ObjectiveTo investigate the relationship between carotid intima-media thickness (IMT)and plaque extent of carotid artery with coronary heart disease (CHD).Methods 131 inpatients were divided into 3 groups,in which 54 cases of coronary heart disease group,46 cases of risk group with coronary heart disease,31 cases of control group.The carotid wall IMT,plaque length and thickness was measured by Color Doppler ultrasound.The obtained data using SPSS 17.0 software for statistical processing.ResultsCarotid intimal thickening and the incidence had no significant difference between the group of coronary heart disease and risk group with coronary heart disease risk( all P ＞ 0.05),carotid artery IMT and incidence rate between the above two groups and the control group had statistical differene( t =3.26,3.48,all P ＜ 0.05 ),and the three groups of carotid artery plaque score and plaque classification were statistically significant( F =4.28,P ＜ 0.05 ).ConclusionCarotid IMT and plaque formation was the independent risk factor of CHD,and it could predict the occurrence and development of CHD,especially in carotid artery plaque specificity is higher,in the primary hospital could be used as the auxiliary examination method of CHD.

AIM: To study the bioequivalence of domestic and imported Metoprolol Tartrate Tablets in Chinese healthy volunteers.METHODS: According to the rule published by SFDA,the serum concentration of 20 selected volunteers among 18 to 40 years old was determined by HPLC-fluorescence detection after giving domestic and imported Metoprolol Tartrate Tablets 0.1g,and the pharmacokinetic parameters were calculated by DAS software.RESULTS: The method of HPLC-fluorescence detection to study the pharmakokinetics of Metoprolol Tartrate was sensitive,reliable,accurate and reasonable.The main pharmakokinetics parameters of domestic and imported Metoprolol Tartrate Tablets were T_(max):(1.11)?(0.36 h) and(1.39)?(0.65 h) respectively;C_(max):(269.20)?(87.15)(?g?L~(-1)) and(262.03)?(75.52)(?g?L~(-1)) respectively;AUC_(0-12h):(1088.91)?(510.52)(?g?L~(-1)?h) and(1098.29)?5(55.14)(?g?L~(-1)?h) respectively.The relative bioavailability of domestic Metoprolol Tartrate Tablets was(100.09)%.CONCLUSION: The domestic and imported Metoprolol Tartrate Tablets was bioequivalents.

Objective HupA is one of the potential drugs which can be used to treat Alzheimer's disease(AD).The aim of this study was to explore the pharmacokinetics and biodistribution of HupA in vivo by using 11C-HupA.Methods A total of 25 SD rats were studied.They were divided into 5 groups (5 rats in each group).All had intravenous injection of 22 MBq(in0.2 ml)11C-HupA through tail vein.Dynamic im-aging Was acquired from 5 to 90 minutes after injection.Venous blood and organ activities were collected at 5,15,30,60.and 90 minutes after injection.Percentage activity of injected dose per gram of tissue(%ID/g)was calculated to characterize the biodistribution of tracer in different brain regions: frontal,apical, temporal,occipital,cerebellum,hippocampus,striatum,thalamencephalon, and brain stem, Variance analysis using SPSS 11.5 software was performed and compared among the study groups.Results 11C-HupA was character-istic for its quick clearance from blood,with half time T1/2 of (14.61±1.77) min,and clearance rate (CL)macokinetics of 11C-HupA in rats corresponded to a one-compartment model.with an activity curve(area 11C-HupA distribution in different brain regions,being greater in cerebral cortex,hippocampus,hypothala-mus and brain stem. Conclusions Pharmacokinetic study of 11C-HupA in brain was fast.convenient and showed high specificity and sensitivity.Its ability to quantitatively evaluate brain function and its character-istic distribution in mice provided some evidence for monitoring therapy in AD patients.

Humans ; Sinus of Valsalva ; Death, Sudden, Cardiac/etiology* ; Coronary Stenosis/complications*

In the treatment of hypertensive crisis, the novel Rho kinase inhibitor DL0805-2 can rapidly lower systematic blood pressure, reduce pulmonary artery pressure, and has a significant protective effect on lung injury. This experiment intends to evaluate the efficacy of DL0805-2 against pulmonary arterial hypertension (PAH) and preliminarily reveals its underlying mechanism. Animal welfare and experimental procedures are in accordance with the provision of the Animal Ethics Committee of the Institute of Materia Medica, Chinese Academy of Medical Sciences. Sprague Dawley (SD) rats were randomly divided into DL0805-2 low, medium, and high dose groups (1, 3, and 10 mg·kg^-1), bosentan positive control group, model group, and blank control group. The drug was administered daily on the 7th day after model establishment by monocrotaline injection. On the 25th day of the experiment, relevant indicators were examined to observe the therapeutic effect of DL0805-2 on pulmonary hypertension. DL0805-2 significantly relieved the abnormal changes in the physiological parameters related to PAH induced by monocrotaline, including reducing right ventricular systolic pressure, alleviating cardiac damage caused by pressure overload, and reducing the levels of endothelin-1 and inflammatory factors in lung tissues. DL0805-2 also attenuated pulmonary arteries remodeling. It was preliminarily discovered that DL0805-2 exerts preventive and therapeutic effect on PAH through Rho-kinase pathway. Our results suggested that DL0805-2 had good therapeutic effects on monocrotaline-induced PAH rat model. It intervened early in the disease process, effectively prevented the development of the disease, and reduced the mortality of the diseased animals. The mechanism is related to Rho-kinase pathway.

