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Conformational re-analysis of(+)-meptazinol:an opioid with mixed anal-gesic pharmacophores

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Acta Pharmacologica Sinica 2006年第9期27卷 1247-1252页

作者： Wei LI~2 Xing-hai WANG~2 Choi-wan LAU~3 Yun TANG~(2,4)Qiong XIE~2 Zhui-bai QIU~(2,5)2 Department of Medicinal Chemistry 3 NMR Laboratory,school of pharmacy,Fudan University,Shanghai 200032,China 4 school of pharmacy,East China University of Science and Technology,Shanghai 200237,China Department of Medicinal Chemistry School of Pharmacy Fudan University Shanghai China NMR Laboratory School of Pharmacy Fudan University Shanghai China school of pharmacy East China University of Science and Technology Shanghai China

Aim:To further investigate the analgesic pharmacophore of(+)-***:Two different opioid pharmacophores,Pharm-Ⅰ and Pharm-Ⅱ,were es-tablished from structures of nine typical opiates and meperidine by using molecu-lar modeling approaches according to their different structure activity relation-ship *** were further validated by a set of conformationally con-strained *** conformers of(+)-meptazinol(Conformer-Ⅰ and Con-former-Ⅱ)detected in solution were then fitted into the pharmacophores,respectively,by Fit Atoms facilities available in SYBYL,a computational modelingtool kit for molecular design and ***:Conformer-Ⅰ fit Pharm-Ⅰ fromtypical opiates ***,Conformer-Ⅱ fit none of these ***,it was found to be similar to another potent analgesic,benzofuro[2,3-c]pyridin-6-ol,whose pharmacophore was suggested to hold the transitional statebetween the two established *** typical analgesics derivedfrom 4-aryl piperidine(eg,meperidine)with one conformer absolutely overwhelming,the(+)-meptazinol exists in two conformers with similar amounts in ***,both conformers can not transform to each other freely in ordinaryconditions based on our NMR ***:(+)-meptazinol was suggestedto be an opioid with mixed analgesic pharmacophores,which may account for thecomplicated pharmacological properties of meptazinol.

关键词： (+)meptazinol opioid analgesics arylpiperidines Conformational Analysis,pharmacophore.

Design and synthesis of new 7,8-dimethoxy-α-naphthoflavones as CYP1A1 inhibitors

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Chinese Chemical Letters 2013年第3期24卷 215-218页

作者： Jia-Hua Cui Dagula Hu Xu Zhang Zheng Jing Jing Ding Ru-Bing Wang Shao-Shun Li school of pharmacy Shanghai Jiaotong University

The flavonoids as inhibitors of CYP1A1 exhibit chemopreventive effects against certain procarcinogens and have been considered as the promising cancer preventive agents. A series of novel 7,8-dimethoxy-a- naphthoflavones as the substrate analogs were designed and prepared, The enzyme assay suggested that all of these new flavones were stronger inhibitors of CYP1A1 than the lead compound a-naphthoflavone, Among the tested ones, 3h showed the most potent inhibitory effects,

关键词： a-NaphthoflavoneCYPIA1 inhibitors7 8-Dimethoxy-a-naphthoflavoneFlavonoids

Isoniazid metabolism and hepatotoxicity

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Acta Pharmaceutica Sinica B 2016年第5期6卷 384-392页

作者： Pengcheng Wang Komal Pradhan Xiao-bo Zhong Xiaochao Ma Center for Pharmacogenetics Department of Pharmaceutical SciencesSchool of PharmacyUniversity of Pittsburgh Department of Pharmaceutical Sciences School of PharmacyUniversity of Connecticut

Isoniazid(INH) is highly effective for the management of ***,it can cause liver injury and even liver *** metabolism has been thought to be associated with INH-induced liver *** review summarized the metabolic pathway... 详细信息

关键词： Isoniazid Metabolism Hepatotoxicity Anti-tuberculosis N-Acetyltransferase 2 Amidase

Green synthesis of 1,2,4-thiadizoles from thioamides in water using molecular oxygen as an oxidant

