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Chinese Chemical Letters 2024年第1期35卷 227-232页

作者： Yanqing Zhu Shuai Chen Zhen Zhou Yun He Zhengli Liu Yang Liu Zhang Feng Chongqing Key Laboratory of Natural Product Synthesis and Drug Research School of Pharmaceutical SciencesChongqing UniversityChongqing 401331China Department of Medicinal Chemistry School of PharmacyFujian Medical University(FMU)Fuzhou 350005China Affiliated Hospital of north sichuan medical college and medical Imaging Key Laboratory of sichuan Province Nanchong 637503China

A method for the generation of alkyl radicals from inert alkyl C-o bonds has been developed via an iron/borane reagent/alkoxide catalytic system,which can be employed for the synthesis of amines from nitroarenes with excellent *** reductive amination features good functional group compatibility and enables the late-stage amination of bio-relevant compounds,thus providing good opportunities for applications in medicinal *** mechanistic studies reveal that the amine synthesis may be involving a Fe/Li cation-assisted single electron transfer pathway to form alkyl radicals,and the low-valent iron speciesmaybetheactive intermediates.

关键词： C-N bond formation Reductive amination Borane reagent Iron catalysis Green chemistry

Hydrogel microspheres for bone regeneration through regulation of the regenerative microenvironment

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Biomaterials Translational 2024年第3期5卷 205-235页

作者： Pengrui Zhang Qiwei Qin Xinna Cao Honglin Xiang Dechao Feng Dilinaer Wusiman Yuling Li Department of Orthopaedics Laboratory of Biological Tissue Engineering and Digital MedicineAffiliated Hospital of North Sichuan Medical CollegeNanchongSichuan ProvinceChina Division of Surgery&Interventional Science University College LondonLondonUK Department of Comparative Pathobiology College of Veterinary MedicinePurdue UniversityWest LafayetteINUSA

Bone defects are a prevalent category of skeletal tissue disorders in clinical practice,with a range of pathogenic factors and frequently suboptimal clinical treatment *** bone regeneration of bone defects,the bone regeneration microenvironment-composed of physiological,chemical,and physical components-is the core element that dynamically coordinates to promote bone *** recent years,medical biomaterials with bioactivity and functional tunability have been widely researched upon and applied in the fields of tissue replacement/regeneration,and remodelling of organ structure and *** biomaterial treatment system based on the comprehensive regulation strategy of bone regeneration microenvironment is expected to solve the clinical problem of bone *** microspheres(HMS)possess a highly specific surface area and porosity,an easily adjustable physical structure,and high encapsulation efficiency for drugs and stem *** can serve as highly efficient carriers for bioactive factors,gene agents,and stem cells,showing potential advantages in the comprehensive regulation of bone regeneration microenvironment to enhance bone *** review aims to clarify the components of the bone regeneration microenvironment,the application of HMS in bone regeneration,and the associated *** also discusses various preparation materials and methods of HMS and their applications in bone tissue ***,it elaborates on the relevant mechanisms by which HMS regulates the physiological,chemical,and physical microenvironment in bone regeneration to achieve bone ***,we discuss the future prospects of the HMS system application for comprehensive regulation of bone regeneration microenvironment,to provide novel perspectives for the research and application of HMS in the bone tissue engineering field.

关键词： bone regeneration bone tissue engineering hydrogel microspheres regeneration microenvironment

Morphometric study of the testis and reproductive tract （including sperm granuloma） after vasectomy in mature rats

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Asian Journal of Andrology 2016年第1期18卷 66-73页

作者： Li Ma Yang Guo Yong Yuan Yu-Gen Li Xian-Zhong Deng Zheng-Wei Yang Morphometric Research Laboratory North Sichuan Medical College Nanchong 637000 Sichuan China Department of Urological Surgery The Affiliated Hospital of North Sichuan Medical College Nanchong 637000 Sichuan China

