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Chinese Chemical Letters 2024年第9期35卷 210-213页

作者： Qi Tan run-zhu fan Wencong Yang Ge Zou Tao Chen Jianying Wu Bo Wang Sheng Yin Zhigang She School of Chemistry Sun Yat-sen UniversityGuangzhou 510006China School of Pharmaceutical Sciences Sun Yat-sen UniversityGuangzhou 510006China

(±)-Mycosphatide A(1a/1b),a pair of highly oxidized enantiomeric polyketides featuring a unique5/5/6/5-fused tetracyclic ring system,were isolated from the mangrove endophytic fungus Mycosphaerella *** structures were established by extensive spectroscopic analyses,single crystal Xray diffraction,and experimental electronic circular dichroism(ECD)spectra *** plausible biosynthetic pathway of 1 was proposed,which involved the generation of a key spiro[4.5]decane ***(+)-1a and(-)-1b exhibited significant lipid-lowering activity in 3T3-L1 adipocytes model,with EC50values of 7.85±1.56 and 8.87±0.80μmol/L,respectively.

关键词： Mangrove endophytic fungus Mycosphaerella sp. Polyketide Highly oxidized Lipid-lowering activity

Discovery of a highly potent and orally available importin-β1 inhibitor that overcomes enzalutamide-resistance in advanced prostate cancer

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Acta Pharmaceutica Sinica B 2023年第12期13卷 4934-4944页

作者： Jia-Luo Huang Xue-Long Yan Dong Huang Lu Gan Huahua Gao run-zhu fan Shen Li fang-Yu Yuan Xinying zhu Gui-Hua Tang Hong-Wu Chen Junjian Wang Sheng Yin School of Pharmaceutical Sciences Sun Yat-sen UniversityGuangzhou 510006China School of Pharmacy Guizhou Medical UniversityGuian New DistrictGuizhou 550025China School of Medicine University of California DavisSacramentoCA 95817USA

Nuclear transporter importin-β1 is emerging as an attractive target by virtue of its prevalence in many ***,the lack of druggable inhibitors restricts its therapeutic proof of *** the present work,we optimized a natural importin-β1 inhibitor DD1 to afford an improved analog DD1-Br with better tolerability(>25 folds)and oral ***1-Br inhibited the survival of castration-resistant prostate cancer(CRPC)cells with sub-nanomolar potency and completely prevented tumor growth in resistant CRPC models both in monotherapy(0.5 mg/kg)and in enzalutamidecombination *** study revealed that by targeting importin-β1,DD1-Br markedly inhibited the nuclear accumulation of multiple CRPC drivers,particularly AR-V7,a main contributor to enzalutamide resistance,leading to the integral suppression of downstream oncogenic *** study provides a promising lead for CRPC and demonstrates the potential of overcoming drug resistance in advanced CRPC via targeting importin-β1.

关键词： Importin-β1 CRPC Drug discovery Enzalutamide-resistance Natural product Cancer Daphnane diterpenoid Nuclear transporter

RE-SEGNN:recurrent semantic evidence-aware graph neural network for temporal knowledge graph forecasting

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Science China(Information Sciences) 2025年

作者： Wenyu CAI Mengfan LI Xuanhua SHI Yuanxin fan Quntao zhu Hai JIN National Engineering Research Center for Big Data Technology and System Services Computing Technology and System Lab Cluster and Grid Computing Lab School of Computer Science and TechnologyHuazhong University of Science and Technology

Temporal knowledge graph(TKG) reasoning, has seen widespread use for modeling real-world events, particularly in extrapolation settings. Nevertheless, most previous studies are embedded models, which require both entity and relation embedding to make predictions, ignoring the semantic correlations among different entities and relations within the same timestamp. This can lead to random and nonsensical predictions when unseen entities or relations occur. Furthermore, many existing models exhibit limitations in handling highly correlated historical facts with extensive temporal depth. They often either overlook such facts or overly accentuate the relationships between recurring past occurrences and their current counterparts. Due to the dynamic nature of TKG, effectively capturing the evolving semantics between different timestamps can be *** address these shortcomings, we propose the recurrent semantic evidenceaware graph neural network(RE-SEGNN), a novel graph neural network that can learn the semantics of entities and relations simultaneously. For the former challenge, our model can predict a possible answer to missing quadruples based on semantics when facing unseen entities or relations. For the latter problem, based on an obvious established force, both the recency and frequency of semantic history tend to confer a higher reference value for the current. We use the Hawkes process to compute the semantic trend, which allows the semantics of recent facts to gain more attention than those of distant facts. Experimental results show that RE-SEGNN outperforms all SOTA models in entity prediction on 6 widely used datasets, and 5 datasets in relation prediction. Furthermore, the case study shows how our model can deal with unseen entities and relations.

