Viola yedoensis Makino alleviates lipopolysaccharide-induced intestinal oxidative stress and inflammatory response by regulating the gut microbiota and NF-κB-NLRP3/ Nrf2-MAPK signaling pathway in broiler.

Viola yedoensis Makino (Vy) is a well-known traditional Chinese medicine widely used to treat inflammatory diseases. However, the regulatory effects of dietary Vy supplementation on lipopolysaccharide (LPS)-induced intestinal damage in broilers and the underlying molecular mechanisms remain unclear. In this study, broilers were intraperitoneally injected with 1 mg/kg LPS on days 17, 19 and 21 to induce intestinal damage. Vy supplementation at 0.5, 1.5 and 4.5 % in the diet was administered separately for 21 days to investigate the potential protective effects of Vy supplementation against LPS-induced intestinal impairment in broilers. Vy supplementation improved intestinal morphology and restored growth performance. Vy supplementation attenuated intestinal inflammation by regulating the nuclear factor kappa B (NF-κB) / NLR family pyrin domain-containing 3 (NLRP3) signaling pathway and inhibited its downstream pro-inflammatory factor levels. In addition, Vy supplementation relieved intestinal oxidative impairment by regulating the nuclear factor erythroid-2 related factor 2 (Nrf2) / mitogen-activated protein kinase (MAPK) signaling pathway and downstream antioxidant enzyme activity. Vy supplementation reduced LPS-induced mitochondrial damage and apoptosis. Furthermore, Vy supplementation alleviated LPS-induced intestinal inflammation and oxidative damage in chickens by increasing the abundance of protective bacteria (Lactobacillus and Romboutsia) and reducing the number of pathogenic bacteria (unclassified_f_Ruminococcaceae, unclassified_f_Oscillospiraceae and norank_f_norank_o_Clostridia_vadinBB60_group). Overall, Vy supplementation effectively ameliorated LPS-induced intestinal damage by regulating the NF-κB-NLRP3/Nrf2-MAPK signaling pathway and maintaining intestinal microbiota balance. Vy supplementation can be used as a dietary supplement to protect broilers against intestinal inflammation and oxidative damage.

Inhibition of the NF-κB pathway and ERK-mediated mitochondrial apoptotic pathway takes part in the mitigative effect of betulinic acid on inflammation and oxidative stress in cyclophosphamide-triggered renal damage of mice.

Betulinic acid (BA), an occurring pentacyclic triterpenoid, has various biological activities, such as anti-inflammation and antioxidation. Previous studies found that BA attenuated cyclophosphamide (CYP)-induced intestinal mucosal damage by inhibiting intestinal mucosal barrier dysfunctions and cell apoptosis. However, the effects and regulation mechanisms of BA on CYP-induced renal damage has not been reported in literature. Here, we found that BA pretreatment alleviated the elevation of serum urea level and inhibited the increase in serum neutrophil gelatinase-associated lipocalin level induced by CYP. Meanwhile, BA ameliorated renal tubular epithelial cell edema, and vacuolization of renal cortical tubular and renal glomerulus. Moreover, pretreatment with BA inhibited the mRNA expressions of pro-inflammatory cytokines interleukin-1ß (IL-1ß), IL-6, and tumor necrosis factor-α, and increased mRNA expressions of anti-inflammatory cytokines such as IL-10 and transforming growth factor-ß by inactivation nuclear factor kappa-B. Simultaneously, BA decreased the accumulation of reactive oxygen species and malondialdehyde, and lowered the levels of superoxide dismutase and glutathione, while increased the activity of glutathione peroxidase in CYP-induced kidney damage mice. Besides, BA reduced the phosphorylation of extracellular signal-regulated kinases (ERK), inhibited the ratio of Bcl-2/Bax and cell apoptosis in CYP-triggered kidney damage. Furthermore, BA and/or PD98059 (an inhibitor of ERK) regulated mitigation of CYP-elicited renal injury and deactivation of the ERK pathway and mitochondrial apoptotic pathway, indicating that the protective effect of BA on CYP-induced renal damage may be associated with the down-regulation of ERK-mediated mitochondrial apoptotic pathway. Thus, BA could be a candidate agent against chemotherapy drug-induced nephrotoxicity by reducing inflammation and oxidative stress through suppression of ERK-mediated mitochondrial apoptotic pathway.

