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Efficacy of verbascoside,echinacoside,crenatoside on altitudeinduced fatigue in rats and possible mechanism

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Journal of Traditional Chinese Medicine 2023年第5期43卷 934-943页

作者： GUO Ziliang QIAN Qingyuan LI Xiaolin ZHU Yuting REN Jun LI Maoxing college of pharmacy Lanzhou UniversityLanzhou 730030China Department of pharmacy the 940th Hospital of Joint Logistic Support Force of Chinese of the People's Liberation ArmyLanzhou 730050China Department of pharmacy 3201 HospitalHanzhong 723000China

ObJECTIVE:To study the efficacy and mechanism of three phenylethanoid glycosides(PhG s)(verbascoside,echinacoside,and crenatoside)on altitude-induced fatigue in ***:Altitude-induced fatigue model rats were established in a large hypobaric *** time,energy storage substances,metabolic enzymes,and metabolites were used to evaluate the anti-fatigue activities and mechanism of three PhG s(verbascoside,echinacoside,and crenatoside)(150 mg/kg,intragastric administration)in the hypoxic ***:The three PhGs,especially verbascoside,could prolong the swimming time of rats,ameliorate the edema and inflammatory infiltration of liver and skeletal muscle,increase the level of energy storage substances,reduce the decomposition of proteins,and exhibit positive effects on the metabolism-related enzyme activity and ***:The PhG s,especially verbascoside,are very potential with anti-fatigue activity in *** mechanism may be explained with regulation of energy metabolism and reduction of oxidative stress.

关键词： phenylethanoid glycosides verbascoside hypoxia fatigue energy metabolism

synthesis, Crystal structure and spectroscopy studies on Complex cis-Os^Ⅱ(bpy)_2Cl_2 and Its Oxidation Product [cis-Os^Ⅲ(bpy)_2Cl_2](PF_6)

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Chinese Journal of structural Chemistry 2018年第6期37卷 995-1003页

作者：于孟王勇胡建梅 college of Chemical Engineering and pharmacy Jingchu University of Technology school of Chemical Engineering & pharmacy Wuhan Institute of Technology

The treatment of（NH_4）_2 OsCl_6 with 2 equiv of bpy in ethylene glycol produced complex 1, cis-Os^Ⅱ（bpy）_2Cl_2（bpy = 2,2＇-bipyridine）. Its one-electron oxidation product 2, [cis-Os^Ⅲ-（bpy）_2Cl_2]（PF_6）, was obtained by the oxidation of 1 with（Cp）_2 FePF_6. Complex 1 crystallizes in the orthorhombic space group Pbca, and adopts distorted [MCl_2 N_4] octahedral coordination, in which four coordination sites are occupied by four nitrogen atoms from two bpy ligands and the other two sites are occupied by two chlorine atoms in a cis-position. Complex 2 crystallizes in monoclinic space group C2/c, and contains one [Os（bpy）_2Cl_2]^＋ cation, one PF_6^- anion and two uncoordinated water solvent molecules.

关键词： osmium crystal structure electrochemistry electronic absorption spectra

synthesis, structure and Luminescent Property of a 2D Cd(Ⅱ) Coordination Polymer based on Mixed-ligands of 1,3-bis(imidazol)propane and Pyridine-3,5-dicarboxylic Acid

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Chinese Journal of structural Chemistry 2015年第2期34卷 248-252页

作者：卢久富刘举姜敏葛红光 shaanxi University of Technology Chemical Engineering College college of pharmacy Liaoning University

A new Cd（Ⅱ） coordination polymer, namely, [Cd（1,3-bip）（3,5-pdc）]n （1,3-bip = 1,3-bis（imidazol）propane and 3,5-pdc = pyridine-3,5-dicarboxylic acid） has been synthesized under hydrothermal conditions. Compound 1 was characterized by infrared spectrum, elemental analysis, powder X-ray diffraction （PXRD） and single-crystal X-ray diffraction analysis. It crystallizes in monoclinic, space group P21/c with a = 1.40178（7）, b = 1.72502（12）, c = 1.41635（6） ran, β = 92.653（4）°, V = 3.4212（3） nm3, Z = 4, C16HIsCdNsO4, Mr = 453.73, Dc = 1.762 g/cm3, F（000） = 1808,μ = 1.310 mm1, R = 0.0899 and wR = 0.1945. In compound 1, each 3,5-pdc ligand links three Cd（lI） ions and each Cd（Ⅱ） attaches to bip ligands to form a complicated 2D double-layer structure. In addition, the thermal stability and luminescent property of 1 have been studied in the solid state at room temperature.

