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Palladium-catalyzed vinylation of indoles with vinyl ethers via deoxygenative coupling

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Science China Chemistry 2024年第11期67卷 3785-3790页

作者： Bowen Wang Jianxiao Li Wanqing Wu Liangbin Huang Huanfeng Jiang key laboratory of Functional Molecular Engineering of guangdong province School of Chemistry and Chemical EngineeringSouth China University of Technology

Indole is a promising heteroarene in many natural products and pharmaceuticals; therefore, various synthetic methods for indole functionalizations have arisen in recent years. Herein, we report a Pd-catalyzed deoxygenative coupling for the N-vinylation of indoles by employing vinyl ethers. The vinylated indoles could be readily prepared in good to excellent yields with N1-regioselectivity regardless of the electronic characteristics and substitution patterns of indole substrates. Some indole-based pharmaceutical molecules, such as gramine, evodiamine, rutaecarpine, and melatonine, are also successfully vinylated. Moreover, carbazoles and indazoles are shown to participate. Additionally, vinylated indole can readily transform into structurally interesting indole derivatives.

关键词： indole vinylation regioselectivity N-vinyl indole palladium catalyst

Palladium-Catalyzed anti-Markovnikov Halosulfonamidation of Unactivated Alkene

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Chinese Journal of Chemistry 2024年第5期42卷 464-470页

作者： Bowen Wang Jianxiao Li Wanqing Wu Huanfeng Jiang State key laboratory of Pulp and Paper Engineering Key Laboratory of Functional Molecular Engineering of Guangdong ProvinceSchool of Chemistry and Chemical EngineeringSouth China University of TechnologyGuangzhouGuangdong510641 China

Palladium-catalyzed regioselective amination of unactivated alkene remains a challenge and is of great ***,a three-component coupling of unactivated alkene,sulfonamide,and N-halo compounds accessing vicinal haloamine has been *** aminohalogenation represents a modular and regioselective *** electrophilic halogenating agent enables regioselective anti-Markovnikov aminopalladation and facilitates subsequent halogenation *** this protocol is characterized by gram-scale syntheses and late-stage *** note,the recovered byproduct phthalimide allows for reusing by conversion to the starting material.

关键词： Unactivated alkene anti-Markovnikov aminopalladation Vicinal haloamine Palladium catalysis Halosulfonamidation Selectivity N-Halo compounds

Ultrafast pulse-dilation framing camera and its application for time-resolved X-ray diagnostic

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Nuclear Science and Techniques 2024年第7期35卷 101-114页

作者： Hou-Zhi Cai Qiu-Yan Luo Kai-Xuan Lin Xuan Deng Jun-Kai Liu Kai-Zhi Yang Dong Wang Jia-Jie Chen Jia-Heng Wang Jing-Hua Long Li-Hong Niu Yun-Fei Lei Jin-Yuan Liu key laboratory of Optoelectronic Devices and Systems of Ministry of Education and guangdong province Shenzhen Key Laboratory of Photonics and BiophotonicsCollege of Physics and Optoelectronic EngineeringShenzhen UniversityShenzhen518060China

An ultrafast framing camera with a pulse-dilation device,a microchannel plate(MCP)imager,and an electronic imaging system were *** camera achieved a temporal resolution of 10 ps by using a pulse-dilation device and gated MCP imager,and a spatial resolution of 100μm by using an electronic imaging system comprising combined magnetic *** spatial resolution characteristics of the camera were studied both theoretically and *** results showed that the camera with combined magnetic lenses reduced the field curvature and acquired a larger working area.A working area with a diameter of 53 mm was created by applying four magnetic lenses to the ***,the camera was used to detect the X-rays produced by the laser-targeting *** diagnostic results indicated that the width of the X-ray pulse was approximately 18 ps.

