The title compound （Z）-ethyl-4-（4-methoxy）benzylidene-2-（3,5-dimethoxyphenyl）- tetrahydrofuran-3,3-dicarboxylate has been synthesized, and its crystal structure was characterized by X-ray single-crystal diffract...The title compound （Z）-ethyl-4-（4-methoxy）benzylidene-2-（3,5-dimethoxyphenyl）- tetrahydrofuran-3,3-dicarboxylate has been synthesized, and its crystal structure was characterized by X-ray single-crystal diffraction. The crystal belongs to triclinic, space group P1, with a = 8.140（3）, b = 11.966（4）, c = 13.771（5）Aα= 67.366（4）, β= 85.165（5）, γ= 75.806（4）°, V = 1200.1（7） A3, Z = 2, C26H3008, Mr = 470.50, Dc = 1.302 g/cm^3, F（000） = 500,λ（MoKa） = 0.71073 A, μ= 0.096 mm^-1, R = 0.0659 and wR = 0.1841 for 3080 observed reflections （I 〉 2σ（I））. As a key intermediate of HIV-1 integrase inhibitor, the synthesis and structure confirmation of the title compound are important for further studies.展开更多
Selective hydrogenation of unsaturated aldehydes remains a grand challenge in controlling chemoselectivity up to now.We synthesized a series of PtFex/CeO_(2)catalysts,which were characterized by X-ray diffraction(XRD)...Selective hydrogenation of unsaturated aldehydes remains a grand challenge in controlling chemoselectivity up to now.We synthesized a series of PtFex/CeO_(2)catalysts,which were characterized by X-ray diffraction(XRD),transmission electron microscopy(TEM),X-ray photoelectron spectroscopy(XPS)as well as temperature-programmed-reduction by hydrogen(H2-TPR).The catalytic performance of PtFex/CeO_(2),including cinnamaldehyde(CAL)conversion and selectivity toward cinnamyl alcohol(COL),is improved remarkably by introduction of Fe species in the Pt particles in the selective CAL hydrogenation under mild conditions.XPS results indicate that the electron transfer from Fe to Pt promotes CAL adsorption,resulting in the enhanced CAL conversion.And the COL selectivity is improved by CAL adsorption via an interaction of C=O group with surface oxygen defect sites because of interaction between PtFe and CeO_(2)support.In all,this study may provide some hints to design efficient nano Pt particles for the selective hydrogenation.展开更多
Background Retinol binding protein 4 （RBP4）, as an adipocyte secreted cytokine, was recently found to be inversely correlated with expression of glucose transporter 4 （GLUT4） in insulin resistance （IR） state and...Background Retinol binding protein 4 （RBP4）, as an adipocyte secreted cytokine, was recently found to be inversely correlated with expression of glucose transporter 4 （GLUT4） in insulin resistance （IR） state and to have an intimate relationship with IR and type 2 diabetes mellitus （T2DM）. The present study aimed to evaluate the anti-diabetic efficacy of cinnamaldehyde （Cin）, berberine （Ber）, and metformin （Met） as well as their impacts on the RBP4-GLUT4 system. Methods Rat models of T2DM were established by combination of intraperitoneal injection of low-dose streptozotocin and high fat diet induction. Rats were divided into five groups： the control group, the diabetes group, the diabetes＋Ber group, the diabetes＋Cin group, and the diabetes＋Met group. Western blotting was used to detect the serum or tissue RBP4 and GLUT4 protein levels. Results After treatment for four weeks, both Cin and Ber displayed significant hypolipidemic, hypoglycemic, and insulin sensitizing functions （P 〈0.01） compared with the control group. Their effects on lowering fasting plasma glucose （FPG）, low density lipoprotein-cholesterol （LDL-C） and homeostasis model assessment of insulin resistance （HOMA-IR） seem even better than that of Met. Cin and Ber markedly lowered serum RBP4 levels and up-regulated the expression of tissue GLUT4 protein, and Cin seemed more notable in affecting these two proteins. Conclusions Both Cin and Ber display an exciting anti-diabetic efficacy in this study and may be of great value for the treatment of type 2 diabetes. Their mechanisms involve the RBP4-GLUT4 system, during which the serum RBP4 levels are lowered and the expression of tissue GLUT4 protein is up-regulated.展开更多