99m Tc-labeled DTPA-colchicine dimer with improved tumor uptake.

This work reports the synthesis, radiolabeling, and biological studies of 99m Tc-diethylene triamine pentaacetic acid (DTPA)-colchicine dimer in tumor-bearing mice. The novel colchicine dimer was successfully synthesized by conjugation of DTPA to 2 colchicine biomolecules. The ligand could be labeled by 99m Tc in high yield to get 99m Tc-DTPA-colchicine dimer, which was hydrophilic and stable at room temperature. Biodistribution and imaging studies in tumor-bearing mice showed that 99m Tc-DTPA-colchicine dimer accumulated in the tumor with improved uptake and retention. The results indicate the need for synthetic modification of the parent colchicine derivative and the 99m Tc-chelate with a view to improve the tumor-targeting efficacy and in vivo kinetic profiles.

Synthesis, 99m Tc-labeling, and preliminary biological evaluation of DTPA-melphalan conjugates.

Melphalan (MFL) is a typical nitrogen mustard for the treatment of many types of cancer. For the purpose to develop novel 99m Tc-labeled tumor imaging agents with SPECT, MFL was directly labeled by 99m Tc using diethylene triamine pentacetate acid (DTPA) as bifunctional chelating agent. The novel ligands were successfully synthesized by conjugation of DTPA to MFL to get monosubstituted DTPA-MFL and bis-substituted DTPA-2MFL. Radiolabeling was performed in high yield to get 99m Tc-DTPA-MFL and 99m Tc-DTPA-2MFL, respectively, which were hydrophilic and stable at room temperature. The high initial tumor uptake with retention, good tumor/muscle ratios, and satisfactory scintigraphic images suggested the potential of 99m Tc-DTPA-MFL and 99m Tc-DTPA-2MFL for tumor imaging. However, the slow normal tissue clearance would be a great obstacle. Further modification on the linker and/or 99m Tc-chelate to improve the tumor targeting efficacy and in vivo kinetic profiles is currently in progress.

Metabolizer in vivo of fullerenes and metallofullerenes by positron emission tomography.

Fullerenes (C60) and metallofullerenes (Gd@C82) have similar chemical structure, but the bio-effects of both fullerene-based materials are distinct in vivo. Tracking organic carbon-based materials such as C60 and Gd@C82 is difficult in vivo due to the high content of carbon element in the living tissues themselves. In this study, the biodistribution and metabolism of fullerenes (C60 and Gd@C82) radiolabeled with (64)Cu were observed by positron emission tomography (PET). (64)Cu-C60 and (64)Cu-Gd@C82 were prepared using 1, 4, 7, 10-tetrakis (carbamoylmethyl)-1, 4, 7, 10-tetra-azacyclodo-decanes grafted on carbon cages as a chelator for (64)Cu, and were obtained rapidly with high radiochemical yield (≥90%). The new radio-conjugates were evaluated in vivo in the normal mouse model and tissue distribution by small animal PET/CT imaging and histology was carried out. The PET imaging, the biodistribution and the excretion of C60 and Gd@C82 indicated that C60 samples have higher blood retention and lower renal clearance than the Gd@C82 samples in vivo and suggested that the differences in metabolism and distribution in vivo were caused by the structural differences of the groups on the fullerene cages though there is chemical similarity between C60 and Gd@C82.

Highly efficient one-pot labeling of new phosphonium cations with fluorine-18 as potential PET agents for myocardial perfusion imaging.

