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Journal of Thermal Science 2020年第6期29卷 1606-1616页

作者： YAN Hao SU Xiaozhen SHI Haixia cheng maosheng LI Yunqing School of mechanical engineering Hefei University of TechnologyHefei 230009China Anhui Line Pump Co. LtdNingguo 242300China

The management of a cooling-water supply system in a nuclear reactor is performed by valve and reactor coolant pump(RCP)control,which regulates both the pressure and the discharge between certain ***,the RCP has a significant unsteady flow when operating at different *** unsteady pressure pulsation and radial force vector are difficult to calculate because these are affected by the transient properties of the unsteady *** study explores the use of a commercial Computational Fluid Dynamics(CFD)code to comprehensively estimate the unsteady flow of the *** full 3D-URANS equations were solved for different flow rates,and some optimised cases for the unsteady flow were *** results showed that the numerical predictions were validated with the experimental data of a model *** code was used to estimate the velocity streamlines,pressure pulsation and radial force vector in the steady and transient *** flow rates were not equal for the inner and outer passage in the double volute ***,the pulsation of the pressure and radial force was effectively reduced by optimising the staggered angleα.An optimal case was observed whenα=30°.

关键词： unsteady flow reactor coolant pump(RCP) radial force pressure pulsation

Synthesis and Tumor Cytotoxicity of Novel1,2,3-Triazole-substituted 3-Oxo-oleanolic Acid Derivatives

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Chemical Research in Chinese Universities 2016年第6期32卷 938-942页

作者： LI Fengran LIU Yang WANG Shuai WEI Gaofei cheng maosheng Key Laboratory of Structure-based Drug Design and Discovery Ministry of Education Shenyang Pharmaceutical University Shenyang'110016 P. R. China

Fifteen novel 3-oxo-oleanolic acid esters bearing aryl substituted 1,2,3-triazolyl methyl moiety weresynthesized via the method of Copper（I）-catalyzed Huisgen cycloaddifion. The cytotoxicity evaluation results of thesecompounds against five human tumor cell lines show that most of these compounds presented potent activity andselectivity against A375-S2 and HT1080 cells. Compound 6c, with a p-NO2 at the bezene ring, possesses the bestinhibitory activity against A375-S2（IC50=2.82 μmol/L） and HT1080（IC50=1.69 μmol/L）.

关键词： 3-Oxo-oleanolic acid 1,2,3-Triazole Tumor cytotoxicity

Design,Synthesis and Biological Evaluation of Pyrrolo[2,1-c][1,4]benzodiazepine-3,11-dione Derivatives as Novel Neuroprotective Agents

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Chemical Research in Chinese Universities 2021年第3期37卷 647-654页

作者： QUAN Jishun ZHANG Dongping ZHANG Zhuo WANG Jian MA Chao cheng maosheng Key Laboratory of Structure-based Drug Design&Discovery of Ministry of Education School of Pharmaceutical EngineeringShenyang Pharmaceutical UniversityShenyang110016P.R.China

A series of pyrrolo[2,1-c][1,4]benzodiazepine-3,11-dione derivatives was designed and synthesized,and their neuroprotective activity against SH-SY5Y cell injury induced by N-methyl-D-aspartic acid(NMDA)was *** the compounds showed significant neuroprotective effects,especially B16,which showed excellent performance and better activity than the positive control ifenprodil(B16:56.2%±0.6%;ifenprodil:41.0%±2.7%).Further investigation indicated that B16 could attenuate the Ca^(2+)influx induced by NMDA in SH-SY5Y cells and Western blotting also showed that B16 could attenuate the NR2B upregulation in SH-SY5Y cells induced by *** molecular docking results showed that compound B16 fitted in the binding pocket of NR2B-NMDAR well and could interact with binding sites of compounds 1 and 2 *** ADME/Tox prediction results suggested that compound B16 had good blood-brain barrier(BBB)permeability and the zero alert of Pan Assay Interference Structures(PAINS)indicated that B16 could not elicit false-positive *** results strongly suggest that B16 is a promising and effective candidate neuroprotective compound,and that NR2B-NMDAR is a potential target of B16.

