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Wang H.,Nankai University | Kong L.-Y.,Tianjin Institute of Pharmaceutical science | Li N.,Tianjin Institute of Pharmaceutical science | Wang Q.,Tianjin Institute of Pharmaceutical science
Jiegou Huaxue | Year: 2013

Solvothermal reaction of 2,5-furandicarboxylic acid (H2FDA) ligand and Ca(NO3)24H2O affords a new coordination polymer, [Ca2(FDA)2(DMAC)(H2O)]n (1). The structure has been determined by single-crystal X-ray diffraction analyses and further characterized by elemental analyses, IR, powder X-ray diffraction and TGA. Compound 1 crystallizes in triclinic, space group P1 with a=9.5387(19), b=10.425(2), c=11.590(2) , α=75.02(3), ?=84.80(3), ?=80.99(3), V=1098.1(4) 3, Dc=1.492 g/cm3, C16H15Ca2NO12, Mr=493.45, F(000)=508, μ(MoKα)= 0.580 mm-1, Z=2, R=0.0436 and wR=0.0944 for 3865 observed reflections (I > 2(I)), and R=0.0595 and wR=0.1015 for all data. The structure of 1 exhibits a three-dimensional network with layer-pillar structure.

Wang H.,Nankai University | Hu T.-L.,Nankai University | Wen R.-M.,Nankai University | Wang Q.,Tianjin Institute of Pharmaceutical science | Bu X.-H.,Nankai University
Journal of Materials Chemistry B | Year: 2013

Two new metal-drug complexes constructed from non-toxic zinc and theophylline (TPL), an anti-asthmatic active drug, have been introduced into a release system based on matrices of hydroxypropylmethylcellulose (HPMC) and microcrystalline cellulose (MC). The release rate of TPL from the metal-drug complexes could be controlled by the amount of MC added, and the release mechanism changed from anomalous transport to Fickian diffusion. This journal is © The Royal Society of Chemistry.

Ma B.,Nankai University | Hu X.,Nankai University | Zhao X.,University of Florida | Zhang Y.,Nankai University | And 6 more authors.
Experimental and Clinical Endocrinology and Diabetes | Year: 2014

Recombinant orally long-acting glucagon-like peptide 1 (rolGLP-1), a novel analog of native GLP-1 that can stimulate insulin secretion, was constructed via site-directed mutagenesis by our laboratory. This study was designed to investigate the pharmacokinetics, pharmacodynamics, and the cytotoxicity of rolGLP-1. Diabetic db/db mice were given 125I-rolGLP-1 through a single dose of oral administration to evaluate the pharmacokinetics of rolGLP-1 by trichloroacetic acid-Radioactive assay (TCA-RA). Separately, rolGLP-1 was orally administered to the db/db mice daily for 28 days to evaluate its therapeutic effect. In addition, the safety of rolGLP-1 was assessed based on cytotoxicity testing on the cell line SH-SY5Y by both the MTT assay and the cell counts method. The results showed that the half-life of rolGLP-1 in db/db mice was 68.2h, which is longer than that of native GLP-1. Results after the 28 day treatment showed glucose homeostasis was improved. Furthermore, rolGLP-1 was also proved to mitigate insulin resistance, alleviate hyperinsulinemia and decreased glycosylated hemoglobin content. Lastly, no visible adverse events were observed in cytotoxicity treatments on SH-SY5Y. Our results revealed that oral administration of rolGLP-1 harbored a longer half-life and a good therapeutic effect for type 2 db/db mice. All the results suggest the capacity and safety of rolGLP-1 for further use as an anti-diabetic agent for type 2 diabetes. This study was supported by Project 863 of China (2008AA02Z205). © J. A. Barth Verlag in Georg Thieme Verlag KG Stuttgart. New York.

Wang H.,Nankai University | Wen R.-M.,Nankai University | Chang Z.,Nankai University | Wang Q.,Tianjin Institute of Pharmaceutical science | And 2 more authors.
Jiegou Huaxue | Year: 2014

Two new Cu(II) coordination polymers, [Cu(FDA)(BPY)(H2O)] n (1) and {[Cu(FDA)(BPY)(H2O)]·2H 2O}n (2) (H2FDA = 2,5-furandicarboxylic acid, BPY = 2,2′-bipyridine), have been synthesized and structurally characterized by single-crystal X-ray diffraction as well as elemental analysis and IR. Compound 1 crystallizes in monoclinic, space group P21/c, with a = 7.5915(15), b = 8.4050(17), c = 24.204(6) Å, β = 99.05(3)°, V = 1525.1(6) Å3, Dc = 1.706 g/cm3, C16H12CuN2O6, Mr = 391.82, F(000) = 796, μ(MoKα) = 1.470 mm-1, Z = 4, R = 0.0633 and wR = 0.1059 for 2389 observed reflections (I > 2σ(I)), R = 0.0738, and wR = 0.1098 for all data. Complex 2 belongs to triclinic space group P1 - with a = 8.8660(18), b = 8.9112(18), c = 12.525(3) Å, α = 88.41(3), β = 69.38(3), γ = 66.95(3)°, V = 845.2(3) Å3, Dc = 1.681 g/cm3, C 16H16CuN2O8, Mr = 427.85, F(000) = 438, μ(MoKα) = 1.342 mm-1, Z = 2, R = 0.0290 and wR = 0.0690 for 2767 observed reflections (I > 2σ(I)), R = 0.0329 and wR = 0.0706 for all data. Complexes 1 and 2 are both coordination polymers with one-dimensional chain structures bridged by the protonated FDA ligands, which are assembled into three-dimensional supramolecular structures through hydrogen bonding interactions and π-π packing interactions between the chains. Copyright © 2013 Editorial Board of Chinese Journal of Structurnal Chemistry.

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