关键词： Cd(Ⅱ) coordination polymer mixed-ligands crystal structure,luminescent property

Effect of ionization of drug on drug solubilization in sMEDDs prepared using Capmul MCM and caprylic acid

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Asian Journal of Pharmaceutical sciences 2017年第1期12卷 73-82页

作者： suhua Li Parshotam Madan senshang Lin school of pharmacy Fairleigh Dickinson UniversityFlorham ParkNJ 07932USA college of pharmacy and Health sciences St.John’s UniversityQueensNYUSA

The purpose of this study was to investigate the effect of ionization of drug on drug solubilization in sMEDDs(self-microemulsifying drug delivery system) prepared using Capmul MCM and caprylic acid. solubilization capacity of blank sMEDDs dispersions for danazol,indomethacin and haloperidol as model drugs was determined. based on the outcomes of solubilization capacity study, drug-loaded sMEDDs formulations were prepared and subjected to dispersion/precipitation study and droplet size analysis. blank sMEDDs dispersions exhibited the highest solubilization capacity for haloperidol followed by indomethacin and danazol. Furthermore, the solubilization of the three drugs in blank sMEDDs dispersions was explained by a modified mathematical model. Dispersion/precipitation studies indicate that drug-loaded sMEDDs formulations exhibited superiority in solubilizing the drugs in comparison to their respective drug powder. In addition, indomethacin and haloperidol were found to reduce the droplet size of the microemulsions while danazol did not affect droplet size formation for drug-loaded sMEDDs formulations. These findings suggest that ionization of drug affects drug solubilization, droplet size formation, drug loading and drug dispersion/precipitation profiles for the sMEDDs formulations.

关键词： sMEDDs Capmul MCM Caprylic acid Ionization Indomethacin Haloperidol

Inclusion complexes of cefuroxime axetil with β-cyclodextrin:Physicochemical characterization, molecular modeling and effect of Larginine on complexation

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Journal of Pharmaceutical Analysis 2016年第5期6卷 300-306页

作者： sarika sapte Yogesh Pore Department of Pharmaceutical Chemistry Government College of Pharmacy

The inclusion complexes of poorly water-soluble cephalosporin, cefuroxime axetil(CFA), were prepared with β-cyclodextrin(βCD) with or without addition of L-arginine(ARG) to improve its physicochemical properties. We also investigated the effect of ARG on complexation efficiency(CE) of βCD towards CFA in an aqueous medium through phase solubility behaviour according to Higuchi and Connors. Although phase solubility studies showed AL(linear) type of solubility curve in presence and absence of ARG, the CE and association constant(Ks) of βCD towards CFA were significantly promoted in presence of ARG,justifying its use as a ternary component. The solid systems of CFA with βCD were obtained by spray drying technique with or without incorporation of ARG and characterized by differential scanning calorimetry(DsC), X-ray powder diffractometry(XRPD), scanning electron microscopy(sEM), and saturation solubility and dissolution studies. The molecular modeling studies provided a better insight into geometry and inclusion mode of CFA inside βCD cavity. The solubility and dissolution rate of CFA were significantly improved upon complexation with βCD as compared to CFA alone. However, ternary system incorporated with ARG performed better than binary system in physicochemical evaluation. In conclusion, ARG could be exploited as a ternary component to improve the physicochemical properties of CFA via βCD complexation.

关键词： Cefuroxime axetil β-cyclodextrin Inclusion complex Molecular modeling Physicochemical characterization

synthesis,spectroscopic characterization and in vitro antitumor activities of some novel mononuclear Ru(Ⅱ) complexes

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Chinese Chemical Letters 2012年第4期23卷 466-469页

作者： sreekanth Thota Mohammad Imran Manasa Udugula Rajeshwar Yerra subhas s.Karki Jan balzarini Erik De Clercq Department of Pharmaceutical Chemistry&Toxicology S.R.College of Pharmacy.Ananthasagar Warangal 506371Andhra Pradesh.India Department of Pharmaceutical Chemistry KLES College of PharmacyRajajinagarBangalore 560010India Rega Institute for Medical Research Katholieke Universiteit Leuven.Minderbroedersstraat 10.B-3000 Leuven.Belgium

The synthesis and spectroscopic characterization of ruthenium complexes（R-l to R-8） of the type[Ru（A）2（b）],（where A = 1,10-phenanthroline/2,2′-bipyridine and b = 3.4.5-tri-OCH_3DPC,4-CH3-DPC,4-N-（CH3）2-DPC,4-NO2-DPC arc described. These ligands form bidentate octahedral ruthenium *** title complexes were subjected to in vitro cytotoxic activity measurements against the human cancer T-lymphocyte cell lines MTT *** vitro evaluation of these ruthenium complexes revealed cytotoxic activity from 0.24 to 1.4μg/mL against CEM,0.44 to 1.9μg/mL against Molt4/C8.0.28 to 1.5μg/mL against L1210,0.24 to 0.98μg/mL against HL60,and 0.25 to 1.2μg/mL against bEL7402,depending the nature of the compound.