关键词： Neuroprotective activity Ca^(2+)influx Western blotting NR2B-NMDA receptor Molecular docking

A review of structural modification and biological activities of oleanolic acid

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Chinese Journal of Natural Medicines 2024年第1期22卷 15-30页

作者： YANG Huali DENG Minghui JIA Hongwei ZHANG Kaicheng LIU Yang cheng maosheng XIAO Wei State Key Laboratory of New-tech for Chinese Medicine Pharmaceutical Process Jiangsu Kanion Pharmaceutical Co.Ltd.Lianyungang 222001China Key Laboratory of Structure-Based Drug Design&Discovery of Ministry of Education School of Pharmaceutical EngineeringShenyang Pharmaceutical UniversityShenyang 110016China

Oleanolic acid(OA),a pentacyclic triterpenoid,exhibits a broad spectrum of biological activities,including antitumor,antiviral,antibacterial,anti-inflammatory,hepatoprotective,hypoglycemic,and hypolipidemic *** its initial isolation and identification,numerous studies have reported on the structural modifications and pharmacological activities of OA and its *** this,there has been a dearth of comprehensive reviews in the past two decades,leading to challenges in subsequent research on *** on the main biological activities of OA,this paper comprehensively summarized the modification strategies and structureactivity relationships(SARs)of OA and its derivatives to provide valuable reference for future investigations into OA.

关键词： Oleanolic acid Derivatives Pentacyclic triterpenoid Structural modification Biological activities

A boronic acid conjugation integrates antitumor drugs into albumin-binding prodrugs-based nanoparticles with robust efficiency for cancer therapy

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Nano Research 2023年第5期16卷 7422-7430页

作者： Weiyue Ban Qiuhua Luo chengda Yan Xiaoying Fan Guorui Zhu maosheng cheng Zhonggui He Mengchi Sun Jin Sun Department of Pharmaceutics Wuya College of InnovationShenyang Pharmaceutical UniversityShenyang 110016China Department of Pharmacy The First Hospital of China Medical UniversityShenyang 110001China Phase I Clinical Trials Center The First Hospital of China Medical UniversityShenyang 110102China Key Laboratory of Structure-Based Drug Design and Discovery Ministry of EducationShenyang Pharmaceutical UniversityShenyang 110016China School of Pharmacy Shenyang Pharmaceutical UniversityShenyang 110016China

Despite great therapeutic effect of Abraxane®,complex preparation technology and unfavorable pharmacokinetics still restricted the clinical application of albumin-based paclitaxel(PTX)nanoparticles(NPs).Herein,we reported that an albumin-binding prodrug,phenylboronic acid-conjugated PTX(P-PTX),can form the uniform NPs with the diameters around 100 nm with the help of albumin via simple one-step nano-precipitation *** albumin-based nanomedicines were stabilized by the integration of a single boronic acid with PTX due to the increased affinity based on multiple intermolecular *** found that albumin-based P-PTX NPs exhibited superior colloidal stability over albumin-based PTX NPs through one-step nanoprecipitation approach,achieving longer in vivo circulation time and higher concentration in tumor than those of the marketed Abraxane®.Furthermore,the albumin-based P-PTX NPs with great stability and enhanced intratumoral enrichment,increased the maximum tolerated dose of PTX,remarkably suppressed the growth of breast tumor and lung metastasis,prolonged survival of melanoma tumors-bearing *** a convenient and effective system gains an insight into the impact of phenylboronic acid group on the albumin-based PTX NPs,provides potent strategy for the rational design of albumin-based antitumor nanomedicines.

关键词： drug delivery Abraxane® albumin-based paclitaxel nanoparticles phenylboronic acid group antitumor nanomedicines

Novel Pt(IV) complex OAP2 induces STING activation and pyroptosis via mitochondrial membrane remodeling for synergistic chemo-immunotherapy

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Acta Pharmaceutica Sinica B 2024年第4期14卷 1742-1758页

