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Analysis of large datasets for identifying molecular targets in intestinal polyps and metabolic disorders

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BIOCELL 2024年第3期48卷 415-429页

作者： SHAN OU YUN XU QINGLAN LIU TIANWEN yang WEI CHEN xiu YUAN XIN ZUO PENG SHI jie YAO Department of Gastroenterology The First Affiliated Hospital of Chongqing Medical and Pharmaceutical CollegeChongqingChina

Background:The interrelation between intestinal polyps,metabolic syndrome(MetS),and colorectal cancer(CRC)is a critical area of *** research focuses on pinpointing potential molecular targets to understand the link between intestinal polyp formation,metabolic irregularities,and CRC ***:We examined clinical samples from patients with intestinal polyps coexisting with MetS and compared them with samples from patients with standard intestinal *** sequencing and public database analysis were employed to identify significant pathways and *** targets were then validated through immunohistochemistry(IHC).Following the RNA interference of key target expression,a series of experiments,including the cell counting kit-8 assay,colony formation,wound healing,and Transwell assays,were ***:Comparative analysis revealed 75 up-regulated and 61 down-regulated differentially expressed genes(DEGs)in the MetS polyp group *** *** encyclopedia of genes and genomes(KEGG)pathway enrichment suggested these DEGs were primarily associated with cell cycle and *** with comparative toxicogenomics database(CTD)and the cancer genome atlas(TCGA)databases highlighted 44 key CRC-related *** interaction networks indicated connections of purkinje cell protein 4(PCP4),olfactomedin 1(OLFM1),fibronectin 1(FN1),and transforming growth factor beta 3(TGF-β3)with the mitogen-activated protein kinase(MAPK)*** correlation studies suggested higher risk associations with FN1,PCP4,and TGF-β3,while OLFM1 was identified as a lower risk *** analysis revealed a decrease in OLFM1 in MetS-associated intestinal *** interference with OLFM1 in polyp epithelial cells,there was a significant enhancement in cell proliferation,colony formation,and cell migration and invasion ***:Our study highlights a significant decrease in OLFM1 expression in MetS-associated intestinal

关键词： Colorectal cancer Metabolic syndrome Intestinal polyp OLFM1 Exosome

Sequential enantioselective Ugi-4CR/post-Ugi transformation strategy:a precise construction of structurally diverse azaspiro polycyclic scaffolds

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Science China Chemistry 2024年第2期67卷 576-586页

作者： Xiao-Bao Wu Jun-xiu Shi Yi-Ming Ou Hua-jie Jiang Yi-Jun Fang Qi-Ming Wang Quan Gao jie Yu Department of Applied Chemistry Anhui Province Engineering Laboratory for Green Pesticide Development and ApplicationAnhui Province Key Laboratory of Crop Integrated Pest ManagementAnhui Agricultural UniversityHefei230036China

A privileged strategy has been developed for the precise construction of enantioenriched azaspiro polycyclic *** diverse azaspiro polycycles bearing multiple contiguous stereocenters are obtained with excellent results(up to 99:1 e.r.,>95:5 d.r.) via sequential enantioselective four-component Ugi reactions/post-Ugi transformations with substrates containing prerequisite functional groups in the presence of anionic stereogenic-at-cobalt(Ⅲ) complexes.

关键词： asymmetric catalysis post-Ugi transformation anionic stereogenic-at-cobalt(Ⅲ)complex azaspiro polycyclic scaffold one-pot synthesis

In situ meso-tetra(4-carboxyphenyl)porphyrin ligand substitution in Hf-MOF for enhanced catalytic activity and stability in photoredox reactions

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Rare Metals 2024年第6期43卷 2682-2694页

作者： jie Hu Hong-Xin Lao xiu-Wu Xu Wei-Kang Wang Le-Le Wang Qin-Qin Liu School of Materials Science and Engineering Jiangsu UniversityZhenjiang 212013China College of Chemistry and Materials Engineering Research Center of Carbon NeutralityAnhui Normal UniversityWuhu 241002China Fujian Provincial Key Laboratory of Ecology-Toxicological Effects and Control for Emerging Contaminants Putian UniversityPutian 351100China

Though there are numerous intrinsic merits of metal-organic frameworks(MOFs),low charge separation efficiency has imposed heavy restrictions on their photocatalytic ***,in situ porphyrin ligand substitution,as a strategy for improving the charge separation efficiency and increasing the amounts of active sites,has been designed and realized in a Hf-biphenyl dicarboxylic acid(BPDC)***,a size and geometry matched meso-tetra(4-carboxyphenyl)porphyrin(TCPP)ligand was selected and doped into Hf-BPDC MOF by forming coordinating bonds with Hf centers,forming dualligand Hf-BPDC-TCPP *** resultant Hf-BPDC-TCPP MOF showed significantly improved activity and chemical stability in the photocatalytic H_(2)generation(261μmol·g^(-1)·h^(-1))and tetracycline(TC)degradation reactions(95.8%),which was 48 and 1.47 folds higher than that of the Hf-BPDC *** and electrochemical studies revealed that the introduction of porphyrin ligand could generate a stronger internal electric field for boosting the charge separation and transfer,increase the specific surface area for providing more active sites,and narrow the band gap to enhance the visible light *** in situ ligand substitution method provides a promising approach to build a tunable platform for constructing high-performance MOF photocatalysts.