Lipophilic cations such as phosphonium salts can accumulate in mitochondria of heart in response to the negative inner-transmembrane potentials. Two phosphonium salts [(18)F]FMBTP and [(18)F]mFMBTP were prepared and evaluated as potential myocardial perfusion imaging (MPI) agents in this study. The cations were radiolabeled via a simplified one-pot method starting from [(18)F]fluoride and followed by physicochemical property tests, in vitro cellular uptake assay, ex vivo mouse biodistribution, and in vivo rat microPET imaging. The total radiosynthesis time was less than 60 min including HPLC purification. The [(18)F] labeled compounds were obtained in high radiolabeling yield (∼50%) and good radiochemical purity (>99%). Both compounds were electropositive, and their log P values at pH 7.4 were 1.16 ± 0.003 (n = 3) and 1.05 ± 0.01 (n = 3), respectively. Both [(18)F]FMBTP and [(18)F]mFMBTP had high heart uptake (25.24 ± 2.97% ID/g and 31.02 ± 0.33% ID/g at 5 min postinjection (p.i.)) in mice with good retention (28.99 ± 3.54% ID/g and 26.82 ± 3.46% ID/g at 120 min p.i.). From the PET images in rats, the cations exhibited high myocardium uptake and fast clearance from liver and small intestine to give high-contrast images across all time points. These phosphonium cations were radiosynthesized via a highly efficient one-pot procedure for potential MPI offering high heart accumulation and rapid nontarget clearance.

Prostate cancer with elevated free prostate-specific antigen density: A case report.

BACKGROUND: Prostate cancer is the second most common cancer among men worldwide, and prostate-specific antigen (PSA) is often used in clinical practice to screen for prostate cancer. Normal total PSA (tPSA) level initially excludes prostate cancer. Here, we report a case of prostate cancer with elevated free PSA density (fPSAD). CASE SUMMARY: A patient diagnosed with benign prostatic hyperplasia underwent prostatectomy, and the postoperative pathological results showed acinar adenocarcinoma of the prostate. The patient is currently undergoing endocrine chemotherapy. CONCLUSION: We provide a clinical reference for diagnosis and treatment of patients with normal tPSA but elevated fPSAD.

Synthesis and Evaluation of 18F-Labeled Phenylpiperazine-like Dopamine D3 Receptor Radioligands for Positron Emission Tomography Imaging.

The dopamine D3 receptor (D3R) is important in the pathophysiology of various neuropsychiatric disorders, such as depression, bipolar disorder, schizophrenia, drug addiction, and Parkinson's disease. Positron emission tomography (PET) with innovative radioligands provides an opportunity to assess D3R in vivo and to elucidate D3R-related disease mechanisms. Herein, we present the synthesis of eight 18F-labeled phenylpiperazine-like D3R-selective radioligands possessing good radiochemical purity (>97%), in vitro stability (>95%), and befitting lipophilicity. Based on in vitro binding assays and static microPET studies, the phenylpiperazine-like radioligands [18F]FBPC01 and [18F]FBPC03 were chosen as lead radioligands targeting D3R. Molecular docking further elucidated their binding mechanism. Radiolabeling conditions were optimized and then applied to an automated radiolabeling process, affording products with high specific activity (>112 GBq/µmol). Dynamic rat PET study demonstrated the specific binding of [18F]FBPC01 and [18F]FBPC03 to D3R in the brain ventricles and the pituitary gland. Validated by dynamic PET data analysis, biodistribution study, and metabolism analysis, [18F]FBPC03 exhibited the highest PET signal-to-noise ratio, good D3R-specific binding in the brain ventricles and pituitary gland of rats with few off-target binding, negligible defluorination, and stable brain metabolism, which indicated that [18F]FBPC03 was a promising D3R radioligand.

Betulinic acid attenuates T-2 toxin-induced lung injury by activating Nrf2 signaling pathway and inhibiting MAPK/NF-κB signaling pathway.