Objective： To examine the mechanism underlying the beneficial role of cinnamaldehyde on oxidative damage and apoptosis in high glucose （HG）-induced dorsal root ganglion （DRG） neurons in vitro. Methods： HG-treate...Objective： To examine the mechanism underlying the beneficial role of cinnamaldehyde on oxidative damage and apoptosis in high glucose （HG）-induced dorsal root ganglion （DRG） neurons in vitro. Methods： HG-treated DRG neurons were developed as an in vitro model of diabetic neuropathy. The neurons were randomly divided into five groups： the control group, the HG group and the HG groups treated with 25, 50 and 100 nmol/L cinnamaldehyde, respectively. Cell viability was examined by 3-（4,5-dimethylthiazol-2-yl）-2,5- diphenyltetrazolium bromide （MTT） assay and apoptosis rate was evaluated by the in situ TdT-mediated dUTP nick end labeling （TUNEL） assay. The intracellular level of reactive oxygen species （ROS） was measured with flow cytometry. Expression of nuclear factor-kappa B （NF-κ B）, inhibitor of κ B （I κ B）, phosphorylated I κ B （p-IκB）, tumor necrosis factor （TNF）-α, interleukin-6 （IL-6） and caspase-3 were determined by western blotting and real-time quantitative reverse transcription polymerase chain reaction （RT-PCR）. Expression of nuclear factor erythroid 2-related factor 2 （Nrf2） and hemeoxygenase-1 （HO-1） were also measured by western blotting. Results： Cinnamaldehyde reduced HG-induced loss of viability, apoptosis and intracellular generation of ROS in the DRG neurons via inhibiting NF- K B activity. The western blot assay results showed that the HG-induced elevated expressions of NF- κB, I κ B and p-I κ B were remarkably reduced by cinnamaldehyde treatment in a dose-dependent manner （P〈0.01）. The HG-induced over-expression of NF-κ B p65 mRNA was remarkably attenuated after cinnamaldehyde treatment in a dose-dependent manner （P〈0.01）. However, the expressions of Nrf2 and HO-1 were not upregulated. Treatment with cinnamaldehyde not only attenuated caspase-3 activation and the caspase cleavage cascade in DRG neurons, but also lowered the elevated IL-6, TNF-α, cyclo-oxygenase and inducible nitric oxide synthase levels, indicating a reduction in inflammatory damage. Conclusions： Cinnamaldehyde protected DRG neurons from the deleterious effects of HG through inactivation of NF- κB pathway but not through activation of Nrf2/HO-1. And thus cinnamaldehyde may have potential application as a treatment for DPN.展开更多
OBJECTIVE:To investigate the effects of cinnamaldehyde(CA),an active and major compound in cinnamon,on glucose metabolism and insulin resistance in C57BLKS/J db/db mice.METHODS:Sixteen male C57BLKS db/db mice were ran...OBJECTIVE:To investigate the effects of cinnamaldehyde(CA),an active and major compound in cinnamon,on glucose metabolism and insulin resistance in C57BLKS/J db/db mice.METHODS:Sixteen male C57BLKS db/db mice were randomly divided into control and CA treatment groups.CA was given(20 mg.kg-1.day-1,p.o.) for 4 weeks.Pure water was given to control and db/+ mice.Subsequently,the levels of fasting blood glucose(FBG),fasting serum insulin,triglyeride,cholesterol,low-density lipoprotein-cholesterol(LDL-C),high-density lipoprotein-cholesterol(HDL-C),and free fatty acids(FFA),as well as the mRNA content of adiponectin and tumor necrosis factor(TNF)-α in adipose tissue,glucose transporter type 4(GLUT-4) in skeletal muscle,and protein expressions of Akt,phospho-Akt(Thr308),AMPKα,phospho-AMPKα(Thr172) in skeletal muscle were measured.RESULTS:1) CA decreased serum levels of FBG and insulin as well as body weight in db/db mice;2) CA increased serum HDL-C levels;3) CA significantly decreased the mRNA expression of TNF-α in adipose tissue and upregulated mRNA expression of GLUT-4 in skeletal muscle;4) protein expression of p-Akt was increased in CA-treated mice,but Akt,AMPKα and p-AMPKα showed no change.CONCLUSION:CA has antihyperglycemic and antihyperlipidemic actions in db/db mice and could be useful in the treatment of type-2 diabetes.展开更多
