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Neural Regeneration Research 2011年第18期6卷 1380-1385页

作者： Dong Wan Huifeng Zhu Yong Luo Peng Xie Department of Emergency First Affiliated Hospital of Chongqing Medical University Chongqing 400016 China College of pharmaceutical Sciences & College of Chinese Medicine Southwest University Chongqing 400715 China Department of Neurology First Affiliated Hospital of Chongqing Medical University Chongqing 400016 China

The present study investigated the effects of catalpol, the main constituent of the Chinese herb Rehmannia root, on neurons following brain ischemia, A rat model of focal permanent brain ischemia was established using electrocoagulation, The rats were intrapedtoneally injected with catalpol, at a dose of 5 mg/kg, daily for 1 week, Results showed that the number of neuronal synapses in the motor cortex and growth associated protein 43 expression were increased following catalpol treatment, indicating that catalpol might contribute to neuroplasticity and ameliorate functional neurological deficits induced by cerebral ischemia.

关键词： catalpol growth-associated protein 4:3 neurological function permanent middle cerebral artery occlusion behavioral assessment neurological deficit neuroplasticity neural regeneration

Highly selective oxidation of amines to imines by Mn2O3 catalyst under eco-friendly conditions

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Chinese Chemical Letters 2019年第12期30卷 2282-2286页

作者： Fushan Chen Tao Yang Songlin Zhao Taotao Jiang Lu Yu Houfeng Xiong Chuankun Guo Yufang Rao Yan Liu Liu Liu Jian Zhou Pengxiang Tu Jun Ni Qunfeng Zhang Xiaonian Li Industrial Catalysis Institute of Zhejiang university of Technology Hangzhou 310014China Jiangxi Province Engineering Research Center of Ecological Chemical Industry Jiujiang UniversityJiujiang 332005China School of pharmaceutical and Chemical Engineering Taizhou UniversityTaizhou 318000China

Enhancing the selectivity of imines for the oxidative self-coupling of primary amines was found to be challenging in the heterogeneous *** different manganese oxides(M-3,M-4,M-5) were synthesized by controlling the calcination temperature using a simple template-free oxalate *** prepared manganese oxides were systematically characterized using XRD,N2 sorption,SEM,TEM,XPS,H2-TPR techniques.M-4 gave 96.2% selectivity of imine at 100% conversion of benzylamine,which was far more superior than other existing ***^3+/Mn^4+ ratio was found to affect the selectivity of the *** probable reaction pathway for amines oxidation catalyzed by manganese oxides was proposed for the first time.

关键词： Oxalate route Mn2O3 Self-coupling of amines Heterogeneous catalysis Aerobic oxidation

Quantitative structure-activity relationships of antimicrobial fatty acids and derivatives against Staphylococcus aureus

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Journal of Zhejiang university-Science B(Biomedicine & Biotechnology) 2012年第2期13卷 83-93页

作者： Hui ZHANG Lu ZHANG Li-juan PENG Xiao-wu DONG Di WU Vivian Chi-Hua WU Feng-qin FENG Department of Food Science and Nutrition Zhejiang UniversityHangzhou 310058China ZJU-ENS Joint Laboratory of Medicinal Chemistry College of Pharmaceutical SciencesZhejiang UniversityHangzhou 310058China Department of Food Science and Human Nutrition University of MaineOrono 04469USA

Fatty acids and derivatives(FADs)are resources for natural *** order to screen for additional potent antimicrobial agents,the antimicrobial activities of FADs against Staphylococcus aureus were examined using a microplate *** of fatty acids were the most potent class of fatty acids,among which monotridecanoin possessed the most potent antimicrobial *** conventional quantitative structure-activity relationship(QSAR)and comparative molecular field analysis(CoMFA)were performed to establish two statistically reliable models(conventional QSAR:R2=0.942,Q 2 LOO=0.910;CoMFA:R 2=0.979,Q 2=0.588,respectively).Improved forecasting can be achieved by the combination of these two models that provide a good insight into the structureactivity relationships of the FADs and that may be useful to design new FADs as antimicrobial agents.

