Norfriedelins A-C with acetylcholinesterase inhibitory activity from acerola tree (Malpighia emarginata).

Three novel norfriedelanes, A-C (1-3), were isolated from the branches and roots of Malpighia emarginata . Their structures and absolute configurations were determined by 1D and 2D NMR techniques and X-ray crystallographic analysis. Norfriedelin A (possessing an α-oxo-β-lactone group) and norfriedelin B (with a keto-lactone group) showed acetylcholinesterase inhibitory effects with the IC50 values of 10.

Affibody modified and radiolabeled gold-iron oxide hetero-nanostructures for tumor PET, optical and MR imaging.

A highly monodispersed hetero-nanostructure with two different functional nanomaterials (gold (Au) and iron oxide (Fe(3)O(4,) IO)) within one structure was successfully developed as Affibody based trimodality nanoprobe (positron emission tomography, PET; optical imaging; and magnetic resonance imaging, MRI) for imaging of epidermal growth factor receptor (EGFR) positive tumors. Unlike other regular nanostructures with a single component, the Au-IO hetero-nanostructures (Au-IONPs) with unique chemical and physical properties have capability to combine several imaging modalities together to provide complementary information. The IO component within hetero-nanostructures serve as a T(2) reporter for MRI; and gold component serve as both optical and PET reporters.

Comparison between air and carbon dioxide insufflation in the endoscopic submucosal excavation of gastrointestinal stromal tumors.

Aim: To evaluate the safety and efficacy of CO(2) insufflation compared with air insufflation in the endoscopic submucosal excavation (ESE) of gastrointestinal stromal tumors.

Methods: Sixty patients were randomized to undergo endoscopic submucosal excavation, with the CO(2) group (n = 30) and the air group (n = 30) undergoing CO(2) insufflation and air insufflation in the ESE, respectively. The end-tidal CO(2) level (pETCO(2)) was observed at 4 time points: at the beginning of ESE, at total removal of the tumors, at completed wound management, and 10 min after ESE.

A comparative evaluation of the efficacy of two novel desensitising dentifrices.

A comparison of the desensitising efficacy of two commercially available dentifrices with different modes of action was conducted in a randomised, examiner-blind, two-arm, parallel group, 8-week, longitudinal clinical study. Dentifrice A, (Sensodyne Multi Action Iso-Active), contained 50000 ppm KNO(3) and 1450 ppm fluoride as NaF. Dentifrice B, Colgate Sensitive Pro-Relief, contained a combination of 80000 ppm arginine, bicarbonate, calcium carbonate, and 1450 ppm fluorine as NaMFP.

Development and characterization of lactoferrin nanoliposome: cellular uptake and stability.

Lactoferrin was purported in consumer literature to enhance and support the immune system response through their antioxidant, antibacterial, and anticarcinogenic properties. To improve the effectiveness of lactoferrin, liposomes were used as a carrier in this study. The main purpose of this study was to compare three different methods to prepare the lactoferrin nanoliposomes based on the encapsulation efficiency and size distribution and evaluate the stability and cellular uptake of lactoferrin nanoliposomes.

Cerenkov Luminescence Imaging (CLI) for cancer therapy monitoring.

In molecular imaging, positron emission tomography (PET) and optical imaging (OI) are two of the most important and thus most widely used modalities. PET is characterized by its excellent sensitivity and quantification ability while OI is notable for non-radiation, relative low cost, short scanning time, high throughput, and wide availability to basic researchers. However, both modalities have their shortcomings as well.

Galactosylated chitosan/5-fluorouracil nanoparticles inhibit mouse hepatic cancer growth and its side effects.

Aim: To observe the curative effect of galactosylated chitosan (GC)/5-fluorouracil (5-FU) nanoparticles in liver caner mice and its side effects.

Methods: The GC/5-FU nanoparticle is a nanomaterial made by coupling GC and 5-FU. The release experiment was performed in vitro.

Novel, cysteine-modified chelation strategy for the incorporation of [M(I)(CO)(3)](+) (M = Re, (99m)Tc) in an α-MSH peptide.

Engineering peptide-based targeting agents with residues for site-specific and stable complexation of radionuclides is a highly desirable strategy for producing diagnostic and therapeutic agents for cancer and other diseases. In this report, a model N-S-N(Py) ligand (3) and a cysteine-derived α-melanocyte stimulating hormone (α-MSH) peptide (6) were used as novel demonstrations of a widely applicable chelation strategy for incorporation of the [M(I)(CO)(3)](+) (M = Re, (99m)Tc) core into peptide-based molecules for radiopharmaceutical applications. The structural details of the core ligand-metal complexes as model systems were demonstrated by full chemical characterization of fac-[Re(I)(CO)(3)(N,S,N(Py)-3)](+) (4) and comparative high-performance liquid chromatography (HPLC) analysis between 4 and [(99m)Tc(I)(CO)(3)(N,S,N(Py)-3)](+) (4a).