关键词： Inertial confinement fusion Plasma diagnostics Framing camera Combined lenses Pulse-dilation

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Multimodal Nature of the Single-cell Primate Brain Atlas:Morphology,Transcriptome,electrophysiology,and Connectivity

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Neuroscience Bulletin 2024年第4期40卷 517-532页

作者： Yuhui Shen Mingting Shao Zhao-Zhe Hao Mengyao Huang Nana Xu Sheng Liu State key laboratory of Ophthalmology Zhongshan Ophthalmic CenterSun Yat-sen UniversityGuangdong Provincial Key Laboratory of Ophthalmology and Visual ScienceGuangzhou510060China guangdong province key laboratory of Brain Function and Disease Guangzhou510080China

Primates exhibit complex brain structures that augment cognitive *** neocortex fulfills high-cognitive functions through billions of connected *** neurons have distinct transcriptomic,morphological,and electrophysiological properties,and their connectivity principles *** features endow the primate brain atlas with a multimodal *** recent integration of next-generation sequencing with modified patch-clamp techniques is revolutionizing the way to census the primate neocortex,enabling a multimodal neuronal atlas to be established in great detail:(1)single-cell/single-nucleus RNA-seq technology establishes high-throughput transcriptomic references,covering all major transcriptomic cell types;(2)patch-seq links the morphological and electrophysiological features to the transcriptomic reference;(3)multicell patch-clamp delineates the principles of local ***,we review the applications of these technologies in the primate neocortex and discuss the current advances and tentative gaps for a comprehensive understanding of the primate neocortex.

关键词： Neuron Brain atlas Patch-seq Connectivity Primate

Synergistic induction of mitotic pyroptosis and tumor remission by inhibiting proteasome and WEE family kinases

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Signal Transduction and Targeted Therapy 2024年第8期9卷 3467-3482页

作者： Zhan-Li Chen Chen Xie Wei Zeng Rui-Qi Huang Jin-E Yang Jin-Yu Liu Ya-Jing Chen Shi-Mei Zhuang MOE key laboratory of Gene Function and Regulation Guangdong Province Key Laboratory of Pharmaceutical Functional GenesSchool of Life SciencesState Key Laboratory of Oncology in Southern ChinaSun Yat-sen UniversityGuangzhouPR China key laboratory of Liver Disease of guangdong province The Third Affiliated HospitalSun Yat-sen UniversityGuangzhou 510630PR China

Mitotic catastrophe(MC),which occurs under dysregulated mitosis,represents a fascinating tactic to specifically eradicate tumor *** pyroptosis can be a death form of MC remains ***-mediated protein degradation is crucial for ***(BTZ),which inhibits the 20S catalytic particle of proteasome,is approved to treat multiple myeloma and mantle cell lymphoma,but not solid tumors due to primary *** date,whether and how proteasome inhibitor affected the fates of cells in M-phase remains ***,we show that BTZ treatment,or silencing of PSMC5,a subunit of 19S regulatory particle of proteasome,causes G2-and M-phase arrest,multi-polar spindle formation,and consequent caspase-3/GSDME-mediated pyroptosis in M-phase(designated as mitotic pyroptosis).Further investigations reveal that inhibitor of WEE1/PKMYT1(PD0166285),but not inhibitor of ATR,CHK1 or CHK2,abrogates the BTZ-induced G2-phase arrest,thus exacerbates the BTZ-induced mitotic arrest and *** BTZ and PD0166285 treatment(named BP-Combo)selectively kills various types of solid tumor cells,and significantly lessens the IC50 of both BTZ and PD0166285 compared to BTZ or PD0166285 *** using various mouse models show that BP-Combo has much stronger inhibition on tumor growth and metastasis than BTZ or PD0166285 monotreatment,and no obvious toxicity is observed in BP-Combo-treated *** findings disclose the effect of proteasome inhibitors in inducing pyroptosis in M-phase,characterize pyroptosis as a new death form of mitotic catastrophe,and identify dual inhibition of proteasome and WEE family kinases as a promising anti-cancer strategy to selectively kill solid tumor cells.