关键词： Ligand substitution Metal organic frameworks Meso-tetra(4-carboxyphenyl)porphyrin Hydrogen evolution reaction Tetracycline degradation

Efficacy and Safety of Ganyushu Granule in Treatment of Premenstrual Syndrome with Gan(Liver)Depression and Qi Stagnation Syndrome:A Randomized,Double-Blind,Multicenter,Phase-ⅡClinical Trial

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Chinese Journal of Integrative Medicine 2024年第9期30卷 771-779页

作者： TENG xiu-xiang XU Lian-wei LIN jie ZHANG Jin-feng ZHANG Qin SUN Yun yang De-feng LI Hong-mei ZHAO Pei LIU Jun Department of Gynecology Beijing Hospital of Traditional Chinese MedicineCapital Medical UniversityBeijing100700China Department of Gynecology Longhua HospitalShanghai University of Traditional Chinese MedicineShanghai200032China Department of Gynecology The First Hospital of Hunan University of Chinese MedicineChangsha410021China Department of Gynecology Shanxi Traditional Chinese Medicine HospitalTaiyuan030024China Department of Gynecology Hangzhou Hospital of Traditional Chinese MedicineHangzhou310005China Department of Gynecology Wenzhou Hospital Affiliated to Zhejiang University of Traditional Chinese MedicineWenzhouZhejiang Province325000China Department of Gynecology Luoyang First People’s HospitalLuoyangHenan Province471000China Department of Gynecology The Second Affiliated Hospital of Heilongjiang University of Chinese MedicineHarbin150001China

Objective:To confirm the efficacy and safety of Ganyushu Granule(GYSG)in treating premenstrual syndrome(PMS)in patients with Gan(Liver)depression and qi stagnation syndrome(GDQSS)and determine its effective ***:From June 2018 to March 2021,a total of 240 PMS women with GDQSS were included and randomly divided into 3 groups in a 1:1:1 ratio using central block randomization:high-dose GYSG group(n=78,GYSG 2 packs/time),low-dose GYSG group(n=82,GYSG and its simulant 1 pack/time),and placebo group(n=80,GYSG simulant 2 packs/time).Treatment with GYSG or placebo was given thrice daily and for up to 3 menstrual *** outcomes were PMS diary(PMSD)score and premenstrual tension syndrome self-rating scale(PMTS).Secondary outcomes were Chinese medicine(CM)syndrome ***,PMTS,and efficacy of CM were evaluated with menstrual cycles during the treatment *** indicators were analyzed after each menstrual *** analyses were performed using an intention-to-treat method,and clinical safety was ***:Of the 216 patients included in the effectiveness analysis,70,75,and 71 patients were in the high-,low-dose GYSG,and placebo groups,*** the 2nd treatment cycle,the change in PMSD scores in the high-and low-dose groups was lower than that in the placebo group(P<0.05).PMTS scores in the high-dose GYSG group after the 1st treatment cycle was lower than that in the placebo group(P<0.05),while after the 3rd treatment cycle,that in the low-dose group was lower than that in the placebo group(P<0.05).After the 2nd treatment cycle,the high-dose GYSG group had the best CM syndrome efficacy(P<0.05).No serious adverse reactions were ***:GYSG was safe and well-tolerated at both doses for treating PMS patients with ***-dose GYSG might be the optimal dose for a phaseⅢtrial.

关键词： premenstrual syndrome Chinese medicine Ganyushu Granule randomized controlled trial

Analyzing the surface passivity effect of germanium oxynitride:a comprehensive approach through first principles simulation and interface state density

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Nuclear Science and Techniques 2024年第5期35卷 74-84页

作者： Sheng-jie Du xiu-Xia Li yang Tian Yuan-Yuan Liu Ke Jia Zhong-Zheng Tang Jian-Ping Cheng Zhi Deng Yu-Lan Li Zheng-Cao Li Sha-Sha Lv College of Nuclear Science and Technology Joint Laboratory of Jinping Ultra‑Low Radiation Background Measurement of Ministry of Ecology and Environment Key Laboratory of Beam Technology of Ministry of Education Beijing Normal UniversityBeijing Normal UniversityBeijing 100875China Joint Research Center Nuctech Company LimitedBeijing 100084China Department of Engineering Physics Key Laboratory of Particle&Radiation Imaging of Ministry of EducationTsinghua UniversityBeijing 100084China Key Laboratory of Advanced Materials(MOE) School of Materials Science and EngineeringTsinghua UniversityBeijing 100084China

