The synergy of Lu-FAPI-46 with tyrosine kinase inhibitor in a sarcoma patient-derived xenograft mouse model.

Background: Given the heterogeneity and high mortality associated with metastatic soft tissue sarcoma, this study aims to evaluate the therapeutic efficacy of combining Lu-FAPI-46 with Pazopanib against this malignancy.

Methods: Patient-derived xenograft (PDX)-bearing mice were randomly divided into three groups: the control group, the Lu-FAPI-46 monotherapy group, and the Lu-FAPI-46 combined with Pazopanib therapy group. Therapeutic efficacy was regularly monitored.

In vivo SPECT imaging of Tc-99m radiolabeled exosomes from human umbilical-cord derived mesenchymal stem cells in small animals.

Extracellular vesicles derived from human umbilical cord-derived mesenchymal stem cells (UCMSC-EVs) have been postulated to have therapeutic potential for various diseases. However, the biodistribution and pharmacokinetics of these vesicles are still unclear. For a better understanding of the in vivo properties of UCMSC-EVs, in the present study, these vesicles were first radiolabeled with Technetium-99m (Tc-UCMSC-EVs) and evaluated using in vivo single photon emission computed tomography (SPECT) imaging and biodistribution experiments.

Imaging diabetic cardiomyopathy in a type 1 diabetic rat model using F-FEPPA PET.

Objective: Diabetic patients often experience chronic inflammation and fibrosis in their cardiac tissues, highlighting the pressing need for the development of sensitive diagnostic methods for longitudinal assessment of diabetic cardiomyopathy. This study aims to evaluate the significance of an inflammatory marker known as translocator protein (TSPO) in a positron emission tomography (PET) protocol for longitudinally monitoring cardiac dysfunction in a diabetic animal model. Additionally, we compared the commonly used radiotracer, F-fluoro-2-deoxy-d-glucose (F-FDG).

The effect of estrogen therapy on cerebral metabolism in diabetic female rats.

The impact of estrogen on brain function, especially in individuals with diabetes, remains uncertain. This study aims to compare cerebral glucose metabolism levels in intact rats, ovariectomized (OVX) rats, and 17β-estradiol (E2)-treated OVX diabetic female rats. Sixteen rats were administered a single intraperitoneal injection of 70 mg/kg streptozotocin (STZ) to induce diabetes (intact, n = 6; OVX, n = 6; OVX+E2-treated, n = 4).

Environmentally friendly Nafion-catalyzed synthesis of 3-substituted isoquinoline by using hexamethyldisilazane as a nitrogen source under microwave irradiation.

This study developed an eco-friendly method to synthesize 3-arylisoquinoline from 2-alkynylbenzaldehydes using Nafion® NR50 as an acidic catalyst and hexamethyldisilazane (HMDS) as a nitrogen source. The reaction proceeded a 6- cyclization under microwave irradiation, giving the corresponding isoquinolines in excellent yields. The advantages of this protocol include: (1) the use of recyclable acid catalysts, (2) transition-metal-free catalysis, and (3) the effective formation of the target product.

Drugs to Treat Neuroinflammation in Neurodegenerative Disorders.

Neuroinflammation is associated with disorders of the nervous system, and it is induced in response to many factors, including pathogen infection, brain injury, toxic substances, and autoimmune diseases. Astrocytes and microglia have critical roles in neuroinflammation. Microglia are innate immune cells in the central nervous system (CNS), which are activated in reaction to neuroinflammation-inducing factors.

Glycolytic Plasticity of Metastatic Lung Cancer Captured by Noninvasive F-FDG PET/CT and Serum H-NMR Analysis: An Orthotopic Murine Model Study.

We aim to establish a noninvasive diagnostic platform to capture early phenotypic transformation for metastasis using 18F-FDG PET and 1H-NMR-based serum metabolomics. Mice with implantation of NCI-H460 cells grew only primary lung tumors in the localized group and had both primary and metastatic lung tumors in the metastatic group. The serum metabolites were analyzed using 1H-NMR at the time of PET/CT scan.

Acid-controlled multicomponent selective synthesis of 2,4,6-triaryl pyridines and pyrimidines by using hexamethyldisilazane as a nitrogen source under microwave irradiation.

An efficient and general protocol for the synthesis of functionalized 2,4,6-triaryl pyridines and pyrimidines was developed from commercially available aromatic ketones, aldehydes and hexamethyldisilazane (HMDS) as a nitrogen source under microwave irradiation. In this multicomponent synthetic route, Lewis acids play an important role in selectively synthesizing six-membered heterocycles, including pyridines (1N) and pyrimidines (2N), by involving [2 + 1 + 2 + 1] or [2 + 1 + 1 + 1 + 1] annulated processes.

TMSOTf-mediated Kröhnke pyridine synthesis using HMDS as the nitrogen source under microwave irradiation.