关键词： proteasome inhibiting catastrophe

Relationship among Parkinson’s disease, constipation, microbes, and microbiological therapy

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World Journal of Gastroenterology 2024年第3期30卷 225-237页

作者： Xin-Yang Yuan Yu-Sen Chen Zhou Liu Department of Neurology Affiliated Hospital of Guangdong Medical UniversityZhanjiang 524000Guangdong ProvinceChina Institute of Neurology Guangdong Key Laboratory of Age-Related Cardiac and Cerebral DiseasesZhanjiang 524000Guangdong ProvinceChina

This comprehensive review elucidates the complex interplay between gut microbiota and constipation in Parkinson’s disease(PD),a prevalent non-motor symptom contributing significantly to patients’morbidity.A marked alteration in the gut microbiota,predominantly an increase in the abundance of Proteobacteria and Bacteroidetes,is observed in PD-related *** treatments,although safe,have failed to effectively alleviate symptoms,thereby necessitating the development of novel therapeutic *** interventions such as prebiotics,probiotics,and fecal microbiota transplantation(FMT)hold therapeutic *** prebiotics improve bowel movements,probiotics are effective in enhancing stool consistency and alleviating abdominal *** shows potential for significantly alleviating constipation symptoms by restoring gut microbiota balance in patients with *** promising developments,the causal relationship between changes in gut microbiota and PD-related constipation remains elusive,highlighting the need for further research in this expanding field.

关键词： Parkinson disease Constipation Gut microbiota Prebiotics Probiotics Fecal microbiota transplantation

Effect of Sonic hedgehog gene-modified bone marrow mesenchymal stem cells on graft-induced retinal gliosis and retinal ganglion cells survival in diabetic mice

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International Journal of Ophthalmology(English edition) 2024年第1期17卷 34-41页

作者： Tong Wang Hai-Chun Li Jin Ma Xi-Ling Yu State key laboratory of Ophthalmology Zhongshan Ophthalmic CenterSun Yat-sen UniversityGuangdong Provincial Key Laboratory of Ophthalmology and Visual ScienceGuangzhou 510060Guangdong ProvinceChina

AIM:To investigate the effects of Sonic hedgehog(Shh)gene-modified bone marrow mesenchymal stem cells(MSCs)on graft-induced retinal gliosis and retinal ganglion cells(RGCs)survival in diabetic ***:Bone marrow-derived MSCs were genetically modified with the Shh gene to generate a stably transfected cell line of Shh-modified MSCs(MSC-Shh).Intravitreal injections of MSC-Shh and green fluorescent protein-modified MSCs(MSC-Gfp;control)were administered in diabetic *** 4wk,the effects of MSC-Shh on retinal gliosis were evaluated using fundus photography,and markers of gliosis were examined by immunofluorescence and Western *** neurotrophic factors expression and RGCs survival in the host retina were evaluated using Western blotting and *** mechanisms underlying the effects of MSC-Shh was ***:A significant reduction of proliferative vitreoretinopathy(PVR)was observed after intravitreal injection of MSC-Shh compared to *** downregulation of glial fibrillary acidic protein(GFAP)was demonstrated in the host retina after MSC-Shh administration compared to *** extracellular signal-regulated kinase 1/2(ERK1/2),protein kinase B(AKT)and phosphatidylin-ositol-3-kinase(PI3K)pathways were significantly downregulated after MSC-Shh administration compared to ***-derived neurotrophic factor(BDNF)and ciliary neurotrophic factor(CNTF)levels were significantly increased in the host retina,and RGCs loss was significantly prevented after MSC-Shh ***:MSC-Shh administration reduces graft-induced reactive gliosis following intravitreal injection in diabetic *** ERK1/2,AKT and PI3K pathways are involved in this ***-Shh also increases the levels of neurotrophic factors in the host retina and promoted RGCs survival in diabetic mice.

