The α4β2-nicotinic acetylcholine receptor (nAChR) is a ligand-gated ion channel that is distributed throughout the nervous system. It is involved in the regulation of various neurotransmitters including acetylcholine, dopamine, γ-aminobutyric acid, and norepinephrine. α4β2-nAChR plays an important role in learning, memory, cognition, attention, inflammation, and pain. A large number of studies have shown that α4β2-nAChR is an important therapeutic target for neurological diseases such as Alzheimer's disease, Parkinson's disease, epilepsy, depression, nicotine dependence, pain, etc. It is an important target in the early diagnosis and curative effect detection of neurodegenerative diseases including Alzheimer's disease. This review summarizes the role, mechanisms and related drug research advances on α4β2-nAChR ligand drugs in neurological diseases, as well as providing a theoretical basis for identifying and developing more suitable α4β2-nAChR-related compounds.

To investigate the chemical constituents of the whole plants of Bidens bipinnata, the separation and purification of constituents were performed by chromatography on macroporous resin, silica gel, MCI and Sephadex LH-20. Their structures were elucidated by spectroscopic data as quercetin (1), quercetin-3-0-alpha-L-rhamnoside (2), keampferol-3-O-beta-D-glucopyranoside (3), keampferol-3-O-alpha-L-rhamnoside (4), 3', 5-dyhydroxy-3, 6, 4'-trimethoxyl -7-O-beta-D-glucopyranoside flavonoid (5), 7, 8, 3', 4'-tetraflavanone(6), (2S)- and (2R)-isookanin-7-O-beta-D- glucopyranoside (7a/7b), (2S)- and (2R)-3'-methoxy-isookanin-8-O-beta-D-glucopyranoside (8a/8b), 6, 7, 3', 4'-tetrahydroxyaurone(9), maritimetin (10), esculetin (11), 3-O-caffeoyl-2-methyl-d-erythrono-1, 4-lactone (12), (7S, 8R) balanophonin-4-O-beta-D-glucopyranoside (13), eugenyl-O-beta-apiofuranosyl-( 1"-6') -O-beta-glucopyranoside (14), and (+)-syringaresinol-4'-O-beta-D-glucopyranoside (15). Compounds 8, 13, 14, and 15 were isolated from this genus for the first time. Compounds 1 and 6 were potent inhibitors against HSC-T6 cells in vitro and compounds 1, 2, 6, and 7 were capable of decreasing the inflammatory cytokine production of macrophage cells in vitro.
Bidens ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization

The paper is aimed to establish a methods for identication of pearl powder and conch powder from different origins. Hermetic aluminum pan was used to encapsulate samples. The optimal testing conditions were: heating rate 10 degrees C x min(-1), sample weight 3 mg and nitrogen gas flow rate 40 mL x min(-1). The enthalpy values of pearl powder and conch powder was obvious different. Identication of pearl powder and conch powder by DSC is a practical method for its accuracy, convenience and practificality.
Animal Shells ; chemistry ; Animals ; Calorimetry, Differential Scanning ; methods ; China ; Discriminant Analysis ; Pinctada ; chemistry ; classification ; Powders ; chemistry

OBJECTIVE To evaluate the effect of Guizhi Fuling Capsule active pharmaceutical ingredient (API) and its fractions on human breast cancer cells proliferation by high-throughput screening assay. METHODS The crude fractions were obtained from the extraction and elution of the API of Guizhi Fuling Capsule, and 929 standard fractions were obtained by the optimal separation conditions. Sulforhodamine B (SRB) method was used to evaluate the effects of the Guizhi Fuling capsule API and 929 kinds of fractions on the proliferation of human breast cancer cells MCF- 7 and MDA- MB- 231. RESULTS The Guizhi Fuling capsule API had a strong ability to inhibit the proliferation of MCF-7 cells at high concentration and the ability to inhibit MDA-MB-231 cells' proliferate at low concentration follow?ing 72 h treatment;some samples of 929 fractions (5 μg·mL-1) was found to have a breast cancer cell growth inhibition rate above 50%, without toxicity on HUVECs proliferation. CONCLUSION The API of Guizhi Fuling capsule had significant cytotoxicity effects on these two human breast cancer cells, with significant concentration- and time-dependent manner.

[Objective]To investigate the etiology,clinical manifestation,treatment and prognosis of optic disc vas-culitis.[Method]Twenty-four eyes of 21 patients were enrolled in this retrospective study.Eye examinations,treatment, and effect were recorded.[Result]Six were male and 15 were female.The age was between 19 and 43 years old(average:28.7±1.6).85.7% of the patients referred to the clinic with mild to moderate decreased vision.Edema of the optic disc can be seen in both types while tortuous veins can also be found in type 2.Similar characteristics were noticed in OCT,FFA, and etc.With a follow-up of 4.52±0.98 months after treatment(prednisone:initial dose 1.0-1.2 mg/kg),the BCVA of the affected eyes improved significantly.[Conclusion]Optic disc vasculitis is affected by autoimmune disorder,infection,hy-perlipidemia,and etc.Edema of the optic disc with/without tortuous veins and retinal hemorrhage can be noticed.Similar diseases should be excluded in avoidance of misdiagnosis. Systemic examination and complete solution should be per-formed.Glucocorticoid helps to improve the visual function.The application of anti-VEGF is effective in secondary macu-lar edema.However,the long-term efficacy is awaiting being confirmed.

