Activity

Recently, pyrrolizine derivatives have been reported to possess numerous anticancer activities. In a previous study, (EZ)-6-((4-chlorobenzylidene)-amino)-7-cyano-N-(p-tolyl)-2,3-dihydro-1H-pyrrolizine carboxamide (EZPCA) compound was synthesized and the cytotoxic activity of EZPCA toward COX-2 enzyme (overexpressed in cancer cells) was reported. In order to assess the suitability of this compound as a promising pilot structure for in vivo applications, EZPCA was radiolabeled with radioiodine-131 (131I) and various factors affecting radiolabeling process were studied. Quality control studies of [131I]iodo-EZPCA were performed using paper chromatography and HPLC was used as a co-chromatographic technique for confirming the radiochemical yield. Biodistribution studies of [131I]iodo-EZPCA were undertaken in normal and tumor bearing mice. The radiochemical yield percentage of [131I]iodo-EZPCA was 94.20 ± 0.12%. The biodistribution results showed evident tumor uptake of [131I]iodo-EZPCA with promising target/non-target (T/NT) ratios. As a conclusion, these data suggest that [131I]iodo-EZPCA had high binding efficiency, high tumor uptake and sufficient stability to be used be used in diagnostic studies.A straightforward and scalable method for the synthesis of protected 2-hydroxyglycals is described. The approach is based on the chlorination of carbohydrate-derived hemiacetals, followed by an elimination reaction to establish the glycal moiety. 1,2-dehydrochlorination reactions were studied on a range of glycosyl chlorides to provide suitable reaction conditions for this transformation. Benzyl ether, isopropylidene and benzylidene protecting groups, as well as interglycosidic linkage, were found to be compatible with this protocol. The described method is operationally simple and allows for the quick preparation of 2-hydroxyglycals with other than ester protecting groups, providing a feasible alternative to existing methods.

[

F]SiTATE (formerly known as [

F]SiFAlin-TATE) was recently introduced as a highly promising imaging agent for the diagnosis of well-differentiated neuroendocrine tumors (NET) using positron emission tomography/computed tomography (PET/CT). A high tumor uptake and excellent image quality, the straightforward labeling approach, as well as the economic and logistic advantages of

F- over

Ga-labeled compounds predestinate [

F]SiTATE to become a potential new clinical reference standard. A novel state-of-the-art methodology of automated radiopharmaceutical production is required to establish [

F]SiTATE in clinical routine. This work illustrates the development of a novel synthesis procedure of [

F]SiTATE on an automated synthesis unit (ASU) and the clinical applicability of the tracer in human NET imaging.

A new synthesis protocol was generated for the production of [

F]SiTATE on the Scintomics GRP™ platform for clinical NET imaging. The synthesis was carried out according to common Good Manufacturi investigations.

The automated process for the manufacture of [

F]SiTATE described herein represents an important contribution to make [

F]SiTATE routinely accessible for its use in clinical NET diagnosis.

The automated process for the manufacture of [18F]SiTATE described herein represents an important contribution to make [18F]SiTATE routinely accessible for its use in clinical NET diagnosis.

Reliability in the use of placentome (including placenta, umbilical cord, and cord blood) biomarkers requires an understanding of their distributions. Here we aim to develop a simple and proper placenta sampling scheme, and to evaluate the placental distributions of biomarkers.

We developed a continuous cooling chain protocol off delivery room and cryo-subsampling method for placenta sampling. The levels of thyroid hormones (THs), elements, persistent organic pollutants (POPs), monoamines, and vitamin E were measured using UPLC-Q-TOF-MS, HPLC-ICP-MS, HPLC-EcD, and HRGC-HRMS, respectively. The distributions of biomarkers were assessed.

In human placentome,

-thyroxine (T

), Cd, Se, Zn, Cu, Fe, Ca, K, Mg, α-tocopherol, β-tocopherol, and β-tocotrienol levels were higher in placenta than in umbilical cord, while Pb and Mn were concentrated in human cord. In porcine placentome, T

, 3,3′,5′-triiodo-

-thyronine (rT

), 3,3′-diiodo-

-thyronine, Cd, Pb, Zn, K, and Al levels were higher in the cord. The intraclass correlation coefficient (ICC) was <0.4 for 3,3′,5-triiodo-

-thyronine, rT

, α-tocopherol, and 7 elements in human basal plate, indicating low reliability. rT

, Cd, Zn, Mn, and Cu were significantly concentrated in the central region in human placenta, while higher levels of As, Cd, Cr, and Al were found in the periphery region in porcine placenta. Polychlorinated biphenyls (PCBs) and polybrominated diphenyl ethers (PBDEs) showed moderate reliability (ICC 0.40-0.98) except PCB-81, -126, and BDE-208, while polychlorinated dibenzo-p-doixins/furans (PCDD/Fs) showed poor reliability (ICC 0.07-0.31).

These results highlight the complexity of placenta sampling. This study provides a novel and simple sampling approach in investigating placental exposomics.

These results highlight the complexity of placenta sampling. This study provides a novel and simple sampling approach in investigating placental exposomics.

To develop and validate a measure of asthma knowledge and to translate and culturally adapt the measure into the Arabic language and context.

Medically diagnosed individuals 18 years and older were recruited in primary care and specialty asthma clinics in the United Arab Emirates. The National Asthma Education and Prevention Program recommendations for education on asthma were used as a framework to develop the Asthma Knowledge Test (AKT). A measurement scale of “Yes,” “No,” and “I don’t know” was selected. Descriptive statistics were calculated for participant demographics and other healthcare information. GSK3326595 Cronbach α ≥ 0.7 was used to measure reliability. Principal component analysis was used to determine the distinct areas of asthma knowledge covered by the AKT. Differences in asthma knowledge depending on sex, age, marital status, and education were tested using multivariate analyses of variance.

Cronbach α= .70. Four components were retained and included asthma as a common disease, triggers and control issues, inhalers, and beliefs and myths.