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Alisol B 23-acetate promotes white adipose tissue browning to mitigate high-fat diet-induced obesity by regulating mTOR-SREBP1 signaling

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Journal of Integrative Medicine 2024年第1期22卷 83-92页

作者： Lu-lu Han Xin Zhang Hui Zhang Ting Li Yi-chen Zhao Ming-hui Tian Feng-lei sun bo Feng Department of Neurology Three The Fifth People’s Hospital of JinanJinan 250013Shandong ProvinceChina Department of gastroenterology Affiliated Hospital of Shandong University of Traditional Chinese MedicineJinan 250014Shandong ProvinceChina The First Clinical Medical College Shandong University of Traditional Chinese MedicineJinan 250014Shandong ProvinceChina Department of geriatrics the First Affiliated Hospital of Shandong First Medical University(Shandong Provincial Qianfoshan Hospital)Jinan 250014Shandong ProvinceChina Chinese Medicine Culture and Literature Research Institute Shandong University of Traditional Chinese MedicineJinan 250014Shandong ProvinceChina Department of general Medicine Affiliated Hospital of Shandong University of Traditional Chinese MedicineJinan 250014Shandong ProvinceChina Department of Traditional Chinese Medicine the Second People’s Hospital of Haibei PrefectureZangzu Autonomous Prefecture of Haibei810300Qinghai ProvinceChina

Objective Obesity is a global health concern with management strategies encompassing bariatric surgery and anti-obesity drugs;however,concerns regarding complexities and side effects persist,driving research for more effective,low-risk *** promotion of white adipose tissue(WAT)browning has emerged as a promising ***,alisol B 23-acetate(AB23A)has demonstrated efficacy in addressing metabolic disorders,suggesting its potential as a therapeutic agent in obesity ***,in this study,we aimed to investigate the therapeutic potential of AB23A for mitigating obesity by regulating metabolic phenotypes and lipid distribution in mice fed a high-fat diet(HFD).Methods An obesity mouse model was established by administration of an *** and insulin metabolism were assessed via glucose and insulin tolerance *** size was determined using hematoxylin and eosin *** expression of browning markers in WAT was evaluated using Western blotting and quantitative real-time polymerase chain *** cage monitoring involved the assessment of various parameters,including food and water intake,energy metabolism,respiratory exchange rates,and physical ***,oil red O staining was used to evaluate intracellular lipid accumulation.A bioinformatic analysis tool for identifying the molecular mechanisms of traditional Chinese medicine was used to examine AB23A targets and associated signaling *** AB23A administration significantly reduced the weight of obese mice,decreased the mass of inguinal WAT,epididymal WAT,and perirenal adipose tissue,improved glucose and insulin metabolism,and reduced adipocyte ***,treatment with AB23A promoted the expression of browning markers in WAT,enhanced overall energy metabolism in mice,and had no discernible effect on food intake,water consumption,or physical *** 3T3-L1 cells,AB23A inhibited lipid accumulation,and both AB23A and rapamycin inhibited t

关键词： Obesity Alisol B 23-acetate Adipose tissue mTOR-SREBP1 High-fat diet

Mulberry leaf supplementation inhibits skatole deposition by regulating gut microbiota and upregulating liver cytochrome P4501A1 expression in finishing pigs

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Animal Nutrition 2024年第1期16卷 34-44页

作者： Yuqing sun Xiaoming Men Tianbao Lin bo Deng Shi Zhong Jinxi Huo Kaipeng Qin Zhiqiang Lv Ziwei Xu yougui Li Institute of Sericulture and Tea Zhejiang Academy of Agricultural Sciences298 Deshengzhong RoadShangchengHangzhou 310021China Institute of Animal Husbandry and Veterinary Science Zhejiang Academy of Agricultural Sciences298 Deshengzhong RoadShangchengHangzhou 310021China

Skatole,a strong fecal odor substance,is generated through microbial degradation of tryptophan in the animal *** easily accumulates in adipose tissue and affects meat *** this study,the effect of mulberry leaf supplementation on skatole in finishing pigs was *** a 35-day trial,20 finishing pigs(barrows and gilts)were fed with a basal diet or basal diet with 6%mulberry *** performance of the pigs(n=10)was automatically recorded by a performance-testing feeder system and 8 pigs in each treatment were slaughtered and sampled for the remaining *** and short-chain fatty acids were detected using HPLC and gas chromatography,*** microbiota were analyzed using 16S r RNA gene *** metabolomics analysis of feces and serum was performed with UHPLC-MS/*** major cytochrome P450(CYP)enzymes that catalyze skatole degradation in the liver were tested by using RT-PCR and Western *** of major bioactive compounds in mulberry leaves on the CYP genes were verified in the hepatic cell line Hep g2 in an in vitro test(n=3).In finishing pigs,mulberry leaf supplementation had no significant effect on the average daily gain,average daily feed intake,and feed conversion ratio(P>0.05),but reduced skatole levels in feces,serum,and backfat(Pg bacteria Megasphaera and Olsenella(Pgnificantly reduced in feces by mulberry leaf supplementation(Pgs treated with mulberry leaves,liver CYP1A1 expression was increased(Pgatively correlated with skatole content in backfat(P=0.045).The in vitro test demonstrated that mulberry leaf polyphenols and polysaccharides could directly stimulate CYP1A1 expression in

