Beijing Haiyan Pharmaceutical Co.

Beijing, China

Beijing Haiyan Pharmaceutical Co.

Beijing, China
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Hou P.,Beijing University of Chinese Medicine | Hou P.,Beijing Haiyan Pharmaceutical Co. | Ni J.,Beijing University of Chinese Medicine | Cao S.,Beijing University of Chinese Medicine | And 5 more authors.
AAPS PharmSciTech | Year: 2013

Ensuring sufficient drug solubility is a crucial problem in pharmaceutical-related research. For water-insoluble drugs, various formulation approaches are employed to enhance the solubility and bioavailability of lead compounds. The goal of this study was to enhance the dissolution and absorption of a new antitumor lead compound, T-OA. Early-stage preparation discovery concept was employed in this study. Based on this concept, a solid dispersion system was chosen as the method of improving drug solubility and bioavailability. Solid dispersions of T-OA in polyvinylpyrrolidone (PVP) K30 were prepared by the solvent evaporation method. Dissolution testing determined that the ideal drug-to-PVP ratio was 1:5. X-ray diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry were employed to confirm the formation of solid dispersions. Scanning electron microscopy demonstrated that T-OA was converted into an amorphous form. Both in vitro dissolution testing and the in vivo studies demonstrated that the solubility and bioavailability of T-OA were significantly improved when formulated in a solid dispersion with PVP. The dissolution rate of the T-OA/PVP solid dispersion was greatly enhanced relative to the pure drug, and the relative bioavailability of T-OA solid dispersions was found to be 392.0%, which is 4-fold higher than the pure drug. © 2013 American Association of Pharmaceutical Scientists.


Liu D.,Chinese Institute of Basic Medical Sciences | Yang Z.,Chinese Institute of Basic Medical Sciences | Wang T.,307 Hospital of Peoples Liberation Army | Yang Z.,Beijing Haiyan Pharmaceutical Co. | And 10 more authors.
Oncogene | Year: 2016

Currently, trastuzumab resistance is a major clinical problem in the treatment of Her2-overexpressing breast cancer. The underlying molecular mechanisms are not fully understood. Our previous study demonstrates that β2-adrenergic receptor (β2-AR) and Her2 comprise a positive feedback loop in human breast cancer cells and that crosstalk between Her2 and β2-AR affects the bio-behaviors of breast cancer cells, suggesting that the β2-AR activation may be involved in trastuzumab resistance. In this study, we show that the expression of β2-AR, which mediates most catecholamine-induced effects, negatively correlates with trastuzumab response in the patients with Her2-overexpressing breast cancer. Catecholamines potently antagonize the anti-proliferative effects of trastuzumab both in vitro and in vivo. Catecholamine stimulation upregulates the expression of miR-21 and MUC-1 by activating Her2 and STAT3, leading to deficiency of phosphatase and tensin homolog and activation of phosphatidylinositol-3-kinase (PI3K) and Akt. Through inhibition of miR-199a/b-3p, catecholamines induce the mammalian target of rapamycin (mTOR) activation. Thus, trastuzumab resistance-dependent PI3K/Akt/mTOR pathway is controlled by catecholamine-induced β2-AR activation. The data indicate that β2-AR is a reliable molecular marker for prediction of response probability to trastuzumab-based therapy in breast cancer. We also demonstrate that β-blocker propranolol not only enhances the antitumor activities of trastuzumab but also re-sensitizes the resistant cells to trastuzumab. Our retrospective study shows that concurrent treatment of β-blocker and trastuzumab significantly improved progression-free survival and overall survival in the patients with Her2-overexpressing metastatic breast cancer, implicating the possibility for combination therapy with trastuzumab plus β-blocker in Her2-overexpressing breast cancer. © 2016 Macmillan Publishers Limited.


Mei G.-M.,Marine Fishery Research Institute of Zhejiang Province | Hao Q.,Beijing HaiYan Pharmaceutical CO. | Zhang X.-J.,Marine Fishery Research Institute of Zhejiang Province | Guo Y.-M.,Marine Fishery Research Institute of Zhejiang Province | Chen X.-C.,Marine Fishery Research Institute of Zhejiang Province
Modern Food Science and Technology | Year: 2014

A new polysaccharide SP2 was isolated from Lentinusedodes using an aqueous HCl solution and purified using gel column chromatography, the purity was determined using filter paper electrophoresis. The relative molecular mass and distribution of SP2 were analyzed by high-performance gel permeation chromatography, and the structure was analyzed by UV-Vis spectroscopy, gas chromatography, infrared spectroscopy, X-ray diffraction, and differential scanning calorimetry, as well as periodate oxidation, Smith degradation, and Congo red experiments. The results indicated that SP2 showed a typical absorption peak for polysaccharides after the color reaction and had a relatively homogeneous composition. In addition, the molecular weight distribution range was relatively narrow, with a weight-average molecular weight of 5.203×104 u. SP2 was found to be composed of mannose, glucose, and galactose with a molar ratio of 0.32:58.6:2.82. Periodate oxidation and Smith degradation experiments indicated that the C-C bonds in the branches of SP2 were composed of (1→2), (1→3), and (1→6) linkages with a molar ratio of 9.43:5.44:1. SP2 was found to be a glycoprotein conjugate containing pyranose rings that was amorphous and could not form the monocry stalline structure. SP2 contained spiral structures and had no strong intermolecular interactions. These results provided evidence to explain the structure-activity relationships of polysaccharides from L. edodes.


