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Generation of(E)-β-trifluoromethyl vinylsulfonohydrazides under photocatalysis and their anti-bacteria activity

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Chinese Chemical Letters 2023年第6期34卷 350-353页

作者： Xinhua Wang Wei Zhou wenlin xie Qi Chen Jie Wu Taizhou Central Hospital(Taizhou University Hospital)&School of Pharmaceutical and Chemical Engineering Taizhou UniversityTaizhou 318000China Department of Chemistry Fudan UniversityShanghai 200438China State Key Laboratory of Organometallic Chemistry Shanghai Institute of Organic ChemistryChinese Academy of SciencesShanghai 200032China School of Chemistry and Chemical Engineering Henan Normal UniversityXinxiang 453007China School of Chemistry and Chemical Engineering Hunan University of Science and TechnologyXiangtan 411201China

Trifluoromethylation/sulfonylation of alkynes from trifluoromethyl thianthrenium triflate and sulfur dioxide under extremely mild reaction conditions provides a facile access to trifluoromethyl-substituted vinyl sulfonohydrazides in moderate to good yields.This multicomponent reaction of trifluoromethyl thianthrenium triflate,alkynes,sulfur dioxide and hydrazines proceeds efficiently under visible light irradiation in the presence of photocatalyst at room temperature with broad substrate scope and excellent functional group compatibility.This reaction is highly stereoselective,and only(E)-isomers are obtained.Additionally,these trifluoromethyl-substituted vinyl sulfonohydrazides are further evaluated for anti-bacteria activity.In vitro activities of these compounds against Staphylococcus aureus(G+)and Escherichia coli(G-)are examined.

关键词： Alkyne Hydrazine Photocatalysis Sulfur dioxide Trifluoromethyl thianthrenium triflate

AHA1 upregulates IDH1 and metabolic activity to promote growth and metastasis and predicts prognosis in osteosarcoma

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Signal Transduction and Targeted Therapy 2021年第2期6卷 507-518页

作者： Diwei Zheng Weihai Liu wenlin xie Guanyu Huang Qiwei Jiang Yang Yang Jiarong Huang Zihao Xing Mengling Yuan Mengning Wei Yao Li Junqiang Yin Jingnan Shen Zhi Shi Department of Cell Biology&Institute of Biomedicine National Engineering Research Center of Genetic MedicineMOE Key Laboratory of Tumor Molecular BiologyGuangdong Provincial Key Laboratory of Bioengineering MedicineCollege of Life Science and TechnologyJinan UniversityGuangzhouGuangdong 510632China Department of Musculoskeletal Oncology.the First Alilated Hospital of Sun Yat-sen University GuangzhouGuangdong 510080China Guangdong Provincial Key Laboratory of Orthopedics and Traumatology GuangzhouGuangdong 510080China Department of Pathology the Seventh Aflited Hospital of Sun Yat-sen UniversityShenzhenGuangdong 518017China

Osteosarcoma(OS)is the most common primary malignant bone tumor in children and adolescents.Although activator of HSP90 ATPase activity 1(AHA1)is reported to be a potential oncogene,its role in osteosarcoma progression remains largely unclear.Since metabolism reprogramming is involved in tumorigenesis and cancer metastasis,the relationship between AHA1 and cancer metabolism is unknown.In this study,we found that AHA1 is significantly overexpressed in osteosarcoma and related to the prognosis of osteosarcoma patients.AHA1 promotes the growth and metastasis of osteosarcoma both in vitro and in vivo.Mechanistically,AHA1 upregulates the metabolic activity to meet cellular bioenergetic needs in osteosarcoma.Notably,we identifed that isocitrate dehydrogenase 1(IDH1)is a novel client protein of Hsp90 AHA1.Furthermore,the IDH1 protein level was positively correlated with AHA1 in osteosarcoma.And IDH1 overexpression could partially reverse the effect of AHA1 knockdown on cell growth and migration of osteosarcoma.Moreover,high IDH1 level was also associated with poor prognosis of osteosarcoma patients.This study demonstrates that AHA1 positively regulates IDH1 and metabolic activity to promote osteosarcoma growth and metastasis,which provides novel prognostic biomarkers and promising therapeutic targets for osteosarcoma patients.

关键词： IDH1 osteosarcoma metastasis

Design,synthesis and biological evaluations of novel pyridone-thiazole hybrids molecules as antitumor agents

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Design,synthesis and biological evaluations of novel pyridon...