T-2 toxin, a type-A trichothecene mycotoxin, exists ubiquitously in mildewed foods and feeds. Betulinic acid (BA), a pentacyclic triterpenoid derived from plants, has the effect of relieving inflammation and oxidative stress. The purpose of this study was to investigate whether BA mitigates lung impairment caused by T-2 toxin and elucidate the underlying mechanism. The results indicated that T-2 toxin triggered the inflammatory cell infiltration, morphological alterations and cell apoptosis in the lungs. It is gratifying that BA ameliorated T-2 toxin-caused lung injury. The protein expression of nuclear factor erythrocyte 2-related factor 2 (Nrf2) pathway and the markers of antioxidative capability were improved in T-2 toxin induced lung injury by BA mediated protection. Simultaneously, BA supplementation could suppress T-2 toxin-induced mitogen-activated protein kinase (MAPK)/nuclear factor-kappa B (NF-κB)-dependent inflammatory response and mitochondrial apoptotic pathway. Therefore, T-2 toxin gave rise to pulmonary toxicity, but these changes were moderated by BA administration through regulation of the Nrf2/MAPK/NF-κB pathway, which maybe offer a viable alternative for mitigating the lung impairments caused by the mycotoxin.

Pyrolytic Graphite for an In-Plane Force Study of Diamagnetic Levitation: A Potential Microdetector of Cracks in Magnetic Material.

The diamagnetic levitation technique can be applied in non-destructive testing for identifying cracks and defects in magnetic materials. Pyrolytic graphite is a material that can be leveraged in micromachines due to its no-power diamagnetic levitation on a permanent magnet (PM) array. However, the damping force applied to pyrolytic graphite prevents it from maintaining continuous motion along the PM array. This study investigated the diamagnetic levitation process of pyrolytic graphite on a permanent magnet array from various aspects and drew several important conclusions. Firstly, the intersection points on the permanent magnet array had the lowest potential energy and validated the stable levitation of pyrolytic graphite on these points. Secondly, the force exerted on the pyrolytic graphite during in-plane motion was at the micronewton level. The magnitude of the in-plane force and the stable time of the pyrolytic graphite were related to the size ratio between it and the PM. During the fixed-axis rotation process, the friction coefficient and friction force decreased as the rotational speed decreased. Smaller-sized pyrolytic graphite can be used for magnetic detection, precise positioning and other microdevices. The diamagnetic levitation of pyrolytic graphite can also be used for detecting cracks and defects in magnetic materials. We hope this technique will be used in crack detection, magnetic detection and other micromachines.

Synthesis and biological evaluation of 99mTc(CO)3(His-CB) as a tumor imaging agent.

The chlorambucil l-histidine conjugate was synthesized and radiolabeled with [(99m)Tc(CO)(3)](+) core to form the (99m)Tc(CO)(3)(His-CB) complex. The radiochemical purity of the complex was over 90%. It had good hydrophilicity and was stable at room temperature. The high initial tumor uptake with certain retention, fast clearance from background, good tumor/non-tumor ratios and satisfactory scintigraphic images highlighted the potential of (99m)Tc(CO)(3)(His-CB) as a tumor imaging agent.

Synthesis and characterization of folic acid modified water-soluble chitosan derivatives for folate-receptor-mediated targeting.

Three chemical modification methods of carboxymethylation, quaternization and hydroxypropylation were used to synthesize water-soluble chitosan derivatives. In order to study the feasibility of these chitosan derivatives as backbones of nuclear imaging agents, folic acid (FA) and Technetium-99m were introduced onto the water-soluble chitosan chains. The bifunctional chelating agent 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) was conjugated to the folate grafted chitosan derivatives for chelating with radionuclides such as (64)Cu and (68)Ga. The structures of these new ligands were characterized with multiple methods. The solubility and stability of the (99m)Tc-complexes were both favorable. Further study of their radiochemical and biological properties will be performed to evaluate the usefulness of these water-soluble chitosan derivatives for nuclear imaging agent design.

Suppression of endoplasmic reticulum stress-associated pathways and hepatocyte apoptosis participates in the attenuation of betulinic acid on alcohol-provoked liver injury in mice.