关键词： Fatty acid derivatives Quantitative structure-activity relationship Comparative molecular field analysis Antimicrobial activity

Oral nano-formulation improves pancreatic islets dysfunction via lymphatic transport for antidiabetic treatment

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药学学报:英文版 2023年第7期13卷 3137-3152页

作者： Lin Hou Xueyuan Peng Ruiting Wang Yifei Wang Hong Li Huijuan Zhang Yun Zhang Zhenzhong Zhang School of pharmaceutical Sciences Zhengzhou UniversityZhengzhou 450001China Key Laboratory of Targeting Therapy and Diagnosis for Critical Diseases Zhengzhou UniversityZhengzhou 450001China Collaborative Innovation Center of New Drug Research and Safety Evaluation Zhengzhou UniversityZhengzhou 450001China

Type 2 diabetes mellitus(T2DM)therapy is facing the challenges of long-term medication and gradual destruction of pancreatic isletβ-***,it is timely to develop oral prolonged action formulations to improve compliance,while restoringβ-cells survival and ***,we designed a simple nanoparticle with enhanced oral absorption and pancreas accumulation property,which combined apical sodiumdependent bile acid transporter-mediated intestinal uptake and lymphatic *** this system,taurocholic acid(TCA)modified poly(lactic-co-glycolic acid)(PLGA)was employed to achieve pancreas location,hydroxychloroquine(HCQ)was loaded to execute therapeutic efficacy,and 1,2-dilauroyl-sn-glycero-3-phosphocholine(DLPC)was introduced as stabilizer together with synergist(PLGA-TCA/DLPC/HCQ).In vitro and in vivo results have proven that PLGA-TCA/DLPC/HCQ reversed the pancreatic islets damage and dysfunction,thus impeding hyperglycemia progression and restoring systemic glucose homeostasis via only once administration every *** terms of mechanism PLGA-TCA/DLPC/HCQ ameliorated oxidative stress,remodeled the inflammatory pancreas microenvironment,and activated PI3K/AKT signaling pathway without obvious *** strategy not only provides an oral delivery platform for increasing absorption and pancreas targetability but also opens a new avenue for thorough T2DM treatment.

关键词： Type 2 diabetes mellitus Oral drug delivery PLGA nanoparticles Pancreatic isletβ-cells Lymphatic transportation Taurocholic acid Hydroxychloroquine Pancreas microenvironment

Evaluation of the effectiveness of alginate-based hydrogels in preventing peritoneal adhesions

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Regenerative Biomaterials 2023年第1期10卷 614-625页

作者： Zhu Meng Han Wang Yu Liu Minyi Yang Hang Zeng Qianqian Han National Institutes for Food and Drug Control People’s Republic of China School of Materials Science and Engineering Beijing Institute of TechnologyPeople’s Republic of China YanTai university People’s Republic of China China pharmaceutical university People’s Republic of China

Infertility and intestinal blockage are just two examples of the postoperative consequences that can arise from peritoneal damage,which can also result in severe peritoneal fibrosis and peritoneal *** adhesions are still not effectively treated,and both pharmaceutical therapy and biomaterial barriers have only had modest preventative *** this work,we looked into the effectiveness of in-place injectable sodium alginate hydrogel for peritoneal adhesion *** findings demonstrated that sodium alginate hydrogel promoted human peritoneal mesothelial cell proliferation and migration,prevented peritoneal fibrosis by suppressing the production of transforming growth factor-β1,and,most importantly,promoted mesothelium *** findings imply that this brand-new sodium alginate hydrogel is a good candidate material for peritoneal adhesion prevention.