Radical N-centered 6-endo aza-cyclization of 2-alkynylbenzamide

中国化学会第十二届全国物理有机化学学术会议

作者： Huilin Zhang Yiqiang Wu Qihong Mei wenlin xie School of Chemistry and Chemical Engineering Hunan University of Science and Technology Key Laboratory of Theoretical Organic Chemistry and Function Molecule of Ministry of Education Hunan University of Science and Technology

A hybrid pharmacophore approach was adopted to design and synthesize new series of pyridone-thiazole hybr ids.The structures of the compounds were established by IR,H NMR,C NMR,and HRMS.All the newly pre pared hybrids were in vitro evaluated for their antiproliferative activity against three human cancer cell lines,na

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Radical N-centered 6-endo aza-cyclization of 2-alkynylbenzam...

桥接系统内固定术联合术后高位直肠灌肠治疗骨盆骨折的效果及对直肠便意感觉容量、肛门功能评分的影响

中国化学会·第十六届全国有机合成化学学术研讨会

作者： Renzhi Liu Hongwei Zhou wenlin xie 邱观音生 School of Chemistry and Chemical Engineering Hunan University of Science and Technology College of Biological Chemical Science and EngineeringJiaxing University 嘉兴学院

Considering its ubiquity of N-containing compounds,various N-containing synthons were developed for accordingly.Among them,N-center radical species was a history-long yet many-issues-unsettled topic in the field of organic chemistry.As such,tremendous efforts were made in past decades,thus enabling signficant progress of amidyl-nitrogen radical and imine-nitrogen radical chemistry. To the best of our knowledge,amidyl nitrogen-radical could be achieved through a metal-free process,metal catalysis and photocatalysis etc.In our works,we have developed a copper-catalyzed radical cyclization of 2-alkynylbenzamide for the synthesis of isoquinolin-1-one under N2 atmosphere. Interestingly,the above strategy could be used to the formation of3-hydroxylisoquinolin-1,4-diones as well when the reaction was conducted in the presence of O balloon.Mechanism studies showed that the reaction proceeds in a regio selective manner via an N-center radical-based 6-endo-dig aza-cyclization pathway.

关键词： Copper catalysis nitrogen radical isoquinolinone

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中华实验外科杂志 2024年第6期41卷 1188-1188页

作者：陈丽君倪晓伟谢文林金华市中心医院创伤外科金华

本研究旨在探讨桥接系统内固定术联合术后高位直肠灌肠治疗骨盆骨折与单纯桥接系统内固定术治疗骨盆骨折的效果及对直肠便意感觉容量、肛门功能评分的影响, 以期为临床提供参考。

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Mass extinctions, their causes and consequences: an interview with Douglas H.Erwin and Shuzhong Shen

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National Science Review 2024年第1期11卷 66-70页

作者： Shucheng xie State Key Laboratory of Biogeology and Environmental Geology China University of Geosciences at Wuhan

‘Mass extinctions’ have been a hot topic for several decades. What triggers a mass extinction? How does a mass extinction impact the evolution of life? How does our ecosystem recover after a mass extinction? These questions attracted the interest of both scientists and the public alike.NSR spoke to two renowned researchers in the field of mass extinctions: Prof. Douglas H. Erwin from the National Museum of Natural History of the USA, and Prof. Shuzhong Shen from Nanjing University, China.

关键词： Stratigraphy

Synthesis and Biological Evaluation of Kojic Acid Derivatives Containing 1,2,4-triazole as Potent Tyrosinase Inhibitors

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Synthesis and Biological Evaluation of Kojic Acid Derivative...

Effects of Aromatherapy on Physical and Mental Health of Cancer Patients Undergoing Radiotherapy and/or Chemotherapy: A Meta-Analysis

中国化学会第九届全国有机化学学术会议

作者： wenlin xie Qiuyan Yu Jingai Zhang Xinrui Li Chunxiang Luo Jianbin Liu Shangru Li Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education College of Chemistry and Materials ScienceNorthwest University

Although the melanin production in human skin is a major defense mechanism against UV light,excessive accumulations of epidermal pigmentation can cause various hyperpigmentation disorders,such as freckle,senile lentigines,and melasma.Tyrosinase is a multifunctional copper-containing enzyme that is widely distributed in microorganisms,animals,and plants[1].It can catalyze two distinct reactions during the biosynthesis of melanin,involving the hydroxylation of L-tyrosine to L-dopa and the oxidation of L-dopa to dopaquinone,which is highly reactive and can polymerize spontaneously to form melanin.Therefore,the regulation of melanin synthesis via the inhibition of tyrosinase is a important research topic.In clinical usage,tyrosinase inhibitors are used for treatments of dermatological disorders related to melanin hyperaccumulation and are essential in cosmetics for depigmentation[2],such as age spots and freckle,caused by the accumulation of an excessive level of epidermal pigmentation.Accordingly,the development of safe and effective tyrosinase inhibitors is of great concern in clinical medicine,and cosmetic industries.Kojic acid（1） is produced by various bacteria and fungi,such as,Penicillium and Aspergillus,and is widely used as a skin-whitening agent because it can inhibit tyrosinase[3].However,it’s inhibiting effect and storage properties are inadequate for use in cosmetics.Triazole is the core structural motif in a variety of different compounds in medicinal chemistry and has been reported to exhibit a broad range of biological properties,including enzyme inhibition,antimicrobial,antinociceptive,and anti-inflammatory activities[4].Studies by Usman Ghani et al.[5]have demonstrated that 5-substituted-3- mercapto-4-amino-1,2,4- triazole（4） derivatives have promising inhibitory activities of tyrosinase.Therefore,in view of exploring new,potent and safer inhibitors of tyrosinase,we designed a novel compounds by combining structures of two putative tyrosinase inhibitors,kojic acid（1） and 5-substituted-3-mercapto-4-am

