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| 1 | Synthesis and biological evaluation of 8-substituted berberine derivatives as novel anti-mycobacterial agents显示文摘Tuberculosis(TB)is a disease which kills two million people every year and infects over one-third of the world's population.Eighteen new 8-substituted berberine derivatives were synthesized and evaluated for their anti-mycobacterial activities against M ycobacterium tuberculosis(M.tuberculosis)strain H_(37)Rv.Among these compounds,compound 6i was the most effective antitubercular agent with an MIC of 1.0μg/mL.Most importantly,compound 6i also exhibited a potent effect against clinically isolated rifampicin-and isoniazid-resistant M.tuberculosis strains,suggesting a different mode of action from the current drugs.Therefore,it shows potential for the development of new anti-TB agents. | Yanxiang Wang Haigen Fu Yinghong Li Jiandong Jiang Danqing Song | 2012 | Acta Pharmaceutica Sinica B2012，2，6： | 4 |
| 2 | Influence of electric field on the quenched-in vacancy and solute clustering during early stage ageing of Al-Cu alloy显示文摘The effects of electric field on the evolution of excess quenched-in vacancy as well as solute clustering in Al-4wt%Cu alloy, and on the vacancy migration and formation enthalpy of pure aluminum were investigated, using positron annihilation lifetime spectroscopy, high-angle annular dark-field scanning transmission electron microscopy, transmission electron microscopy, hardness measurement and four-probe electrical resistivity measurement. The results showed that the electric field improved age hardening response obviously and postponed the decay of excess vacancies for 30 min during the early stage ageing of Al-4wt%Cu alloy. A large number of 2–4 nm GP zones with dense distribution were observed after 1 min ageing with an electric field applied. The electric field-assisted-aged sample owned a lower coarsening rate of GP zone, which was about three fifths of that in the aged sample without an electric field, from 1 min to 120 min ageing. The electric field contributed 8% increase of the vacancy migration enthalpy(0.663 ± 0.021 e V) of pure Al, comparing with that(0.611 ± 0.023 e V) of pure Al without an electric field. The increase of vacancy migration enthalpy, induced by the electric field, was responsible for the difference on evolution of quenched-in vacancy, rapid solute clustering and age hardening improvement during the early stage ageing of Al-4wt%Cu alloy. | Shang Fu Ying Zhang Huiqun Liu Danqing Yi Bin Wang Yong Jiang Zhiquan Chen Ning Qi | 2018 | Journal of Materials Science & Technology2018，34，2： | 3 |
| 3 | Trophic relationships in the Changjiang River estuarine salt marshes: preliminary investigation from δ^(13)C and δ^(15)N analysis显示文摘To obtain information on food web structure in salt marshes of the Changjiang (Yangtze) River Estuary, the δ13C and δ15N values of primary producers and consumers were determined. The mean δ13C values of 31 dominant consumers ranged from -23.13‰ to -14.37‰. Except for several species (Eriocheir sinensis, Sinonovacula constricta and Potamocorbula ustulata), consumers had intermediate δ13C values between those of benthic microalgae and Spartina alterniflora. The mean δ15N values of 31 dominant consumers varied between 6.87‰ and 13.33‰, which indicate three trophic levels in salt marshes of the Changjiang River Estuary. A total of 18 macroinvertebrates species and four fish species represented primary consumers with trophic levels ranging from 2.0 to 2.7. Secondary consumers included two macroinvertebrates and seven fishes with trophic levels varying between 3.0 and 3.9. The consumers were divided into three trophic guilds, i.e., detritivorous/algae feeders, omnivores and carnivores. The detrital food chain was the main energy flow pathway in the salt marsh food web of the Changjiang River Estuary, and the marsh vascular plants were at least as equally important as microphytobenthos for secondary production. The important trophic function of the salt marsh habitats in the estuary is revealed. | QUAN Weimin HUANG Danqing CHU Tianjiang SHENG Qiang FU Cuizhang CHEN Jiakuan WU Jihua | 2009 | Acta Oceanologica Sinica2009，28，3： | 2 |
