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Synthesis and characterization of HPMA copolymer-5-FU conjugates

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Chinese Chemical Letters 2008年第2期19卷 137-140页

作者： Fang Yuan Fu Chen Qing Yu Xiang Xuan Qin Zhi Rong Zhang Yuan Huang Key Laboratory of Drug Targeting of Ministry of Education West China School of Pharmacy Sichuan University Chengdu 610041 China

N-（2-Hydroxypropyl） methacrylamide copolymer-5-fluorouracil （PHPMA-FU） conjugates were synthesized by a novel and simplified synthetic route, and characterized by UV, FTIR and HPLC analyses. The conjugated content of 5-fluorouracil （5-FU） was 3.41 ± 0.07 wt%. The stabilities of PHPMA-FU conjugates under different conditions were studied. The results showed that HPMA copolymer was a potential carrier for tumor-targeting delivery of 5-FU.

关键词： HPMA copolymer 5-Fluorouracil conjugates Characterization Stability

Chemotactic Activity of Site-Specific Multivalent conjugates of Stromal Cell-Derived Factor 1<i>α</i>on Branched Nanoparticles

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Journal of Biomaterials and Nanobiotechnology 2018年第1期9卷 51-63页

作者： Yu-Fang Hsieh Fang Huang Shyam Patel Song Li Department of Bioengineering and Medicine University of California Los Angeles (UCLA) Los Angeles CA USA

Stromal cell-derived factor 1α (SDF1α) is a potent chemokine for the recruitment of stem cells. A challenge is to maintain its activity and control its release. In this study, we engineered a recombinant cysteine-SDF1α (cysSDF1α) protein, and performed multivalent conjugation of cysSDF1 through the maleimide functional group to two forms of branched nanoparticles: multi-arm poly (ethylene glycol) (MA-PEG) and hyaluronic acid (HA). We characterized the chemotactic activity of the conjugates, and determined how the molecular weight (MW) of MA-PEG and HA affected the chemotactic activity. CysSDF1α had similar efficiency to wild-type SDF1α in cell recruitment. Multivalent conjugation of cysSDF1α to low MW MA-PEG (~18 nm) did not significantly affect the chemotactic activity, while the conjugation of cysSDF1α to high MW MA-PEG (~72 nm) lowered the efficiency, possibly due to the larger spacing between conjugated SDF1α molecules. HA has a linear backbone and a high density of multivalent binding sites;however, the chemotactic activity of HA-linked cys-SDF1α was much lower, which further decreased with the increase of HA MW from 200 kDa (~0.78 μm) to 700 kDa (~2.7 μm). Digestion of HA into smaller fragments using hyaluronidase partially recovered the chemotactic activity of cysSDF1α, suggesting that high MW HA might exert steric hindrance for SDF1α binding to its receptors on cell surface and that HA could be used as a depot for SDF1α storage and release. These results demonstrate that multivalent conjugates of SDF1α to nanoparticles may be used to engineer SDF1α delivery for cell recruitment and tissue regeneration.

关键词： SDF1α Delivery Cell Recruitment Site-Specific Protein Ligation Multivalent Protein conjugates

Hydrolysis of soy isoflavone conjugates using enzyme may underestimate isoflavone concentrations in tissue

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Journal of Nanjing Medical University 2005年第1期19卷 10-14页

作者： Hebron C.Chang Myriam Laly Melody Harrison Thomas M.Badger Arkansas Children’s Nutrition Center Agricultural Research ServiceUSA Department of Physiology/Biophysics University of Arkansas for Medical SciencesLittle RockAR72202USA Current address:Institute ofToxicology.NanjingMedicalUniver.sity Nanjing 210029China.

Objective:To investigate the differences of using enzymatic hydrolysis and acid hydrolysis for identification and quantification of isoflavone aglycones from ***:β-glucuronidase/sulfatase isolated from Helix pomatia for routine enzymatic hydrolysis or 6N HCl was used to release glucuronide and sulfate conjugates in the serum,urine and tissue *** of soy isoflavones after enzymatic hydrolysis or acid hydrolysis in several tissues of rat fed with diets containing soy protein isolate were also compared using LC/MS and ***:Acid hydrolysis released more aglycone than enzymatic digestion(P<0.05)in liver *** total genistein,daidzein and other metabolites were 20%to 60%lower in samples from enzymatic hydrolysis than in acid ***:These results indicated that unknown factors in tissues reduced the enzymatic hydrolytic efficiency for releasing isoflavone aglycones even in optimized *** would underestimate isoflavone tissue concentrations up to 60%.