5-Fluorouracil nanoparticles inhibit hepatocellular carcinoma via activation of the p53 pathway in the orthotopic transplant mouse model.

Biodegradable polymer nanoparticle drug delivery systems provide targeted drug delivery, improved pharmacokinetic and biodistribution, enhanced drug stability and fewer side effects. These drug delivery systems are widely used for delivering cytotoxic agents. In the present study, we synthesized GC/5-FU nanoparticles by combining galactosylated chitosan (GC) material with 5-FU, and tested its effect on liver cancer in vitro and in vivo.

Preliminary pharmacology of galactosylated chitosan/5-fluorouracil nanoparticles and its inhibition of hepatocellular carcinoma in mice.

Biodegradable polymer nanoparticle drug delivery systems are characterized by targeted drug delivery, improved pharmacokinetic and biodistribution, enhanced drug stability and lowered side effects; these drug delivery systems are widely used for delivery of cytotoxic agents. The galactosylated chitosan (GC)/5-fluorouracil (5-FU) nanoparticle is a nanomaterial made by coupling GC, a polymer known to have the advantages described above, and 5-FU. The GC/5-FU nanoparticle is a sustained release system, it was showed that the peak time, half-life time, mean residence time (MRT) and area of under curve (AUC) of GC/5-FU were longer or more than those of the 5-FU group, but the maximum concentration (Cmax) was lower.

A novel radiofluorinated agouti-related protein for tumor angiogenesis imaging.

A novel protein scaffold based on the cystine knot domain of the agouti-related protein (AgRP) has been used to engineer mutants that can bind to the α(v)β(3) integrin receptor with high affinity and specificity. In the current study, an (18)F-labeled AgRP mutant (7C) was prepared and evaluated as a positron emission tomography (PET) probe for imaging tumor angiogenesis. AgRP-7C was synthesized by solid phase peptide synthesis and site-specifically conjugated with 4-nitrophenyl 2-(18/19)F-fluoropropionate ((18/19)F-NFP) to produce the fluorinated peptide, (18/19)F-FP-AgRP-7C.

Evaluation of in vivo antioxidant and immunity enhancing activities of sodium aescinate injection liquid.

Oxidative stress is involved in the development and progression of disease. Because sodium aescinate has been reported to have immunity enhancing and antioxidative effects, we investigated its activity by employing a hepatocellular carcinoma (HCC) mouse model. Sixty BALB/c mice were randomly divided into four groups, including a 1.

Intraoperative imaging of tumors using Cerenkov luminescence endoscopy: a feasibility experimental study.

Unlabelled: Cerenkov luminescence imaging (CLI) is an emerging new molecular imaging modality that is relatively inexpensive, easy to use, and has high throughput. CLI can image clinically available PET and SPECT probes using optical instrumentation. Cerenkov luminescence endoscopy (CLE) is one of the most intriguing applications that promise potential clinical translation.

Synthesis of galactosylated chitosan/5-fluorouracil nanoparticles and its characteristics, in vitro and in vivo release studies.

Biodegradable polymer nanoparticle drug delivery systems are characterized by targeted drug delivery, improved pharmacokinetic and biodistribution, enhanced drug stability, and lowered side effects; these drug delivery systems are widely used for delivery of cytotoxic agents. The galactosylated chitosan (GC)/5-fluorouracil (5-FU) nanoparticle is a nanomaterial made by coupling GC, a polymer known to have the advantages described above, and 5-FU. We found that when 5-FU and GC were mixed at the mass ratio of 10:1, the nanoparticle reached a maximum encapsulation efficiency of 81.

Gene transfer to the developing mouse inner ear by in vivo electroporation.

The mammalian inner ear has 6 distinct sensory epithelia: 3 cristae in the ampullae of the semicircular canals; maculae in the utricle and saccule; and the organ of Corti in the coiled cochlea. The cristae and maculae contain vestibular hair cells that transduce mechanical stimuli to subserve the special sense of balance, while auditory hair cells in the organ of Corti are the primary transducers for hearing. Cell fate specification in these sensory epithelia and morphogenesis of the semicircular canals and cochlea take place during the second week of gestation in the mouse and are largely completed before birth.

A Four-Arm Star-Shaped Poly(ethylene glycol) (StarPEG) Platform for Bombesin Peptide Delivery to Gastrin-Releasing Peptide Receptors in Prostate Cancer.

We present the design, synthesis, and characterization of a novel cancer biomarker delivery platform, the star-shaped four-arm poly(ethylene glycol) (StarPEG). Using the multidisplay platform we were able to synthesize a bombesin (BBN) positron emission tomography (PET) probe featuring four copies of 8-Aoc-BBN peptides (where 8-Aoc is 8-aminooctanic acid), which we named StarPEG-BBN. Cell binding studies showed that StarPEG-BBN had a good binding affinity to PC3 cells (IC = 65.