目的:为探讨桂皮醛对糖尿病视网膜病变新生血管的作用及机制,观察了桂皮醛对血管内皮生长因子(VEGF)诱导EA. hy926细胞增殖、迁移、成管以及Janus激酶2/信号传导与转录激活因子3(JAK2/STAT3)通路的影响。方法:将EA.hy926细胞分成空白组...目的:为探讨桂皮醛对糖尿病视网膜病变新生血管的作用及机制,观察了桂皮醛对血管内皮生长因子(VEGF)诱导EA. hy926细胞增殖、迁移、成管以及Janus激酶2/信号传导与转录激活因子3(JAK2/STAT3)通路的影响。方法:将EA.hy926细胞分成空白组、模型组(7μg·L-1VEGF),VEGF+桂皮醛(60,90,120,150μmol·L-1)组,分别采用噻唑蓝(MTT)比色法和划痕实验检测桂皮醛对VEGF诱导EA. hy 926细胞增殖和迁移作用的影响;将EA. hy 926细胞分成空白组,模型组(7μg·L-1VEGF),VEGF+桂皮醛(90,150μmol·L-1)组,采用管腔形成实验检测桂皮醛对VEGF诱导EA. hy 926细胞成管作用的影响;将EA. hy 926细胞分成空白组,模型组(7μg·L-1VEGF),VEGF+AG490 (50μmol·L-1)组,VEGF+桂皮醛(90μmol·L-1)组,VEGF+桂皮醛(150μmol·L-1)组,VEGF+桂皮醛(150μmol·L-1)+AG490(50μmol·L-1)组,采用蛋白免疫印迹法(Western blot)检测桂皮醛对VEGF诱导EA. hy 926细胞JAK2/STAT3通路的影响。结果:与空白组比较,模型组能够显著地促进EA. hy 926细胞增殖和迁移(P <0. 01)。与模型组比较,桂皮醛(60,90,120,150μmol·L-1)组能显著抑制VEGF诱导EA. hy 926细胞的增殖和迁移(P <0. 01)。与空白组比较,VEGF对EA. hy 926细胞成管具有一定的促进作用,成管的节点数、交叉点数、网眼数和血管分支数均有增加,但无统计学差异。与模型组比较,桂皮醛(90,150μmol·L-1)组对成管的节点数、交叉点数和网眼数均有明显抑制作用(P <0. 05,P <0. 01)。与空白组比较,模型组p-JAK2,p-STAT3,STAT3蛋白表达明显升高(P <0. 05,P <0. 01)。与模型组比较,桂皮醛(150μmol·L-1)能够显著抑制VEGF引起的p-JAK2,p-STAT3,STAT3蛋白表达升高(P <0. 01),桂皮醛(90μmol·L-1)能够显著抑制VEGF引起的p-STAT3,STAT3蛋白表达升高(P <0. 05,P <0. 01)。结论:桂皮醛对VEGF诱导EA. hy 926细胞的增殖、迁移、成管具有明显的抑制作用,该作用与抑制JAK2/STAT3通路的激活有关。展开更多
基金supported by the National Natural Science Foundation of China (No. 30572238)
文摘The title compound （Z）-ethyl-4-（4-methoxy）benzylidene-2-（3,5-dimethoxyphenyl）- tetrahydrofuran-3,3-dicarboxylate has been synthesized, and its crystal structure was characterized by X-ray single-crystal diffraction. The crystal belongs to triclinic, space group P1, with a = 8.140（3）, b = 11.966（4）, c = 13.771（5）Aα= 67.366（4）, β= 85.165（5）, γ= 75.806（4）°, V = 1200.1（7） A3, Z = 2, C26H3008, Mr = 470.50, Dc = 1.302 g/cm^3, F（000） = 500,λ（MoKa） = 0.71073 A, μ= 0.096 mm^-1, R = 0.0659 and wR = 0.1841 for 3080 observed reflections （I 〉 2σ（I））. As a key intermediate of HIV-1 integrase inhibitor, the synthesis and structure confirmation of the title compound are important for further studies.
基金Project supported by the Natural Science Foundation of Inner Mongolia Autonomous Region(2020BS02016)the Program of Higher-level Talents of Inner Mongolia Agricultural University(NDYB2018-23)the Program of Scientific Research of Inner Mongolia Autonomous Region(NJZY19046)。
文摘Selective hydrogenation of unsaturated aldehydes remains a grand challenge in controlling chemoselectivity up to now.We synthesized a series of PtFex/CeO_(2)catalysts,which were characterized by X-ray diffraction(XRD),transmission electron microscopy(TEM),X-ray photoelectron spectroscopy(XPS)as well as temperature-programmed-reduction by hydrogen(H2-TPR).The catalytic performance of PtFex/CeO_(2),including cinnamaldehyde(CAL)conversion and selectivity toward cinnamyl alcohol(COL),is improved remarkably by introduction of Fe species in the Pt particles in the selective CAL hydrogenation under mild conditions.XPS results indicate that the electron transfer from Fe to Pt promotes CAL adsorption,resulting in the enhanced CAL conversion.And the COL selectivity is improved by CAL adsorption via an interaction of C=O group with surface oxygen defect sites because of interaction between PtFe and CeO_(2)support.In all,this study may provide some hints to design efficient nano Pt particles for the selective hydrogenation.