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Chiral phosphoramidite ligand-modulated palladium auto-tandem catalysis for asymmetric dehydrogenative dienylation of imines with α-alkenes

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Science China Chemistry 2025年

作者： Zhong-Sheng Nong Hao-fan Qian Ying-Chun Chen Pu-Sheng Wang Liu-zhu Gong Hefei National Research Center for Physical Sciences at the Microscale and Department of Chemistry University of Science and Technology of China Key Laboratory of Drug Targeting and Drug Delivery System (Sichuan University) Ministry of Education and Sichuan Research Center for Drug Precision Industrial Technology West China School of Pharmacy Sichuan University School of Materials and Chemistry Southwest University of Science and Technology

The development of efficient processes allowing rapid access to complex chiral molecules from easily available alkenes is a long-term pursuit in the synthetic chemistry community. Transition metal-catalyzed asymmetric functionalization of allylic C–H bond represents a unique alternative toward this goal. However, enantioselective dehydrogenative transformation of olefins to value-added optically enriched molecules remains yet to be discovered. Here, we report a highly enantioselective dehydrogenative dienylation of imines with unactivated α-alkenes driven by the synergistic action of palladium complex and carboxylic acid. Chiral phosphoramidite ligands turned out to be superior in modulating the performance of palladium autotandem catalysis and allowed a broad range of α-alkenes and imines to be transformed into chiral dienylamines. Mechanistic studies suggest that the dienes could be in situ generated from α-alkenes through a palladium(0)-mediated dehydrogenative process in the presence of excess benzoquinone oxidants, and then participated in the Pd-chiral phosphoramidite-catalyzed intermolecular vinylogous-type addition to the imines activated by the carboxylic acid co-catalyst. Notably, the second β-H elimination occurring in the dienylation event might be the turnover-limiting step.

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基于电子舌技术市售番茄调味酱滋味品质的分析

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食品科技 2016年第11期41卷 248-253页

作者：刘梦婷沈馨王念张润杰朱科帆郭壮湖北文理学院化学工程与食品科学学院鄂西北传统发酵食品研究所襄阳441053

采用电子舌技术和多变量统计学方法相结合的手段,对市售番茄调味酱的滋味品质评价分析。通过主成分和围绕中心点的分割算法分析均发现纳入该研究的18个市售番茄调味酱样品依据其滋味品质均可划分为2个聚类,由冗余分析发现2个聚类间的差... 详细信息

采用电子舌技术和多变量统计学方法相结合的手段,对市售番茄调味酱的滋味品质评价分析。通过主成分和围绕中心点的分割算法分析均发现纳入该研究的18个市售番茄调味酱样品依据其滋味品质均可划分为2个聚类,由冗余分析发现2个聚类间的差异是由于酸味和后味A(涩味的回味)等2个指标导致的。使用高效液相色谱法检测发现乳酸和醋酸为番茄调味酱中的主要有机酸。

关键词：番茄调味酱电子舌有机酸品质评价

Pharmacological targeting cGAS/STING/NF-κB axis by tryptanthrin induces microglia polarization toward M2 phenotype and promotes functional recovery in a mouse model of spinal cord injury

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Neural Regeneration Research 2025年第11期20卷 3287-3301页

作者： Ziwei fan Mengxian Jia Jian Zhou Zhoule zhu Yumin Wu Xiaowu Lin Yiming Qian Jiashu Lian Xin Hua Jianhong Dong Zheyu fang Yuqing Liu Sibing Chen Xiumin Xue Juanqing Yue Minyu zhu Ying Wang Zhihui Huang Honglin Teng Department of Orthopedics(Spine Surgery) the First Affiliated Hospital of Wenzhou Medical UniversityWenzhouZhejiang ProvinceChina School of Pharmacy Hangzhou Normal UniversityHangzhouZhejiang ProvinceChina Department of Neurology The First Affiliated Hospital of Wenzhou Medical UniversityWenzhouZhejiang ProvinceChina Department of Pathology Affiliated Hangzhou First People’s HospitalSchool of MedicineWestlake UniversityHangzhouZhejiang ProvinceChina Department of Clinical Research Center Affiliated Hangzhou First People’s HospitalSchool of MedicineWestlake UniversityHangzhouZhejiang ProvinceChina