Curcumin is the principal curcuminoid of the rhizomes of Curcuma longa(turmeric,Jiang Huang), which has more than 6000 years of application history in India and other Asian countries. At present,curcumin is sold as an herbal supplement,cosmetics ingredient,food flavoring,and food coloring. In China curcumin is mainly used in food, while in western countries it has been regarded as a health care product and is contained in the British Pharmacopoeia (2017), United States Pharmacopeia (40) and European Pharmacopoeia (8.7th ed.). Curcumin has been proved to have multiple pharmacology effects including anti-fibrosis, anti-tumor, anti-inflammation effects and so on. As its broad biological activities, it is applicated in a lot of diseases such as hyperlipidemia, infection and cancer. Among them, the anti-cancer effect of curcumin is the most attractive. In the treatment of cancer and related diseases, curcumin has been tested in phase I and II clinical trials in several research centers across the world and has been approved by the U.S.FDA into the phase III clinical trial.It has been listed as the third generation of cancer chemoprevention agent by the U.S.National Cancer Institute.Curcumin has been proved to inhibit the proliferation of a variety of tumor cells through regulating a variety of tran-scription factors(NF-κB,AP-1,etc),mitogen-activated protein kinase(MAPK),growth factor receptor ki-nase(PDGFR,VEGFR,etc)and cyclooxygenase.It plays an important role in the cell cycle and further to inhibit proliferation.Curcumin can also inhibit the migration of tumor cells by activating caspase and in-ducing tumor cell apoptosis.However,curcumin still needs researches to confirm its effects and mecha-nisms and find its exact indications. There is still a long way to go to make curcumin better applied in clinical practice in the further.

This study investigated the effect of puerarin on human umbilical vein endothelial cells (HUVEC) injured with hydrogen peroxide (H₂O₂). HUVEC were divided into three groups: a control group, a model group (H₂O₂ 400 μmol·L^-1) and a puerarin-treated group (3, 10, 30 and 100 μmol·L^-1). HUVEC were cultured with varied concentration of puerarin for 2 h and treated with H₂O₂ for another 24 h. Cell proliferation was detected by a CCK-8 assay. The mitochondrial membrane potential was measured by a JC-1 fluorescent probe. A transwell chamber assay was adopted to observe cell migration ability. Mitochondrial respiratory function was measured in a two-chamber titration injection respirometer (Oxygraph-2k). The expression of interleukin-1β (IL-1β), interleukin-18 (IL-18) and tumor necrosis factor-α (TNF-α) was detected by quantitative real-time PCR. The expression of pyroptosis-mediated proteins, including cleaved-cysteinyl aspartate-specific proteinase-1 (caspase-1), N-gasdermin D (N-GSDMD), NOD-like receptor protein 3 (NLRP3) and purinergic ligand-gated ion channel 7 receptor (P2X7R) was detected by Western blot. The results show that 400 μmol·L^-1 H₂O₂ treatment for 24 h causes obvious damage to HUVEC. Compared with the model group, puerarin protected against cellular injury in a dose-dependent manner, with the greatest effect at a dose of 30 and 100 μmol·L^-1. Puerarin significantly decreased the mitochondrial membrane potential and improved mitochondrial function. Puerarin inhibited cell migration induced by H₂O₂, suppressed the expression of IL-1β, IL-18 and TNF-α, and down-regulated the pyroptosis-mediated protein. These changes are statistically significant (P < 0.05). These findings demonstrate that puerarin has a protective effect against H₂O₂-induced oxidative damage of HUVEC by inhibiting the migration of HUVEC cells. The mechanism may be related to improved mitochondrial respiratory function and inhibition of pyroptosis.

Tumor brings great threat to human public health. In recent years, incidence rate and mortality of tumor were rapidly increased in the world. Anti-tumor therapies have undergone the development of cytotoxic therapy, targeted therapy, and immunotherapy. Among them, tumor immunotherapy is rapidly developed and becomes an important anti-tumor therapy in recent years, although it also brings some related side effects. Tumor microenvironment (TME) is composed of immune cells, vascular vessels, fibroblasts, the extracellular matrix, etc. TME significantly affects the efficacy of immunotherapy. Macrophages in the TME are named as tumor associated macrophages (TAMs). Recently, increasing studies have shown that TAMs play an important role in the regulation of tumor immunity, especially in tumor immune surveillance and immune escape. Currently, more and more anti-tumor immunotherapy strategies targeting TAMs are at the development stage. Based on the important role of TAMs in the TME and their potential as therapeutic targets in tumor immunotherapy, we first reviewed the subtypes and functions of TAMs, as well as the roles of TAMs in tumors. Furthermore, we summarized the research progress on anti-tumor strategies targeting TAMs and the current status of drug targeting TAMs. The current review will provide new ideas and novel insights for tumor immunotherapy.

