Hydrothermal reactions of 5-（tetrazol-5-yl） isophthalic acid with cadmium nitrate/praseodymium nitrate led to two complexes of [Cd3（TZI）2（H2O）（11）]n（1） and [Pr（TZI）（H2O）5]n（2）. Their structures and pro...Hydrothermal reactions of 5-（tetrazol-5-yl） isophthalic acid with cadmium nitrate/praseodymium nitrate led to two complexes of [Cd3（TZI）2（H2O）（11）]n（1） and [Pr（TZI）（H2O）5]n（2）. Their structures and properties were determined by X-ray diffraction, IR spectroscopy, fluorescence spectrum, thermal gravimetric analyses and elemental analysis. Complex 1 belongs to monoclinic system, I2/c space group, with a = 12.8688（3）, b = 18.0925（3）, c = 14.5190（3）A, β = 116.054（3）°, V =3036.92（13） A^3, Z = 4; complex 2 crystallizes in triclinic, space group P 1, with a = 7.9690（5）, b =9.7665（8）, c = 10.4353（9） A, α = 116.709（9）, β = 107.461（6）, γ = 95.671（6）°, V = 665.54（9）A^3 and Z =2. Complex 1 is a 3D planar structure. Complex 2 is a one-dimensional double chain configuration and extends into a 3D network by hydrogen bonds and π-π interactions.展开更多
The title Mn（Ⅱ） coordination polymer,poly{[heptaaqua-（μ4-bi-phenyl-3,3？,5,5？-tetracarboxylate）-bimanganese（Ⅱ）] pentahydrate},[Mn_2（bpta）（H_2O）_7]_n·5n H_2O（I）,is crystallized from a mixture of bi...The title Mn（Ⅱ） coordination polymer,poly{[heptaaqua-（μ4-bi-phenyl-3,3？,5,5？-tetracarboxylate）-bimanganese（Ⅱ）] pentahydrate},[Mn_2（bpta）（H_2O）_7]_n·5n H_2O（I）,is crystallized from a mixture of biphenyl-3,3？,5,5？-tetracarboxylic acid（H_4bpta） and MnCl_2·4H_2O in waterethanol under room temperature. Its asymmetric unit consists of one and two halves of crystallographically independent Mn（Ⅱ） cations,one fully deprotonated H4 bpta ligand,seven coordinated water molecules and five solvent water as guest molecules. In I,each Mn（Ⅱ） atom is octahedrally coordinated by six oxygen atoms from bpta^（4-） anions and coordinated water molecules. In the Mn（Ⅱ） cations,one half Mn（Ⅱ） ion of them located at a 2-fold axis generating a trinuclear [Mn_3（H_2O）_2（RCOO）_2] linker by μ1,1-O（water） and μ1,3-O,O？（carboxylate） bridges and another half Mn（Ⅱ） ion with an inversion is a mononuclear linker. These neighbouring trinuclear and mononuclear Mn（Ⅱ） cations are linked together by biphenyl-3,3？,5,5？-tetracarboxylates to form a three-dimensional framework with a（42.84） topology of a（4,4）-connected net,in which the positions of the trinuclear [Mn_3（H_2O）_2（R-COO）_2] linker as a 4-connector linking four bpta^（4-） ligands in I reproduce an eagle-shaped arrangement. The polymeric structure exhibits a water channel with an accessible void of 797.1 ？~3,amounting to 15.7% of the total unit-cell volume. Each of the cavities in the network is occupied by solvent water molecules.展开更多
Objective: The aim of our study was to detect whether Vitamin E Succinic Acid (VES) could regulate the expression level of DR5 in the cells and further elucidate the potential mechanisms involving that VES enhances th...Objective: The aim of our study was to detect whether Vitamin E Succinic Acid (VES) could regulate the expression level of DR5 in the cells and further elucidate the potential mechanisms involving that VES enhances the effect of mDRA-6 to eradicate leukemia Raji and K562 cells. Methods: MTT method was used to detect the growth inhibition of VES and mDRA-6 to Raji and K562 cells. Annexin V-FITC/PI double staining assay was used to analysis the apoptosis of leukemia cell. Flow cytometry was used to detect the cell surface DR5 expression. Immunoblotting technique was used to detect the DR5 protein expression. Results: MTT detection showed that 10 μmol/L mDRA-6 on the cell death rates of Raji and K562 cells were 21.98% and 5.23%, respectively. While increasing concentration of VES (5 μmol/L, 10 μmol/L, 20 μmol/L) and mDRA-6 both on the cell viability of Raji or K562 cells, the mortality of Raji cells elevated to 24.67%, 35.65% (P<0.01) and 40.22% (P<0.01), respectively. Similarly, the