摘要：Background： Using a cross-sectional design comparison, two overhead press techniques （in-front of the head or behind the head） were compared. The purpose of this study was to determine the impact of behind the head or in-front of the head overhead pressing technique on shoulder range of movement （ROM） and spine posture. The overhead press is commonly prescribed exercise. The two techniques （in-front of the head or behind the head） may influence joint mechanics and therefore require an objective analysis. Methods： Passive shoulder ROM quantified using goniometric measures, dynamic ROM utilised three-dimensional （3D） biomechanical mea- sures （120 Hz） of 33 participants performing overhead pressing in a seated position. The timing and synchronisation of the upper limb shoulder and spine segments were quantified and influence of each technique was investigated. Results： The in-front technique commenced in lordotic position, whilst behind the head technique commenced in kyphotic position. Behind the head technique started with less thoracic extension than in-front condition. The thoracic spine remained extended and moved between 12~ and 15~ regardless of gender or technique. The techniques resulted in a significant difference between genders. Males were able to maintain a flat or normal lumbar lordosis, whereas females tended to kyphotic. Conclusion： Shoulder ROM was within passive ROM for all measures except external rotation for males with the behind the head technique. To avoid possible injury passive ROM should be increased prior to behind the head protocol. Females showed greater spine movements, suggesting trunk strengthening may assist overhead pressing techniques. For participants with normal trunk stability and ideal shoulder ROM, overhead pressing is a safe exercise （for the shoulder and spine） when performed either in-front of or behind the head.

摘要：We hypothesized that neuroprotective agents targeting various pathways involved in cerebral ischemia/reperfusion(I/R)injury might be superior to that targeting single ***,we prepared a fusion protein(B-I)by combining anti-apoptotic Bcl-x L(B)and anti-inflammatory IL-10(I).B-I could cross blood brain barrier by its N-terminal TAT domain,and be cleaved into separate B and I by Caspase-1.B-I treatment significantly reduced the cerebral infarct volume,better than B or I treatment alone,and equivalent to B and I treatment(B+I).Treatment with B or B-I significantly attenuated I/R-induced neuronal apoptosis as shown by the decrease in apoptotic rate and the inhibition of caspase-3 ***,all recombinant proteins,especially B-I,remarkably attenuated I/R-induced up-regulation of TNF-α.These results suggested that fusion protein B-I inhibiting both inflammation and apoptosis provided better neuroprotective effects than inhibiting either one *** study suggested that multiple pathways targeting brain I-R injury could enhance the neuroprotective effect,and it provided a new idea for the study of neuroprotective drugs for ischemic stroke.

摘要：A series of new 6-substituted 3 H-quinazolin-4-ones（3 a-3 d） were designed, synthesized and evaluated as the type I positive allosteric modulators（PAMs） of human α7 n ACh R expressed in Xenopus ooctyes by two-electrode voltage clamp. However, no compound showed a better efficacious PAM than lead compound 2 in the presence of acetylcholine（100 μM）. The structure-activity relationship（SAR） analysis suggested that thiazolo[4,5-d]pyrimidin-7（6 H）-one was the key biological skeleton.

摘要：As a valuable resource for drug discovery, natural products remain largely unexplored. The cheminformatics analysis of natural product databases could help us know better about natural products, providing valuable information in drug design. In this study, we collected an in-home natural product library consisting of more than 220 000 molecules. The results showed that natural products were distributed more diversely than synthetic compounds and approved drugs in chemical space, and natural products still possessed better scaffold diversity. Besides, natural product scaffolds had more potential in some specific indications, such as antiarthritic, antihypertensive, antiallergic and analgesic. However, the utilization rate of natural product scaffolds is relatively low, especially in terms of potential indications. Therefore, we recommend the greater use of natural products while designing lead libraries.