The M1/M2 phenotypic shift of microglia after spinal cord injury plays an important role in the regulation of neuroinflammation during the secondary injury phase of spinal cord *** of shifting microglia polarization from M1(neurotoxic and proinflammatory type)to M2(neuroprotective and anti-inflammatory type)after spinal cord injury appears to be *** possesses an anti-inflammatory biological ***,its roles and the underlying molecular mechanisms in spinal cord injury remain *** this study,we found that tryptanthrin inhibited microglia-derived inflammation by promoting polarization to the M2 phenotype in *** promoted M2 polarization through inactivating the cGAS/STING/NF-κB ***,we found that targeting the cGAS/STING/NF-κB pathway with tryptanthrin shifted microglia from the M1 to M2 phenotype after spinal cord injury,inhibited neuronal loss,and promoted tissue repair and functional recovery in a mouse model of spinal cord ***,using a conditional co-culture system,we found that microglia treated with tryptanthrin suppressed endoplasmic reticulum stress-related neuronal *** together,these results suggest that by targeting the cGAS/STING/NF-κB axis,tryptanthrin attenuates microglia-derived neuroinflammation and promotes functional recovery after spinal cord injury through shifting microglia polarization to the M2 phenotype.

关键词： cGAS/STING functional recovery microglia neuroinflammation neuroprotection nuclear factor-κB polarization spinal cord injury tryptanthrin

含硫天然气与氨气的层流火焰速度测量与反应动力学研究

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能源工程 2021年第5期41卷 1-4,9页

作者：季然韩昕璐朱润凡何勇朱燕群王智化浙江大学能源清洁利用国家重点实验室浙江杭州310027

采用热流量法,在常温常压下对不同掺混比例的CH_(4),/H_(2)S、NH_(3)/CH_(4)/H_(2)S的绝热层流火焰速度进行了测量,并通过Chemkin软件对实验气体的层流火焰速度进行了模拟计算。采用Mulvihill+Han组合机理,在当量比为0.7~1.5的范围内都... 详细信息

采用热流量法,在常温常压下对不同掺混比例的CH_(4),/H_(2)S、NH_(3)/CH_(4)/H_(2)S的绝热层流火焰速度进行了测量,并通过Chemkin软件对实验气体的层流火焰速度进行了模拟计算。采用Mulvihill+Han组合机理,在当量比为0.7~1.5的范围内都给出了较为吻合实验数据的结果。实验结果显示,提高H_(2)S的比例,CH_(4)/H_(2)S和NH_(3)/CH_(4)/H_(2)S的绝热层流火焰速度值都有所下降;并且在不同工况下,层流火焰速度峰值始终在当量比φ=1.05处。

关键词：层流火焰速度热流量法氨气酸性天然气

使用合规农药能确保农产品“地头”质量安全吗?——基于豇豆农户的扎根理论分析

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海南大学学报（人文社会科学版） 2025年第1期43卷 119-128页

作者：樊孝凤张娇朱月季海南大学国际商学院海南海口570228

新的农产品质量安全法首次将小农户施药行为纳入监管范围,进一步厘清农户施药行为的影响机理与因素,有助于政府精准施策。通过对海南3个村32户农民豇豆种植过程的全程蹲点跟踪,对豇豆施药环节的参与式观察与深度访谈,运用扎根理论分析... 详细信息

新的农产品质量安全法首次将小农户施药行为纳入监管范围,进一步厘清农户施药行为的影响机理与因素,有助于政府精准施策。通过对海南3个村32户农民豇豆种植过程的全程蹲点跟踪,对豇豆施药环节的参与式观察与深度访谈,运用扎根理论分析了访谈资料。研究发现:农户施药环节是一个复杂的行为选择过程,即使施用合规农药也不能确保农产品在产地的质量安全。在合规农药视角下影响农户施药行为选择的最重要因素是信息渠道,其次是农产品质量安全管理的政策强度、农产品市场价格和农村劳动用工成本。同时,邻里效应在农户施药行为选择中的作用越来越弱。在此基础上提出,要增加农户用药信息的有效供给渠道,加强农产品质量安全的全面检测,坚持为农户提供形式多样的有针对性的有效培训,增加重要食用农产品质量安全关键技术供给与推广,加强农产品“优质优价”市场建设的政策建议,并进一步指出海南自贸港建设和RECP协议实施背景下提升海南农产品质量安全水平的紧迫性。