关键词： peritoneal adhesions sodium alginate hydrogel mesothelial cells TGF-β1

Bioautography and its scope in the field of natural product chemistry

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Journal of pharmaceutical Analysis 2015年第2期5卷 75-84页

作者： Saikat Dewanjee Moumita Gangopadhyay Niloy Bhattacharya Ritu Khanra Tarun K.Dua Advanced Pharmacognosy Research Laboratory Department of Pharmaceutical Technology Jadavpur University Biophysics Division Saha Institute of Nuclear Physics

Medicinal plants, vegetables and fruits are the sources of huge number of bioactive lead/scaffolds with therapeutic and nutraceutical importance. Bioautography is a means of target-directed isolation of active molecules on chromatogram. Organic solvents employed in chromatographic separation process can be completely removed before biological detection because these solvents cause inactivation of enzymes and/or death of living organisms. They offer a rapid and easy identification of bioactive lead/scaffolds in complex matrices of plant extracts. Bioautography is a technique to isolate hit（s）/lead（s） by employing a suitable chromatographic process followed by a biological detection system. This review critically describes the methodologies to identify antimicrobial, antioxidant, enzyme inhibitor lead/scaffolds by employing bioautography. A significant number of examples have been incorporated to authenticate the methodologies.

关键词： Bioactivity Bioassay Bioautography Detection principle Thin layer chromatography

Aromatic Polyimides with Tertbutyl-substituted and Pendent Naphthalene Units:Synthesis and Soluble,Transparent Properties

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Chinese Journal of Polymer Science 2015年第8期33卷 1074-1085页

作者： Chan-juan Liu Mei Mei Xiang-lin Pei 黄孝华 Chun Wei Key Laboratory of New Processing Technology for Nonferrous Metal & Materials Ministry of Educationand School of Material Science and EngineeringGuilin University of Technology Ministry of Education Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources School of Chemistry and Pharmaceutical ScienceGuangxi Normal University

A novel non-coplanar aromatic diamine monomer, 3,3＇-ditertbutyl-4,4＇-diaminodiphenyl-4＂-naphthylmethane （TAPN） was synthesized by a condensation reaction of 2-tertbutylaniline and 1-naphthaldehyde under catalyst hydrochloric acid. The structure of the monomer was confirmed by FTIR, NMR, elementary analysis and mass spectrometry. A series of aromatic polyimides （PIs） were synthesized via conventional one-step polycondensation from TAPN and various commercial aromatic dianhydrides. All of the PIs exhibit excellent solubility in common organic solvents, even in low boiling point solvents such as chloroform （CHC13）, tetrahydrofuran （THF） and acetone. The PIs present outstanding thermal stability with the glass transition temperature （Tg） ranged from 299 ℃ to 350 ℃, and the temperature at 10% weight loss ranged from 490 ℃ to 504 ℃, and high optical transparency with the cutoff wavelengths of 306-356 nm. Moreover, the flexible and tough PI films have prominent mechanical properties with tensile strengths in the range of 77.6-90.5 MPa, tensile modulus in the range of 1.8-2.4 GPa and elongation at break in the range of 6.3%-9.5%, as well as lower dielectric constant （2.89-3.12 at 1 MHz） and lower moisture absorption （0.35%-0.66%）.

关键词： Polyimides Solubility Dielectric constant Tertbutyl Naphthyl.

The Mechanism on Cyclization, Debenzylation and Oxidation of 1-[1-(Benzyloxy)-3-methylnaphthalen-4-yloxy]propan-2-one

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Chinese Chemical Letters 2006年第6期17卷 769-772页

作者： Shi Liang HUANG Yi LUO Zhi Shu HUANG Xian Zhang BU Pei Qing LIU Lin MA Yue Ming LI Albert S. C. CHAN Lian Quan GU School of Chemistry and Chemical Engineering Sun Yat-Sen University Guangzhou 510275 School of pharmaceutical Science Sun Yat-Sen University Guangzhou 510275 Department of Applied Bioiogy ＆ Chemical Technology The Hong Kong Polytechnic University Kowloon Hong Kong

1-[1-（Benzyloxy）-3-methylnaphthalen-4-yloxy]propan-2-one （la） took place a cyclization, debenzylation and oxidation to form 9-substitued benzo[de]chromene-7,8-dione （2a） and 5-benzyl-9-substitued benzo[de]chrome... 详细信息

关键词： Mansonone F cyclization selenium dioxide sigmatropic rearrangement.

