作者机构：
[Zhang, He-Ming; Deng, Gui-Ming] S China Normal Univ, Coll Biophoton, MOE Key Lab Laser Life Sci, Guangzhou 510631, Guangdong, Peoples R China.;[Zhang, He-Ming; Deng, Gui-Ming] S China Normal Univ, Coll Biophoton, Inst Laser Life Sci, Guangzhou 510631, Guangdong, Peoples R China.;[Wang, Chao-Run; Chen, Zhen; Deng, Gui-Ming] Hunan Univ Chinese Med, Affiliated Hosp 1, Changsha 410007, Hunan, Peoples R China.
通讯机构：
[Zhang, He-Ming] S;S China Normal Univ, Coll Biophoton, MOE Key Lab Laser Life Sci, Guangzhou 510631, Guangdong, Peoples R China.
摘要：
The asymmetric unit of the title compound, C 8H 7N 3O 5, contains two independent molecules in which the amide plane is oriented at dihedral angles of 29.82(2) and 31.17(2)° with respect to the benzene ring. In the crystal, molecules are connected via intermolecular N-H··· O hydrogen bonds, forming chains running along the b axis.
摘要：
OBJECTIVE: This study evaluated variation in blood pressure (BP) in hypertensive subacute stroke patients performing eight different types of active movement, and variations in BP over time. METHODS: The study included 35 subacute stroke patients (60 - 74 years old) and 15 age-matched healthy volunteers. Ambulatory systolic and diastolic BP was measured over 4 consecutive days, before and during active movement. RESULTS: The greatest effect of the different active movements in stroke patients was on mean systolic BP variability (BPV). There was a significant difference in systolic and diastolic BPV between stroke patients at different time-points and compared with healthy volunteers. Systolic BPV during shifting from the ward to the rehabilitation centre was significantly higher than for all other active movements. Mean systolic BPVs during the sessions on the first and second days were significantly higher than for the sessions on the third and fourth days in stroke patients and compared with healthy volunteers. CONCLUSIONS: Systolic BP was found to be increased in hypertensive subacute stroke patients during their first and/or second attempts at performing active movements. Therapists should consider the BP of hypertensive subacute stroke patients during these first two attempts, especially for activities involving the patient moving from the ward to the rehabilitation centre.
摘要：
The objective of this study was to apply the "on/off" switch consisting of 3' phosphorothioate-modified allele specific primers and exo(+) polymerase in single base discrimination of A1555G and C1494T mutations in the highly conserved sites of the mitochondrial 12S rRNA. The two point mutations are the hotspot mutations associated with either aminoglycoside antibiotics induced deafness or inherited nonsyndromic hearing loss. The PCR products of mitochondrial DNA (mtDNA) 12S rRNA gene were inserted into the pMD19-T vector for transformation into Escherichia coli JM109 competent cells for preparing wild-type pMD19-T/mt vector. Inverse PCR was carried out for mtDNA 12S rRNA gene C1494T and A1555G mutagenesis and DpnI endonuclease degradating methylated pMD19-T/mt vector existing in the inverse PCR products was carried out to construct the mutation-type pMD19-T/mtM vector. These constructed vectors were confirmed by DNA sequencing. Allelic specific primers targeting wild-type and mutation-type templates were designed with 3' terminal phosphorothioate modification. Two-directional primer extension was performed using Pfu polymerases. Amplified by exo(+) polymerase, allelic specific primers perfectly matching wild-type allele were extended while no products were produced from primers targeting point-mutated deafness-related allele. Similarly, allelic specific primers perfectly matching point-mutated deafness-related mutation-type allele were extended and no products were yielded from primers targeting wild-type allele. No specific product was observed in the primer extension reaction mediated by on/off switch in screening the mtDNA 12S rRNA gene harboring either C1494T or A1555G mutation in 40 healthy volunteers tested. These data suggest that the "off switch" mediated by exo(+) polymerase is highly reliable in the diagnosis of monogenic diseases and the novel "on/off" switch has enormous applications in systematic and extended screening of the12S rRNA gene A1555G and C1494T mutations. The established assay can be widely used not only for hearing loss patients but also for normal subjects before the use of aminoglycoside antibiotics.