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Chinese Chemical Letters 2014年第11期25卷 1499-1502页

作者： Jin-Wu Zhao Jing-Xiu Xu Xiu-Zhen Guo school of pharmacy Guangdong Medical College

We present here an efficient green process for the synthesis of 1,2,4-thiadiazoles via iodine-catalyzed,oxidative dimerization of thioamides in water using molecular oxygen as a terminal oxidant. Under the optimized reaction conditions, aryl thioamides produced 3,5-diaryl-1,2,4-thiadiazoles in good to excellent yields. Alkyl thioamides and substituted thioureas could also provide corresponding 1,2,4-thiadiazole products.

关键词： 1 2 4-Thiadizole Thioamide Water Oxygen

Synthesis and physiochemical property evaluation of carbamate derivatives of scutellarin methyl ester

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Chinese Chemical Letters 2013年第4期24卷 338-340页

作者： Feng-Jie Jiang Xiao-Zhong Fu Shan-Wu Wang Yong Huang Wen Zhou Ai-Min Wang Yong-Lin Wang school of pharmacy Guiyang Medical College

A series of carbamate prodrugs of scutellarin methyl ester （4a-4e） were prepared in the presence of bis（trichloromethyl） carbonate （BTC） with scutellarin methyl esters and L-amino acid tert-butyl ester hydrochloride as starting materials. In vitro stability and aqueous solubility of target compounds were evaluated. The results indicated that compounds 4d and 4e have higher solubility and in vitro stability than scutellarin respectively.

关键词： ScutellarinBis(trichloromethyl) carbonatePhysiochemical property

Metabonomic analysis of plasma biochemical changes in pyrexia rats after treatment with Gegenqinlian decoction,aspirin and itraconazole by UHPLC-FT-ICR-MS

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Journal of Pharmaceutical Analysis 2020年第6期10卷 581-587页

作者： Ting Liu Ruiyun Li Yue Cui Zhiguo Yu Yunli Zhao school of pharmacy Shenyang Pharmaceutical UniversityShenyang110016China school of pharmacy Shenyang Medical CollegeShenyang110034China

A metabonomic approach involving an ultrahigh-performance liquid chromatography combined with Fourier transform ion cyclotron resonance mass spectrometry(UHPLC-FT-ICR-MS)was used to investigate the changes in the endogenous metabolites in the plasma of rats with yeast-induced pyrexia treated with Gegenqinlian decoction(GQLD),aspirin and *** differences in the small molecule profiles of treatment using traditional Chinese medicine,etiological treatment and symptomatic treatment were ***-six plasma metabolites were identified or putatively identified,and the effects of the three medicines on the thirty-six metabolites were *** metabolic pathways indicated that GQLD,aspirin and itraconazole ameliorated the rats with yeast-induced pyrexia predominantly by regulating the metabolisms of phospholipid,sphingolipid,fatty acid oxidation,fatty acid amides,amino acid and glycerolipid in *** pharmacodynamics and metabonomic results showed that the three medicines exhibited the therapeutic effects on pyrexia by regulating the perturbations of multiple *** study provided a scientific basis for an in-depth understanding of the therapeutic effects of GQLD,aspirin and itraconazole on rats with yeast-induced pyrexia.

关键词： Gegenqinlian decoction Aspirin Itraconazole Pyrexia UHPLC-FT-ICR-MS Metabonomic

Emission colour tuning in KLnF_(4):Yb^(3+),Er^(3+)/Ho^(3+)phosphor

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Journal of Rare Earths 2024年第1期42卷 57-65,I0002页

作者： Janani K Gayathri E Vijayatha V Ramasubramanian S Thiyagarajan P Department of Science and Humanities Nehru Institute of TechnologyKaliapuramThirumalayampalayamCoimbatoreIndia Department of Sciences Amrita School of Physical SciencesAmrita Vishwa VidyapeethamCoimbatoreIndia Department of Physics Anna UniversityChennaiIndia

