Objective To study the clinical efficacy and safety of clopidogrel combined with aspirin in doub-le loading dosage and ordinary dosage in the treatment of acute non -cardiac cerebral infarction.Methods A total of 110 patients with acute non -cardiac infarction were equally assigned into two groups,each group had 55 patients.The patients in group A were treated with clopidogrel 300mg and aspirin 300mg on the 1st day,and followed by clopidogrel 75mg and aspirin 100mg every day.Patients in group B were treated with clopdogrel 75mg and aspirin 100mg every day.Clinical efficacy and safety were evaluated in one week,NIHSS scores were evaluated,and adverse effects were recorded during treatment.Results After one week treatment,the deteriorate rates of group A and B were 12.7%, 18.2%.Compared with group B,group A had lower cerebral infarction deteriorate rate,but there was no statistically significant difference(P =0.429).After seven days treatment,the NIHSS score of A group had improved[(4.42 ± 3.34)points vs.(3.15 ±2.58)points],the difference was statistically significant(t =3.713,P <0.01 ),which in group B had no significant improvement[(4.16 ±2.76)points vs.(3.80 ±3.15)points,t =1.209,P =0.232].After seven days treatment,the NIHSS score improvement of group A was (1.27 ±2.54)points,which of group B was (0.36 ±2.23)points,the difference was statistically significant(t =1.994,P =0.049).No severe adverse effects occurred in both two groups.Conclusion Using clopidogrel combined with aspirin in double loading dosage may effectively attenuate stroke process and improve prognosis than ordinary dosage.Using clopidogrel combined with aspirin had no severe adverse effects in short -term treatment of acute non -cardiac cerebral infarction.

Objective To explore the suitable type of macroporous adsorbent resin to purity swertiaman from Swertia pesudochinensis Hara., and determine the parameters and conditions for its purification procedures. Method Purification effect of 8 types of macroporous resins used to purify the Swertia pesudochinensis Hara. were inspected, with the content of swertiaman as index. Result HPD-100 type resin showed better effect than others, it had optimum adsorption and elution parameters with its dynamic saturated adsorption ratio was 70.48 mg/g. After eluted with 2 BV of distilled water, 4 BV 30% ethanol and collected, the content of swertiaman in the spray dried powder was 52.29%. Conclusion HPD-100 types macroporous resin showed a better comprehensive adsorption property and can be used to enrich and purify the swertiaman included active fraction of iridoid glycosides for industrialization.

ObjectiveTo assess different treatments on nonspecific low back pain.Methods246 subjects were assigned to 3 groups, a control group(n=82), a home exercise group(n=82) or a strengthening exercise group(n=82). Follow-up data were obtained at 1 months, 3 months and 6 months after the treatment. Primary outcome measures were modified Oswestry Low Back Pain Disability Questionnaire for disability and Numeric Pain Rating Scale for pain.ResultsThe home exercise and strengthening exercise groups experienced greater improvements in disability than the control group 6 months after the treatment. The strengthening exercise group demonstrated greater change than home exercise group.ConclusionActive rehabilitation therapy may benefit nonspecific low back pain patients.

Objective To evaluate the value of three dimensional CT angiography in the diagnosis of intracranial aneurysms by the comparison with DSA.Methods CTA and DSA were performed in 30 patients(aged 34~76 years) who were highly suspected with intracranial aneurysms.Feasible endovascular treatment were performed simultaneously.The sensitivity,specificity,accuracy in detecting the aneurysms,in demonstrating the neck of the aneurysms and the relationship of parent artery were compared between CTA and DSA.Results 26 intracranial aneurysms were detected by CTA,the sensitivity,sepcificity and accuracy were 95.5%,87.5% and 93.3% respectively.There were no statistical differences among the sensitivity,specificity,accuracy between CT and DSA(?

Objective:To establish and validate a malignant risk prediction model of solitary pulmonary nodules (SPNs) with pulmonary fibrosis in long-term smokers based on 18F-flurodeoxyglucose (FDG) PET/CT. Methods:PET/CT images of 222 SPNs combined with pulmonary fibrosis which were shown in integrated CT scan in 169 patients (all males; age 68(63, 75) years) were analyzed retrospectively. All patients were examined in PET/CT Center of the Affiliated Hospital of Qingdao University from January 2011 to December 2019 and all had definite smoking history. The benign and malignant nodules were judged according to the pathological diagnosis or follow-up imaging data of lung lesions (follow-up≥2 years). The clinical characteristics (age, smoking index), morphological characteristics (longest diameter of lesion, density, location, distribution, relative position of fibrosis, spiculation, lobulation, calcification, vacuole, vascular convergence, pleural indentation, emphysema and severity of bilateral pulmonary fibrosis) and metabolic characteristics (maximum standardized uptake value (SUV max)) of the benign and malignant lesions were analyzed by χ2 test and Mann-Whitney U test. Then multivariate logistic regression analysis was applied to select independent risk factors of malignant nodules, and a risk prediction model was established and verified by the area under the receiver operating characteristic (ROC) curve and k-fold cross validation ( k=10) respectively. Results:Among 169 patients, 222 SPNs were detected (157 malignant nodules, 65 benign nodules). Univariate analysis showed that smoking index, speculation, lobulation, vascular convergence sign, calcification, emphysema, nodule size, relative position of nodule and fibrosis, SUV max and severity of bilateral pulmonary fibrosis were significantly different between the benign and malignant nodules ( z values: 2.514-9.858, χ2 values: 4.353-18.442, all P<0.05). Result of multivariate logistic regression analysis showed that calcification, vascular convergence and SUV max were the independent risk factors of malignant nodules combined with pulmonary fibrosis (odds ratio ( OR): 0.048-2.534, all P<0.05). The risk prediction model was as follow: P=1/(1+ e - x), x=-1.839-3.033×calcification+ 0.930×vascular convergence+ 0.754×SUV max(with calcification/vascular convergence=1, without calcification/vascular convergence=0). The area under ROC curve was 0.932(95% CI: 0.895-0.969), and the sensitivity and specificity of the model were 87.9% and 86.2%, respectively. Results of k-fold cross validation showed that the prediction accuracy of 10 test sets was 0.847±0.075, and was 0.862±0.010 in training sets. Conclusions:Calcification, vascular convergence and SUV max are independent risk factors of malignant SPNs combined with pulmonary fibrosis in long-term asymptomatic smokers. The model based on the above variables presents high diagnostic efficiency in diagnosing malignant SPNs.