| 4 | Gypenoside, the Main Active Compound of Gynostemma pentaphyllum , Mitigates the Diabetic Nephropathy through Down-regulating mTOR显示文摘Background:Diabetic nephropathy(DN),as a complication of diabetes,is featured with hypertension,hyper-glycemia,proteinuria and edema.Gypenoside(GP),the main active compound of Gynostemma pentaphyllum,is proved to be effective for DN.In our previous research,we found that GP could protect the glomerulus and re-duce proteinuria by up-regulating the expression of nestin and down-regulating TGFB1.However,the panoramic mechanism of GP against DN is still unclear.Objective:This research is designed to reveal the mechanism of GP on DN through network pharmacology and in vivo and in vitro experimental verification.Methods:In this study,active compounds and targets of Gynostemma pentaphyllum were collected from TCMSP.DisGeNET was used for obtaining the targets of DN.The protein-protein interaction network was acquired from the STRING database and analyzed by the MCODE plugin.GO and KEGG enrichment analysis were constructed to explore further information.In vivo and in vitro experiments were also carried out to evaluate the reliability of this study.Western blotting and RT-PCR were used to detect mTOR,4E-BP1,p70s6k protein expression and Mtor mRNA expression in DN rats,respectively.AKT1,TP53,ESR1 and PTEN protein expression in MPC-5 cells were detected by Western blotting.Results:Twenty-four compounds and 217 targets were selected from Gynostemma pentaphyllum,of which 36 targets overlapped with DN were taken for the potential targets.The results showed that Quercetin,Rhamnazin,Isofucosterol and 3′-methyleriodictyol corresponded to more targets,AKT1,TP53,MYC,ESR1,PTEN were more active.36 potential targets were mainly involved in autoimmunity,inflammatory response,metabolism and autophagy.In vivo and in vitro experiments showed that GP might protect the podocytes of DN rats by decreasing the protein expression of mTOR,4EBP1,p70s6k,as well as the mRNA expression of Mtor,and it had the function in regulating the potential targets through decreasing the protein expression of AKT1,TP53 and ESR1 and increasing the expression of PTEN.Conclusion:This research demonstrates that various compounds of Gynostemma pentaphyllum may intervenes in DN through targets of multiple signaling pathways,which involves a large number of biological processes.It can provide novel insights for further research of the mechanism of GP in the treatment of DN. | Chao Chen Danqing Fu Yuqian Wu Chen Huang Ping Huang | 2023 | Clinical Complementary Medicine and Pharmacology2023，3，2： | 0 |
| 5 | A hierarchical bilayer architecture for complex tissue regeneration显示文摘Engineering a complete,physiologically functional,periodontal complex structure remains a great clinical challenge due to the highly hierarchical architecture of the periodontium and coordinated regulation of multiple growth factors required to induce stem cell multilineage differentiation.Using biomimetic self-assembly and microstamping techniques,we construct a hierarchical bilayer architecture consisting of intrafibrillarly mineralized collagen resembling bone and cementum,and unmineralized parallel-aligned fibrils mimicking periodontal ligament.The prepared biphasic scaffold possesses unique micro/nano structure,differential mechanical properties,and growth factor-rich microenvironment between the two phases,realizing a perfect simulation of natural periodontal hard/soft tissue interface.The interconnected porous hard compartment with a Young’s modulus of 1409.00±160.83 MPa could induce cross-arrangement and osteogenic differentiation of stem cells in vitro,whereas the micropatterned soft compartment with a Young’s modulus of 42.62±4.58 MPa containing abundant endogenous growth factors,could guide parallel arrangement and fibrogenic differentiation of stem cells in vitro.After implantation in critical-sized complete periodontal tissue defect,the biomimetic bilayer architecture potently reconstructs native periodontium with the insertion of periodontal ligament fibers into newly formed cementum and alveolar bone by recruiting host mesenchymal stem cells and activating the transforming growth factor beta 1/Smad3 signaling pathway.Taken together,integration of self-assembly and microstamping strategies could successfully fabricate a hierarchical bilayer architecture,which exhibits great potential for recruiting and regulating host stem cells to promote synergistic regeneration of hard/soft tissues. | Min Yu Dan Luo Jing Qiao Jiusi Guo Danqing He Shanshan Jin Lin Tang Yu Wang Xin Shi Jing Mao Shengjie Cui Yu Fu Zixin Li Dawei Liu Ting Zhang Chi Zhang Zhou Li Yongsheng Zhou Yan Liu | 2022 | Bioactive Materials2022，7，4： | 0 |