关键词： Pig Skatole Mulberry leaf Microbiota Cytochrome P450

Discovery of proqodine A derivatives with antitumor activity targeting NAD(P)H:quinone oxidoreductase 1 and nicotinamide phosphoribosyltransferase

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Chinese Journal of Natural Medicines 2024年第1期22卷 75-88页

作者： SONg Jiangzhou ZOU guiqing ZHAO Zhou ZHU Ya XUE Jiayu AO Lanjia sun Huiyong HAO Haiping ZHANg bo XU Xiaowei State Key Laboratory of Natural Medicines Key Lab of Drug Metabolism and PharmacokineticsChina Pharmaceutical UniversityNanjing 210009China State Key Laboratory of Natural Medicines China Pharmaceutical UniversityNanjing 210009China

NAD(P)H:quinone oxidoreductase 1(NQO1)is a flavin protease highly expressed in various cancer ***1 catalyzes a futile redox cycle in substrates,leading to substantial reactive oxygen species(ROS)*** ROS generation results in extensive DNA damage and elevated poly(ADP-ribose)polymerase 1(PARP1)-mediated consumption of nicotinamide adenine dinucleotide(NAD^(+)),ultimately causing cell *** phosphoribosyltransferase(NAMPT),the rate-limiting enzyme in the NAD^(+)salvage synthesis pathway,emerges as a critical target in cancer *** concurrent inhibition of NQO1 and NAMPT triggers hyperactivation of PARP1 and intensive NAD+*** this study,we designed,synthesized,and assessed a novel series of proqodine A derivatives targeting both NQO1 and *** these,compound T8 demonstrated potent antitumor ***,T8 selectively inhibited the proliferation of MCF-7 cells and induced apoptosis through mechanisms dependent on both NQO1 and *** discovery offers a promising new molecular entity for advancing anticancer research.

关键词： NQO1 ROS NAMPT NAD^(+) T8

Cross section determination of^(27)Al(n,2n)^(26)Al reaction induced by 14-MeV neutrons uniting with D-T neutron activation and AMS techniques

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Nuclear Science and Techniques 2024年第6期35卷 78-89页

作者： Xian-Lin Yang Chang-Lin Lan Yu-Ting Wei Yi Zhang gong Jiang bo Xie Yu Liu Hong-Tao Shen Xiao-Jun sun School of Nuclear Science and Technology Lanzhou UniversityLanzhou 730000China MOE Frontiers Science Center for Rare Isotopes Lanzhou UniversityLanzhou 730000China State Key Laboratory of Environmental geochemistry Institute of GeochemistryChinese Academy of SciencesGuiyang 550081China guangxi Key Laboratory of Nuclear Physics and Nuclear Technology Guangxi Normal UniversityGuilin 541004China

Aluminum is the primary structural material in nuclear engineering,and its cross section induced by 14-MeV neutrons is of great *** address the issue of insufficient accuracy for the^(27)Al(n,2n)^(26)Al reaction cross section,the activation method and accelerator mass spectrometry(AMS)technique were used to determine the^(27)Al(n,2n)^(26)Al cross section,which could be used as a D-T plasma ion temperature monitor in fusion *** the China Academy of Engineering Physics,neutron activation was performed using a K-400 neutron generator produced by the T(d,n)4He ***^(26)Al∕^(27)Al isotope ratios were measured using the newly installed gYIg 1 MV AMS at the Institute of geochemistry,Chinese Academy of *** neutron flux was monitored by measuring the activity of 92mNb produced by the 93Nb(n,2n)92mNb *** measured results were compared with available data in the experimental nuclear reaction database,and the measured values showed a reasonable degree of consistency with partially available literature *** newly acquired cross-sectional data at 12 neutron energy points through systematic measurements clarified the divergence,which has two different growth trends from the existing experimental *** obtained results are also compared with the corresponding evaluated database,and the newly calculated excitation functions with TALYS−1.95 and EMPIRE−3.2 codes,the agreement with CENDL−3.2,TENDL-2021 and EMPIRE−3.2 results are generally acceptable.A substantial improvement in the knowledge of the^(27)Al(n,2n)^(26)Al reaction excitation function was obtained in the present work,which will lay the foundation for the diagnosis of the fusion ion temperature,testing of the nuclear physics model,evaluation of nuclear data,etc.