摘要：
Acetyl-CoA carboxylases (ACCs) play a rate-limiting role in fatty acid biosynthesis in plants, microbes, mammals and humans. ACCs have the activity of both biotin carboxylase (BC) and carboxyltransferase (CT), catalyzing carboxylation of Acetyl-CoA to malonyl-CoA. In the past years, ACCs have been used as targets for herbicides in agriculture and for drug discovery and development of human diseases, such as microbial infections, diabetes, obesity and cancer. A great number of small molecule ACC inhibitors have been developed, including natural and non-natural (artificial) products. These chemicals target BC reaction, CT reaction or ACC phosphorylation. This article provides a comprehensive review and updates of ACC inhibitors, with a focus on their therapeutic application in metabolic syndromes and malignant diseases. The patent status of common ACC inhibitors is discussed.
摘要：
After gene mutation, the pcDNA3.1/APP595/596 plasmid was transfected into HEK293 cells to establish a cell model of Alzheimer's disease. The cell model was treated with donepezil or compound Danshen tablets after culture for 72 hours. Reverse transcription-PCR showed that the mRNA expression of amyloid protein precursor decreased in all groups following culture for 24 hours, and that there was no significant difference in the amount of decrease between donepezil and compound Danshen tablets. Our results suggest that compound Danshen tablets can reduce expression of the mRNA for amyloid protein precursor in a transgenic cell model of Alzheimer's disease, with similar effects to donepezil.
摘要：
Using microcalorimetry, the characteristic metabolic heat flow power-time curves of S. aureus growth affected by Ursodesoxycholic acid and Hyodeoxycholic acid were measured at 37 °C. The thermal-kinetic parameters such as, growth rate constant k, the maximum power output (P
m), the time corresponding to the maximum power output (t
p), total heat-production Q
t
, half inhibitory concentration of the drugs (IC
50) were calculated from the growth curves. For both HDCA and UDCA, with the increasing of concentration, k, P
m, and Q
t
decreased, meanwhile, k–c fit a linear equation, t
p was prolonged correspondingly. Principle component analysis, the results indicated t
p might be the main parameter in evaluating the antibacterial activity of HDCA and UDCA in microcalorimetric method. Combining with t
p and IC
50, the results revealed that the differences and trends of antibacterial activity of these bile acid derivatives were: HDCA > UDCA. Structure-activity relationship (SAR) analysis showed that the α-OH at C-3 and C-6 position at equal pace on the steroid nucleus enhanced the hydrophilicity of HDCA, which led to a stronger antibacterial effect than UDCA. In this study, a useful tool was provided to accurately evaluate the antibacterial effects of bile acid derivatives. The thermolysis curve recorded by microcalorimetry could provide a lot of kinetic and thermodynamic information for the study of growth process of living microbial, which could be helpful in the screening of high efficacy antibacterial agents.
作者机构：
[Shen, Jing-Shan; Zhang, Qiang; Li, Jian-Feng; Zhang, Rong-Xia; Jiang, Xiang-Rui; Suo, Jin] Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China.;[Tian, Guang-Hui; Shen, Jing-Shan; Sun, Jin] Topharman Shanghai Co Ltd, Shanghai 201209, Peoples R China.;[Feng, Xin; Fang, Du] Hunan Univ Tradit Chinese Med, Coll Pharmaceut, Changsha 410208, Hunan, Peoples R China.
通讯机构：
[Jiang, Xiang-Rui] C;Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China.
摘要：
A practical and enantioselective synthetic method for tapentadol has been described. Starting from inexpensive and readily available (E)-3-(3-(benzyloxy)phenyl)acrylic acid, tapentadol was prepared in seven steps (44% overall yield and 99.9% de) in more than 100 g batches, without any chromatographic purification. An Evans' chiral auxiliary based conjugate addition and alkylation were used as the key steps. (C) 2012 Elsevier Ltd. All rights reserved.
摘要：
The review article covers the hypervalent organoantimony compounds that are with intramolecular N, O, S→Sb coordinations synthesized in the past 20 years. We describe their structures and the related coordination chemistry, highlighting a number of hypervalent stibines. These compounds have shown many applications in organic synthesis. They are useful reagents for reactions such as crosscoupling and arylation with organic halides, and addition with carbonyl compounds. They can be used as Lewis acid catalysts in organic synthesis. Furthermore, they can be utilized as catalysts or reagents for CO2 chemical fixation. It is envisaged that more hypervalent organoantimony compounds of novel structure will be synthesized and find new applications in the near future.