KLnF_(4):Yb^(3+),Er^(3+)/Ho^(3+)(Ln=Y,Yb,Gd)phosphors were prepared by solid-state reaction *** each of the Yb^(3+)/Er^(3+)and Yb^(3+)/Ho^(3+)co-doped phosphors independently,phase confirmation and morphological examination were accomplished using the X-ray diffraction technique and scanning electron microscope analysis.X-ray photoelectron spectroscopy analysis shows the charge state and existence of lanthanides and *** luminescence emissions of green and red colour were detected for the synthesized *** changes in the upconverted emission intensities and colour output pertaining to the change of the lanthanide host matrix along with dopants were investigated for the prepared *** the upconversion luminescence,erbium-doped samples exhibit a predominance of red emission while holmium-doped samples display a prevalence of green *** rare-earth Er/Ho doped KYbF4shows strong red emission compared to other ***_(4):Yb,Er/Ho exhibits relatively significant green upconve rsion emissions,while Yb,Er-doped KGdF_(4)host displays a 10-fold increase in green/red emission ratio with an increase in the input power of 20-780 *** photoluminescence studies and decay curve analysis were carried out using UV light excitation for the developed phosphors.A higher lifetime of 2.2 ms was measured for the downshifting red emission in the Ho doped KYbF_(4)*** study suggests a potential for colour tunability in the upconversion and downshifting emissions through host modifications to the fluoride phosphor.

关键词： Rare earths Energy transfer upconversion Downshifting Colour coordinates

The engineering of doxorubicin-loaded liposome-quantum dot hybrids for cancer theranostics

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Chinese Physics B 2014年第8期23卷 125-128页

作者：田博文 Wafa' T. Al-Jamal Kostas Kostarelos Nanomedicine Laboratory UCL School of Pharmacy University College London Laboratory of Biophysics and Surface Analysis School of Pharmacy University of Nottingham school of pharmacy University of East Anglia Nanomedicine Laboratory Faculty of Medical & Human Sciences University of Manchester

Many studies have recently attempted to develop multifunctional nanoconstructs by integrating the superior fluores- cence properties of quantum dots （QD） with therapeutic capabilities into a single vesicle for cancer theranostics. Liposome- quantum dot （L-QD） hybrid vesicles have shown promising potential for the construction of multifunctional nanoconstructs for cancer imaging and therapy. To fulfil such a potential, we report here the further functionalization of L-QD hybrid vesi- cles with therapeutic capabilities by loading anticancer drug doxorubicin （Dox） into their aqueous core. L-QD hybrid vesi- cles are first engineered by the incorporation of TOPO-capped, CdSe/ZnS QD into the lipid bilayers of DSPC：Chol：DSPE- PEG2000, followed by Dox loading using the pH-gradient technique. The loading efficiency of Dox into L-QD hybrid vesicles is achieved up to 97%, comparable to liposome control. All these evidences prove that the incorporation of QD into the lipid bilayer does not affect Dox loading through the lipid membrane of liposomes using the pH-gradient technique. Moreover, the release study shows that Dox release profile can be modulated simply by changing lipid composition. In conclusion, the Dox-loaded L-QD hybrid vesicles presented here constitute a promising multifunctional nanoconstruct capable of transporting combinations of therapeutic and diagnostic modalities.

关键词： nanomedicine theranostic multimodality nanotechnology

New Myrsinol Diterpenes from Euphorbia prolifera

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Chinese Journal of Chemistry 2004年第1期22卷 103-108页

作者：张万金陈道峰侯爱君 Department of Pharmacognosy School of PharmacyFudan University

Four new myrsinol diterpenes, euphorprolitherins AD (13, 5), were isolated from the ethanolic extract of the root of Euphorbia prolifera, along with a knownone, SPr5 (4). The structures were elucidated on the basis of their spectroscopic evidences. The structure and relative stereochemistry of 1 were confirmed by X-ray crystallog-raphy.

关键词： Euphorbia prolifera Euphorbiaceae myrsinol diterpene euphorprolitherins A—D