Yan R.,Beijing Haiyan Pharmaceutical Co. | Yang Z.-Y.,Beijing Haiyan Pharmaceutical Co.
Chinese Journal of Biologicals | Year: 2011

Because of their special blood glucose concentration-dependent effect in controlling blood glucose, glucagon-like peptide-1 (GLP-1) analogues provide a new choice for the patients with type 2 diabetes mellitus (T2DM). Most developments of new drugs are based on the endogenous human GLP-1 and their natural analogue Exendin-4. This paper reviews the structures, important sites, remodeling strategies, modification mode and new forms of GLP-1 and Exendin-4 as well as GLP-1 analogues as new drugs.


Xiong C.-W.,Qinghai Institute for Drug Control | Sun B.,Chinese Institute of Basic Medical Sciences | Xing W.-W.,State Intellectual Property Office of the Peoples Republic of China | Jia Y.-H.,Beijing Haiyan Pharmaceutical Co.
Chinese Journal of New Drugs | Year: 2012

Objective: To investigate the anti-endotoxin effect of Swertia macrosperma C.B. Clark. Methods: Endotoxin-induced death in mice was observed to evaluate the protective effect of Swertia macrosperma C.B. Clark. Its anti-endotoxin activities were tested in vivo and in vitro. Results: Extraction of Swertia macrosperma C.B. Clark prolonged the survival time in mice that were attacked by endotoxin. Swertia macrosperma C.B. Clark solution significantly attenuated the intensity of endotoxin effect as the concentration was more than 0.0625 g ·mL -1(1:16), but the effect was weaker or lost when the concentration was 0.0312 g ·mL -1(1:32). Conclusion: Swertia macrosperma C.B. Clark has a significant anti-endotoxin effect.


He J.,Beijing Institute of Technology | Dai J.,Beijing Institute of Technology | Li J.,Beijing Haiyan Pharmaceutical Co. | Peng X.,Uppsala University | And 3 more authors.
Journal of Chemical Physics | Year: 2015

The human islet amyloid polypeptide (hIAPP) co-operates with insulin to maintain glycemic balance. It also constitutes the amyloid plaques that aggregate in the pancreas of type-II diabetic patients. We have performed extensive in silico investigations to analyse the structural landscape of monomeric hIAPP, which is presumed to be intrinsically disordered. For this, we construct from first principles a highly predictive energy function that describes a monomeric hIAPP observed in a nuclear magnetic resonance experiment, as a local energy minimum. We subject our theoretical model of hIAPP to repeated heating and cooling simulations, back and forth between a high temperature regime where the conformation resembles a random walker and a low temperature limit where no thermal motions prevail. We find that the final low temperature conformations display a high level of degeneracy, in a manner which is fully in line with the presumed intrinsically disordered character of hIAPP. In particular, we identify an isolated family of α-helical conformations that might cause the transition to amyloidosis, by nucleation. © 2015 AIP Publishing LLC.


PubMed | The First Affiliated Hospital, 307 Hospital of Peoples Liberation Army, Beijing Haiyan Pharmaceutical Co., Chinese Institute of Basic Medical Sciences and Beijing Institute of Microbiology and Epidemiology
Type: Journal Article | Journal: Oncogene | Year: 2016

Currently, trastuzumab resistance is a major clinical problem in the treatment of Her2-overexpressing breast cancer. The underlying molecular mechanisms are not fully understood. Our previous study demonstrates that 2-adrenergic receptor (2-AR) and Her2 comprise a positive feedback loop in human breast cancer cells and that crosstalk between Her2 and 2-AR affects the bio-behaviors of breast cancer cells, suggesting that the 2-AR activation may be involved in trastuzumab resistance. In this study, we show that the expression of 2-AR, which mediates most catecholamine-induced effects, negatively correlates with trastuzumab response in the patients with Her2-overexpressing breast cancer. Catecholamines potently antagonize the anti-proliferative effects of trastuzumab both in vitro and in vivo. Catecholamine stimulation upregulates the expression of miR-21 and MUC-1 by activating Her2 and STAT3, leading to deficiency of phosphatase and tensin homolog and activation of phosphatidylinositol-3-kinase (PI3K) and Akt. Through inhibition of miR-199a/b-3p, catecholamines induce the mammalian target of rapamycin (mTOR) activation. Thus, trastuzumab resistance-dependent PI3K/Akt/mTOR pathway is controlled by catecholamine-induced 2-AR activation. The data indicate that 2-AR is a reliable molecular marker for prediction of response probability to trastuzumab-based therapy in breast cancer. We also demonstrate that -blocker propranolol not only enhances the antitumor activities of trastuzumab but also re-sensitizes the resistant cells to trastuzumab. Our retrospective study shows that concurrent treatment of -blocker and trastuzumab significantly improved progression-free survival and overall survival in the patients with Her2-overexpressing metastatic breast cancer, implicating the possibility for combination therapy with trastuzumab plus -blocker in Her2-overexpressing breast cancer.

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