摘要：
Organometallic Lewis acids play an important role in modern organic synthesis. How to design and synthesize highly efficient and recyclable organometallic Lewis acid catalysts that can be conveniently applied in chemical reactions are key issues for sustainable synthetic processes. In general, stronger acidity means higher catalytic activity for organometallic Lewis acids. However, with the rise in acidity, the compound becomes more susceptible to hydrolysis and cannot be recycled. Simultaneous improvement of the hygroscopic character and Lewis acidity/catalytic activity of organometallic Lewis acids is highly desirable from the standpoint of practical applications. In this mini-review, the history of air-stable organometallic Lewis acids is introduced, with emphasis on our research works on metallocene, organobismuth, and organoantimony Lewis acids to the aspects of synthesis, characterization and catalytic application in carbon–carbon bond (Friedel–Crafts acylation, Mukaiyama aldol reactions; allylation, cyclotrimerization, Mannich reactions, cross-condensation reactions) and carbon–heteroatom bond (acylation, S–S bond cleavage, glycosylation) formation reactions. In terms of stability, storage, versatile ability, high catalytic activity and chemo-/stereo-selectivity, the complexes will find broad applications in organic synthesis.
作者机构：
[Zeng, Heng; Chen, Jian-Xiong] Univ Mississippi, Med Ctr, Dept Pharmacol & Toxicol, Jackson, MS 39216 USA.;[Tuo, Qinhui] Univ S China, Dept Pharmacol, Hengyang 421001, Peoples R China.;[Liao, Duan-Fang] Hunan Univ Chinese Med, Dept Tradit Chinese Diagnost, Sch Pharm, Changsha 410208, Hunan, Peoples R China.;[Chen, Jian-Xiong] Univ Mississippi, Med Ctr, Dept Pharmacol & Toxicol, 2500 N State St, Jackson, MS 39216 USA.
通讯机构：
[Chen, Jian-Xiong] U;Univ Mississippi, Med Ctr, Dept Pharmacol & Toxicol, 2500 N State St, Jackson, MS 39216 USA.
摘要：
Diabetes is associated with impairment of angiogenesis such as reduction of myocardial capillary formation. Our previous studies demonstrate that disruption of Angiopoietin-1 (Ang-1)/Tie-2 signaling pathway contributes to the diabetes-associated impairment of angiogenesis. Protein tyrosine phosphatase (PTP) has a critical role in the regulation of insulin signal by inhibition of tyrosine kinase phosphorylation. In present study, we examined the role of protein tyrosine phosphatase-1 (SHP-1) in diabetes-associated impairment of Ang-1/Tie-2 angiogenic signaling and angiogenesis. SHP-1 expression was significantly increased in diabetic db/db mouse hearts. Furthermore, SHP-1 bond to Tie-2 receptor and stimulation with Ang-1 led to SHP-1 dissociation from Tie-2 in mouse heart microvascular endothelial cell (MHMEC). Exposure of MHMEC to high glucose (HG, 30 mmol/L) increased SHP-1/Tie-2 association accompanied by a significant reduction of Tie-2 phosphorylation. Exposure of MHMEC to HG also blunted Ang-1-mediated SHP-1/Tie-2 dissociation. Knockdown of SHP-1 significantly attenuated HG-induced caspase-3 activation and apoptosis in MHMEC. Treatment with PTP inhibitors restored Ang-1-induced Akt/eNOS phosphorylation and angiogenesis. Our data implicate a critical role of SHP-1 in diabetes-associated vascular complications, and that upregulation of Ang-1/Tie-2 signaling by targeting SHP-1 should be considered as a new therapeutic strategy for the treatment of diabetes-associated impairment of angiogenesis.
作者：
Ling, H. -y.;Hu, B.;Hu, X. -b.;Zhong, J.;Feng, S. -d.;...
期刊：
Experimental and Clinical Endocrinology and Diabetes,2012年120(9):553-559 ISSN：0947-7349
通讯作者：
Liao, D. -f.