文摘Background Retinol binding protein 4 （RBP4）, as an adipocyte secreted cytokine, was recently found to be inversely correlated with expression of glucose transporter 4 （GLUT4） in insulin resistance （IR） state and to have an intimate relationship with IR and type 2 diabetes mellitus （T2DM）. The present study aimed to evaluate the anti-diabetic efficacy of cinnamaldehyde （Cin）, berberine （Ber）, and metformin （Met） as well as their impacts on the RBP4-GLUT4 system. Methods Rat models of T2DM were established by combination of intraperitoneal injection of low-dose streptozotocin and high fat diet induction. Rats were divided into five groups： the control group, the diabetes group, the diabetes＋Ber group, the diabetes＋Cin group, and the diabetes＋Met group. Western blotting was used to detect the serum or tissue RBP4 and GLUT4 protein levels. Results After treatment for four weeks, both Cin and Ber displayed significant hypolipidemic, hypoglycemic, and insulin sensitizing functions （P 〈0.01） compared with the control group. Their effects on lowering fasting plasma glucose （FPG）, low density lipoprotein-cholesterol （LDL-C） and homeostasis model assessment of insulin resistance （HOMA-IR） seem even better than that of Met. Cin and Ber markedly lowered serum RBP4 levels and up-regulated the expression of tissue GLUT4 protein, and Cin seemed more notable in affecting these two proteins. Conclusions Both Cin and Ber display an exciting anti-diabetic efficacy in this study and may be of great value for the treatment of type 2 diabetes. Their mechanisms involve the RBP4-GLUT4 system, during which the serum RBP4 levels are lowered and the expression of tissue GLUT4 protein is up-regulated.
基金Supported by the National Natural Science Foundation of China(No.81473639)the Natural Science Foundation of Beijing(No.7122147)
文摘Objective： To examine the mechanism underlying the beneficial role of cinnamaldehyde on oxidative damage and apoptosis in high glucose （HG）-induced dorsal root ganglion （DRG） neurons in vitro. Methods： HG-treated DRG neurons were developed as an in vitro model of diabetic neuropathy. The neurons were randomly divided into five groups： the control group, the HG group and the HG groups treated with 25, 50 and 100 nmol/L cinnamaldehyde, respectively. Cell viability was examined by 3-（4,5-dimethylthiazol-2-yl）-2,5- diphenyltetrazolium bromide （MTT） assay and apoptosis rate was evaluated by the in situ TdT-mediated dUTP nick end labeling （TUNEL） assay. The intracellular level of reactive oxygen species （ROS） was measured with flow cytometry. Expression of nuclear factor-kappa B （NF-κ B）, inhibitor of κ B （I κ B）, phosphorylated I κ B （p-IκB）, tumor necrosis factor （TNF）-α, interleukin-6 （IL-6） and caspase-3 were determined by western blotting and real-time quantitative reverse transcription polymerase chain reaction （RT-PCR）. Expression of nuclear factor erythroid 2-related factor 2 （Nrf2） and hemeoxygenase-1 （HO-1） were also measured by western blotting. Results： Cinnamaldehyde reduced HG-induced loss of viability, apoptosis and intracellular generation of ROS in the DRG neurons via inhibiting NF- K B activity. The western blot assay results showed that the HG-induced elevated expressions of NF- κB, I κ B and p-I κ B were remarkably reduced by cinnamaldehyde treatment in a dose-dependent manner （P〈0.01）. The HG-induced over-expression of NF-κ B p65 mRNA was remarkably attenuated after cinnamaldehyde treatment in a dose-dependent manner （P〈0.01）. However, the expressions of Nrf2 and HO-1 were not upregulated. Treatment with cinnamaldehyde not only attenuated caspase-3 activation and the caspase cleavage cascade in DRG neurons, but also lowered the elevated IL-6, TNF-α, cyclo-oxygenase and inducible nitric oxide synthase levels, indicating a reduction in inflammatory damage. Conclusions： Cinnamaldehyde protected DRG neurons from the deleterious effects of HG through inactivation of NF- κB pathway but not through activation of Nrf2/HO-1. And thus cinnamaldehyde may have potential application as a treatment for DPN.