High-purity germanium(HPGe)detectors,which are used for direct dark matter detection,have the advantages of a low threshold and excellent energy *** surface passivation of HPGe has become crucial for achieving an extremely low energy *** this study,first-principles simulations,passivation film preparation,and metal oxide semiconductor(MOS)capacitor characterization were combined to study surface *** calculations of the energy band structure of the -H,-OH,and -NH_(2) passivation groups on the surface of Ge were performed,and the interface state density and potential with five different passivation groups with N/O atomic ratios were accurately analyzed to obtain a stable surface *** on the theoretical calculation results,the surface passivation layers of the Ge_(2)ON_(2) film were prepared via magnetron sputtering in accordance with the optimum atomic ratio *** microstructure,C-V,and I-V electrical properties of the layers,and the passivation effect of the Al/Ge_(2)ON_(2)/Ge MOS were characterized to test the interface state *** mean interface state density obtained by the Terman method was 8.4×10^(11) cm^(-2) eV^(-1).The processing of germanium oxynitrogen passivation films is expected to be used in direct dark matter detection of the HPGe detector surface passivation technology to reduce the detector leakage currents.

关键词： Surface passivation High purity germanium detector Germanium nitrogen oxide Interface state density

Discovery of a potential bladder cancer inhibitor CHNQD-01281 by regulating EGFR and promoting infiltration of cytotoxic T cells

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Marine Life Science & Technology 2024年第3期6卷 502-514页

作者： Jian-Yu Liu Yao-Yao Jiang Peng-jie Li Bo Yao Yi-Jing Song Ji-xiu Gao Gulab Said yang Gao Jun-Yu Lai Chang-Lun Shao Key Laboratory of Marine Drugs the Ministry of Education of ChinaSchool of Medicine and PharmacyOcean University of ChinaQingdao 266003China Department of Critical Care Medicine the Affiliated Hospital of Qingdao UniversityQingdao 266003China Department of Chemistry Women University SwabiSwabi 23430Pakistan Laoshan Laboratory Qingdao 266237China Key Laboratory of Tropical Medicinal Resource Chemistry of Ministry of Education College of Chemistry and Chemical EngineeringHainan Normal UniversityHaikou 571158China

As one of the common malignancies that threaten human life,bladder cancer occurs frequently with a high mortality rate in the world,due to its invasion,recurrence and drug *** products from marine microorganisms are becoming the hotspots in discovery of new candidate drug entities,especially in the area of *** A(BFA)is a natural Arf-GEFs inhibitor,but due to the low aqueous solubility,strong toxicity,and poor bioavailability,it is urgent to conduct structural optimization ***,a new BFA pyridine acrylate derivative CHNQD-01281 with improved solubility was prepared and found to exert moderate to strong antiproliferative activity on a variety of human cancer cell *** was noteworthy that CHNQD-01281 was most sensitive to two bladder cancer cell lines T24 and J82(IC50=0.079 and 0.081μmol/L)with high selectivity index(SI=14.68 and 14.32),suggesting a superior safety to *** vivo studies revealed that CHNQD-01281 remarkably suppressed tumor growth in a T24 nude mice xenograft model(TGI=52.63%)and prolonged the survival time(ILS=68.16%)in an MB49 allogeneic mouse model via inducing infiltration of cytotoxic T *** mechanism exploration indicated that CHNQD-01281 regulated both EGFR/PI3K/AKT and EGFR/ERK pathways and mediated the chemotactic effect of chemokines on immune effector ***,CHNQD-01281 may serve as a potential therapeutic agent for bladder cancer through multiple mechanisms.

关键词： Bladder cancer Marine natural products Brefeldin A EGFR/PI3K/AKT EGFR/ERK T-cell infiltration

De novo Synthesis of Chiral 3,4-Dihydroquinazolines via One-Pot Enantioselective Ugi-Azide/Cyclization Sequences

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Chinese Journal of Chemistry 2024年第18期42卷 2140-2146页

作者： Zu-Kui Xie Jun-Jun Ding Yi-Ming Ou Jun-xiu Shi Meng-Lan Shen Chuan-Zhi Yao Hua-jie Jiang jie Yu Department of Applied Chemistry Anhui Province Engineering Laboratory for Green Pesticide Development and Applicationand Anhui Province Key Laboratory of Crop Integrated Pest ManagementAnhui Agricultural UniversityHefeiAnhui 230036China