Endoplasmic reticulum stress (ERS) plays a vital role in the pathogenesis of the alcoholic liver disease (ALD). Betulinic acid (BA) has been reported to be effective in the attenuation of ALD; however, its role in ERS and associated stress-signaling pathways remains elusive. Here, we found that the BA pretreatment significantly reduced the alcohol-induced liver injury by decreasing the activities of serum alanine aminotransferase and aspartate aminotransferase, alleviating fat deposition and rupturing the ER in hepatocytes. Moreover, the protective effect of BA on ALD was associated with the inhibition of reactive oxygen species accumulation and ERS, accompanied by the downregulation of glucose-regulated protein 78 (Grp78), Grp94, phosphorylation-inositol-requiring enzyme 1α (p-IRE1α), and phosphorylation-protein kinase R-like endoplasmic reticulum kinase (p-PERK), activating the transcription factor 6 (ATF6) and C/EBP homologous protein (CHOP). Moreover, the alcohol-induced hepatocyte apoptosis was reduced, along with the downregulation of the mitogen-activated protein kinase pathway, caspase-12, caspase-3, and caspase-7, following BA administration. Additionally, the BA-mediated mitigation of alcohol-induced liver injury and deactivation of the ER pathways were the same with 4-PBA, an inhibitor of ERS, indicating that the protective effect of BA on ALD may be regulated by ERS-associated pathways. Collectively, BA is a potentially desirable agent for the ALD, which may reduce hepatocyte apoptosis by suppressing excessive ERS in the liver.

Radiolabeling of folic acid-modified chitosan with (99m)Tc as potential agents for folate-receptor-mediated targeting.

The feasibility of chitosan (CS) as a backbone for the design of (99m)Tc-labeled targeting agent was evaluated in this study. Chitosan-folate conjugate (CSFA) and chitosan-folate dithiocarbamate (CSFADTC) were synthesized, characterized and radiolabeled with (99m)Tc as model compounds for folate-receptor (FR) targeting. (99m)Tc-complexes were prepared with high radiochemical purity and high stability. The hydrophilicities of these (99m)Tc-complexes were determined by partition coefficient experiments. The results of biodistribution in normal mice showed that the folic-acid modified agents ((99m)Tc-CSFA and (99m)TcN-CSFADTC) had obviously higher uptake in FR-positive kidney and much lower liver and spleen uptakes than that of non-folic-acid modified (99m)Tc-agent, and the kidney uptakes of FA-modified agents could be blocked significantly by the corresponding cold ligand. Furthermore in vitro and in vivo specific studies will be done in cell line and tumor bearing mice to confirm the usefulness of this chitosan backbone for FR targeting agent design.

BTN2A2 protein negatively regulates T cells to ameliorate collagen-induced arthritis in mice.

Rheumatoid arthritis (RA) is an autoimmune disorder characterized by persistent inflammatory responses in target tissues and organs, resulting in the destruction of joints. Collagen type II (CII)-induced arthritis (CIA) is the most used animal model for human RA. Although BTN2A2 protein has been previously shown to inhibit T cell functions in vitro, its effect on autoimmune arthritis has not been reported. In this study, we investigate the ability of a recombinant BTN2A2-IgG2a Fc (BTN2A2-Ig) fusion protein to treat CIA. We show here that administration of BTN2A2-Ig attenuates established CIA, as compared with control Ig protein treatment. This is associated with reduced activation, proliferation and Th1/Th17 cytokine production of T cells in BTN2A2-Ig-treated CIA mice. BTN2A2-Ig also inhibits CII-specific T cell proliferation and Th1/Th17 cytokine production. Although the percentage of effector T cells is decreased in BTN2A2-Ig-treated CIA mice, the proportions of naive T cells and regulatory T cells is increased. Furthermore, BTN2A2-Ig reduces the percentage of proinflammatory M1 macrophages but increases the percentage of anti-inflammatory M2 macrophages in the CIA mice. Our results suggest that BTN2A2-Ig protein has the potential to be used in the treatment of collagen-induced arthritis models.

Effects of Stimulating Local and Distal Acupoints on Diabetic Gastroparesis: A New Insight in Revealing Acupuncture Therapeutics.