关键词： isoflavone aglycones enzymatic hydrolysis acid hydrolysis glucuronide sulfate conjugates

Synthesis and Photophysical Properties of conjugates of Green Fluorescent Protein (GFP) Chromophore and 2'-Deoxy-Uridine Developed as Labelled Building Blocks for Oligonucleotide Probes

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Journal of Pharmacy and Pharmacology 2019年第9期7卷 510-519页

作者： Abed Saady Bilha Fischer Department of Chemistry Bar-Ilan University Ramat-Gan 52900 Israel

Fluorescent probes with high signal/background ratio are needed for hybridization assays. Hence, the chromophore of green fluorescent protein (GFP), 4-hydroxybenzylidene-imidazolinone (HBI), was targeted as a potential fluorescent intercalator. For producing a building block for fluorescent oligonucleotide probes, 2'-deoxyuridine (dU) was conjugated with HBI via a flexible carbon-spacer. dUHBI conjugates highly fluoresce in glycerol (λem 460 nm,Φ 0.31), and are 109-fold more emissive than in methanol, implying the potential of dUHBI-labeled oligonucleotides as probes for hybridization assays.

关键词： Intercalator GFP 2'-deoxyuridine intercalator conjugates

Biophysical interactions between silver nanoparticle-albumin interface and curcumin

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Journal of Pharmaceutical Analysis 2020年第2期10卷 164-177页

作者： Vinod D.Jaiswal P.M.Dongre Department of Biophysics University of MumbaiVidyanagariSantacruzMumbai400098India

Active targeted drug delivery methods facilitate effective uptake of functionalized nanoparticles through receptor-mediated *** recent years,albumin-nanoparticle interaction has been critically examined so that this functionalized nanoparticle can be efficiently loaded with *** present investigation aims at understanding the adsorption of Bovine Serum Albumin(BSA)on Silver Nano-particle(SNP)surface,preparation of soft conjugates(SC)and hard conjugates(HC)of BSA-functionalized SNP(SNP-BSA),and their interaction with curcumin(CUR).HC contains tightly bound BSA whereas SC involves tightly and loosely bound *** in the hydrodynamic radii of conjugates was observed upon SNP incubation with increased concentration of *** different SNP-BSA conjugate ratios were selected to study their interaction with *** spectroscopy showed a strong association between CUR and SNP:BSA ***,binding varied with a change in the conjugate *** Dichroism(CD)/Fourier Transform Infrared(FTIR)spectroscopy revealed the alterations in the secondary structure of BSA upon CUR binding to the *** potential data indicated stable conjugate *** in SNP:BSA conjugate was found to have a higher half-life as compared to the *** believe that this is the first biophysical characterization report of conjugates that can be effectively extrapolated for targeted drug delivery.

关键词： CUR Bovine serum albumin Silver nanoparticles Soft conjugates Hard conjugates Spectroscopy

Delivery strategies of amphotericin B for invasive fungal infections

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Acta Pharmaceutica Sinica B 2021年第8期11卷 2585-2604页

作者： Xiaochun Wang Imran Shair Mohammad Lifang Fan Zongmin Zhao Md Nurunnabi Marwa A.Sallam Jun Wu Zhongjian Chen Lifang Yin Wei He Department of Pharmaceutics China Pharmaceutical UniversityNanjing 211198China School of Pharmaceutical Sciences Sun Yat-sen UniversityUniversity TownGuangzhou 510006China Jiangsu Aosaikang Pharmaceutical Co. Ltd.Nanjing 211112China School of Engineering and Applied Sciences Harvard UniversityCambridgeMA 02138USA Department of Pharmaceutical Sciences School of PharmacyUniversity of Texas at El PasoEl PasoTX 79902USA Department of Industrial Pharmacy Faculty of PharmacyAlexandria UniversityAlexandria 21521Egypt Department of Geriatric Cardiology Jiangsu Provincial Key Laboratory of Geriatricsthe First Affiliated Hospital of Nanjing Medical UniversityNanjing 210029China Shanghai Skin Disease Hospital Tongji University School of MedicineShanghai 200443China

Invasive fungal infections(IFIs)represent a growing public concern for clinicians to manage in many medical settings,with substantial associated morbidities and *** many current therapeutic options for the treatment of IFIs,amphotericin B(AmB)is the most frequently used *** is considered as a first-line drug in the clinic that has strong antifungal activity and less *** this review,we summarized the most promising research efforts on nanocarriers for AmB delivery and highlighted their efficacy and safety for treating *** have also discussed the mechanism of actions of AmB,rationale for treating IFIs,and recent advances in formulating AmB for clinical ***,this review discusses some practical considerations and provides recommendations for future studies in applying AmB for combating IFIs.

