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An improved installation of 2-hydroxy-4-methoxybenzyl(iHmb)method for chemical protein synthesis

Chinese Chemical Letters 2024年第5期35卷 145-150页

作者： Ying Li long-jie Wang Yong-Kang Zhou Jun Liang Bin Xiao ji-shen Zheng The First Affiliated Hospital of USTC MOE Key Laboratory for Membraneless Organelles and Cellular DynamicsDivision of Life Sciences and MedicineUniversity of Science and Technology of ChinaHefei 230001China Department of Chemistry University of Science and Technology of ChinaHefei 230027China

The 2-hydroxy-4-methoxybenzyl(Hmb)backbone modification can prevent amide bond-mediated sidereactions(e.g.,aspartimide formation,peptide aggregation)by installing the removable Hmb group into a peptide bond,thus improving the synthesis of long and challenging peptides and ***,its use is largely precluded by the limited Hmb’s installation *** this report,an improved installation of Hmb(iHmb)method was developed to achieve the flexible installation and the convenient removal of *** iHmb method involves two critical steps:(1)oxidative diazotization of the readily installed 2-hydroxy-4-methoxy-5-amino-benzyl(Hmab)to give 2-hydroxy-4-methoxy-5-diazonium-benzyl(Hmdab)by combining soamyl nitrite(IAN)/HBF_(4),and(2)reductive elimination of Hmdab to give the desired Hmb by 1,2-ethanedithiol(EDT).The iHmb method enables the installation of Hmb at any primary amino acid including the highly sterically hindered amino acids(e.g.,valine and isoleucine).The practicality and utility of the iHmb method was demonstrated by one-shot solid-phase synthesis of a challenging aspartimide-prone peptide,the mirror-image version of a hydrophobic peptide and a long-chain peptide up to ***,the iHmb method can be utilized to facilitate chemical protein ligation,as exemplified by the synthesis of the single-spanning membrane protein *** iHmb method expands the toolkit for peptide synthesis and ligation and facilitates the preparation of peptides/proteins.

关键词： Chemical protein synthesis Solid-phase peptide synthesis Removable backbone modification 2-Hydroxy-4-methoxybenzyl(Hmb)group Aspartimide-prone peptides Difficult peptides Membrane proteins

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Modeling solubility of oxaprozin and irbesartan in biorelevant complex solutions based on a combination of pH-dependent and micellar solubilization models

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Chinese Journal of Chemical Engineering 2024年第8期72卷 34-43页

作者： Chen shen Yuanhui ji jiangsu Province Hi-Tech Key Laboratory for Biomedical Research School of Chemistry and Chemical EngineeringSoutheast UniversityNanjing 211189China

Biological solubility is one of the important basic parameters in the development process of poorly soluble drugs,but the current measurement methods are mainly based on a large number of experiments,which are time-consuming and *** is still a lack of effective theoretical models to accurately describe and predict the biological solubility of drugs to reduce ***,in this study,osaprazole and irbesartan were selected as model drugs,and their solubility in solutions containing surfactants and biorelevant media was measured *** calculating the parameters of each component using the perturbed-chain statistical associating fluid theory(PC-SAFT)model,combined with pH-dependent and micellar solubilization models,the thermodynamic phase behavior of the two drugs was successfully modeled,and the predicted results were in good agreement with the experimental *** results demonstrate that the model combination used provides important basic parameters and theoretical guidance for the development and screening of poorly soluble drugs and related formulations.

关键词： Biorelevant media pH-dependent solubility Micellar solubilization PC-SAFT Active pharmaceutical ingredients

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Sedimentary and Heavy Mineral Records for the Oligocene-Miocene Exhumation of the Easternmost Tianshan

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Journal of Earth Science 2024年第2期35卷 449-461页

作者： Yan Ding Tianyi shen Guocan Wang Junliang ji School of Earth Sciences Center for Global TectonicsChina University of GeosciencesWuhan430074China State Key Laboratory of Geological Processes and Mineral Resources China University of GeosciencesWuhan430078China Hubei Key Laboratory of Critical Zone Evolution School of Geography and Information EngineeringChina University of GeosciencesWuhan430074China