One of the most important aspects of clinical acupuncture practice, like diabetic gastroparesis, is the selection of suitable acupoints. Furthermore, it is critical to examine the therapeutic impact differences between distal and local acupoints, as well as the prescription of their combination. In this study, diabetic gastroparesis rats were treated by needling Zhongwan (CV12) and Zusanli (ST36), and then used Single Photon Emission Computed Tomography-CT (SPECT-CT) technology to assess the effects of promoting gastric motility. In addition, morphological observation, immunohistochemical examination, and biomarker assays, such as determination of growth factor 1, motilin, and ghrelin contents in serum samples, were performed to better understand the impact of certain various acupuncture treatments. All of the therapies improved the symptoms of diabetic gastroparesis rats, according to the findings. Stimulating these acupoints, on the other hand, can have a different therapeutic effect. In addition, needling local and distal acupoints together can have an antagonistic or synergistic impact on specific physiological and biochemical indexes such as gastric motility, ghrelin, gastrin, and growth factor 1, among others. Our findings demonstrated the benefits of acupoints and acupuncture in the management of diabetic gastroparesis, as well as a new insight into acupuncture therapeutics.

Trp2 Peptide-Assembled Nanoparticles with Intrinsically Self-Chelating 64Cu Properties for PET Imaging Tracking and Dendritic Cell-Based Immunotherapy against Melanoma.

Dendritic cell-based immunotherapy, in which the antigen is effectively delivered to dendritic cells and then the dendritic cells stimulated by the antigen migrate to draining lymph nodes (DLNs) to induce the CD8+ T-cell immune response, shows great promise for tumor immunotherapy. In this study, we used coassembled nanoparticles formed by Trp2 antigen and the conjugates of short-chain poly(ethylene glycol) (PEG) and pyropheophorbide-A (PPa) (Trp2/PPa-PEGm) to deliver Trp2 to DCs. Intrinsically self-chelating 64Cu of coassemblies could be used to sensitively image the migration of DCs in vivo by positron emission tomography (PET) imaging. The coassemblies of the Trp2 antigen were efficiently engulfed by DCs without causing DC cytotoxicity in vitro and induced DC maturation. After injection of DCs labeled by coassemblies of the Trp2 antigen, the homing of DCs to DLNs in vivo could be sensitively observed by PET imaging. The C57BL/6 mice injected with DCs containing the Trp2/PPa-PEGm NP showed antigen-specific immune responses including enhanced interferon-γ (IFN-γ) production, splenocyte proliferation, and percentage of IFN-γ-secreting CD8+ T cells. In addition, C57BL/6 mice inoculated with B16-F10 tumor cells showed delayed tumor growth after immunization with the Trp2/PPa-PEGm NP-labeled DC vaccine and enhanced infiltration of CD8+ T cells in tumors.

Fluorine-18 labeled galactosylated chitosan for asialoglycoprotein-receptor-mediated hepatocyte imaging.

Galactosylated chitosan (GC) was prepared by reacting lactobionic acid with water-soluble chitosan. GC was labeled with fluorine-18 by conjugation with N-succinimidyl-4-(18)F-fluorobenzoate ([(18)F]SFB) under a slightly basic condition. After rapid purification with HiTrap desalting column, [(18)F]FB-GC was obtained with high radiochemical purity (>97%) determined by radio-HPLC. The total reaction time for [(18)F]FB-GC was about 150 min. Typical decay-corrected radiochemical yield was about 4-8%. Ex vivo biodistribution in normal mice showed that [(18)F]FB-GC had moderate activity accumulation in liver with very good retention (11.13+/-1.63, 10.97+/-1.90 and 10.77+/-0.95%ID/g at 10, 60, 120 min after injection, respectively). The other tissues except kidney showed relative low radioactivity accumulation. The high liver/background ratio affords promising biological properties to get clear images. The specific binding of this radiotracer to the ASGP receptor was confirmed by blocking experiment in mice. Compared with the non-blocking group the hepatic uptake of [(18)F]FB-GC significantly declined in all selected time points. The better liver retention properties of [(18)F]FB-GC than that of albumin based imaging agents may improve imaging quality and simplify pharmacokinetic model of liver function in the future application with PET imaging.

