Kunming Pharmaceutical Group Corporation

Kunming, China

Kunming Pharmaceutical Group Corporation

Kunming, China
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Yang X.-J.,Kunming Pharmaceutical Group Corporation | Huang X.,Kunming Pharmaceutical Group Corporation | Tian Z.,Kunming Pharmaceutical Group Corporation | Wang P.,Kunming Pharmaceutical Group Corporation | And 2 more authors.
Chinese Pharmacological Bulletin | Year: 2017

Aim To establish a novel acute hyperuricemia mouse model and apply it to evaluate the hyporuci-cemia effects of Ulodesine, a purine nucleoside Phosphorylase (PNP) inhibitor. Methods The mice were intraperitoneal injected inosine and subcutaneous injected Oteracil potassium to induce accumulation of uric acid, and the animal blood was collected from eyeball or vena angularis in different time points. The levels of serum uric acid were measured and determined to test whether the acute hyperuricemia mouse model were successful or not. In order to verify the hyperuricemia seen in the model was associated with the accumulation of inosine, which was converted to uric acid by action of PNP, hyporucicemia effects of Ulodesine, a PNP inhibitor, was assessed in an enzyme assay and confirmed by using the newly established model. Result Accumulation of uric acid in the blood of mouse models was observed by combined injections of intraperitoneal 200 mg · kg-1 inosine and subcutaneous 200 mg · kg-1 Oteracil potassium respectively after 1.5 h. The enzyme assay indicated that Ulodesine was a potently PNP inhibitor with IC50 of 2.293 nmol · L-1. IV injection of Ulodesine eliminated uric acid accumulations in blood of the mouse model, which was expected as the in vivo action of Ulodesine. Conclusions A novel acute hyperuricemia mouse model is established. This is a relatively easy and more effective protocol to generate the hyperuricemia in mice, which will be a useful platform to assess the anti-hyperuricemia activity of PNP-target drugs in vivo.


Wang F.,Kunming University of Science and Technology | Yang B.,Kunming University of Science and Technology | Zhao Y.,Kunming University of Science and Technology | Liao X.,Kunming University of Science and Technology | And 6 more authors.
Journal of Biomaterials Science, Polymer Edition | Year: 2014

The inclusion complexation behavior of scutellarein (SCUE) with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) has been investigated in both solution and in the solid state. SCUE/HP-β-CD solid system was prepared by suspension method. The formation of SCUE/HP-β-CD complex in aqueous solution was demonstrated by fluorescence spectroscopy, and the Job plot showed a maximum at a molar fraction of 0.5, indicating 1:1 inclusion complexation between SCUE and HP-β-CD. However, SCUE/HP-β-CD inclusion complex was characterized by means of XRD, DSC, 1H, and two-dimensional NMR. Through the complexation between HP-β-CD and SCUE, the water solubility and antitumor activity of SCUE were obviously increased. This satisfactory water solubility and high antitumor activity of the SCUE/HP-β-CD complex will be potentially useful for its application on human colon cancer chemotherapies. © 2014 Taylor & Francis.


Xiao D.,Kunming University of Science and Technology | Yang B.,Kunming University of Science and Technology | Chen Y.-J.,Kunming Pharmaceutical Group Corporation | Liao X.-L.,Kunming University of Science and Technology | And 3 more authors.
Asian Journal of Chemistry | Year: 2013

A sort of C-10-phenoxy artemisinin-chitosan conjugate, in which C-10-phenoxy artemisinin was covalently bound to chitosan, was prepared and its aqueous solubility was evaluated. The results indicated that the conjugate (1.013 mg/mL) had much higher aqueous solubility than artemisinin (0.0084 mg/mL) and C-10-phenoxy artemisinin (0.0245 mg/mL). The conjugate will be potentially useful for their application as the prodrug of artemisinin.


Yang X.,Kunming University of Science and Technology | Zhao Y.,Kunming University of Science and Technology | Chen Y.,Kunming Pharmaceutical Group Corporation | Liao X.,Kunming University of Science and Technology | And 5 more authors.
Materials Science and Engineering C | Year: 2013

The characterization, inclusion complexation behavior and binding ability of the inclusion complexes of mangiferin (MGF) with β-cyclodextrin and its derivatives (hydroxypropyl-β-cyclodextrin (HPβCD), sulfobutyl ether β-cyclodextrin (SBEβCD) and mono (6-ethylene-diamino-6-deoxy)-β- cyclodextrin (ENβCD)) were investigated in both solution and solid state by means of PL spectroscopy, 1H and 2D NMR, XRD, TG and DSC. The results showed that the water solubility and thermal stability of MGF were significantly increased in the inclusion complex with cyclodextrins. The MGF/CDs complexes will be potentially useful for the design of a novel formulation of mangiferin for herbal medicine. © 2013 Elsevier B.V.