| 6 | A Distributed LRTCO Algorithm in Large-Scale DVE Multimedia Systems显示文摘In the large-scale Distributed Virtual Environment(DVE)multimedia systems,one of key challenges is to distributedly preserve causal order delivery of messages in real time.Most of the existing causal order control approaches with real-time constraints use vector time as causal control information which is closely coupled with system scales.As the scale expands,each message is attached a large amount of control information that introduces too much network transmission overhead to maintain the real-time causal order delivery.In this article,a novel Lightweight Real-Time Causal Order(LRTCO)algorithm is proposed for large-scale DVE multimedia systems.LRTCO predicts and compares the network transmission times of messages so as to select the proper causal control information of which the amount is dynamically adapted to the network latency variations and unconcerned with system scales.The control information in LRTCO is effective to preserve causal order delivery of messages and lightweight to maintain the real-time property of DVE systems.Experimental results demonstrate that LRTCO costs low transmission overhead and communication bandwidth,reduces causal order violations efficiently,and improves the scalability of DVE systems. | Hangjun Zhou Guang Sun Sha Fu Wangdong Jiang Tingting Xie Danqing Duan | 2018 | Computers, Materials & Continua2018，，7： | 0 |
| 7 | Christmas Tree-Shaped Microneedles as FOLFIRINOX Spatiotemporal Delivery System for Pancreatic Cancer Treatment显示文摘As an effective combination chemotherapy,FOLFIRINOX regimen(fluorouracil,leucovorin,irinotecan,and oxaliplatin)has shown definite antitumor eficacy for treating pancreatic cancer(PC)nowadays.However,the traditional systematic administration of these chemotherapeutics limits the drug targeting and causes unwanted effects. | Danqing Huang Xiao Fu Xiaoxuan Zhang Yuanjin Zhao | 2023 | Research2023，，2： | 0 |
| 8 | Liver spheroids on chips as emerging platforms for drug screening显示文摘Liver plays a critical role in drug metabolism and nowadays multi-cellular culture systems aiming at imitating liver-specific morphology and functionality are advancing robustly.Numerous immortalized or stem cell-induced hepatic cell lines have been investigated to enhance the hepatic phenotype in establishing co-culture systems.Owing to the robust progresses of microtechnology and bioengineering,two-dimensional(2D)co-cultures such as sandwich culture and micropatterned co-culture systems have emerged.Controllably arranging the hepatocytes and fibroblasts allows bio-mimic homotypic and heterotypic interactions,and the miniaturized co-culture platform realizes high-throughput and sensitive drug screening.Yet,to address the rapid dedifferentiation and the decreased maintenance of hepatic functions existing in 2D cellular systems,various three-dimensional(3D)and dynamic hepatocyte co-culturing formats have been established to obtain more physiologically relevant liver microsystems and prolonged hepatic functionalities,such as spheroid barcodes,liver organoids,bioengineered hepatic spheroids,and microfluidic perfused liver-on-a-chip.In this review,we first introduce the typical structural color spheroid barcodes which facilitate multiple screening and testing.Then we sketch various advances in liver-imitating cellular co-culture protocols through representative examples.Meanwhile,we summarize current difficulties and propose the prospects of bioengineered liver-on-barcode systems for reliable and high-throughput drug screening. | Danqing Huang Xiaoxuan Zhang Xiao Fu Yan Zu Weijian Sun Yuanjin Zhao | 2021 | Engineered Regeneration2021，2，1： | 0 |
| 9 | Evolution and development of potent monobactam sulfonate candidate IMBZ18g as a dual inhibitor against MDR Gram-negative bacteria producing ESBLs显示文摘A series of new monobactam sulfonates is continuously synthesized and evaluated for their antimicrobial efficacies against Gram-negative bacteria.Compound 33a(IMBZ18G)is highly effective in vitro and in vivo against clinically intractable multi-drug-resistant(MDR)Gram-negative strains,with a highly druglike nature.The checkerboard assay reveals its significant synergistic effect withβ-lactamase inhibitor avibactam,and the MIC values against MDR enterobacteria were reduced up to 4—512folds.X-ray co-crystal and chemoproteomic assays indicate that the anti-MDR bacteria effect of 33a results from the dual inhibition of the common PBP3 and some class A and Cβ-lactamases.Accordingly,preclinical studies of 33a alone and 33a-avibactam combination as potential innovative candidates are actively going on,in the treatment ofβ-lactamase-producing MDR Gram-negative bacterial infections. | Zhiwen Li Zhihao Guo Xi Lu Xican Ma Xiukun Wang Rui Zhang Xinxin Hu Yanxiang Wang Jing Pang Tianyun Fan Yonghua Liu Sheng Tang Haigen Fu Jingpu Zhang Yinghong Li Xuefu You Danqing Song | 2023 | Acta Pharmaceutica Sinica B2023，13，7： | 0 |
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