Molecular imaging in tracking tumor stem-like cells.

Cancer remains a major public health problem in many countries. It was found to contain a subset of cancer stem cells (CSCs) that are capable of proliferation and self-renewal, and differentiation into various types of cancer cells. CSCs often display characteristics of chemotherapy resistance and radiotherapy resistance.

177Lu-DO3A-HSA-Z EGFR:1907: characterization as a potential radiopharmaceutical for radionuclide therapy of EGFR-expressing head and neck carcinomas.

Epidermal growth factor receptor 1 (EGFR) is an attractive target for radionuclide therapy of head and neck carcinomas. Affibody molecules against EGFR (Z(EGFR)) show excellent tumor localizations in imaging studies. However, one major drawback is that radiometal-labeled Affibody molecules display extremely high uptakes in the radiosensitive kidneys which may impact their use as radiotherapeutic agents.

Proof-of-concept study of monitoring cancer drug therapy with cerenkov luminescence imaging.

Unlabelled: Cerenkov luminescence imaging (CLI) has emerged as a less expensive, easier-to-use, and higher-throughput alternative to other nuclear imaging modalities such as PET. It is expected that CLI will find many applications in biomedical research such as cancer detection, probe development, drug screening, and therapy monitoring. In this study, we explored the possibility of using CLI to monitor drug efficacy by comparisons against PET.

Non-invasive imaging of cysteine cathepsin activity in solid tumors using a 64Cu-labeled activity-based probe.

The papain family of cysteine cathepsins are actively involved in multiple stages of tumorigenesis. Because elevated cathepsin activity can be found in many types of human cancers, they are promising biomarkers that can be used to target radiological contrast agents for tumor detection. However, currently there are no radiological imaging agents available for these important molecular targets.

In vitro study on apoptosis induced by strontium-89 in human breast carcinoma cell line.

Many radiopharmaceuticals used for medical diagnosis and therapy are beta emitters; however, the mechanism of the cell death caused by beta-irradiation is not well understood. The objective of this study was to investigate the apoptosis of human breast carcinoma MCF-7 cell lines induced by Strontium-89 (⁸⁹Sr) and its regulation and control mechanism. High-metastatic Breast Carcinoma MCF-7 cells were cultured in vitro using ⁸⁹Sr with different radioactive concentration.

One-step radiosynthesis of ¹⁸F-AlF-NOTA-RGD₂ for tumor angiogenesis PET imaging.

Purpose: One of the major obstacles of the clinical translation of (18)F-labeled arginine-glycine-aspartic acid (RGD) peptides has been the laborious multistep radiosynthesis. In order to facilitate the application of RGD-based positron emission tomography (PET) probes in the clinical setting we investigated in this study the feasibility of using the chelation reaction between Al(18)F and a macrocyclic chelator-conjugated dimeric RGD peptide as a simple one-step (18)F labeling strategy for development of a PET probe for tumor angiogenesis imaging.

Methods: Dimeric cyclic peptide E[c(RGDyK)](2) (RGD(2)) was first conjugated with a macrocyclic chelator, 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA), and the resulting bioconjugate NOTA-RGD(2) was then radiofluorinated via Al(18)F intermediate to synthesize (18)F-AlF-NOTA-RGD(2).

Scleraxis is required for differentiation of the stapedius and tensor tympani tendons of the middle ear.

Scleraxis (Scx) is a basic helix-loop-helix transcription factor expressed in tendon and ligament progenitor cells and the differentiated cells within these connective tissues in the axial and appendicular skeleton. Unexpectedly, we found expression of the Scx transgenic reporter mouse, Scx-GFP, in interdental cells, sensory hair cells, and cochlear supporting cells at embryonic day 18.5 (E18.

[Study of dental caries and the influence of social-behavioral risk factors on dental caries of 1,080 15-year-old adolescents].

Objective: To describe the dental caries of 15-year-old adolescents in Hubei province, and to determine the influence of various social-behavioral risk factors on dental caries in the population.

Methods: The survey employed a multistage, stratified, non-geometric proportional randomized sampling, representing adolescents aged 15-year-old in Hubei province. The epidemiological investigation of dental caries was made by clinical oral health examination.

Silver and gold icosahedra: one-pot water-based synthesis and their superior performance in the electrocatalysis for oxygen reduction reactions in alkaline media.

Much effort has gone into generating polyhedral noble metal nanostructures because of their superior electrocatalytic activities for fuel cells. Herein, we report uniform, high-yield icosahedral silver and gold nanoparticles by using a facile one-pot, seedless, water-based approach that incorporates polyvinyl pyrrolidone and ammonia. Electrocatalysis of the oxygen-reduction reaction was carried out in alkaline media to evaluate the performance of the icosahedral nanoparticles.