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Zhang Y.-H.,Suzhou Industrial Park Center for Disease Control and Prevention | Yu L.-G.,Suzhou Industrial Park Center for Disease Control and Prevention | Zhu W.-Z.,Suzhou Industrial Park Center for Disease Control and Prevention | Wang S.-L.,Suzhou Industrial Park Center for Disease Control and Prevention | And 3 more authors.
Asian Pacific Journal of Cancer Prevention | Year: 2014

The objective of the present study was to investigate cloning, expression, and functions of the recombinant protein, Siva1. Siva1 gene was synthesized by RT-PCR from HCT116 cells. Plasmids were cleaved with the restriction endonuclease, BamH1/Sal1 and products were connected to pQE30, which underwent cleavage by BamH1/Sal1. The recombinant plasmid, pQE30-Siva1, was identified after digestion with restriction endonucleases followed by transformation into E. coli M15. Expression of Siva1 was induced by IPTG and identified by SDSPAGE following purification with affinity chromatography. The results showed that size of Siva1 was 12 kDa, consistent with the molecular weight of the His-Siva1 fusion protein. Functional test demonstrated that Siva1 significantly inhibited the invasion and migration of HCT116 cells. It may thus find clinical application for control of cancers. Source

Yang Y.,Beijing Academy of Agriculture and Forestry Sciences | Yang Y.,Beijing Institute of Pharmacology and Toxicology | Lou K.,Beijing Institute of Pharmacology and Toxicology | Lou K.,CSPC Zhongqi Pharmaceutical Technology Co. | And 3 more authors.
Chromatographia | Year: 2011

A method was developed to determine vinpocetine and its metabolite, apovincaminic acid, in beagle plasma by LC-MS-MS. After protein precipitation with methanol, the supernatant of the sample was concentrated and injected into an Agilent Zorbax XDB-C18 column. The sample was separated by a mobile phase consisting of acetonitrile and 0.2% formic acid solution, and the reading was determined on an Agilent 6410 Triple Quad Tandem mass spectrometer in multiple reaction monitoring mode with the following transitions: m/z 351.5 → 280.2/266.3 for vinpocetine, 323.2 → 236.1/280.2 for apovincaminic acid, and 411.2 → 191.1 for the internal standard. The intra- and inter-day variances were less than 15% (RSD%), and average recoveries were higher than 80%. The linearity ranges (LR) between 0.1 and 20.0 ng mL-1 for vinpocetine (r 2 = 0.9980) and between 1.0 and 200.0 ng mL -1 for apovincaminic acid (r 2 = 0.9995) were established. In summary, this method is sensitive, specific, and appropriate for in vivo study of various dosage forms of vinpocetine. © 2011 Springer-Verlag. Source

Yang J.,Chinese Academy of Sciences | Shi Y.,Chinese Academy of Sciences | Li C.,CSPC Zhongqi Pharmaceutical Technology Co. | Gui L.,Chinese Academy of Sciences | And 7 more authors.
Cancer Chemotherapy and Pharmacology | Year: 2014

Purpose: Plm60-s is a pegylated liposomal mitoxantrone formulation, in which mitoxantrone was loaded into small unilamellar vesicles (~60 nm) made from solid lipid membrane. This two-arm, dose-escalating phase I study was designed to determine safety and pharmacokinetics of plm60-s, and to compare with those of conventional mitoxantrone injection (c-MI). Methods: Patients received an intravenous infusion of plm60-s at 6, 10, 12, 14, 16 and 18 mg/m2 every 4 weeks. Three or 6 patients were in each group of dose level. If more than one third patients of a group experienced dose-limiting toxicity, dose climbing will stop. The control group of 3 patients received c-MI at 10 mg/m2 every 28 days. Samples for pharmacokinetic studies were collected. The analysis of the safety and tolerability was done according to the record and laboratory examination, etc. Results: Twenty patients were enrolled. One grade 3 leukocytopenia occurred in plm60-s groups. Plm60-s was safer than c-MI at the same dose of 10 mg/m2. Two complete responses and one partial response occurred in plm60-s group. In plasma, plm60-s exhibited sustained release of the content, resulting in the reduced peak concentrations and enhanced AUC of released MIT. Total mitoxantrone was linearly cleared, and mitoxantrone was predominantly in the liposomal encapsulation form. Repeated administration of plm60-s did not affect the clearance kinetics. Conclusions: At a dose of up to 18 mg/m2, plm60-s could be well tolerated and potential efficacy could be observed. The pharmacokinetic profile of plm60-s was remarkably altered. Further investigations are in progression. © 2014 Springer-Verlag. Source

Wang L.-F.,CSPC Zhongqi Pharmaceutical Technology Co. | Guo W.-M.,CSPC Zhongqi Pharmaceutical Technology Co. | Yang H.-Y.,CSPC Zhongqi Pharmaceutical Technology Co. | Wang B.-L.,CSPC Zhongqi Pharmaceutical Technology Co.
Chinese Journal of New Drugs | Year: 2014

Objective: To establish a method for determination of three methanesulfonates in SIPI5357 mesylate by GC-MS. Methods: The three methanesulfonates were determined by pre-column derivation technology combined with GC-MS. Results: The resolutions of the three methanesulfonates were greater than 2.0. Linear calibration curves were obtained over the range of 2.0~625.0 ng·mL-1 for all the methanesulfonates(r=0.999 9, n=6). The recoveries were all greater than 99.9% with RSDs less than 3.1%. The detection limits were all lower than 0.375 ng·mL-1. Conclusion: The method was proved to be simple, accurate, rapid, and suitable for determination and quality control of SIPI5357 mesylate. Source

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