The topography of the Harlik Mountain has a strong impact on the formation of current arid climate in the Turpan-Hami ***,it is still controversial if Harlik Mountain experienced significant exhumation during the Middle to Late Cenozoic according to the previous thermochronology *** features of the Oligocene to Miocene sediments in the foreland basin could provide productive information for resolving the *** peak ages of detrital apatite fission track analysis of the Oligocene–Miocene sandstone in the Turpan-Hami Basin are well comparable with the cooling age records of the Harlik Mountain rocks,indicating that the Oligocene–Miocene Taoshuyuanzi Formation in the basin was mostly derived from the Harlik *** stratigraphic sequence exhibits coarsening upward,reflecting that the source area was in a tectonically active period during the deposition *** mineral assemblages also suggest that the unstable minerals in the sediment increased significantly at the end of the ***,the proportion of apatite increased up-section,while the garnet content decreased significantly,indicating that the Carboniferous metamorphic rocks have been gradually eroded out and more intrusive rocks have been exposed to the *** observations suggest that the Harlik Mountain experienced exhumation during the Oligocene to Miocene,and the denudation depth afterward was probably less than 2.5 km according to the previously apatite(U-Th)/He *** Oligocene–Miocene exhumation probably acted as one of the triggers for the heavy drought of the Turpan-Hami Basin during the Middle–Late Neogene.

关键词： Turpan-Hami Basin Harlik Mountain Taoshuyuanzi Formation Oligocene–Miocene uplift sedimentology structural geology

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Biotic and abiotic stresses on honeybee health

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Integrative Zoology 2024年第3期19卷 442-457页

作者： Zheguang LIN Siyi shen Kang WANG Ting ji Apicultural Research Institute College of Animal Science and TechnologyYangzhou UniversityYangzhouChina

Honeybees are the most critical pollinators providing key ecosystem services that underpin crop production and sustainable *** a backdrop of rapid global change,this eusocial insect encounters a succession of stressors during nesting,foraging,and *** mites,together with vectored viruses,have been recognized as central biotic threats to honeybee health,while the spread of invasive giant hornets and small hive beetles also increasingly threatens colonies *** of agrochemicals,including acaricides used for mite treatment,and other pollutants of the environment have been widely documented to affect bee health in various ***,expanding urbanization,climate change,and agricultural intensification often result in the destruction or fragmentation of flower-rich bee *** anthropogenic pressures exerted by beekeeping management practices affect the natural selection and evolution of honeybees,and colony translocations facilitate alien species invasion and disease *** this review,the multiple biotic and abiotic threats and their interactions that potentially undermine bee colony health are discussed,while taking into consideration the sensitivity,large foraging area,dense network among related nestmates,and social behaviors of honeybees.

关键词： abiotic stressor Apis biotic stressor colony losses interaction effect pollinator decline

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Access to Versatile Functionalized Cu(Ⅲ) Complexes Enabled by Direct Transmetalation to Well-Defined Copper(Ⅲ) Fluoride Complex Me_(4)N^(+)[Cu(CF_(3))_(3)F]^(-)

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Chinese Journal of Chemistry 2024年第10期42卷 1107-1113页

作者： Guangyu Wang Huaiyuan Li Xuebing Leng long Lu Qilong shen Key Laboratory of Fluorine and Nitrogen Chemistry and Advanced Materials Shanghai Institute of Organic ChemistryUniversity of Chinese Academy of SciencesChinese Academy of Sciences345 Lingling LuShanghai 200032China

The invention of a well-defined Cu(Ⅲ)fluoride complex Me_(4)N^(+)[Cu(CF_(3))_(3)(F)]^(-)1 enabled to access a versatile of functionalized Cu(Ⅲ)complexes[Me_(4)N]^(+)[Cu(X)(CF_(3))_(3)]^(-)(X=C_(6)F_(5),C_(6)F_(5)C≡C,CN,Cl,N_(3),^(t)BuOO,SCN,OAc,SAr),many of them for the first *** availability of these complexes allowed us to evaluate the trans-influence order of ligand in Cu(Ⅲ)complexes:Bn>CF_(3)^(-)>C_(6)F_(5)^(-)>N_(3)^(-)>py~CH_(3)^(-)~C_(6)F_(5)C≡C>NO_(2)PhO^(-)~^(t)BuOO^(-)~CH_(3)COO^(-)>F^(-).