mortality of K562 cells increase to 6%, 7.89% (P<0.01) and 8.67% (P<0.01), respectively. To further specify the increased cell death rate induced by mDRA-6 and VES, the treated cells were analyzed by Annexin-V/PI staining assay. As shown in Fig. 1, the apoptosis rates of Raji and K562 cells treated with 2 μg/mL mDRA-6 for 12 h were 20.79% and 7.74%. Compared with this, the proportion of apoptotic cells increased upon exposure to 2 μg/mL mDRA-6 combination with 10 μmol/L VES, the apoptosis rates of Raji and K562 cells were 43.18% and 16.99%, respectively. To examine the anticancer effects of a combination strategy based on mDRA-6 and VES. We analyzed whether VES could elevated the expression level of DR5 on Raji and K562 cytomembrane by FACS. Interestingly, after treated with 10 μmol/L VES for 12 h, the expression level of DR5 on Raji and K562 cell surface increased from 50.66% to 70.08%, and 15.02% to 16.38%, respectively. Immune imprinting technology test showed that, different concentrations of VES could increase Raji and K562 cell DR5 protein expression. Conclusion: VES enhances the effect of mDRA-6 to eradicate leukemia Raji and K562 cells. The proper mechanism is VES could enhance the Raji and K562 cell membrane expression of DR5, and VES can also enhance the DR5 protein expression of cells.展开更多
G protein-coupled receptors(GPCRs)are a large family of membrane protein receptors,and Takeda G protein-coupled receptor 5(TGR5)is a member of this family.As a membrane receptor,TGR5 is widely distributed in different...G protein-coupled receptors(GPCRs)are a large family of membrane protein receptors,and Takeda G protein-coupled receptor 5(TGR5)is a member of this family.As a membrane receptor,TGR5 is widely distributed in different parts of the human body and plays a vital role in regulating metabolism,including the processes of energy consumption,weight loss and blood glucose homeostasis.Recent studies have shown that TGR5 plays an important role in glucose and lipid metabolism disorders such as fatty liver,obesity and diabetes.With the global obesity situation becoming more and more serious,a comprehensive explanation of the mechanism of TGR5 and filling the gaps in knowledge concerning clinical ligand drugs are urgently needed.In this review,we mainly explain the anti-obesity mechanism of TGR5 to promote the further study of this target,and show the electron microscope structure of TGR5 and review recent studies on TGR5 ligands to illustrate the specific binding between TGR5 receptor binding sites and ligands,which can effectively provide new ideas for ligand research and promote drug research.展开更多
基金Supported by the International Science&Technology Cooperation Program of China(No.2011DFA51980)the International Scientific and Technological Cooperation Projects of Shanxi Province(No.2015081043)+1 种基金“131”Leading Talents Project in Colleges and Universities,Science and Technology Innovation Project of Shanxi Province(No.2014101002)Graduate Student Education Innovation Project of Shanxi Province(No.20141101)
文摘Hydrothermal reactions of 5-（tetrazol-5-yl） isophthalic acid with cadmium nitrate/praseodymium nitrate led to two complexes of [Cd3（TZI）2（H2O）（11）]n（1） and [Pr（TZI）（H2O）5]n（2）. Their structures and properties were determined by X-ray diffraction, IR spectroscopy, fluorescence spectrum, thermal gravimetric analyses and elemental analysis. Complex 1 belongs to monoclinic system, I2/c space group, with a = 12.8688（3）, b = 18.0925（3）, c = 14.5190（3）A, β = 116.054（3）°, V =3036.92（13） A^3, Z = 4; complex 2 crystallizes in triclinic, space group P 1, with a = 7.9690（5）, b =9.7665（8）, c = 10.4353（9） A, α = 116.709（9）, β = 107.461（6）, γ = 95.671（6）°, V = 665.54（9）A^3 and Z =2. Complex 1 is a 3D planar structure. Complex 2 is a one-dimensional double chain configuration and extends into a 3D network by hydrogen bonds and π-π interactions.