关键词：合规农药施药行为农产品质量安全扎根理论

Quantitative Trait Loci for Grain Chalkiness and Endosperm Transparency Detected in Three Recombinant Inbred Line Populations of Indica Rice

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Journal of Integrative Agriculture 2013年第1期12卷 1-11页

作者： MEI De-yong zhu Yu-jun YU Yong-hong fan Ye-yang HUANG De-run zhuANG Jie-yun China National Rice Research Institute

Quantitative trait loci（QTL） for percentage of chalky grain,degree of chalkiness,and endosperm transparency were detected using 3 recombinant inbred line populations derived from crosses between parental lines of commercial three-line hybrids of indica *** of the populations showed great variations on heading date,and the other had a short range of heading date variation.A total of 40 QTLs were detected and fell into 15 regions of 10 chromosomes,of which 5 regions were detected for 1 or more same traits over different populations,2 were detected for different traits in different populations,3 were detected for 2 or all the 3 traits in a single population,and 5 were detected for a single trait in a single *** of these QTLs have been reported previously,but a region located on the long arm of chromosome 10 showing significant effects in all the 3 populations has not been reported *** was shown that a number of gene cloned,including the Wx and Alk for the physiochemical property of rice grain,and GW2,GS3 and GW5 for grain weight and grain size,could have played important roles for the genetic control of grain chalkiness in rice,but there are many more QTLs exerting stable effects for rice chalkiness over different genetic *** is worth paying more attentions to these regions which harbor QTL such as the qPCG5.2/qDC5.2/qET5.2 and qPCG10/qDC10/qET10 detected in our *** results also showed that the use of segregating populations having high-uniform heading date could greatly increase the efficiency of the identification of QTL responsible for traits that are subjected to great environmental influence.

关键词： percentage of chalky grain degree of chalkiness endosperm transparency quantitative trait locus headingdate variation indica rice(Oryza sativa L.subsp.indica)

Rapid development methodology of agricultural robot navigation system working in GNSS-denied environment

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Advances in Manufacturing 2023年第4期11卷 601-617页

作者： run-Mao Zhao Zheng zhu Jian-Neng Chen Tao-Jie Yu Jun-Jie Ma Guo-Shuai fan Min Wu Pei-Chen Huang School of Mechanical Engineering Zhejiang Sci-Tech UniversityHangzhou310018People’s Republic of China Key Laboratory of Transplanting Equipment and Technology of Zhejiang ProvinceHangzhou310018People’s Republic of China School of Transportation Zhejiang Industry Polytechnic CollegeShaoxing312000ZhejiangPeople’s Republic of China College of Automation Zhongkai University of Agriculture and EngineeringGuangzhou510225People’s Republic of China

Robotic autonomous operating systems in global n40avigation satellite system(GNSS)-denied agricultural environments(green houses,feeding farms,and under canopy)have recently become a research hotspot.3D light detection and ranging(LiDAR)locates the robot depending on environment and has become a popular perception sensor to navigate agricultural robots.A rapid development methodology of a 3D LiDAR-based navigation system for agricultural robots is proposed in this study,which includes:(i)individual plant clustering and its location estimation method(improved Euclidean clustering algorithm);(ii)robot path planning and tracking control method(Lyapunov direct method);(iii)construction of a robot-LiDAR-plant unified virtual simulation environment(combination use of Gazebo and SolidWorks);and(vi)evaluating the accuracy of the navigation system(triple evaluation:virtual simulation test,physical simulation test,and field test).Applying the proposed methodology,a navigation system for a grape field operation robot has been *** virtual simulation test,physical simulation test with GNSS as ground truth,and field test with path tracer showed that the robot could travel along the planned path quickly and *** maximum and mean absolute errors of path tracking are 2.72 cm,1.02 cm;3.12 cm,1.31 cm,respectively,which meet the accuracy requirements of field operations,establishing the effectiveness of the proposed *** proposed methodology has good scalability and can be implemented in a wide variety of field robot,which is promising to shorten the development cycle of agricultural robot navigation system working in GNSS-denied environment.

关键词： Agricultural robot Global navigation satellite system(GNSS)-denied environment Navigation system 3D light detection and ranging(LiDAR) Rapid developing Methodology