QAAR exploration on pesticides with high solubility:An investigation on sulfonylurea herbicide dimers formed through π–π stacking interactions

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Chinese Chemical Letters 2014年第7期25卷 973-977,962页

作者： Shuang Xia Yue Feng Jia-Gao Cheng Hai-Bin Luo Zhong Li Zheng-Ming Li Shanghai Key Laboratory of Chemical Biology School of PharmacyEast China University of Science and Technology School of pharmaceutical Sciences Sun Yat-Sen University State Key Laboratory of Elemento-Organic Chemistry Institute of Elemento-Organic ChemistryNankai University

Bioactive compounds could form aggregates that influence the bio-interactive processes. In this letter, based on π-π stacking models, quantitative aggregation-activity relationship （QAAR） studies were carried out on a series of sulfonylurea herbicides with good solubility. Four QAAR/QSAR models were constructed, which indicated that the bioactivity may strongly depend on both the characters of the dimeric aggregates and the monomer, The QAAR approach based on dimer-aggregates was also applicable for the highly water-soluble sulfonylurea herbicides that can form π-π stacking interactions. It was expected that the QAAR studies based on molecular aggregation state would be applied to other pesticide systems.

关键词： Aggregate QAAR/QSAR π-π Interaction Sulfonylurea

Small interfering RNA for cancer treatment:overcoming hurdles in delivery

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Acta Pharmaceutica Sinica B 2020年第11期10卷 2075-2109页

作者： Nitin Bharat Charbe Nikhil D.Amnerkar B.Ramesh Murtaza M.Tambuwala Hamid A.Bakshi Alaa A.A.Aljabali Saurabh C.Khadse Rajendran Satheeshkumar Saurabh Satija Meenu Metha Dinesh Kumar Chellappan Garima Shrivastava Gaurav Gupta Poonam Negi Kamal Dua Flavia C.Zacconin Departamento de Quimica Orgánica Facultad de Química y de FarmaciaPontificia Universidad Católica de ChileSantiago 7820436Chile Sri Adichunchunagiri College of Pharmacy Sri Adichunchunagiri UniversityBG NagarKarnataka 571418India Adv V.R.Manohar Institute of Diploma in Pharmacy NagpurMaharashtra 441110India School of Pharmacy and pharmaceutical Science Ulster UniversityColeraineNorthern Ireland BT521SAUK Faculty of Pharmacy Department of Pharmaceutics and Pharmaceutical TechnologyYarmouk UniversityIrbid 21163Jordan Department of pharmaceutical Chemistry R.C.Patel Institute of Pharmaceutical Education and ResearchDist.DhuleMaharashtra 425405India Discipline of Pharmacy Graduate School of HealthUniversity of Technology SydneyNSW 2007Australia School of pharmaceutical Sciences Lovely Professional UniversityPhagwara 144411 PunjabIndia Department of Life Sciences School of PharmacyInternational Medical UniversityBukit Jalil 57000Kuala LumpurMalaysia Department of Biochemical Engineering and Biotechnology Indian Institute of TechnologyDelhiNew Delhi 110016India School of Pharmacy Suresh Gyan Vihar UniversityJagatpuraJaipur 302017India School of pharmaceutical Sciences Shoolini University of Biotechnology and Management SciencesSolan 173229India Priority Research Centre for Healthy Lungs Hunter Medical Research Institute(HMRI)and School of Biomedical Sciences and PharmacyUniversity of NewcastleNSW 2308Australia Institute for Biological and Medical Engineering Schools of EngineeringMedicine and Biological SciencesPontificia Universidad Católica de ChileSantiago 4860Chile

In many ways,cancer cells are different from healthy cells.A lot of tactical nano-based drug delivery systems are based on the difference between cancer and healthy ***,nanotechnology-based delivery systems are the most promising tool to deliver DNA-based products to cancer *** review aims to highlight the latest development in the lipids and polymeric nanocarrier for siRNA delivery to the cancer *** also provides the necessary information about siRNA development and its mechanism of ***,this review gives us a clear picture of lipid and polymer-based drug delivery systems,which in the future could form the base to translate the basic siRNA biology into siRNA-based cancer therapies.

关键词： Small interfering RNA(siRNA) Nanomedicine Liposomes Micelles Cancer Polymer