By utilizing the rabbit model, previous studies have found good evidence indicating that vasectomy-induced spermatogenic damage is pressure-mediated： the damage occurs when the occluded reproductive tract is unable to accommodate additional spermatozoa produced by the testis. More studies with the more commonly used rat model have shown, however, controversial results on whether and why the damage occurs. In this study, 12 mature male Sprague-Dawley rats were subjected to unilateral vasectomy： double ligation （without severing） of the vas deferens exposed via a small inguinal incision; 37 days after the operation, the testes, epididymides, vasa deferentia （juxta-epididymal segments）, and sperm granulomas （at the vasectomy site） were removed to obtain methacrylate resin-embedded sections and morphometric studies carried out with light microscopy. Marked spermatogenic damage with spermatids and spermatocytes depleted in the seminiferous epithelium in 43% of the seminiferous tubule profiles was demonstrated in 5 of the 12 testes on the vasectomized side, and the damage was associated with smaller or absent sperm granulomas; in the other 7 testes with essentially normal spermatogenesis, there was an increase （by 111% on average） in the volume of the tubule lumen, associated with larger granulomas or granulomas containing more spermatozoa. There was an overall increase （by 66%） in the thickness of the rete testis in the 12 testes; the epididymis or vas deferens showed no distension. It seems therefore that the spermatogenic damage induced by vasectomy in rats is pressure-mediated as well, and that variation in the damage depends mainly on the postoperative development of the sperm granuloma.

关键词： morphometry rat sperm granuloma spermatogenesis vasectomy

In situ self-assembly of amphiphilic dextran micelles and superparamagnetic iron oxide nanoparticle-loading as magnetic resonance imaging contrast agents

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Regenerative Biomaterials 2023年第1期10卷 194-204页

作者： Linrui Jiang Rong Zheng Ni Zeng ChangqiangWu Hongying Su Faculty of Chemical Engineering Kunming University of Science and TechnologyKunming 650500China sichuan Key Laboratory of medical Imaging North Sichuan Medical CollegeNanchong 637000China

Polymeric micelles have long been considered as promising nanocarrier for hydrophobic drugs and imaging probes,due to their nanoscale particle size,biocompatibility and ability to loading reasonable amount of ***,a facile method for dextran micelles preparation was developed and their performance as carriers of superparamagnetic iron oxide(SPIO)nanocrystals was *** dextran(Dex-g-OA)was synthesized via the Schiff base reactions between oxidized dextran and oleylamine,and self-assembled in situ into nano-size micelles in the reaction *** self-assembling behaviors of the amphiphilic dextran were identified using fluorescence resonance energy transfer technique by detection the energy transfer signal between the fluorophore pairs,Cy5 and *** SPIO nanoparticles(Fe_(3)O_(4)NPs)were successfully loaded into the dextran micelles via the in situ self-assembly process,leading to a series of Fe_(3)O_(4)NPs-loaded micelle nanocomposites(Fe_(3)O_(4)@Dex-g-OA)with good biocompatibility,superparamagnetism and strongly enhanced T_(2)*** the magnetic field of 0.5 T,the Fe_(3)O_(4)@Dex-g-OA nanocomposite with particle size of 116.2±53.7 nm presented a higher T_(2)relaxivity of 327.9 mM_(re)^(-1)·s^(-1)·s^(−1).The prepared magnetic nanocomposites hold the promise to be used as contrast agents in magnetic resonance imaging.

关键词： micelle dextran superparamagnetic iron oxide magnetic resonance imaging Schiff base

Boron-promoted reductive deoxygenation coupling reaction of sulfonyl chlorides for the C(sp3)-S bond construction

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Chinese Chemical Letters 2022年第12期33卷 5101-5105页

作者： Shuo Chen Qingru Wen Yanqing Zhu Yanru Ji Yu Pu Zhengli Liu Yun He Zhang Feng Chongqing Key Laboratory of Natural Product Synthesis and Drug Research School of Pharmaceutical SciencesChongqing UniversityChongqing 401331China medical Imaging Key Laboratory of sichuan Province North Sichuan Medical CollegeNanchong 637000China

Herein,we report a borane-promoted reductive deoxygenation coupling reaction to synthesize *** reaction features excellent functional group compatibility,high efficiency,broad substrate scope,and application in late-stage functionalization of *** mechanistic studies suggest diaryl sulfides are the intermediates of this ***,the real active aryl sulfide anions may be generated in situ with the aid of B2pin2 and react with alkyl tosylates through a concerted SN2 pathway.

关键词： C-S bond formation Reductive deoxygenation coupling Borane Organosulfur compounds Green chemistry

Effect of S1P5 on proliferation and migration of human esophageal cancer cells

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World Journal of Gastroenterology 2010年第15期16卷 1859-1866页

作者： Hu, Wei-Min Li, Li Ing, Bao-Qian Zhao, Yong-Sheng Wang, Chao-Li Feng, Li Xie, Yong-En N sichuan Med Coll Dept Microbiol & Immunol Nanchong 637007 Sichuan Prov Peoples R China N sichuan Med Coll Inst Immunol & Mol Biol Nanchong 637007 Sichuan Prov Peoples R China N sichuan Med Coll Affiliated Hosp Dept Thorac Surg Nanchong 637007 Sichuan Prov Peoples R China

