Designed fabrication of mesoporous silica-templated self-assembled theranostic nanomedicines

Theranostic nanosystems that integrate diagnosis and therapy have garnered increasing attention for personalized medicine.The integration of the versatile nanoparticles to fabricate self-assembled theranostic nanomedicines becomes increasingly important in current medical research.Mesoporous silica nanoparticles(MSN)with their highly attractive physicochemical properties and favorable morphological attributes represent ideal templates for the controlled assembly and integration of functional nanomaterials to fabricate self-assembled theranostic nanomedicines.The rationally designed combination strategy and heterostructure will improve the overall bioavailability and preserve the unique property of each nanocomponent.In this review,the cutting-edge strategies for the designed fabrication of MSN-templated self-assembled nanomedicines are summarized.We categorize MSN-based nanomedicines by their unique heterostructures,including core-shell,yolk-shell,core-satellite,heterodimer and core-shell-satellite structures,and discuss the controlled assembly approaches as well as the intriguing applications for disease theranostics.Finally,a perspective on the challenges in the clinical translation of self-assembled theranostic nanomedicines is highlighted.     

Hydrogen peroxide-generating nanomedicine for enhanced chemodynamic therapy

Chemodynamic therapy(CDT) is an emerging endogenous stimulation activated tumor treatment approach that exploiting iron-containing nanomedicine as catalyst to convert hydrogen peroxide(H_2O_2)into toxic hydroxyl radical(·OH) through Fenton reaction.Due to the unique characteristics(weak acidity and the high H_2O_2 level) of the tumor microenvironment,CDT has advantages of high selectivity and low side effect.However,as an important substrate of Fenton reaction,the endogenous H_2O_2 in tumor is still insufficient,which may be an important factor limiting the efficacy of CDT.In order to optimize CDT,various H_2O_2-generating nanomedicines that can promote the production of H_2O_2 in tumor have been designed and developed for enhanced CDT.In this review,we summarize recently developed nanomedicines based on catalytic enzymes,nanozymes,drugs,metal peroxides and bacteria.Finally,the challenges and possible development directions for further enhancing CDT are prospected.     

Pulmonary Drugs and Genes Delivery Systems for Lung Disease Treatment

Pulmonary drugs and genes delivery systems have become an attractive approach in the treatment of lung diseases with the advantages of minimal drug loss,precise quantization,high local drugs concentration and low side effects.However,special attention should be paid to the biological barriers of the lung.The delivery systems need to be designed carefully in order to overcome these biological barriers and maximize the drugs and genes deposition to the lungs.Pulmonary drugs and genes delivery systems can offer some encouraging results for delivering drugs and genes to the lungs.Specifically,some lipid-based and polymer-based delivery systems could control and sustain the release of drugs and genes with minimal or negligible toxicity.This review focuses on the latest development of pulmonary delivery of drugs and genes for the treatment of various lung diseases.The barriers to the lung,the delivery devices,the route of the administration and the delivery systems for drugs and genes pulmonary delivery are described.Based on the rapid development of clinical requirement,novel approaches using delivery systems for pulmonary delivery drugs and genes need to be constructed,which is believed to play an important role in the therapy of lung diseases in the future.     

Study on the Interaction of Mitomycin C with ct-DNA by Pd-Porphin Room Temperature Phosphorescence Probe

Study of the interaction of drugs with calf thymus DNA (ct-DNA) in molecular level1-4 is helpful to understand the fundamental aspects of activation of anticancer drugs and provide the valuable information for designing and developing new antitumor agents. Mitomycin C (MMC) is an anticancer drugs being widely used in clinic with high activity and effectiveness for many cancers. DNA has been proved to be the main target molecule of MMC in the body. The activated MMC can hinder the rep…     

PREFACE

正Supramolecular self-assembly has been recognized as one of the most important and powerful methodologies to fabricate complex and high-ordered nanostructures.These supramolecular assemblies have found versatile applications in nanomedicines,tissue engineering,and smart electronic devices and so on.Recent efforts in this field have been devoted to design novel self-     

Racemic ofloxacin separation by supported-liquid membrane extraction with two organic phases