An efficient protocol for the preparation of pyridine skeletons has been successfully developed involving the TMSOTf/HMDS (trifluoromethanesulfonic acid/hexamethyldisilane) system for the intermolecular cyclization of chalcones under MW (microwave) irradiation conditions. This method provides a facile approach to synthesize 2,4,6-triaryl or 3-benzyl-2,4,6-triarylpyridines in good to excellent yields. Interestingly, the 2,6-diazabicyclo[2.

Globo H Is a Promising Theranostic Marker for Intrahepatic Cholangiocarcinoma.

Recent studies support the development of cancer therapeutics to target Globo H-ceramide, the most prevalent tumor-associated carbohydrate antigen in epithelial cancers. Herein, we evaluated the expression of Globo H and its prognostic significance in intrahepatic cholangiocarcinoma (ICC) and conducted preclinical studies to assess the antitumor activity of Globo H-specific antibody in thioacetamide (TAA)-induced ICC in rats. Globo H-ceramide in tumor specimens was detected by immunohistochemistry (IHC) and mass spectrometry.

Radiation-Induced Metabolic Shifts in the Hepatic Parenchyma: Findings from F-FDG PET Imaging and Tissue NMR Metabolomics in a Mouse Model for Hepatocellular Carcinoma.

Purpose: By taking advantage of 18F-FDG PET imaging and tissue nuclear magnetic resonance (NMR) metabolomics, we examined the dynamic metabolic alterations induced by liver irradiation in a mouse model for hepatocellular carcinoma (HCC).

Methods: After orthotopic implantation with the mouse liver cancer BNL cells in the right hepatic lobe, animals were divided into two experimental groups. The first received irradiation (RT) at 15 Gy, while the second (no-RT) did not.

Irisin, an exercise myokine, potently suppresses tumor proliferation, invasion, and growth in glioma.

Glioblastoma multiforme is the most common and aggressive glial tumor with poor prognosis. Importantly, effective treatment options for glioblastoma are unmet needs. Obesity and low physical activity have been linked with a high risk of cancer, and exercise is related to delayed cancer development and progression.

SOX4 activates CXCL12 in hepatocellular carcinoma cells to modulate endothelial cell migration and angiogenesis in vivo.

The overexpression of SOX4 in various kinds of cancer cells was associated with poor prognosis for patients. The role of SOX4 in angiogenesis and tumor microenvironment modulation was recently documented in breast cancer but remains unclear in hepatocellular carcinoma (HCC). In our study, the clinical relevance of SOX4 overexpression in HCC and its role in the tumor microenvironment were investigated.

Diffusion-weighted MRI and F-FDG PET correlation with immunity in early radiotherapy response in BNL hepatocellular carcinoma mouse model: timeline validation.

Purpose: Imaging probes/biomarkers that are correlated with molecular or microenvironmental alterations in tumors have been used not only in diagnosing cancer but also in assessing the efficacy of cancer treatment. We evaluated the early response of hepatocellular carcinoma (HCC) to radiation treatment using T2-weighted magnetic resonance imaging (MRI), diffusion-weighted (DW) MRI, and F-fluorodeoxyglucose (F-FDG) positron emission tomography (PET).

Methods: Orthotopic HCC tumors were established in the right liver lobe of Balb/c mice.

The effect of caffeine on cerebral metabolism during alpha-chloralose anesthesia differs from isoflurane anesthesia in the rat brain.

Rationale: Caffeine is a widely studied psychostimulant, even though its exact effect on brain activity remains to be elucidated. Positron emission tomography (PET) allows studying mechanisms underlying cerebral metabolic responses to caffeine in caffeine-naïve rats. Rodent studies are typically performed under anesthesia.

Focused Ultrasound-Induced Blood-Brain Barrier Opening Enhances GSK-3 Inhibitor Delivery for Amyloid-Beta Plaque Reduction.

Alzheimer's disease (AD) is a neurodegenerative disease that is the leading cause of age-related dementia. Currently, therapeutic agent delivery to the CNS is a valued approach for AD therapy. Unfortunately, the CNS penetration is greatly hampered by the blood-brain barrier (BBB).

Early Imaging Biomarker of Myocardial Glucose Adaptations in High-Fat-Diet-Induced Insulin Resistance Model by Using F-FDG PET and [U-C]glucose Nuclear Magnetic Resonance Tracer.

Background: High-fat diet (HFD) induces systemic insulin resistance leading to myocardial dysfunction. We aim to characterize the early adaptations of myocardial glucose utility to HFD-induced insulin resistance.

Methods: Male Sprague-Dawley rats were assigned into two groups, fed a regular chow diet or HFD ad libitum for 10 weeks.

Nab-paclitaxel is effective against intrahepatic cholangiocarcinoma via disruption of desmoplastic stroma.