AIM:To investigate the sphingosine 1phosphate (S1P) receptor expression profile in human esophageal cancer cells and the effects of S1P5 on proliferation and migration of human esophageal cancer cells. METHODS: S1P receptor expression profile in human esophageal squamous cell carcinoma cell line Eca109 was detected by semiquantitative reverse trans cription polymerase chain reaction. Eca109 cells were stably transfected with S1P5EGFP or controlEGFP constructs. The relation between the responses of cell proliferationand migration to S1P and S1P5 expres sion was evaluated by 3(4,5dimethylthiazol2yl)2,5diphenyl tetrazolium bromide and migration assay, respectively. RESULTS: Both normal human esophageal mucosal epithelium and Eca109 cells expressed S1P1, S1P2, S1P3 and S1P5, respectively. Esophageal mucosal epithelium expressed S1P5 at a higher level than Eca109 cell line. S1P5 overexpressing Eca109 cells displayed spindle cell morphology with elongated and extended filopodialike projections. The proliferation response of S1P5transfected Eca109 cells was lower than that of control vectortransfected cells with or without S1P stimulation (P < 0.05 or 0.01). S1P significantly inhibited the migration of S1P5transfected Eca109 cells (P < 0.001). However, without S1P in transwell lower chamber, the number of migrated S1P5transfected Eca109 cells was greater than that of control vectortransfected Eca109 cells (P < 0.001).CONCLUSION: S1P binding to S1P5 inhibits the proliferation and migration of S1P5transfected Eca109 cells. Esophageal cancer cells may downregulate the expression of S1P5 to escape the inhibitory effect.

关键词： Sphingosine 1phosphate Esophageal cancer Sphingosine 1phosphate 5 Proliferation Migration

Dopamine multivalent-modified polyaspartic acid for MRI-guided near-infrared photothermal therapy

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Regenerative Biomaterials 2023年第1期10卷 678-689页

作者： Liang Du Wei Chen Jie Zhong Shuang Yan Chenwu Yang Yu Pu Jiang Zhu Tianwu Chen Xiaoming Zhang Changqiang Wu medical Imaging Key Laboratory of sichuan Province and School of medical Imaging Affiliated Hospital of North Sichuan Medical CollegeNanchong 637000PR China

Nanophotothermal agents that provide efficient and precise treatment at tumor sites are attracting increasing attention in *** particular,the method combination of nanophotothermal agents and magnetic resonance imaging(MRI)shows great promise for biomedical therapeutic ***,a simple nanophotothermal agent with dopamine multivalent-modified polyaspartic acid chelated superparamagnetic iron oxide(SPIO)and ferric ion(SPIO@PAsp-DAFe/PEG)was developed for MRI-guided near-infrared photothermal therapy(PTT).SPIO@PAsp-DAFe/PEG was random SPIO nanocluster with good water solubility,had a diameter of 57.8±7.8 nm in dynamic light scattering,negatively charged surface(zeta potential=−11 mV),exhibited good stability and outstanding photothermal conversion efficiency(35.4%)and produced superior magnetic resonance enhanced *** the experiment with tumor-bearing mice,the MRI not only monitored the accumulation of SPIO@PAsp-DAFe/PEG nanocomposites enhanced by near-infrared irradiation after intravenous administration but also determined the appropriate time window for *** the use of MRI-guided near-infrared therapy,the SPIO@PAsp-DAFe/PEG nanocomposites provided excellent therapeutic effects,confirming their great potential as effective MRI/PTT therapeutic agents.

关键词： dopamine superparamagnetic iron oxide nanocomposites magnetic resonance imaging photothermal therapy

Radiation therapy concurrent with weekly cisplatin therapy for loco-regionally advanced nasopharyngeal carcinoma:outcomes of a clinical trial

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The Chinese-German Journal of Clinical Oncology 2011年第4期10卷 187-191页

作者： Daiyuan Ma Chunqiao Fu Bangxian Tan Mi Liu Xianfu Li Yeqin Zhou Department of Radiation Oncology 1st Affiliated Hospital of North Sichuan Medical College Nanchong 637000China