Objective To investigate the clinical and imaging features of patients with Alzheimer' s disease (AD) and vascular dementia (VaD) and find an effective method to make differential diagnosis between the 2 entities. Methods One hundred and sixty-two patients with dementia,admitted to our hospital from August 2006 to June 2011, and 42 patients with dementia found from community epidemiological survey were chosen in our study; their clinical data were retrospectively collected and analyzed; in these patients,114 patients were with AD and 90 patients were with VaD.Mini Mental State Examination (MMSE) was performed on these patients and the cognitive competence,behavioral symptoms and imaging data of these patients were analyzed and compared. Results More female,higher education level and longer course of disease in patients with AD were noted as compared with those in patients with VaD (P＜0.05); the scores of attention and calculation in patients with VaD were obviously lower than those in patients with AD (P＜0.05); the scores of short-term memory,retelling and reading comprehension in patients with VaD were obviously higher than those in patients with AD (P＜0.05); the happening of repeated convergence behavior in patients with AD was much more often than that in patients with VaD (P＜0.05); patients with AD had higher ratio of shrinking hippocampus than patients with VaD, and the incidence of vascular disease in the brain of patients with VaD was significantly higher than that of patients with AD (P＜0.05). Conclusion Substantial differences on clinical and imaging features exist in AD and VaD patients,which can be attributed to the differences of lesion nature and distribution,as well as the underlying pathophysiological procedures of each disease.

AIM:To observe the changes of autophagy-related indexes during endoplasmic reticulum stress (ERS) induced by dithiothreitol (DTT) and its effect on apoptosis in human normal hepatocytes.METHODS:LO2 cells were treated with DTT at 2.0 mmol/L for 0, 6, 12 and 24 h to induce ERS.The expression of glucose-regulated protein 78 (GRP78) , protein kinase R-like endoplasmic reticulum kinase (PERK) , activating transcription factor 4 (ATF4) , C/EBP homologous protein (CHOP) , autophagy-related gene 12 (Atg12) , autophagy-related gene 5 (Atg5) and microtubule-associated protein 1 light chain 3 (LC3) at mRNA and protein levels was determined by real-time PCR and Western blot.The apoptosis was analyzed by flow cytometry.The formation of autophagosomes was observed under transmission electron microscope.After the LO2 cells were pretreated with rapamycin at 400 nmol/L for 1 h and treated with DTT at 2.0mmol/L for 24 h, the effect of rapamycin pretreatment on the apoptosis was analyzed by flow cytometry.RESULTS:After treatment with DTT at 2.0 mmol/L for 6, 12 and 24 h, the mRNA and protein levels of GRP78, PERK, ATF4, CHOP, Atg12, Atg5 and LC3 in the LO2 cells were significantly higher than those in 0 h group (P<0.05).At the same time, the ratio of LC3Ⅱ/LC3Ⅰwas also increased after DTT treatment (P<0.05).Observation under transmission electron microscope showed that autophagosomes were found in the LO2 cells treated with DTT for 6, 12 and 24 h.After DTT treatment for 6, 12 and 24 h, the apoptosis rate of LO2 cells was significantly higher than that in DTT 0 h group, while the apoptosis induced by DTT was significantly decreased after rapamycin pretreatment (P<0.05).CONCLUSION:ERS induces autophagy and rapamycin pretreatment alleviates the apoptosis of LO2 cells to some extent.

AIM:To investigate the effect of SET7/9 (SET domain containing 7/9) -mediated endoplasmic reticulum stress (ERS) on protein kinase R-like endoplasmic reticulum kinase (PERK) signaling pathway, and to explore the mechanisms of arsenic-induced hepatocyte apoptosis.METHODS:Human liver LO2 cells were divided into control group, arsenic poisoning model group, negative transfection group and SET7/9 siRNA transfection group.The apoptosis of the LO2 cells in each group was analyzed by flow cytometry.The protein levels of SET7/9, glucose-regulated protein 78 (GRP78) , PERK and p-PERK in the LO2 cells of each group were observed by Western blot.RESULTS:Inhibition of SET7/9 expression reduced the apoptotic rate of arsenic-induced LO2 cells.Arsenic exposure increased the expression of SET7/9 in the LO2 cells.Arsenic exposure increased the protein levels of GRP78 and p-PERK in the LO2 cells, but decreased the protein levels of GRP78 and p-PERK after transfection with SET7/9 siRNA (P<0.05).CONCLUSION:Arsenic exposure induces hepatocyte apoptosis by increasing SET7/9 to activate ERS by PERK signaling pathway.

Objective To summarize the thoracolumbar injuries and treatment in children and adolescents.Methods Since 2000,clinical data,surgical methods,efficacy and mechanism of 177 children and adolescents with thoracolumbar spine injury treated in Honghui Hospital of Xi'an Jiaotong University School of Medicine were analyzed and compared.Treatment was in accordance with easy typing method of Honghui Hospital of Xi'an Jiaotong University School of Medicine.The principles and systematic methods of analysis of such damage was emphasized.Clinical,physiological and psychological effects were observed.Results According to easy typing method of Honghui Hospital of Xi'an Jiaotong University School of Medicine.Ⅰ a-c 77 cases,Ⅱ a 40 cases.Twenty-seven cases of Frankel A were unchanged.There were 28 cases that had been restored to Frankel C in 30 cases of Frankel B.There were 2 cases that had been restored to Frankel D in 30 cases of Frankel B.There were 2 cases that had been restored to Frankel D in 27 cases of Frankel C.There were 25 cases that had been restored to Frankel E in 27 cases of Frankel C.There were 30 cases that had been restored to Frankel E in 30 cases of Frankel D.In 177 patients,imaging,VAS,ODI,SF-36,DPQ,MMSE,Barthel and psychology had achieved significant differences before and after treatment for follow-up of 7-12 months(all P ＜ 0.05).Conclusions Simple type is easy to grasp.It applies to children and adolescents treatment of thoracic and lumbar spine injury to good effect.It is a reasonable treatment strategy.