catalyzed transformation yield from strictosamide to vincoside lactam was 52%. Conclusion: The reaction mechanism of the transformation from strictosamide to vincoside lactam may be related to the stability of the three-dimensional configuration of the compound. These results offer a new way to obtain vincoside lactam from the widely distributed indole alkaloid strictosamide by acid-catalysis. © 2013 China Pharmaceutical University.

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