作者： Renming Fan Ruizhuo Lin Shuo Zhang Aohua Deng Yongrui Hai Junyan Zhuang Yang Liu maosheng cheng Gaofei Wei Institute of Medical Research Northwestern Polytechnical UniversityXi'an 710072China Research&Development Institute of Northwestern Polytechnical University in Shenzhen Shenzhen 518057China Key Laboratory of Structure-Based Drug Design and Discovery Ministry of EducationSchool of Pharmaceutical EngineeringShenyang Pharmaceutical UniversityShenyang 110016China

Mitochondrial membrane remodeling can trigger the release of mitochondrial DNA (mtDNA), leading to the activation of cellular oxidative stress and immune responses. While the role of mitochondrial membrane remodeling in promoting inflammation in hepatocytes is well-established, its effects on tumors have remained unclear. In this study, we designed a novel Pt(IV) complex, OAP2, which is composed of oxaliplatin (Oxa) and acetaminophen (APAP), to enhance its anti-tumor effects and amplify the immune response. Our findings demonstrate that OAP2 induces nuclear DNA damage, resulting in the production of nuclear DNA. Additionally, OAP2 downregulates the expression of mitochondrial Sam50, to promote mitochondrial membrane remodeling and trigger mtDNA secretion, leading to double-stranded DNA accumulation and ultimately synergistically activating the intracellular cGAS-STING pathway. The mitochondrial membrane remodeling induced by OAP2 overcomes the limitations of Oxa in activating the STING pathway and simultaneously promotes gasdermin-D-mediated cell pyroptosis. OAP2 also promotes dendritic cell maturation and enhances the quantity and efficacy of cytotoxic T cells, thereby inhibiting cancer cell proliferation and metastasis. Briefly, our study introduces the first novel small-molecule inhibitor that regulates mitochondrial membrane remodeling for active immunotherapy in anti-tumor research, which may provide a creative idea for targeting organelle in anti-tumor therapy.

关键词： Anti-tumor drug Prodrug Platinum Chemo-immunotherapy Mitochondrial membrane modeling STING Pyroptosis mtDNA

Synthesis and Tumor Cytotoxicity of Novel N-Substituted Glucosamine-bearing Oleanolic Acid Derivatives

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Chemical Research in Chinese Universities 2014年第4期30卷 639-643页

作者： REN Li LIU Yang YU Guihua GAO Yuan LIU Xin WANG Bo DENG Xiaonan cheng maosheng Key Laboratory of Structure-based Drug Design and Discovery Ministry of Education Shenyang Pharmaceutical University Shenyang 110016 P. R. China

Eleven novel triterpenoid saponins,N-substituted-β-D-glucosaminide derivatives of oleanolic acid,were designed and synthesized via a stepwise glycosylation *** compounds were evaluated for in vitro cytotoxic activity against six different tumor cell *** of the compounds inhibited the growth of,at least,one tumor cell line effectively at micromolar *** structure-activity relationships（SARs） indicate that acylation of the nitrogen of the glucosamine-bearing triterpenoid saponins affords the compounds that are highly cytotoxic towards specific tumor cell lines.

关键词： N-Substituted glucosamine-bearing triterpenoid saponin Tumor cytotoxicity Oleanolic acid

Investigation of Linarinic acid and one of its derivatives against cerebral ischemia in mice

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Asian Journal of Pharmaceutical Sciences 2017年第2期12卷 165-171页

作者： Yihan Wang Chao Zhao Qiujv Wang Huimin Wen Yaru Gu Linlin Fan Chao Ma maosheng cheng Yuyang Zhang School of Life Science and Biopharmaceutics Shenyang Pharmaceutical UniversityNo.103Wenhua RoadShenyang 110016China School of Pharmaceutical Engineering Shenyang Pharmaceutical UniversityNo.103Wenhua RoadShenyang 110016China Key Laboratory of Structure-Based Drug Design and Discovery Shenyang Pharmaceutical UniversityMinistry of EducationNo.103Wenhua RoadShenyang110016China