关键词： Ruthenium complexes Leukemia cells MTT assay

Hydrothermal synthesis,Crystal structure and Fluorescence spectrum studies of a Novel supramolecular Compound {[2-(2-Pyridyl)benzimidazoleH_2]_2·[biCl_6]·Cl}

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Chinese Journal of structural Chemistry 2010年第5期29卷 811-815页

作者：邱东方李玉玲王宏伟郭应臣 college of Chemistry and pharmacy Engineering Nanyang Normal University

A novel supramolecular compound,{[2-（2-pyridyl）benzimidazoleH2]2·[biCl6]·Cl},was synthesized by the hydrothermal reaction of o-phenylenediamine and α-pyridinecarboxylic acid with biCl3 in 6.0 mol·L-1 HCl solution,and characterized by elemental analysis,IR,X-ray single-crystal diffraction and photoluminescence *** crystal （C24H22N6Cl7bi,Mr= 851.61） belongs to the triclinic system,space group P1 with a =7.2887（18）,b =9.548（2）,c= 12.469（3）,α=85.306（4）,β=82.814（4）,γ=71.349（4）°,Z=1,V=814.9（3）3,Dc=1.735 g/cm3,μ（MoKα）=6.007 mm-1,F（000）=410,R=0.0307 and wR=*** bismuth ion and six chlorine ions construct a distorted octahedral *** three-dimensional supramolecular network is built from electrostatic attractions,hydrogen bonds and π-π interaction between the biCl6 anion,Cl anion and [2-（2-pyridyl）benzimidazoleH2] *** photoluminescence spectroscopy study shows that the title compound has a blue fluorescent emission at 450 nm in the solid state.

关键词： 2-(2-pyridyl)benzimidazole supramolecular compound hydrothermal synthesis,crystal structure photoluminescence spectroscopy

Two New Compounds from Lindera chunii Merr.

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Chinese Chemical Letters 2006年第10期17卷 1325-1327页

作者： Mian ZHANG Chao Feng ZHANG Qi shi sUN Zheng Tao WANG college of Traditional Chinese pharmacy China Pharmaceutical University Nanjing 210038 college of Traditional Chinese pharmacy Shenyang Pharmaceutical University Shenyang 110016

Two new compounds, linderafurane A and linchuniinone, were isolated from the root of Lindera chunii Merr.. The structures were elucidated by spectroscopic methods, and their activities against HIV-1 integrase were eva... 详细信息

关键词： Lauraceae Lindera chunii linderafurane A linchuniinone HIV- 1 integrase.

Nose-to-brain delivery of macromolecules mediated by cell-penetrating peptides

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Acta Pharmaceutica sinica b 2016年第4期6卷 352-358页

作者： Tingting Lin Ergang Liu Huining He Meong Cheol shin Cheol Moon Victor C.Yang Yongzhuo Huang Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnosis School of Pharmacy Tianjin Medical University shanghai Institute of Materia Medica Chinese Academy of Sciences college of pharmacy The University of Michigan college of pharmacy and Research Institute of Pharmaceutical sciences Gyeongsang National University college of pharmacy Sunchon National University

brain delivery of macromolecular therapeutics (e.g., proteins) remains an unsolved problem because of the formidable blood brain bather (bbb). Although a direct pathway of nose-to-brain transfer provides an answer to circumventing the bbb and has already been intensively investigated for brain delivery of small drugs, new challenges arise for intranasal delivery of proteins because of their larger size and hydrophilicity. h order to overcome the bathers and take advantage of available pathways (e.g., epithelial tight junctions, uptake by olfactory neurons, transport into brain tissues, and intra-brain diffusion), a low molecular weight protamine (LMWP) cell-penetrating peptide was utilized to facilitate nose-to-brain transport. Cell-penetrating peptides (CPP) have been widely used to mediate macromolecular delivery through many kinds of biobarriers. Our results show that conjugates of LMWP proteinsare able to effectively penetrate into the brain after intranasal administration. The CPP-based intranasal method highlights a promising solution for protein therapy of brain diseases. (C) 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical sciences. Production and hosting by Elsevier b.V.

关键词： Intranasal protein delivery brain targeting Cell-penetrating peptide Low molecular weigh protamine blood brain barrier