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Cardiac imaging is one of the most important tools for diagnosing many diseases related to the heart. This work was devoted to developing this method using experiments on mice. The formation of a complex of [99mTc]dithiocarbamate of procainamide under optimum conditions of reaction temperature (37°C), reaction time (30 min), pH of the reaction mixture (8), amount of substrate (100 μg), amount of reducing agent tin(II) (content, 50 μg), and stability in rat serum (8 h) was achieved using radioactive Tc-99m (300 – 500 MBq) to give high labeling yield (98.5%) and radiochemical purity. Procainamide works through sodium channel blocker. Normal mice were used in biodistribution investigations. High absorption uptake of the [99mTc]dithiocarbamate of procainamide complex was found to be 33.47 ± 0.83% injected dose/g organ (ID/g) as observed in mice for up to 5 min, which demonstrated its usefulness as a radiotracer for heart imaging. [ABSTRACT FROM AUTHOR]

This study focuses on the synthesis and preliminary bio-evaluation of [99mTc]-technetium tricarbonyl procainamide ([99mTc]-technetium tricarbony PA) as a viable cardiac imaging agent. The compound, [99mTc]-technetium tricarbony PA, was synthesized by labelling procainamide with a [99mTc]-technetium tricarbonyl core, yielding a high radiochemical yield and radiochemical purity of 98%. Under optimal circumstances, high radiochemical yield and purity were obtained utilizing [99mTc]-technetium tricarbonyl core within 30 min of incubation at pH 9, 200 µg substrate concentration, and 100 °C reaction temperature. The heart showed a high absorption of 32.39 ± 0.88% of the injected dose/g organ (ID/g), confirming the suitability of [99mTc]-technetium tricarbonyl PA as a viable complex for heart imaging. [ABSTRACT FROM AUTHOR]

This work focuses on tracking peptic ulcer localized in mice. The formation of a [99mTc]dithiocarbamate of famotidine complex at optimum conditions of reaction temperature (37 °C), reaction time (30 min), pH of the reaction mixture (5), amount of substrate (100 µg), amount of reducing agent (tin (II) content, 50 µg), was achieved using radioactive Tc-99m (250–400 MBq), with labelling yield of 98% and high radiochemical purity. The in-vitro stability of [99mTc]dithiocarbamate of famotidine complex was shown to be high in rat serum for up to 8 h. Normal and ulcerated mice were used in biodistribution studies. Famotidine works by blocking histamine-2-receptor antagonists (H2RAs). The high absorption of [99mTc]dithiocarbamate of famotidine complex in stomach in amount of 27.15% injected dose/g organ (ID/g) observed in ulcerated mice for up to 24 h demonstrated its usefulness as a novel radiotracer for stomach imaging. [ABSTRACT FROM AUTHOR]

This study demonstrated the tracking of ulcerative colitis, which is considered a stressful immune disease. Although there are many ways to test for this disease including dependence on gases, dyes, and painful anal endoscopy, these treatment modalities have many disadvantages. Hence, it is the utmost need of time to discover new methods to detect this chronic immune disease and to avoid the defects of traditional methodologies. Sulfasalazine (SSD) was labeled with iodine‐131 (half‐life: 8 days, Energy: 971 keV) under optimum reaction conditions including the amount of reducing agent, pH factor, chloramine‐T (Ch‐T) amount, and incubation period. Characterization was performed using 1H/ 13C‐NMR, ESI‐MS, and HPLC (UV/ Radio) techniques. The biodistribution study was performed in normal and ulcerative mice models, and in silico molecular docking study was performed to evaluate the possible mechanism of action to target peroxisome proliferator‐activated receptor gamma (PPARγ). The high radiolabeling yield of [131I]‐sulfasalazine ([131I]‐SSD) was achieved ≥90% through the direct labeling method with radioactive iodine‐131 in the presence of chloramine‐T (100 μg). The radiotracer [131I]‐SSD was observed to be stable in normal saline and freshly eluted serum up to 12 hr at ambient temperature (37℃ ± 2℃). The radiotracer [131I]‐SSD showed the highest uptake in the targeted organ (i.e., ulcerative colon) which was observed to be ≥75% injected dose per gram (% ID/g) organ for 24 hr postinjection (p.i). Furthermore, in silico data collected from molecular modeling analysis of SSD and [131I]‐SSD with antimicrobial protein (PDB code: 3KEG) and peroxisome proliferator‐activated receptor gamma (PPARγ) (PDB code: 4XTA) showed azoreductase activity and high binding potential for PPAR‐γ site, respectively. The results of biological studies obtained in this study enlighten the usefulness of radiotracer [131I]‐SSD as a potential imaging agent for ulcerative colitis. [ABSTRACT FROM AUTHOR]

A convenient synthesis of a novel series of dihydropyridine and pyridine thioglycosides was developed. The evaluation of anti-proliferative activity against HepG-2 cell lines (liver carcinoma cell lines) shows that most of the compounds have antitumor activity, especially5b, 5f, 5j, 5n, 7b, 7f, 7j, 7n, 8b, 8f, and8j. The results of molecular docking reveal that these compounds have high binding affinity by hydrogen bond formation with the binding pocket of thymidylate synthase dihydrofolate reductase (TS-DHFR). [ABSTRACT FROM AUTHOR]

This study demonstrated the tracking of ulcerative colitis, which is considered a stressful immune disease. Although there are many ways to test for this disease including dependence on gases, dyes, and painful anal endoscopy, these treatment modalities have many disadvantages. Hence, it is the utmost need of time to discover new methods to detect this chronic immune disease and to avoid the defects of traditional methodologies. Sulfasalazine (SSD) was labeled with iodine-131 (half-life: 8 days, Energy: 971 keV) under optimum reaction conditions including the amount of reducing agent, pH factor, chloramine-T (Ch-T) amount, and incubation period. Characterization was performed using 1 H/ 13 C-NMR, ESI-MS, and HPLC (UV/ Radio) techniques. The biodistribution study was performed in normal and ulcerative mice models, and in silico molecular docking study was performed to evaluate the possible mechanism of action to target peroxisome proliferator-activated receptor gamma (PPARγ). The high radiolabeling yield of [ 131 I]-sulfasalazine ([ 131 I]-SSD) was achieved ≥90% through the direct labeling method with radioactive iodine-131 in the presence of chloramine-T (100 μg). The radiotracer [ 131 I]-SSD was observed to be stable in normal saline and freshly eluted serum up to 12 hr at ambient temperature (37℃ ± 2℃). The radiotracer [ 131 I]-SSD showed the highest uptake in the targeted organ (i.e., ulcerative colon) which was observed to be ≥75% injected dose per gram (% ID/g) organ for 24 hr postinjection (p.i). Furthermore, in silico data collected from molecular modeling analysis of SSD and [ 131 I]-SSD with antimicrobial protein (PDB code: 3KEG) and peroxisome proliferator-activated receptor gamma (PPARγ) (PDB code: 4XTA) showed azoreductase activity and high binding potential for PPAR-γ site, respectively. The results of biological studies obtained in this study enlighten the usefulness of radiotracer [ 131 I]-SSD as a potential imaging agent for ulcerative colitis., (© 2021 John Wiley & Sons Ltd.)