关键词： kojic acid derivatives tyrosinase inhibitors mushroom tyrosinase 1,2,4-triazole

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Chinese Journal of Integrative Medicine 2024年第5期30卷 449-457页

作者： xie Shuang-ran MA Liang XU Xin-yu ZHOU Shu xie Hui-miao xie Chang-sheng The First Clinical Medical College Zhejiang Chinese Medical UniversityHangzhou 310053China Department of Medical Oncology Hangzhou Traditional Chinese Medicine Hospital Affiliated to Zhejiang Chinese Medical UniversityHangzhou 310007China Department of Dermatology the Third Xiangya HospitalCentral South UniversityChangsha 410013China Department of Famous Chinese Medicine Clinic the Second Affiliated Hospital of Zhejiang Chinese Medical UniversityHangzhou 310005China Department of Medical Oncology the First Affiliated Hospital of Zhejiang Chinese Medical UniversityHangzhou 310006China

Backgroup:Currently,aromatherapy is being increasingly utilized in clinical practice,particularly in managing the side effects associated with radiotherapy and chemoradiotherapy.However,it remains to be established whether aromatherapy can effectively alleviate these symptoms.Objective:To investigate the effects of aromatherapy on the physical and mental health of patients with cancer undergoing radiotherapy and chemotherapy.Methods:Seven databases were researched from inception until September 29,2023,including PubMed,Scopus,and Web of Science,Chinese National Knowledge Infrastructure,Wanfang database,China Biology Medicine disc and VIP Chinese Medical Journal Database.Review Manager version 5.3 was utilized for data analysis.The Cochrane Risk of Bias tool RoB2 was employed to evaluate the quality of the literature included in the study.Evidence quality rating was assessed using the Grading of Recommendations Assessment,Development,and Evaluation(GRADE) approach through the GRADEpro GDT online tool.Results:Nineteen studies involving 1,541 patients were included.Aromatherapy can alleviate nausea [relative risk(RR)=0.64,95% confidence interval(CI):0.53 to 0.78,Pxiety.The risk of bias was high in the included studies using the Cochrane Risk of Bias tool RoB2,and no studies were considered to be of high grade according to the GRADE system.Conclusions:Aromatherapy is an efficacious,safe and economic adjunctive therapy for cancer patien

关键词： aromatherapy cancer chemoradiotherapy physical psychological

Turbulence Statistics of Thermo-Buoyancy Supercritical Fuel Flow in a Regenerative Cooling Channel

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Journal of Thermal Science 2024年第1期33卷 126-137页

作者： SUN Feng xie Gongnan School of Marine Science and Technology Northwestern Polytechnical UniversityXi'an 710072China Department of Thermal Engineering Tsinghua UniversityBeijing 100084China

Active regenerative cooling with supercritical hydrocarbon fuel is considered as the most promising thermal protection method.The existence of buoyancy force would lead to strongly anisotropic flow and thermal transport characteristics.It is closely related to the cooling performance of the engine.To elucidate the mechanisms of turbulent transport,the large eddy simulation(LES) was performed to assess turbulence statistics within different turbulence scales.The results indicated that the buoyancy and inertial force together dominated the change of turbulent structure.Moreover,the spatial thermal buoyancy effect significantly suppressed the vertical velocity fluctuation.This is due to the laminar motion caused by the buoyancy force,thereby weakening the thermal transport.For the statistics of velocity fluctuation,it was found that the buoyancy force and inertial force greatly weaken the vertical and streamwise velocity fluctuation,respectively.For the statistics of thermal transport,the results pointed out that the near-wall heat transport characteristics need to be paid more attention.The thickness of the temperature mixing boundary layer led to the attenuation of vertical heat flux,which inhibited vertical temperature diffusion and predisposed to extreme conditions of heat transfer deterioration.The results can enhance the academic understanding of the heat transfer mechanism of supercritical fluids,and give guidance for further applications of thermal protection.

关键词： active regenerative cooling large eddy simulation(LES) buoyancy force turbulence statistics