关键词： Invasive fungal infections Amphotericin B Poor water-solubility Drug delivery Topical administration Nanoparticles conjugates Toxicity

Drug resistance and new therapies in colorectal cancer

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World Journal of Gastroenterology 2018年第34期24卷 3834-3848页

作者： Kevin Van der Jeught Han-Chen Xu Yu-Jing Li Xiong-Bin Lu Guang Ji Institute of Digestive Diseases Longhua HospitalShanghai University of Traditional Chinese Medicine Department of Medical and Molecular Genetics Indiana University School of Medicine Indiana University Melvin and Bren Simon Cancer Center Indiana University School of Medicine

Colorectal cancer(CRC) is often diagnosed at an advanced stage when tumor cell dissemination has taken place. Chemo-and targeted therapies provide only a limited increase of overall survival for these patients. The major reason for clinical outcome finds its origin in therapy resistance. Escape mechanisms to both chemo-and targeted therapy remain the main culprits. Here, we evaluate major resistant mechanisms and elaborate on potential new therapies. Amongst promising therapies is α-amanitin antibodydrug conjugate targeting hemizygous p53 loss. It becomes clear that a dynamic interaction with the tumor microenvironment exists and that this dictates therapeutic outcome. In addition, CRC displays a limited response to checkpoint inhibitors, as only a minority of patients with microsatellite instable high tumors is susceptible. In this review, we highlight new developments with clinical potentials to augment responses to checkpoint inhibitors.

关键词： Colorectal cancer Therapy resistance Antibody-drug conjugates α-amanitin Tumor microenvironment Immunotherapy Checkpoint inhibitors Microbiome

MINS, a Novel Naphthalimide-Polyamine Conjugate, Induced Apoptosis Depending on p53 Status in Human Colon Cancer Cells

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Open Journal of Apoptosis 2014年第4期3卷 59-69页

作者： Ming Li Tao Yang Fujun Dai Qian Li Yahong Zhang Songqiang Xie Chaojie Wang Institute of Chemical Biology Pharmaceutical College of Henan University Kaifeng China The Key Laboratory of Natural Medicine and Immuno-Engineering Henan University Kaifeng China

Natural polyamine is an ideal antitumor drug carrier because of the great requirement difference between cancer cells and normal cells. Previous data demonstrated that many cytotoxic drugs conjugated with natural or synthetic polyamines have potent antitumor effects. Up to now, the antitumor mechanism of conjugates of naphthalimides with polyamine remains poorly understood in human colon cancer cells. The aim of this study is to evaluate the effect of MINS (a novel naph-thalimide-polyamine conjugate) and mechanism of MINS in human colon cancer cells. Mitochondrial toxicity, which was generated by ROS from mitochondria electron transport chain, might be a major factor in MINS-inducted apoptosis. Our data also demonstrated that MINS-mediated cell apoptosis depend on p53 status, for MINS induced Caco-2 cells (p53 null) only necrosis but not apoptosis. Furthermore, the apoptotic effect of MINS is stronger than that of Amonafide, the parent drug of MINS. Our data suggested that the MINS-mediated cell apoptosis depend on p53 in human colon cancer cells.

关键词： Naphthalimide-Polyamine conjugates Apoptosis p53 Mitochondrial Transmembrane Potential Oxidative Stress

Tumor localization of anti-gastric cancer monoclonal antibody MGb_2-daunomycin conjugate in nude mice bearing human gastric carcinoma SGC-7901

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Journal of Medical Colleges of PLA(China) 1992年第1期7卷 81-83页

作者：陈敏黎松邓敬兰张学庸陈希陶 Department of Nuclear Medicine Xijing Hospital Fourth Military Medical UniversityXi'an 710032 Laboratory of Gastroenterology Xijing HospitalFourth Military Medical UniversityXi'an 710032

In the present study,an anti-gastric cancer monoclonal antibody MGb2-daunomycin（DM）conjugate was prepared by cis-aconitic anhydride *** distribution of the conjugatein nude mice bearing human gastric carcinoma SGC-7901 was *** to five moleculesof DM were introduced into each molecule of antibody while the antigen-binding capacity ofthe antibody was *** conjugate could be satisfactorily localized in the ***-six hours after intraperitoneal injection of 125I-MGb2-DM conjugate,the ratio ofradioactivity per milligram of tumor to that per milligram of blood reached 203,the result beingquite similar to that of unmodified MGb2.

关键词： stomach neoplasms antibodies monoclonal deunomycin antibody-toxin conjugates iodine radioisotops mice nude