关键词： 14-MeV neutron ^(27)Al(n,2n)^(26)Al Cross section AMS

griseofulvin enantiomers and bromine-containing griseofulvin derivatives with antifungal activity produced by the mangrove endophytic fungus Nigrospora ***1

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Marine Life Science & Technology 2024年第1期6卷 102-114页

作者： ge Zou Wencong Yang Tao Chen Zhaoming Liu Yan Chen Taobo Li gulab Said Bing sun bo Wang Zhigang She School of Chemistry Sun Yat-sen UniversityGuangzhou 510275China State Key Laboratory of Applied Microbiology Southern China Guangdong Provincial Key Laboratory of Microbial Culture Collection and ApplicationInstitute of MicrobiologyGuangdong Academy of SciencesGuangzhou 510070China School of Pharmacy Anhui Medical UniversityHefei 230032China Department of Chemistry Women University SwabiSwabi 23430Pakistan

Marine microorganisms have long been recognized as potential sources for drug *** was one of the first antifungal natural products and has been used as an antifungal agent for *** this study,12 new griseofulvin derivatives[(±)-1-2,(+)-3,(±)-4,10-12,and 14-15]and two new griseofulvin natural products(9 and 16)together with six known analogues[(-)-3,5-8,and 13]were isolated from the mangrove-derived fungus Nigrospora ***1 treated with 0.3%NaCl or 2%NaBr in rice solid *** 2D structures and absolute configurations were established by extensive spectroscopic analysis(1D and 2D NMR,HRESIMS),ECD spectra,computational calculation,DP4+analysis,and X-ray single-crystal *** 1-4 represent the first griseofulvin enantiomers with four absolute configurations(2S,6'S;2R,6'R;2S,6'R;2R,6'S),and compounds 9-12 represent the first successful production of brominated griseofulvin derivatives from fungi via the addition of NaBr to the culture *** the antifungal assays,compounds 6 and 9 demonstrated significant inhibitory activities against the fungi Colletotrichum truncatum,Microsporum gypseum,and Trichophyton mentagrophyte with inhibition zones varying between 28 and 41 mm(10μg/disc).The structure-activity relationship(SAR)was analyzed,which showed that substituents at C-6,C-7,C-6'and the positions of the carbonyl and double bond of griseofulvin derivatives significantly affected the antifungal activity.

关键词： Mangrove endophytic fungus Nigrospora sp. griseofulvin Antifungal activity

Chronic infectious unilateral giant thyroid cyst related to diabetes mellitus:A case report

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World Journal of Clinical Cases 2024年第8期12卷 1497-1503页

作者： Jiang-bo Liu Shi-Lei Zhang Wen-Long Jiang Hai-Kuan sun Hao-Chen Yang Department of Thyroid and Breast Surgery The First Affiliated HospitalCollege of Clinical MedicineHenan University of Science and TechnologyLuoyang 471000Henan ProvinceChina Clinical Medicine School The First Clinical CollegeChongqing Medical UniversityChongqing 400016China

BACKgROUND Patients rarely develop complicated infections in thyroid ***,we describe a patient with chronic infected unilateral giant thyroid cyst related to diabetes mellitus(DM).CASE SUMMARY A 66-year-old male was admitted due to an evident neck lump for 5 d after approximately 40 years of gradually progressive neck mass and 7 years of *** ultrasound and computed tomography scan showed a giant lump in the left thyroid gland *** was diagnosed with a large thyroid nodule complicated by tracheal dislocation and had surgical *** exploration revealed evident inflammatory edema and exudation between the left anterior neck muscles,the nodule and glandular ***,inflammatory lesions did not affect major neck ***,a left partial thyroidectomy was *** observation showed that the cystic thyroid mass consisted of extensive cystic wall calcification and was rich in massive rough sand-like calculi content and purulent *** pathology confirmed benign thyroid cyst with chronic *** The progression of this chronic infectious unilateral giant thyroid cyst may have been related to DM,and identifying blood vessels involvement can prevent serious complications during operation.