Objective To study the regional cerebral glucose utilization with 18 F-fluorodeoxyglucose (FDG) PET and to investigate the correlation between cerebral glucose metabolism and the clinical characteristic of progressive supranuclear palsy (PSP).Methods A total of 13 patients with PSP and 30 matched healthy controls were performed 18F-FDG PET imaging at rest state.Visual inspection and statistical parametric mapping (SPM) were used to investigate regional cerebral metabolic rate of glucose (rCMRglc).Results Based on the visual inspection,PET imaging in the PSP patients showed that the focal hypometabolic areas mainly included the bilateral frontal cortex,midbrain and subcortical structures.Compared to the controls,voxel-based analysis showed that the regional glucose metabolism decreased in bilateral superior,middle frontal gyrus,cingulate gyrus,midbrain and subcortical structures including basal ganglion and thalamus,which were consisted with the clinical characteristics,such as vertical gaze palsy,pseudobulbar palsy,postural instability,axial rigidity,dementia and so on.Conclusion 18 F-FDG PET imaging is helpful for the early diagnosis of PSP.

Taxus is the source plant of anti-cancer drug paclitaxel and its biosynthetic precursor, analogs and derivatives, which has been studying for decades. There are many endemic Taxus species in China, which have been studied in the field of multiple disciplines. Based on the recent studies of the researchers, this review comments on the study of Taxus biology and chemistry. The bibliometric method is used to quantify the global scientific production of Taxus-related research, and identify patterns and tendencies of Taxus-related articles. Gaps are present in knowledge about the genomics, epigenomics, transcriptomics, proteomics, metabolomics and bioinformatics of Taxus and their endophytic fungi. Systems biology and various omics technologies will play an increasingly important role in the coming decades.

The discovery of high performance leading antidiabetic compounds containing sulfonamide and 4-aminophenylacetic acid moieties is reported. This was achieved by the synthesis of 6 intermediates and subsequently 20 target molecules using 4-aminophenylacetic acid as the starting materials, and through a few synthetic routes aided by multi-step reactions including sulfonylation of amino group, deacylation of amides and esterification of carboxyl group, as well as acylation of amino group. The chemical structures of the twenty-four new compounds were determined using 1H NMR, 13C NMR and HR-MS techniques. Screening in vitro of their peroxisome proliferator-activated receptor (PPAR) activation activities showed weak relative PPAR activation activities to most of the target molecules. However, 4 target molecules exhibit PPAR over 58%, and as high as 81.79% for TM2-i, presenting itself as potent leading compound for antidiabetic drugs. This research also confirms that it is probable to achieve esterification of carboxyl group and deacylation of fatty acid N-phenyl amides concurrently in SOCl2/alcohol solvent system. This provides new synthetic method for the selective reaction within molecules containing both carboxyl and N-aryl amido groups of fatty acids.

Twenty five new beta-aminoalcohols containing nabumetone moiety were prepared via the reduction of potassium borohydride with a convenient and efficient procedure, starting from beta-aminoketones that have been synthesized by our group. Their chemical structures were determined by IR, MS, 1H NMR, 13C NMR, HR-MS and antidiabetic activities were screened in vitro. Preliminary results revealed that the antidiabetic activity of most beta-aminoalcohols were better than that of the corresponding beta-aminoketones. Although most compounds showed weak antidiabetic activity, the alpha-glucosidase inhibitory activity of compounds 5hd(1) and 5id(2) reached 74.37% and 90.15%, respectively, which were superior to the positive control. The relative peroxisome proliferator-activated receptor response element (PPRE) activity of five compounds were more than 60%, among them compound 5ca possessed the highest activity (112.59%). As lead molecules of antidiabetic agents, compounds 5hd(1), 5id(2) and 5ca deserve further study.

The design, synthesis and bioevaluation of a series of novel L-tyrosine derivatives as peroxisome proliferator-activated receptor (PPAR) agonists are reported. Four intermediates and twenty L-tyrosine derivatives containing phenoxyacetyl moiety TM1 were synthesized starting from L-tyrosine via four step reactions including the esterification of carboxyl group, phenoxyacetylation of a-amino group, bromoalkylation of phenolic hydroxyl group and then nucleophilic substitution reaction with various heterocyclic amines in 21%-75% overall yield. Subsequently TM1 were hydrolyzed to give sixteen corresponding target compounds TM2 in 77%-99% yield. The chemical structures of the thirty-nine new compounds were identified using 1H NMR, 13C NMR techniques and thirty-five were confirmed by HR-MS techniques. Screening results in vitro showed that the PPAR relative activation activities of the target molecules are weak overall, while compound TM2i reaches 50.01%, which hints that the molecular structures of these obtained compounds need to be modified further.