作者机构：
[Ling, H. -y.; Hu, B.] Univ S China, Sch Med, Dept Physiol, Hengyang, Peoples R China.;[Liao, D. -f.] Hunan Univ Chinese Med, State Key Lab Chinese Med Powder & Med Innovat Hu, Div Stem Cell Regulat & Applicat, Changsha 410208, Hunan, Peoples R China.;[Ling, H. -y.] Univ S China, Ctr Basic Med Postdoctoral Studies, Hengyang, Peoples R China.;[Hu, X. -b.] Univ S China, Sch Life Sci & Technol, Dept Biochem & Mol Biol, Hengyang, Peoples R China.;[Wen, G. -b.; Zhong, J.] Univ S China, Affiliated Hosp 1, Inst Clin Res, Hengyang, Peoples R China.
通讯机构：
[Liao, D. -f.] H;Hunan Univ Chinese Med, State Key Lab Chinese Med Powder & Med Innovat Hu, Div Stem Cell Regulat & Applicat, Changsha 410208, Hunan, Peoples R China.
摘要：
At 8 weeks after intragastric administration of icariin to senescence-accelerated mice (P8 strain), Morris water maze results showed that escape latency was shortened, and the number of platform crossings was increased. Immunohistochemical staining and western blot assay detected significantly increased levels of cyclic adenosine monophosphate response element binding protein. These results suggest that icariin upregulates phosphorylated cyclic adenosine monophosphate response element binding protein levels and improves learning and memory functions in hippocampus of the senescence-accelerated mouse.
作者机构：
[Deng, Chang-Qing; Chen, Gang] Hunan Univ Tradit Chinese Med, Pathophysiol Lab, Changsha, Hunan, Peoples R China.;[Wu, Lu] Hunan Univ Tradit Chinese Med, Affiliated Tradit & Western Med Hosp 2, Changsha, Hunan, Peoples R China.;[Deng, Chang-Qing] Hunan Univ Tradit Chinese Med, Pathophysiol Lab, Shaoshan Rd 113, Changsha, Hunan, Peoples R China.
通讯机构：
[Deng, Chang-Qing] H;Hunan Univ Tradit Chinese Med, Pathophysiol Lab, Shaoshan Rd 113, Changsha, Hunan, Peoples R China.
关键词：
BuYang HuanWu Decoction;Vascular smooth muscle cell;Platelet derived growth factor;Proliferating cell nuclear antigen;c-fos;CyclinD(1);Extracellular regulated protein kinases1/2;Mitogen-activated protein kinase;phosphatase-1
摘要：
Buyang Huanwu Decoction (BYHWD) was a commonly used traditional Chinese medicine for the treatment and prevention of ischemic cardiovascular and cerebral disease. Previous studies had shown that BYHWD alkaloids and glycosides could inhibit intimal hyperplasia and vascular smooth muscle cell (VSMC) proliferation after injury caused by balloon catheter. The present study aims to explore the mechanisms by which cell cycle was affected by BYHWD and its components. Primary rat VSMC was treated with platelet-derived growth factor (PDGF) and cell cycle phase and extracellular-signal regulated protein kinase (ERK) transduction pathway factors were measured. PDGF-treated cells were associated with a significant increase in the number of cells in the G(2)/M phase and S phase, and in the expression of P-ERK1/2, proliferating cell nuclear antigen (PCNA), c-fos, cyclinD(1) and cyclin-dependent kinase-4, as well as a decrease in the number of cells in the G(0)/C(1) phase, and in the expression of cyclin-dependent kinase inhibitor P21 protein and mitogen-activated protein kinase phosphatase-1 (MKP-1). Treatment with plasma of rats fed seven doses of BYHWD crude extract (22.2 g/kg), BYHWD alkaloids (1.66 g/kg), BYHWD glycosides (14.2 g/kg) or the negative control atorvastatin (20 mg/kg) inhibited these changes. All drug-containing plasma had similar activity to the mitogen activated protein kinase (MAPK)/ERK antagonist PD098059 which inhibited PDGF-induced expression of P-ERK1/2 and enhanced MKP-1. These suggest that BYHWD and its components may prevent VSMC proliferation by interfering with the ERK transduction pathway. (C) 2011 Elsevier Ireland Ltd. All rights reserved.