Xiao D.,Kunming University of Science and Technology | Yang B.,Kunming University of Science and Technology | Zhao Y.-L.,Kunming University of Science and Technology | Liao X.-L.,Kunming University of Science and Technology | And 4 more authors.
Journal of Inclusion Phenomena and Macrocyclic Chemistry | Year: 2014

The characterization, inclusion complexation behavior and binding ability of the inclusion complexes of dihydroartemisinin with β-cyclodextrin and its derivatives, sulfobutyl ether β-cyclodextrin (SBE-β-CD), mono[6-(2-aminoethylamino)-6-deoxy]-β-cyclodextrin (en-β-CD) and mono{6-[2-(2-aminoethylamino)ethylamino]-6-deoxy}-β-cyclodextrin (dien-β-CD), were studied using phenolphthalein as a spectral probe. Spectral titration was performed in aqueous buffer solution (pH ca. 10.5) at 25 °C to determine the binding constants. The inclusion complexation behaviors were investigated in both solution and solid state by means of NMR, TG, XRD. The results showed that the water solubility and thermal stability of dihydroartemisinin were significantly increased in the inclusion complex with cyclodextrins (CDs). According to 1H NMR and 2D NMR spectroscopy (ROESY), the A, B rings of dihydroartemisinin can be included into the cavity of CDs. The enhanced binding ability of CDs towards dihydroartemisinin was discussed from the viewpoint of the size/shape-fit concept and multiple recognition mechanism between host and guest. © 2013 Springer Science+Business Media Dordrecht.


Jiang R.-J.,Kunming University of Science and Technology | Zhao Y.-L.,Kunming University of Science and Technology | Chen Y.-J.,Kunming Pharmaceutical Group Corporation | Xiao D.,Kunming University of Science and Technology | And 7 more authors.
Carbohydrate Research | Year: 2014

A novel series of artesunate-β-cyclodextrin (ATS-β-CD) conjugates, in which artesunate (ATS) was coupled covalently to one of the primary hydroxyl groups of β-cyclodextrin (β-CD) through amino bond formation, were synthesized and characterized by 1H NMR, HRMS, 2D NMR (ROESY), X-ray diffraction (XRD), and thermogravimetric analysis (TGA). The results showed that the aqueous solubility of ATS-β-CD conjugates was 26-45 times better than that of free ATS. The cytotoxicity of the ATS-β-CD conjugates was evaluated on human colon cancer cell lines HCT116, LOVO, SW480, and HT-29, and the results indicated that ATS-2NβCD exhibited a very high cytotoxicity against HCT116, LOVO, and HT-29 with IC50 values of 0.58, 1.62, and 5.18 μmol/L, respectively. In addition, the supposition of better cytotoxicity was further supported by the control experiment of fluorescent cyclodextrin. © 2014 Elsevier Ltd. All rights reserved.


PubMed | Kunming Pharmaceutical Group Corporation, Yunnan University and Kunming University of Science and Technology
Type: | Journal: Carbohydrate research | Year: 2014

A novel series of artesunate--cyclodextrin (ATS--CD) conjugates, in which artesunate (ATS) was coupled covalently to one of the primary hydroxyl groups of -cyclodextrin (-CD) through amino bond formation, were synthesized and characterized by (1)H NMR, HRMS, 2D NMR (ROESY), X-ray diffraction (XRD), and thermogravimetric analysis (TGA). The results showed that the aqueous solubility of ATS--CD conjugates was 26-45 times better than that of free ATS. The cytotoxicity of the ATS--CD conjugates was evaluated on human colon cancer cell lines HCT116, LOVO, SW480, and HT-29, and the results indicated that ATS-2NCD exhibited a very high cytotoxicity against HCT116, LOVO, and HT-29 with IC50 values of 0.58, 1.62, and 5.18mol/L, respectively. In addition, the supposition of better cytotoxicity was further supported by the control experiment of fluorescent cyclodextrin.

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