The study aims to investigate the effects of(-)-Linarinic acid(LA) and one of its derivatives(LAd) on brain injury induced by ischemia. Malonaldehyde(MDA) is determined as an index for lipid peroxidation both in vitro and vivo. Mice were pre-treated with LA and LAd for 3 ***, they were induced to have incomplete cerebral ischemia with both bilateral carotid artery occlusion and hypotension(BCAOH). In the first part of the in vivo experiment, mice were divided into four groups: sham(control), ischemia, ischemia + LA(200 mg/kg, i.g.) and ischemia + LAd(200 mg/kg, i.g.). In the second part, the dose-response of LAd was investigated at 100, 200 and 400 mg/kg i.g., respectively. A modified neurological severity score was developed for evaluating behavioral deficits of the mice with ischemia. Brains of the mice were excised in order to determinate MDA after ischemia for 6 h. Survival time, survival rate, neurological injury score and MDA level in brains were observed. Results were: 1) The data in vitro showed that both LA and LAd could inhibit the generation of MDA. IC50 values obtained by Probit analysis were 2.9 mM for LAd and 4.88 mM for LA;2) BCAOH could significantly shorten the survival span, reduce the survival rate and cause neurological deficits,which were associated with high level of lipid hydroperoxide production in cerebral tissues;3) LAd decreased lipid peroxidation and improved the neurological outcome more than *** is concluded that LAd offers a better neuroprotection than LA against brain damage caused by cerebral ischemia.

关键词： (-)-Linarinic acid Cerebral ischemia Malonaldehyde Mice

Au(Ⅰ)-Catalyzed 6-endo-dig Cyclizations of Aromatic 1,5-Enynes to 2-(Naphthalen-2-yl)anilines Leading to Divergent Syntheses of Benzo[α]carbazole, Benzo[c,h]cinnoline and Dibenzo[i]phenanthridine Derivatives

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Chinese Journal of Chemistry 2022年第1期40卷 46-52页

作者： Jiayue Fu Bingbing Li Xiugui Wang Qida Liang Xiaoshi Peng Lu Yang Tao Wan Xinxiu Wang Bin Lin maosheng cheng Yongxiang Liu Key Laboratory of Structure-Based Drug Design and Discovery(Shenyang Pharmaceutical University) Ministry of EducationShenyangLiaoning 110016China Wuya College of Innovation Shenyang Pharmaceutical UniversityShenyangLiaoning 110016China Institute of Drug Research in Medicine Capital of China BenxiLiaoning 117000China Liaoning Kangboshi Pharmaceutical Co. LTDAnshanLiaoning 114100China

A gold(Ⅰ)-catalyzed 6-endo-dig cyclization of aromatic 1,5-enynes was developed to synthesize 2-(naphthalen-2-yl)*** functional group tolerance of this cyclization was examined systematically and a possible mechanism was *** derivatization of 2-(naphthalen-2-yl)aniline was carried out to facile access to benzo[α]carbazole,benzo[c,h]cinnoline and dibenzo[i]phenanthridine derivatives in a divergent way.

关键词： Gold Homogeneous catalysis 6-endo-dig Cyclization Heterocycles Divergent synthesis

Asymmetric Synthesis of Dihydrospirotryprostatin B via a Silica Gel-Mediated Cyclization of Tryptamine-Ynamide

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Chinese Journal of Chemistry 2024年第12期42卷 1355-1359页

作者： Changhong Han Lu Yang Kaizong Yao Sen Zhang Jiayue Fu Hanyang Sun Hongsheng Xu Bin Lin maosheng cheng Yongxiang Liu Key Laboratory of Structure:Based Drug Design and Discovery of Ministry of Education Shenyang Pharmaceutical UniversityShenyangLiaoning 110016China Wuya College of Innovation Shenyang Pharmaceutical UniversityShenyangLiaoning 110016China Institute of Drug Research in Medicine Capital of China BenxiLiaoning 117000China Zhejiang Shapuaisi Pharmaceutical Co. LtdPinghuZhejiang 314299China

Comprehensive Summary An asymmetric synthesis of dihydrospirotryprostatin B was achieved in 15 steps(8 purifications)from *** main feature of our synthetic strategy is the efficient construction of spirocyclic oxindole intermediate containing a chiral quaternary carbon center,involving the silica gel-mediated cyclization of tryptamine-ynamide and oxidation under neat conditions.

关键词： Asymmetric synthesis Alkaloids Dihydrospirotryprostatin B Tryptamine-ynamide Cross-coupling Silica gel-mediated cyclization Oxidation