摘要：The development of well-defined TiO2 nanoarchitectures is a versatile strategy to achieve high-efficiency photocatalytic *** this study,mesoporous TiO2 nanofibers consisting of oriented nanocrystals were fabricated by a facile vapothermal-assisted topochemical transformation of preformed H-titanate *** vapothermal temperature is crucial in tuning the microstructures and photocatalytic redox properties of the resulting mesoporous TiO2 *** microstructures were characterized with XRD,TEM,XPS and nitrogen adsorption-desorption isotherms,*** photocatalytic activities were evaluated by photocatalytic oxidation of organic pollutant(Rhodamine B as an example)as well as photocatalytic reduction of water to generate hydrogen(H2).The nanofibers vapothermally treated at 150°C showed the highest photocatalytic activity in both oxidation and reduction reactions,2 times higher than that of *** oriented alignment and suitable mesoporosity in the resulting nanofiber architecture were crucial for enhancing photocatalytic *** oriented alignment of anisotropic anatase nanocrystals shall facilitate faster vectorial charge transportation along the nanofibers ***,the suitable mesoporosity and high surface area would also effectively enhance the mass exchange during photocatalytic *** also demonstrate that efficient energy-recovering photocatalytic water treatments could be accomplished by a cascading oxic-anoxic process where the dye is degraded in the oxic phase and hydrogen is generated in the successive anoxic *** study showcases a novel and facile method to fabricate mesoporous TiO2 nanofibers with high photocatalytic activity for both clean energy production and environmental purification.

摘要：In the present study,novel ester derivatives of CAPE were designed and synthesized as neuroprotective *** anti-inflammatory and antioxidant activities of these compounds were evaluated at the cellular level,while the blood-brain barrier(BBB)permeability was predicted by parallel artificial membrane permeability assay(PAMPA).The results revealed that phenolic hydroxyl groups and double bonds in the structure of CAPE had important effects on neuroprotective ***,a preliminary structure-activity relationship was summarized in this *** addition,we observed a significant improvement on BBB *** results provided important references for the structural modification and optimization of CAPE in the future.

摘要：With rapid spread of HIV(human immunodeficiency virus) on a global scale and increasingly severe drug-resistance of it,it is urgently necessary to develop novel effective anti-HIV ***-nucleoside reverse transcriptase inhibitor(NNRTIs)is one of the most significant antiretroviral drugs for fighting against HIV infection due to their various structures,unique mode of action,good efficacy and low *** derivatives,a type of NNRTIs,have been reported to achieve remarkable development in the past few *** this review,we summarized current drug design and medicinal chemistry efforts toward the development of next-generation pyridinones as HIV-1 NNRTIs.

摘要：A series of 2-arylamino-1,3,5-triazine derivatives(4a–4g),which were designed and synthesized via Sonogashira coupling reaction,were evaluated using two-electrode voltage clamp(TEVC)recordings of humanα7 nAChR expressed in Xenopus *** 4g as a positive allosteric modulator(PAM)showed better efficacy than lead compound 3(HZZ-A-11)with an EC50 value of 1.23±0.41μ*** pharmacological evaluation of compound 4g might lead to the developmental potential for therapy of cognitive deficits commonly shared by neuropsychiatric disorders,such as schizophrenia and Alzheimer’s disease.

摘要：Zinc binding group(ZBG)is the crucial moiety in the chemical structure of any HDAC *** the present study,a series of sulphur-containing ZBG were designed and synthesized in the novel HDAC inhibitors to replace the classical ZBGs of SAHA and BML-210,hydroxamic acids and benzamides,*** HDAC inhibitory activity and the structure-activity relationships of these molecules were analyzed.A sulphur-rich group,diethylcarbamo(dithioperoxo)thioate,was finally identified as a novel potent *** all the synthesized compounds,4 d was much more potent compared with BML-210,and it showed similar inhibitory effect of SAHA against HDAC isoforms 1 and ***,it was chosen as a lead compound.

摘要：In modern terminology,“organoids”refer to cells that grow in a specific three-dimensional(3D)environment in vitro,sharing similar structures with their source organs or *** themorphology or growth characteristics of organoids through a microscope is a commonly used method of organoid ***,it is difficult,time-consuming,and inaccurate to screen and analyze organoids only manually,a problem which cannot be easily solved with traditional *** intelligence(AI)technology has proven to be effective in many biological and medical research fields,especially in the analysis of single-cell or hematoxylin/eosin stained tissue *** used to analyze organoids,AI should also provide more efficient,quantitative,accurate,and fast *** this review,we will first briefly outline the application areas of organoids and then discuss the shortcomings of traditional organoid measurement and analysis ***,we will summarize the development from machine learning to deep learning and the advantages of the latter,and then describe how to utilize a convolutional neural network to solve the challenges in organoid observation and ***,we will discuss the limitations of current AI used in organoid research,as well as opportunities and future research directions.