Intrahepatic cholangiocarcinoma (IH-CCA) is the second predominant hepatic malignancy worldwide. However, effective treatment strategies for IH-CCA have not yet been developed. Nab-paclitaxel may be an effective drug against IH-CCA, a type of desmoid-like tumor, and its antitumor effects may be attributable to its ability to disrupt the cancer-associated fibroblasts.

Synthesis and evaluation of -[F] fluorocelecoxib for COX-2 cholangiocarcinoma imaging.

Background: An F-tagged NSAID analog was prepared for use as a probe for COX-2 expression, which is associated with tumor development.

Methods: The in vivo uptake of celecoxib was monitored with -[F]fluorocelecoxib using positron emission tomography (PET). The binding affinity of -[F]fluorocelecoxib to COX-1 and COX-2 enzymes were assessed using the competitor celecoxib.

Identification of MALT1 as both a prognostic factor and a potential therapeutic target of regorafenib in cholangiocarcinoma patients.

Intrahepatic cholangiocarcinoma (CCA) is an aggressive cancer that lacks an effective targeted therapy. Here, we assessed the therapeutic efficacy of regorafenib in CCA, as well as elucidated its underlying mechanism. We first demonstrated that regorafenib not only inhibited growth but also induced apoptosis in human CCA cells.

Early Response Monitoring Following Radiation Therapy by Using [F]FDG and [C]Acetate PET in Prostate Cancer Xenograft Model with Metabolomics Corroboration.

We aim to characterize the metabolic changes associated with early response to radiation therapy in a prostate cancer mouse model by 2-deoxy-2-[F]fluoro-d-glucose ([F]FDG) and [C]acetate ([C]ACT) positron emission tomography, with nuclear magnetic resonance (NMR) metabolomics corroboration. [F]FDG and [C]ACT PET were performed before and following irradiation (RT, 15Gy) for transgenic adenocarcinoma of mouse prostate xenografts. The underlying metabolomics alterations of tumor tissues were analyzed by using ex vivo NMR.

The Use of PET Imaging for Prognostic Integrin αβ Phenotyping to Detect Non-Small Cell Lung Cancer and Monitor Drug Resistance Responses.

Purpose: Growing evidence has demonstrated that aberrant expression of integrin α2β1 might contribute to the invasion, metastasis and drug resistance of non-small cell lung cancer (NSCLC). Thus, the integrin α2β1 targeting Ga-DOTA-A2B1 tracer was validated in NSCLC in contrast to accumulation of the clinically used F-FDG PET tracer to see if Ga-DOTA-A2B1-PET imaging can offer a valuable and critical diagnostic imaging criterion for the identification of phenotypes of aggressive lung cancer.

Methods: To verify the prognostic value of integrin α2β1, several quantitative and functional assays were validated in different NSCLC cell lines (CL1-0, CL1-5, A549 and selected A549 cells).

Dataset on the synthesis and characterization of boron fenbufen and its F-18 labeled homolog.

The data presented in this article are related to the research article entitled "Synthesis and Characterization of Boron Fenbufen and its F-18 Labeled Homolog for Boron Neutron Capture Therapy of COX-2 Overexpressed Cholangiocarcinoma". The contents of the data article include 1) the set up for performing binding assay, 2) H-, C- and F-NMR of compounds described in main text, 3) HPLC chromatogram of the fluorination mixtures, 4) data of stability test, cell survival assay, western blot and PCR analysis, 5) the modules for fixing the two CCA rats for BNCT, and 6) bar diagram for tumor reduction using [F]FDG-PET 24 h post treatment with BNCT.

Synthesis and characterization of boron fenbufen and its F-18 labeled homolog for boron neutron capture therapy of COX-2 overexpressed cholangiocarcinoma.

Boron neutron capture therapy (BNCT) is a binary therapy that employs neutron irradiation on the boron agents to release high-energy helium and alpha particles to kill cancer cells. An optimal response to BNCT depends critically on the time point of maximal B accumulation and highest tumor to normal ratio (T/N) for performing the neutron irradiation. The aggressive cholangiocarcinoma (CCA) representing a liver cancer that overexpresses COX-2 enzyme is aimed to be targeted by COX-2 selective boron carrier, fenbufen boronopinacol (FBPin).

ALDH1A3, the Major Aldehyde Dehydrogenase Isoform in Human Cholangiocarcinoma Cells, Affects Prognosis and Gemcitabine Resistance in Cholangiocarcinoma Patients.

Purpose: Intrahepatic cholangiocarcinoma is a fatal primary liver cancer resulting from diagnosis at an advanced stage. Understanding the mechanisms of drug resistance and metastasis of cholangiocarcinoma may improve the disease prognosis. Enhanced aldehyde dehydrogenase (ALDH) activity is suggested to be associated with increased drug resistance and the metastasis.