关键词： mesenchymal stem cells Sonic hedgehog signaling reactive gliosis diabetic retinopathy retinal ganglion cells

Rhegmatogenous retinal detachment in highly myopic eyes with implantable collamer lens

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International Journal of Ophthalmology(English edition) 2024年第2期17卷 392-396页

作者： Jun Li Chong-Lin Chen Jia-Qing Li Xiao-Ling Liang Chun Zhang State key laboratory of Ophthalmology Zhongshan Ophthalmic CenterSun Yat-sen UniversityGuangdong Provincial Key Laboratory of Ophthalmology and Visual ScienceGuangzhou 510060Guangdong ProvinceChina

AIM:To investigate the clinical characteristics,treatment methods and outcomes of rhegmatogenous retinal detachment(RRD)in highly myopic eyes with implantable collamer lens(ICL).METHODS:High myopia patients who received treatment for nontraumatic RRD after ICL implantation surgery at the Retinal Department of Zhongshan Ophthalmic Center from Jan 2018 to Dec 2022 were *** ophthalmologic examinations including visual acuity measurement and digital fundus photography were performed in each ***:A total of nine RRD eyes from nine patients who received V4c-ICL implantation were *** mean time from ICL implantation surgery to the diagnosis of RRD was 32.44±22.56mo(range,1-60mo).At the initial visit for RRD,giant retinal tear(GRT),horseshoe tear,simple round hole,and horseshoe tear combined with round hole were detected in 3,3,2,and 1 eye(s),respectively,with maculaoff in *** patients received surgical treatment,and one patient was treated by retinal laser photocoagulation *** ICL was preserved in 7 *** the last followup,the mean best corrected visual acuity(BCVA)improved significantly from 1.76±1.06 logMAR at presentation to 0.81±1.01 logMAR(P=0.035),and no case of recurrent retinal detachment was ***:The morphological presentation of retinal breaks is diverse in this *** ICL can be preserved in most cases during the course of retinal detachment repair surgery in our data,companied with acceptable visual and anatomical outcomes.

关键词： high myopia implantable collamer lens rhegmatogenous retinal detachment

Improved observation of colonized roots reveals the regulation of arbuscule development and senescence by drought stress in the arbuscular mycorrhizae of citrus

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Horticultural Plant Journal 2024年第2期10卷 425-436页

作者： Xilong Yin Wei Zhang Zengwei Feng Guangda Feng Honghui Zhu Qing Yao College of Horticulture South China Agricultural UniversityKey Laboratory of Biology and Genetic Improvement of Horticultural Crops(South China)Ministry of Agriculture and Rural AffairsGuangdong Province Key Laboratory of Microbial Signals and Disease ControlGuangzhouGuangdong 510642China key laboratory of Agricultural Microbiomics and Precision Application Ministry of Agriculture and Rural AffairsGuangdong Provincial Key Laboratory of Microbial Culture Collection and ApplicationKey Laboratory of Agricultural MicrobiomicsState Key Laboratory of Applied Microbiology Southern ChinaGuangdong Microbial Culture Collection Center(GDMCC)Institute of MicrobiologyGuangdong Academy of SciencesGuangzhouGuangdong 510070China

Citrus is the typical mycorrhizal fruit tree species establishing symbiosis with arbuscular mycorrhizal (AM) fungi. However, arbuscule development and senescence in colonized citrus roots, especially in response to drought stress, remain unclear, which is mainly due to the difficulty in clearing and staining lignified roots with the conventional method. Here, we improved the observation of colonized roots of citrus plants with the sectioning method, which enabled the clear observation of AM fungal structures. Furthermore, we investigated the effects of one week of drought stress on arbuscule development and senescence with the sectioning method. Microscopy observations indicated that drought stress significantly decreased mycorrhizal colonization (F%and M%) although it did not affect plant growth performance. Fluorescence probes (WGA 488 and/or Nile red) revealed that drought stress inhibited arbuscule development by increasing the percentage of arbuscules at the early stage and decreasing the percentages of arbuscules at the midterm and mature stages. Meanwhile, drought stress accelerated arbuscule senescence, which was characterized by the increased accumulation of neutral lipids. Overall, the sectioning method developed in this study enables the in-depth investigation of arbuscule status, and drought stress can inhibit arbuscule development but accelerate arbuscule senescence in the colonized roots of citrus plants. This study paves the way to elaborately dissecting the arbuscule dynamics in the roots of fruit tree species in response to diverse abiotic stresses.

关键词： Arbuscular mycorrhizae Citrus Drought stress Arbuscule development Arbuscule senescence Fruit tree species

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