As the relation of chirality and activities of drugs is researched deeply, people become to re-alize the clinic importance of chirality. The different enantiomers of a drug can have vastly differ-ent pharmacological activities, pharmacokinetic processes and toxicity[1,2]. The most well-docu- mented example is that of the drug substance thalidomide. Bitter lessons and scientific research promote the interest in single-enantiomer drugs, so the potential of the chiral drug market is enormous[3]. …     

Chemical and structural biology of nucleic acids and protein-nucleic acid complexes for novel drug discovery

Since nucleic acids(DNA and RNA) play very important roles in cells,they are molecular targets of many clinically used drugs,such as anticancer drugs and antibiotics.Because of clinical demands for treating various deadly cancers and drug-resistant strains of pathogens,there are urgent needs to develop novel therapeutic agents.Targeting nucleic acids hasn’t been the mainstream of drug discovery in the past,and the lack of 3D structural information for designing and developing drug specificity is one of the ...     

A Practical Synthesis of (S)-(+)-2-(6-methoxyl-2-naphthyl) propionic Acid

a-Arylpropionic acids are an important class of non-steroidal anti-inflammatory agents1,2. The therapeutic efficacy of this class of drugs is well demonstrated by the introduction and extensive use of more than a dozen compounds exemplified by ibuprofen, naproxen, ketoprofen and flurbiprofen etc. However, in recent years the use of enantiomerical pure drugs in chemotherapy is becoming almost mandatory for enhancing specificity of drug action and reducing the toxicity. This awareness led to …     

Carrier-free supramolecular nanomedicines assembled by small-molecule therapeutics for cancer treatment

Nanomedicines have shown great promise in cancer therapy, but are challenged by limited drug loading, safety concerns of drug carriers, and complexity of function integration. Recently, carrier-free nanomedicines produced by supramolecular assembly of small-molecule therapeutic functionalities and their conjugates were proposed to address these issues. These nanomedicines achieve very high drug loading, enhanced tumor accumulation and improved therapeutic efficiency, and avoid carrier-related sa...     

Application of liquid pre-column capillary electrophoresis technique to the study of interaction between drug enantiomers and human serum albumin

Based on the chiral separation of several basie drugs, dimetindene, tetryzoline, theodrenaline and verapamil, the liquid pre-colunm capillary electrophoresis (LPC-CE) technique was established. It was used to determine free concentrations of drug enantiomers in mixed solutions with human serum albumin (HSA). To prevent HSA entering the CE chiral separation zone, the mobility differences between HSA and drugs under a specific pH condition were employed in the LPC. Thus, the detection confusion caused by protein was totally avoided. Further study of binding constants determination and protein binding competitions was carried out. The study proves that the LPC technique could be used for complex media, particularly the matrix of protein coexisting with a variety of drugs.     

Synthesis of Tetracycline Analogues and Test of Their Affinity on Synthetic Hydroxyapatite

To develop bone target drugs is an attractive field for increasing the potency and selectivity of these drugs in the treatment of osteoporosis and Pagets disease etc. As known, after systematic administration tetracycline can be distributed in bone and bind to hydroxyapatite with high affinity1. Thus we tried to use tetracycline as a bone targeted carrier. However, tetracycline is less stable, and its complex structure bring much difficulty in the coupling reaction and purification of the p…     

Application of differential pulse stripping voltammetry and chemometrics for the determination of three antibiotic drugs in food samples

A reliable method for simultaneous determination of three antibiotic drugs(levofloxacin,gatifloxacin and lomefloxacin) by differential pulse stripping voltammetry(DPSV) in Britton-Robinson buffer(pH 7.96) was presented.The method is based on adsorptive accumulation of the antibacterial drugs on a hanging mercury dropping electrode(HMDE),followed by the reduction of the adsorptive species by the technique of DPSV.Optimal conditions,the deposition time of 80 s,the deposition potential of—1250 mV,and the scan rate of 25 mV/s,were obtained.The linear concentration ranges of 0.010-0.080μg/mL were obtained for all these three antibiotic drugs,while the detection limits were 2.38,3.20 and 1.60ng/mL for levofloxacin,gatifloxacin and lomefloxacin,respectively.In this work,chemometrics methods,such as classical least squares(CLS),partial least squares(PLS), principle component regression(PCR) and radial basis function-artificial neural networks(RBF-ANN),were used to quantitatively resolve the overlapping signals.It was found that PCR gave the best results with total relative prediction error(RPE_T) of 7.71%.The proposed method was applied to determine these three drugs in several commercial food samples with spiked method and yielded satisfactory recoveries.     