关键词： Thyroid nodule Infection Diabetes mellitus Surgery Case report

Chalcone derivatives as novel,potent and selective inhibitors against human Notum:Structure–activity relationships and biological evaluations

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Chinese Chemical Letters 2024年第3期35卷 321-325页

作者： Jin-Hui Shi Bei Zhao Li-Lin Song Yu-Qing Song Meng-Ru sun Tian Tian Hong-Yu Chen Yun-Qing Song Jian-Ming sun guang-bo.ge Shanghai Frontiers Science Center of TCM Chemical Biology Institute of Interdisciplinary Integrative Medicine Research Shanghai University of Traditional Chinese MedicineShanghai 201203China Dalian Engineering Research Center for Carbohydrate Agricultural Preparations Liaoning Provincial Key Laboratory of CarbohydratesDalian Institute of Chemical PhysicsChinese Academy of SciencesDalian 116023China Seventh People's Hospital of Shanghai University of Traditional Chinese Medicine Shanghai 200137China

Human Notum(hNotum)inhibitors could be used for treating Wnt signalling-associated diseases including colorectal ***,two series of chalcone derivatives were designed and synthesized aiming to find selective and potent hNotum ***–activity relationship(SAR)studies showed that 2-methoxyl and 5-bromine substitutions on A-ring significantly enhanced anti-hNotum effect,while 4’-ethoxyl and 3’-alkyl substitutions on B-ring were beneficial for hNotum *** all tested chalcones,B11 displayed the most potent anti-Notum effect(IC_(50)=3.6 nmol/L),good selectivity,excellent chemical stability and suitable metabolic *** investigations showed that B11 acted as a competitive inhibitor of hNotum,while this agent(5μmol/L)significantly weaken the migration abilities of colorectal cancer ***,this study deciphers the SARs of chalcones as hNotum inhibitors and reports a novel and potent hNotum inhibitor with the anti-migration effect on colorectal cancer cells,which offers a promising lead compound to develop novel anti-cancer agents.

关键词： Human notum(hNotum) Chalcone Computer-assisted drug discovery Structure–activity relationship(SAR) Anti-colorectal cancer agent

Traffic safety helmet wear detection based on improved YOLOv5 network

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Optoelectronics Letters 2024年

作者： gUI Dongdong sun bo College of Software Southeast University Quanzhou Equipment Research Centre Haixi Institute Chinese Academy of Sciences

Aiming at the problem that the current traffic safety helmet detection model can’t balance the accuracy of detection with the size of the model and the poor generalization of the model， a method based on improving YOLOv5 is proposed. By incorporating the lightweight ghostNet module into the YOLOv5 backbone network， we effectively reduce the model size. The addition of the Receptive Fields Block (RFB) module enhances feature extraction and improves the feature acquisition capability of the lightweight model. Subsequently， the high-performance lightweight convolution， gSConv， is integrated into the neck structure for further model size compression. Moreover， the baseline model’s loss function is substituted with EIoU， accelerating network convergence and enhancing detection precision. Experimental results corroborate the effectiveness of this improved algorithm in real-world traffic scenarios.

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A rare missense PAX6 mutation causes atypical aniridia in a three-generation Chinese family

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International Journal of Ophthalmology(English edition) 2024年第3期17卷 466-472页

作者： Zhi-bo Lin Chun-Yun Feng Jin Li An-Peng Pan Hai-Sen sun A-Yong Yu Shi-Hao Chen National Clinical Research Center for Ocular Diseases Eye HospitalWenzhou Medical UniversityWenzhou 325027Zhejiang ProvinceChina Department of Ophthalmology the Quzhou Affiliated Hospital of Wenzhou Medical UniversityQuzhou People’s HospitalQuzhou 324000Zhejiang ProvinceChina

●AIM:To investigate the molecular diagnosis of a threegeneration Chinese family affected with aniridia,and further to identify clinically a PAX6 missense mutation in members with atypical aniridia.●METHODS:Eleven family members with and without atypical aniridia were *** family members underwent comprehensive ophthalmic examinations.A combination of whole exome sequencing(WES)and direct Sanger sequencing were performed to uncover the causative mutation.●RESULTS:Among the 11 family members,8 were clinically diagnosed with congenital aniridia(atypical aniridia phenotype).A rare heterozygous mutation c.622C>T(***208Trp)in exon 8 of PAX6 was identified in all affected family members but not in the unaffected members or in healthy control subjects.●CONCLUSION:A rare missense mutation in the PAX6 gene is found in members of a three-generation Chinese family with congenital atypical *** result contributes to an increase in the phenotypic spectrum caused by PAX6 missense heterozygous variants and provides useful information for the clinical diagnosis of atypical aniridia,which may also contribute to genetic counselling and family planning.

关键词： PAX6 gene atypical aniridia missense mutation mutation