关键词： Fluorine Copper Cu(Ⅲ) Cu(Ⅲ)fluoride Trifluoromethyl

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A Simplified Method for the Stress Analysis of Underground Transfer Structures Crossing Multiple Subway Tunnels

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Computer Modeling in Engineering & Sciences 2024年第6期139卷 2893-2915页

作者： shen Yan Dajiang Geng Ning Dai Mingjian long Zhicheng Bai College of Civil Engineering Tongji UniversityShanghai200092China China Construction 4th Engineering Bureau 6th Corp. Ltd.Shanghai201199China Department of Civil and Architecture Engineering Hubei Polytechnic UniversityHuangshi435003China

According to the design specifications,the construction of extended piles involves traversing the tunnel’s upper region and extending to the underlying rock *** address this challenge,a subterranean transfer structure spanning multiple subway tunnels was *** on the function of piles in the transfer structure as springs with axial and bending stiffness,and taking into account the force balance and deformation coordination conditions of beams and plates within the transfer structure,we established a simplified mechanical model that incorporates soil stratification by combining it with the Winkler elastic foundation beam *** resolved established simplifiedmechanicalmodel employed finite difference technology and the Newton-Simpsonmethod,elucidating the mechanical mechanism of the transfer *** research findings suggest that the load carried by the upper structural columns can be transferred to the pile foundation beneath the beams through the transfer structure,subsequently reaching the deep soil layer and ensuring minimal impact on adjacent *** established simplified analysis method can be used for stress analysis of the transfer structure,concurrently considering soil stratification,pile foundation behavior,and plate *** pile length,pile section size,and beam section size within the transfer structure should account for the characteristics of the upper load,ensuring an even distribution of the beam bending moment.

关键词： Crossing tunnels transfer structure force mechanism simplify analysis layered soil mass

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弓形虫的基因型及其主要效应分子的致病机制

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中国寄生虫学与寄生虫病杂志 2015年第6期33卷 429-435页

作者：沈继龙王林安徽医科大学病原生物学教研室安徽病原生物学省级实验室安徽省人兽共患病重点实验室合肥230032 安徽中医药大学第一附属医院检验中心合肥230031

弓形虫(Toxoplasma gondii)是一种广泛寄生于人和温血动物有核细胞内的顶复门原虫(Apicomplexan),具有复杂的生活史和致病机制。Toxoplasma属下仅此一个虫种,但对其种群遗传结构的研究表明,世界各地的弓形虫存在着丰富的遗传多样性。采... 详细信息

弓形虫(Toxoplasma gondii)是一种广泛寄生于人和温血动物有核细胞内的顶复门原虫(Apicomplexan),具有复杂的生活史和致病机制。Toxoplasma属下仅此一个虫种,但对其种群遗传结构的研究表明,世界各地的弓形虫存在着丰富的遗传多样性。采用PCR-限制性片段长度多态性分析(RFLP)或微卫星标记分型,已从野生动物、家养禽畜和人体分离虫株中发现了232个基因型。其中,北美的弓形虫基因型以typeⅡ、typeⅢ和type12(主要见于野生动物)为主;欧洲以typeⅡ、typeⅢ和typeⅠ为主;非洲以typeⅡ和typeⅢ为主。以上称为原型克隆谱系。但南美的弓形虫表现出丰富的遗传多样性,包括BrⅠ、BrⅡ、BrⅢ和BrⅣ型等。近年研究发现,我国流行的弓形虫优势基因型为Chinese 1型(Toxo DB#9)。该型虫株兼具有原型谱系虫株关键效应分子的多态性。本文综述了世界各地包括我国在内的基因型、宿主免疫应答及其致病特点,为深入研究基因型/效应分子相关的致病机制,以及弓形虫的生物学和流行病学研究提供借鉴。