Preparation of Micron-size Functional Fluorescent Microspheres

As a kind of special functional microspheres, fluorescent polymer microspheres could be used in cell label and separation, blood flow assay, flow cytometer marking, chemical reaction assay, and in analyst of the transform and diffusion of particles in soil . However, one of the most 1 important applications of fluorescent microspheres is in the high-throughput screening of drugs (HTS) . Through affinity interaction, radioactive ligands (latent drugs) are bound to fluorescent 2 microsphere…     

Characterization of Gallic Acid Interaction with Human Serum Albumin by Spectral and Molecular Modeling Methods

The binding of drugs with human serum albumin(HSA)is a crucial factor influencing the distribution and bioactivity of drugs in the body.To understand the action mechanisms between gallic acid(GA,3,4,5-...     

EFFECTS OF SOME Ca~(2+) BLOCKER ON RECEPTOR POTENTIALS OF CRAYFISH RETINA

One drug known to inactivate calmodulin and two others to block Ca~(2+) channels were applied to isolated superfused retinae of the crayfish Astacus leptodactylus and their influence on the receptor potentials (RP) was studied. Trifluoperazine causes an increase of the amplitude of maximum (h_(max))of RP and a prolongation of the time of half decrease (t_2). Furthermore, trifluoperazine could antagonise the effect of raised calcium concentration of superfusate, which decreases h_(max) and shortens t_2 of the RP. Iproveratril and D-600 cause a transient increase and thereafter a progressive decrease of h_(max) of the RP. There is a difference between effects of both drugs on t_2 of the RP. The mechanisms of effects of these drugs on the sensitivity of the isolated retina are discussed.     

Pediatric ocular nanomedicines:Challenges and opportunities

Challenges and opportunities to development of ocular drug delivery systems and nanomedicines for pediatric patients are reviewed.     

Synthesis Structure and Behavbr of Polymeric Drugs Covalently Linked 5-Fluorouracil

Four series of polymeric drugs with 5-Fluorouracil(5-FU) cova-lently linked in side chain were synthesized by the use of starch and carboxylmethylcellulose and two new 5-FU derivatives were also synthesized by using molecular sieve as a catalyst.Their structures were determined by IR,1H NMR and mass spectra.The changes in the Nitrogen content of polymeric drugs with reaction conditions and the influences of the N content on their limiting viscosity were studied.The hydrolysis of 5-FU from starch and carboxylmethylcellulose derivatives in various of buffer were researched by simulating physiologically acid-alkali enviroment.In addition,anticancer activity(in vivo and in vitro) of some starch derivative has been preliminaryly observed.     

An RNA polymerase I-driven human respiratory syncytial virus minigenome as a tool for quantifying virus titers and screening antiviral drug

Human respiratory syncytial virus(RSV) is an important pediatric pathogen of lower respiratory tract worldwide. No vaccines and antiviral drugs are available. Herein the use of an RNA polymerase I-driven RSV minigenome for analyzing RSV replication and screening anti-RSV drugs was investigated. The RNA polymerase I(Pol I) was used to transcribe RSV minigenome from the constructed plasmid, designated p HM-RSV-Gluc, of minigenome c DNA which comprised trailer region, gene start sequence(GS), reverse complementary copy of Gaussia luciferase(Gluc) gene, gene end sequence(GE), and leader region in the direction of 5'–3'end and was flanked by promoter and terminator of Pol I. The expression of Gluc was confirmed in p HM-RSV-Gluc transfected HEp-2 cells following RSV infection and had the characteristics of dose-dependent, which provided a rapid, sensitive, and quantitative method for quantifying virus titers and screening antiviral drugs.