Objective:The purpose of this study was to define the maximum tolerated dose(MTD) by describing the doselimiting toxicity(DLT) of weekly cisplatin concurrently with conventional plus 3-dimensional conformal radiotherapy(CT + 3DCRT) in patients with loco-regionally advanced nasopharyngeal carcinoma(NPC).Methods:Patients with loco-regionally advanced NPC(III/IVa stage) were enrolled into a dose-escalating *** was graded according to Common Terminology Criteria for Adverse Events version 3.0(CTCAE v3.0).MTD was defined when 2 of 6 patients developed *** starting dose of cisplatin was 15 mg/m2/w,with a subsequent dose escalation of 5 mg/m2/w in cohorts of 3 new *** + 3DCRT was given to the nasopharynx and the upper neck;the lower neck was treated by a single anterior field *** prescription dose was 70-80 Gy by 35-40 fractions to the nasopharynx gross tumor,and 66-70 Gy by 33-35 fractions to the positive neck lymph ***:From Jun.2008 to Sep.2009,24 patients received complete chemoradiotherapy,and all of them were eligible for toxicity *** the first five dose levels of 15 mg/m2/w and 35 mg/m2/w,no patient experienced *** the next dose level of 40 mg/m2/w,1 patient experienced DLT of grade 3 myelosuppression for 1.4 weeks,and among the additional 3 patients,no one developed *** the seventh dose level of 45 mg/m2/w,all the patients developed grade 3 myelosuppression for more than 1 weeks,and the dose-escalating trial *** 23(95.8%) patients achieved clinical complete remission(CR) in the local site;22(91.7%) achieved CR in the regional site,and all patients got CR 3 months *** a median follow-up of 16.4 months,1 patient developed liver metastases 2 months later,1 patient developed bone metastases 10 months later and 22 kept disease-free ***:The MTD of cisplatin weekly with concurrent CT + 3DCRT for local advanced NPC is 40 mg/m2/w,with myelosuppression as DLT.

关键词： nasopharyngeal carcinoma(NPC) cisplatin/treatment chemotherapy radiotherapy concurrent treatment dose escalating

Iron-Catalyzed Borylation and Silylation of Unactivated Tertiary,Secondary,and Primary Alkyl Chlorides

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CCS Chemistry 2021年第9期3卷 2164-2173页

作者： Siyu Wang Minghui Sun Huan Zhang Juan Zhang Yun He Zhang Feng Chongqing Key Laboratory of Natural Product Synthesis and Drug Research School of Pharmaceutical SciencesChongqing UniversityChongqing 401331 sichuan Key Laboratory of medical Imaging Department of ChemistrySchool of Preclinical MedicineNorth Sichuan Medical CollegeSichuan 637000

Herein,we describe an iron-catalyzed borylation and silylation of unactivated alkyl chlorides,delivering the tertiary,secondary,and primary alkylboronic esters,and secondary,primary alkylsilanes with high *** protocol exhibits broad substrate scope and good functional group compatibility,allowing the efficient late-stage borylation of biorelevant compounds,thus offering an excellent platform in drug discovery and *** mechanistic studies suggest that an alkyl radical was involved in this catalytic system.

关键词： iron catalysis borylation silylation unactivated alkyl chlorides

Iron-Catalyzed Cross-Electrophile Coupling of Inert C-O Bonds with Alkyl Bromides

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CCS Chemistry 2023年第7期5卷 1674-1685页

作者： Shuo Chen Zijian Wang Shasha Geng Hongdan Zhu Zhengli Liu Yun He Qian Peng Zhang Feng Chongqing Key Laboratory of Natural Product Synthesis and Drug Research School of Pharmaceutical SciencesChongqing UniversityChongqing 401331 State Key Laboratory of Elemento-Organic Chemistry Tianjin Key Laboratory of Biosensing and Molecular RecognitionCollege of ChemistryNankai UniversityTianjin 300071 Haihe Laboratory of Sustainable Chemical Transformation Tianjin 300192 medical Imaging Key Laboratory of sichuan Province Affiliated Hospital of North Sichuan Medical CollegeNanchong 637000

An example of iron-catalyzed cross-electrophile couplingof inert C-O bonds with alkyl bromides via aniron/B_(2)pin_(2) catalytic system has been *** and heteroaryl carbamates can smoothly undergothis transformation under mild conditions, deliveringthe alkylated products with good *** protocol exhibits good functional group compatibilityand enables the late-stage functionalizationof biorelevant compounds, thus providingexcellent opportunities for applications in medicinalchemistry. Control experiments and computationalstudies reveal that a high spin Fe(I/II/III) catalyticmechanism might be involved in this reactionthrough single electron transfer to activate alkylbromides, oxidative addition of aryl carbamates, andreductive elimination to form Csp^(2)-Csp^(3) bonds.

关键词： iron catalysis cross-electrophile coupling inert C-O bonds single-electron transfer pathway