关键词：弓形虫基因型 PCR-限制性片段长度多态性分析致病机制免疫应答

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我国弓形虫病我国弓形虫病流行概况及防治基础研究进展

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中国血吸虫病防治杂志 2019年第1期31卷 71-76页

作者：沈继龙余莉安徽医科大学基础医学院病原生物学教研室人兽共患病安徽省高校重点实验室病原生物学安徽省重点实验室合肥230032

弓形虫是一种重要的人兽共患病原体,弓形虫病严重危害人体健康及畜牧业生产。本文综述了我国弓形虫感染流行情况、基因分型、致病机制、诊断、治疗和疫苗研发等研究进展,旨在为我国弓形虫和弓形虫病研究提供参考。

关键词：弓形虫基因型致病机制诊断治疗疫苗

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FPGA implementation of 500-MHz high-count-rate high-time-resolution real-time digital neutron-gamma discrimination for fast liquid detectors

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Nuclear Science and Techniques 2024年第8期35卷 101-113页

作者： Hui‑Yin shen jing‑long Zhang jie Zhang jian‑Hang Zhou College of Nuclear Technology and Automation Engineering Chengdu University of TechnologyChengdu 610059China Southwestern Institute of Physics P.O.Box 432Chengdu 610041China

Fast neutron flux measurements with high count rates and high time resolution have important applications in equipment such as *** this study,real-time neutron and gamma discrimination was implemented on a self-developed 500-Msps,12-bit digitizer,and the neutron and gamma spectra were calculated directly on an FPGA.A fast neutron flux measurement system with BC-501A and EJ-309 liquid scintillator detectors was developed and a fast neutron measurement experiment was successfully performed on the HL-2 M tokamak at the Southwestern Institute of Physics,*** experimental results demonstrated that the system obtained the neutron and gamma spectra with a time accuracy of 1 *** count rates of up to 1 Mcps,the figure of merit was greater than 1.05 for energies between 50 keV and 2.8 MeV.

关键词： Neutron-gamma discrimination Liquid scintillation detector Real-time spectrum analyzer

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Enhanced expression of the decoy receptor IL-13Rα2 in macrophages of Schistosomajaponicum-infected mice

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Chinese Medical Journal 2009年第14期122卷 1650-1654页

作者： WANG Wei shen Yu-xian LI jing ZHANG Shi-hai LUO Qing-li ZHONG Zhen-rong jiANG Zuo-jun shen ji-long Department of Epidemiology and Biostatistics School of Public Health Department of Pathobiology Anhui Medical University Hefei Anhui 230032 China Key Laboratory of Gene Resource Utilization for Severe Diseases the Ministry of Education of China and Anhui Province Hefei 230032 China

Background Type 2 cytokine interleukin （IL）-13 and its decoy receptor, IL-13 receptor （R）a2 appear to play a major role in tissue fibrosis of schistosomiasis and asthma. IL-13 is a key regulator of the extracellular matrix （ECM）. It is known to signal to cells by binding to the IL-13Rα1, which then heterodimerizes with IL-4Rα. In contrast, IL-13Rα2 binds IL-13 with high affinity but does not signal. IL-13Rα2 is known to down-regulate granulomatous inflammation and prolong host survival in Schistosoma mansoni （S. mansoni） infection, but little is known about the location and expression level of IL-13Rα2 in the context of S. japonicum infection. Methods We established S. japonicum-infected mouse models. Kinetic serum levels of IL-13Rα2 were examined with ELISA. IL-13Rα2 mRNA and protein of liver tissues were determined by PCR and immunoblotting analysis, respectively. Detection of IL-13Rα2 expression and location in macrophages was performed by TaqMan PCR and fluorescent immunocytochemistry technique, respectively. Results A marked elevation of mRNA and protein expression of IL-13Rα2 was observed in mice during S. japonicum infection. An enhanced expression of IL-13Rα2 was further demonstrated in primary macrophages of murine schistosomiasis. Conclusions IL-13Rα2 in macrophages may be a critical contributor to pathogenesis of schistosomiasis. The data highlight the potential importance of cell signaling and antifibrotic gene therapeutics in T helper 2 cell （Th2）-mediated diseases.

关键词： schistosomiasis macrophages interleukin-13R

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