Background and Originality Content,3,4-Dihydroquinazoline frameworks have frequently been encountered in natural products and bioactive *** the past decades,these key structures prompted the development of creative pharmaceuticals owing to their prominent biological properties,including trypanothione reductase(TryR)inhibitor,Hepatitis B virus(HBV)inhibitive activities,anticancer activities,etc.(Scheme 1A).[1]Notably,the chirality of the C4 atom is crucial for drug *** example,the DPC-083 is a potent reverse transcriptase inhibitor for the treatment of HIV infection but the undesired enantiomers exhibit virtually no activity.[ia]Therefore,developing synthetic methods for innovative chiral 4-substituted 3,4-dihydroquinazolines is significant and essential for drug discovery.

关键词： Anionic stereogenic-at-cobalt(ll)complex De novo synthesis post-Ugi transformation One-pot sequence Asymmetric synthesis Multicomponentreactions

Targeting Therapeutic Windows for Rheumatoid Arthritis Prevention

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Chinese Journal of Integrative Medicine 2024年第9期30卷 842-851页

作者： GAO Kai-xin yang Yi-hong LIANG Qi MEI Li-yan LIANG You-bang WANG Mao-jie CHEN xiu-min HUANG Qing-chun WEN Ze-huai HUANG Run-yue Section of Rheumatology and Immunology Research The Second Affiliated Hospital of Guangzhou University of Chinese MedicineGuangzhou510120China The Second Clinical Medical College Guangzhou University of Chinese MedicineGuangzhou510405China State Key Laboratory of Dampness Syndrome of Chinese Medicine The Second Affiliated Hospital of Guangzhou University of Chinese MedicineGuangzhou510120China Guangdong-Hong Kong-Macao Joint Lab on Chinese Medicine and Immune Disease Research Guangzhou University of Chinese MedicineGuangzhou510405China Guangdong Provincial Key Laboratory of Clinical Research on Traditional Chinese Medicine Syndrome Guangzhou510120China Guangdong Provincial Key Laboratory of Chinese Medicine for Prevention and Treatment of Refractory Chronic Diseases Guangzhou510120China The Key Unit of Methodology of Clinical Research The Second Affiliated Hospital of Guangzhou University of Chinese MedicineGuangzhou510120China

Rheumatoid arthritis(RA)is a worldwide public health *** to delay or prevent the onset of RA have attracted much attention in recent years,and researchers are now exploring various prevention *** present,there is still no unified consensus for RA prevention,but targeting therapeutic windows and implementing interventions for at-risk individuals are extremely *** to the limited number of clinical trials on pharmacologic interventions,further studies are needed to explore and establish optimal intervention regimens and effective measures to prevent progression to *** this review,we introduce the RA disease process and risk factors,and present research on the use of both Western and Chinese medicine from clinical perspectives regarding RA ***,we describe several complete and ongoing clinical studies on the use of Chinese herbal formulae for the prevention of RA.

关键词： rheumatoid arthritis prevention Chinese medicine review

Highly Hydrolysis-Resistant Polyimide Fibers Prepared by Thermal Crosslinking with Inherent Carboxyl Groups

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Chinese Journal of Polymer Science 2024年第2期42卷 247-255,I0010页

作者： Can-Can Zhang Jun-Long yang Ya-Jiang Huang Guang-Xian Li College of Polymer Science and Engineering State Key Laboratory of Polymer Materials Engineering of ChinaSichuan UniversityChengdu610065China

Easy hydrolysis in alkaline environments limits the use of polyimide fibers in environmental protection. The hydrolysis resistance levels of polyimide fibers can be improved by crosslinking of the macromolecular chains. In this work, crosslinked polyimide fibers(CPI fibers) were produced by intrinsic carboxyl decarboxylation for the first time. The thermal stability of the polyimide fibers containing the intrinsic carboxyl groups(PIC fibers) was studied, and the temperature of the decarboxylation-crosslinking reaction was determined to be 450 ℃. The PIC fibers were hotdrawn to initiate thermal crosslinking of the carboxyl groups and molecular chain orientation at high temperature. The CPI fibers had high tensile strengths(0.72-1.46 GPa) and compressive strengths(401-604 MPa). The oriented macromolecules and chemically crosslinked structure improved the tightness of the molecular chains and endowed the CPI fibers with excellent hydrolytic resistance. The CPI-50 fiber did not dissolve in a 0.5 wt% NaOH solution during heating at 90 ℃ for 10 h, and the tensile strength retention reached 87% when treated in 0.5 wt% NaOH solutions at 90 ℃ for 1 h, providing a guarantee for its application in alkaline corrosive environments.

关键词： Polyimide Carboxyl group Crosslinking Hydrolysis-resistance