基金supported by the National Natural Science Foundation of China(No.21571118)
文摘The title Mn（Ⅱ） coordination polymer,poly{[heptaaqua-（μ4-bi-phenyl-3,3？,5,5？-tetracarboxylate）-bimanganese（Ⅱ）] pentahydrate},[Mn_2（bpta）（H_2O）_7]_n·5n H_2O（I）,is crystallized from a mixture of biphenyl-3,3？,5,5？-tetracarboxylic acid（H_4bpta） and MnCl_2·4H_2O in waterethanol under room temperature. Its asymmetric unit consists of one and two halves of crystallographically independent Mn（Ⅱ） cations,one fully deprotonated H4 bpta ligand,seven coordinated water molecules and five solvent water as guest molecules. In I,each Mn（Ⅱ） atom is octahedrally coordinated by six oxygen atoms from bpta^（4-） anions and coordinated water molecules. In the Mn（Ⅱ） cations,one half Mn（Ⅱ） ion of them located at a 2-fold axis generating a trinuclear [Mn_3（H_2O）_2（RCOO）_2] linker by μ1,1-O（water） and μ1,3-O,O？（carboxylate） bridges and another half Mn（Ⅱ） ion with an inversion is a mononuclear linker. These neighbouring trinuclear and mononuclear Mn（Ⅱ） cations are linked together by biphenyl-3,3？,5,5？-tetracarboxylates to form a three-dimensional framework with a（42.84） topology of a（4,4）-connected net,in which the positions of the trinuclear [Mn_3（H_2O）_2（R-COO）_2] linker as a 4-connector linking four bpta^（4-） ligands in I reproduce an eagle-shaped arrangement. The polymeric structure exhibits a water channel with an accessible void of 797.1 ？~3,amounting to 15.7% of the total unit-cell volume. Each of the cavities in the network is occupied by solvent water molecules.
基金Supported by grants from the National "863 Plan" (No. 2006AA02A254)Outstanding Talent Program of Henan Province (No. 074200510014)
文摘Objective: The aim of our study was to detect whether Vitamin E Succinic Acid (VES) could regulate the expression level of DR5 in the cells and further elucidate the potential mechanisms involving that VES enhances the effect of mDRA-6 to eradicate leukemia Raji and K562 cells. Methods: MTT method was used to detect the growth inhibition of VES and mDRA-6 to Raji and K562 cells. Annexin V-FITC/PI double staining assay was used to analysis the apoptosis of leukemia cell. Flow cytometry was used to detect the cell surface DR5 expression. Immunoblotting technique was used to detect the DR5 protein expression. Results: MTT detection showed that 10 μmol/L mDRA-6 on the cell death rates of Raji and K562 cells were 21.98% and 5.23%, respectively. While increasing concentration of VES (5 μmol/L, 10 μmol/L, 20 μmol/L) and mDRA-6 both on the cell viability of Raji or K562 cells, the mortality of Raji cells elevated to 24.67%, 35.65% (P<0.01) and 40.22% (P<0.01), respectively. Similarly, the mortality of K562 cells increase to 6%, 7.89% (P<0.01) and 8.67% (P<0.01), respectively. To further specify the increased cell death rate induced by mDRA-6 and VES, the treated cells were analyzed by Annexin-V/PI staining assay. As shown in Fig. 1, the apoptosis rates of Raji and K562 cells treated with 2 μg/mL mDRA-6 for 12 h were 20.79% and 7.74%. Compared with this, the proportion of apoptotic cells increased upon exposure to 2 μg/mL mDRA-6 combination with 10 μmol/L VES, the apoptosis rates of Raji and K562 cells were 43.18% and 16.99%, respectively. To examine the anticancer effects of a combination strategy based on mDRA-6 and VES. We analyzed whether VES could elevated the expression level of DR5 on Raji and K562 cytomembrane by FACS. Interestingly, after treated with 10 μmol/L VES for 12 h, the expression level of DR5 on Raji and K562 cell surface increased from 50.66% to 70.08%, and 15.02% to 16.38%, respectively. Immune imprinting technology test showed that, different concentrations of VES could increase Raji and K562 cell DR5 protein expression. Conclusion: VES enhances the effect of mDRA-6 to eradicate leukemia Raji and K562 cells. The proper mechanism is VES could enhance the Raji and K562 cell membrane expression of DR5, and VES can also enhance the DR5 protein expression of cells.
基金supported by the Science and Technology Program of Guangzhou,China(No.202103000089)the Guangdong Demonstration Base for Joint Cultivation of Postgraduates(2019,China)the Science Foundation for Distinguished Young Scholars of Guangdong(2020B1515020026,China).
文摘G protein-coupled receptors(GPCRs)are a large family of membrane protein receptors,and Takeda G protein-coupled receptor 5(TGR5)is a member of this family.As a membrane receptor,TGR5 is widely distributed in different parts of the human body and plays a vital role in regulating metabolism,including the processes of energy consumption,weight loss and blood glucose homeostasis.Recent studies have shown that TGR5 plays an important role in glucose and lipid metabolism disorders such as fatty liver,obesity and diabetes.With the global obesity situation becoming more and more serious,a comprehensive explanation of the mechanism of TGR5 and filling the gaps in knowledge concerning clinical ligand drugs are urgently needed.In this review,we mainly explain the anti-obesity mechanism of TGR5 to promote the further study of this target,and show the electron microscope structure of TGR5 and review recent studies on TGR5 ligands to illustrate the specific binding between TGR5 receptor binding sites and ligands,which can effectively provide new ideas for ligand research and promote drug research.