The purpose of the present study was to investigate the effect of chronic intermittent hypobaric hypoxia (CIHH) on α(1)-adrenergic receptors and the role of alpha(1)-adrenergic receptors in the protection of CIHH against ischemic injury of myocardium. Sixty-six adult male Sprague-Dawley rats were randomly divided into four groups: control group (Con), 14-day CIHH treatment group (CIHH14), 28-day CIHH treatment group (CIHH28) and 42-day CIHH treatment group (CIHH42). CIHH rats were exposed to hypoxia mimicking 5 000 m altitude (p(B)=404 mmHg, p(O(2))=84 mmHg) in a hypobaric chamber, 6 h daily for 14, 28 and 42 d, respectively. Control animals lived in the same environment as CIHH animals except hypoxia exposure. After anesthesia with sodium pentobarbital (3.0-3.5 mL/kg body weight, i.p.), papillary muscle was taken from the right ventricle of rat and perfused with modified Tyrode's solution continuously, at constant temperature (37 °C) and perfusion speed (12 mL/min). Muscle contraction was evoked by electric stimuli. Different concentrations (1x10(-7), 1x10(-6) and 1x10(-5) mol/L) of phenylephrine (PE), an alpha(1)-adrenergic receptor agonist, were applied cumulatively to investigate the effect of PE on the mechanic contraction of right ventricular papillary muscles of rats in Con, CIHH14, CIHH28 and CIHH42 groups. Also, prazosin (1x10(-6) mol/L), an α(1)-adrenergic receptor antagonist, was used to investigate the role of α(1)-adrenergic receptor in the protective effect of CIHH on papillary muscle. The results showed: (1) PE increased the maximal isometric tension (P(max)) and maximal velocity of tension development (P(dT/dt)) of muscle contraction in a dose-dependent manner (P<0.05), and the increase of the muscle contraction was much greater in CIHH28 and CIHH42 rats than that in Con rats (P<0.05). Under 1x10(-5) mol/L of PE, the increases of P(max) and P(dT/dt) over the baseline were 51.2% and 44.5% in CIHH28 group, 48.6% and 44.5% in CIHH42 group, and 28.7% and 24.5% in Con group, respectively; (2) The contraction of papillary muscle decreased during simulated ischemia, but the decrease was slighter in CIHH rats than that in Con rats (P<0.05). The decreases in P(max) and P(dT/dt) were 59.6% and 53.6% in CIHH28 group, 60.4% and 49.9% in CIHH42 group, and 74.4% and 64.7% in Con group, respectively; (3) The protective effect of CIHH on ischemic papillary muscle was abolished by prazosin (1x10(-6) mol/L). The results of the present study suggest that CIHH increases the activity of α(1)-adrenergic receptor, which is possibly one of the mechanisms for the cardioprotection of CIHH.
Altitude ; Animals ; Heart Ventricles ; physiopathology ; Hypoxia ; metabolism ; Male ; Muscle Contraction ; Myocardium ; metabolism ; Papillary Muscles ; metabolism ; Rats ; Rats, Sprague-Dawley ; Receptors, Adrenergic, alpha-1 ; metabolism

OBJECTIVETo evaluate the efficacy and safety of transoral plate internal fixation for instability atlas fracture.

METHODSA retrospective study was performed in eight patients with instability atlas fractures, who were treated by a transoral plate internal fixation from July 2007 to June 2011. There were 6 males and 2 females,with an average age of 39.5 years old ranging from 23 to 48 years. Among them, 5 case were falling injury, 3 cases were traffic accident injury. Three patients had bilateral fractures of the anterior arch (prehalf Jefferson fractures, Landells type I), 5 had anterior are fracture associated posterior are fracture (Half-ring Jefferson fractures, Landells type II), and 2 had anterior and posterior are fracture associated with single lateral mass fractures (Landells type III).

RESULTSAll patients were followed up for 6 to 24 months after operation (av- eraged 13 months), and all the patients had the clinical symptoms improved to some extent. Operation time ranged from 80 to 140 min (averaged 98 min); the intra-operative blood loss was 120 to 300 ml (averaged 180 ml); and the average fluoroscopic time was 55 s. No patients happened neurological and vertebral artery injuries-related complications or other complications after operation. The followed-up X-ray and CT manifested osseous fusion in all the 8 patients,no loosening or breakage of the screws.

CONCLUSIONTransoral plate internal fixation for instability atlas fracture is a reliable and safety technique that allows maintenance of rotatory mobility in the C1,2 joint and restoration of congruency in the atlanto-occipital and atlanto-axial joints.

Adult ; Bone Plates ; Cervical Atlas ; injuries ; surgery ; Female ; Fracture Fixation, Internal ; methods ; Fractures, Bone ; surgery ; Humans ; Male ; Middle Aged ; Retrospective Studies