Preparation and biodistribution of [18F]FP2OP as myocardial perfusion imaging agent for positron emission tomography.

UNLABELLED: Myocardial extractions of pyridaben, a mitochondrial complex I (MC-I) inhibitor, is well correlated with blood flow. Based on the synthesis and characterization of pyridaben analogue 2-tert-butyl-5-[2-(2-[(18)F]fluroethoxy)ethoxy]benzyloxy]-4-chloro-2H-pyridazin-3-one ([(18)F]FP2OP), this study assessed its potential to be developed as myocardial perfusion imaging (MPI) agent. METHODS: The tosylate labeling precursor 2-(2-(4-(tert-butyl-5-chloro-6-oxo-1,6-dihydro-pyridazin-4-yloxymethyl)benzyloxy)ethoxy)ethyl ester (OTs-P2OP) and the nonradioactive 2-tert-butyl-5-[2-(2-[(19)F]fluroethoxy)ethoxy]benzyloxy]-4-chloro-2H-pyridazin-3-one ([(19)F]FP2OP) were synthesized and characterized by IR, (1)H NMR, (13)C NMR and MS analysis. By substituting tosyl of precursor OTs-P2OP with (18)F, the radiolabeled complex [(18)F]FP2OP was prepared and further evaluated for its in vitro physicochemical properties, in vivo biodistribution, the metabolic stability in mice, ex vivo autoradiography and cardiac PET/CT imaging. RESULTS: Starting with [(18)F]F(-) Kryptofix 2.2.2./K(2)CO(3) solution, the total reaction time for [(18)F]FP2OP was about 100 min, with final high-performance liquid chromatography purification included. Typical decay-corrected radiochemical yield stayed at 41+/-5.3%, the radiochemical purity, 98% or more. Biodistribution in mice showed that the heart uptake of [(18)F]FP2OP was 41.90+/-4.52%ID/g at 2 min post-injection time, when the ratio of heart/liver, heart/lung and heart/blood reached 6.83, 9.49 and 35.74, respectively. Lipophilic molecule was further produced by metabolized [(18)F]FP2OP in blood and urine at 30 min. Ex vivo autoradiography demonstrates that [(18)F]FP2OP may have high affinity with MC-I and that can be blocked by [(19)F]FP2OP or rotenone (a known MC-I inhibitor). Cardiac PET images were obtained in a Chinese mini-swine at 5, 15, 30 and 60 min post-injection time with high quality. CONCLUSION: [(18)F]FP2OP was synthesized with high radiochemical yield. The promising biological properties of [(18)F]FP2OP suggest high potential as MPI agent for positron emission tomography in the future.

Research on Energy Management of Hybrid Unmanned Aerial Vehicles to Improve Energy-Saving and Emission Reduction Performance.

The rapid development of industry results in large energy consumption and a negative impact on the environment. Pollution of the environment caused by conventional energy sources such as petrol leads to increased demand for propulsion systems with higher efficiency and capable of energy-saving and emission reduction. The usage of hybrid technology is expected to improve energy conversion efficiency, reduce energy consumption and environmental pollution. In this paper, the simulation platform for the hybrid unmanned aerial vehicle (UAV) has been built by establishing the subsystem models of the UAV power system. Under the two chosen working conditions, the conventional cruise flight mission and the terrain tracking mission, the power tracking control and Q-Learning method have been used to design the energy management controller for the hybrid UAV. The fuel consumption and pollutant emissions under each working condition were calculated. The results show that the hybrid system can improve the efficiency of the UAV system, reduce the fuel consumption of the UAV, and so reduce the emissions of CO2, NOx, and other pollutants. This contributes to improving of environmental quality, energy-saving, and emission reduction, thereby contributing to the sustainable development of aviation.