基金Supported by International Science and Technology Cooperation Project(grant number 2009DFA31520)Innovation Team Project of Beijing University of Chinese Medicine (2011-CXTD-19)Beijing Municipal Education Commission(2011)
文摘OBJECTIVE:To investigate the effects of cinnamaldehyde(CA),an active and major compound in cinnamon,on glucose metabolism and insulin resistance in C57BLKS/J db/db mice.METHODS:Sixteen male C57BLKS db/db mice were randomly divided into control and CA treatment groups.CA was given(20 mg.kg-1.day-1,p.o.) for 4 weeks.Pure water was given to control and db/+ mice.Subsequently,the levels of fasting blood glucose(FBG),fasting serum insulin,triglyeride,cholesterol,low-density lipoprotein-cholesterol(LDL-C),high-density lipoprotein-cholesterol(HDL-C),and free fatty acids(FFA),as well as the mRNA content of adiponectin and tumor necrosis factor(TNF)-α in adipose tissue,glucose transporter type 4(GLUT-4) in skeletal muscle,and protein expressions of Akt,phospho-Akt(Thr308),AMPKα,phospho-AMPKα(Thr172) in skeletal muscle were measured.RESULTS:1) CA decreased serum levels of FBG and insulin as well as body weight in db/db mice;2) CA increased serum HDL-C levels;3) CA significantly decreased the mRNA expression of TNF-α in adipose tissue and upregulated mRNA expression of GLUT-4 in skeletal muscle;4) protein expression of p-Akt was increased in CA-treated mice,but Akt,AMPKα and p-AMPKα showed no change.CONCLUSION:CA has antihyperglycemic and antihyperlipidemic actions in db/db mice and could be useful in the treatment of type-2 diabetes.
文摘目的:为探讨桂皮醛对糖尿病视网膜病变新生血管的作用及机制,观察了桂皮醛对血管内皮生长因子(VEGF)诱导EA. hy926细胞增殖、迁移、成管以及Janus激酶2/信号传导与转录激活因子3(JAK2/STAT3)通路的影响。方法:将EA.hy926细胞分成空白组、模型组(7μg·L-1VEGF),VEGF+桂皮醛(60,90,120,150μmol·L-1)组,分别采用噻唑蓝(MTT)比色法和划痕实验检测桂皮醛对VEGF诱导EA. hy 926细胞增殖和迁移作用的影响;将EA. hy 926细胞分成空白组,模型组(7μg·L-1VEGF),VEGF+桂皮醛(90,150μmol·L-1)组,采用管腔形成实验检测桂皮醛对VEGF诱导EA. hy 926细胞成管作用的影响;将EA. hy 926细胞分成空白组,模型组(7μg·L-1VEGF),VEGF+AG490 (50μmol·L-1)组,VEGF+桂皮醛(90μmol·L-1)组,VEGF+桂皮醛(150μmol·L-1)组,VEGF+桂皮醛(150μmol·L-1)+AG490(50μmol·L-1)组,采用蛋白免疫印迹法(Western blot)检测桂皮醛对VEGF诱导EA. hy 926细胞JAK2/STAT3通路的影响。结果:与空白组比较,模型组能够显著地促进EA. hy 926细胞增殖和迁移(P <0. 01)。与模型组比较,桂皮醛(60,90,120,150μmol·L-1)组能显著抑制VEGF诱导EA. hy 926细胞的增殖和迁移(P <0. 01)。与空白组比较,VEGF对EA. hy 926细胞成管具有一定的促进作用,成管的节点数、交叉点数、网眼数和血管分支数均有增加,但无统计学差异。与模型组比较,桂皮醛(90,150μmol·L-1)组对成管的节点数、交叉点数和网眼数均有明显抑制作用(P <0. 05,P <0. 01)。与空白组比较,模型组p-JAK2,p-STAT3,STAT3蛋白表达明显升高(P <0. 05,P <0. 01)。与模型组比较,桂皮醛(150μmol·L-1)能够显著抑制VEGF引起的p-JAK2,p-STAT3,STAT3蛋白表达升高(P <0. 01),桂皮醛(90μmol·L-1)能够显著抑制VEGF引起的p-STAT3,STAT3蛋白表达升高(P <0. 05,P <0. 01)。结论:桂皮醛对VEGF诱导EA. hy 926细胞的增殖、迁移、成管具有明显的抑制作用,该作用与抑制JAK2/STAT3通路的激活有关。
