Correction to: Preparation, optimization and pharmacological evaluation of 99mTc-4-hydroxy-3-(2-hydroxy-3-methoxybenzylideneamino) benzoic acid complex: as a novel potential radiopharmaceutical agent with hepatobiliary excretion.

In the published original version, the complete list of authors was omitted. The complete list of contributing authors is updated with this Correction.

Labeling of epirubicin with technetium-99m: Optimization, biodistribution and scintigraphic imaging in tumor bearing mice.

Epirubicin is an antineoplastic agent of anthracycline antibiotic, used for treating a variety of tumor types such as lymphoma, cancer of the breast, lung, ovary and stomach. The objective of this work was to demonstrate direct radiolabeling of epirubicin with 99mTc, quality control, biological characterization and scientigraphic evaluation in tumor bearing mice. The 99mTc-epirubicin labeling was optimized by varying the amounts of ligand 100-350µg, stannous chloride dihydride 20-50µg and pH range 2-10 by using NaOH or HCl. The radiochemical purity of 99mTc-epirubicin was evaluated by chromatographic techniques (Whatman No. 3 paper and ITLC-SG). HPLC analyses were performed to check purity of epirubicin and radiochemical purity of labeled 99mTc- epirubicin. Biodistribution and scintigraphic imaging of 99mTc-epirubicin was performed in normal and tumor bearing mice at various time intervals. The optimum conditions ensuring 99mTc-epirubicin labeling yield as high as 99% by adding 35µg SnCl2.2H2O, 200µg of ligand at pH 6 for 30 min at room temperature (25°C±2°C). HPLC of 99mTc-epirubicin shows about 99% binding of the compound with technetium-99m. Electrophoresis study indicated the neutral nature of 99mTc-epirubicin. Biodistribution data and scintigraphic results showed that 99mTc-epirubicin accumulated in the liver as well as in tumor with significant uptake and excellent retention. 99mTc-epirubicin shows good stability in human serum. In vitro and in vivo studies revealed the significantly uptake of 99mTc-epirubicin in the tumor, and also indicating the efficiency of 99mTc-epirubicin as a tumor diagnostic agent.

Synthesis, optimization and biological evaluation of 99mTc-digoxin as possible cardiac imaging agent.

Heart imaging radiopharmaceuticals could improve the diagnostic value of routine heart scanning for detecting cardiac disorders. The aim of the study was to prepare high radiochemical purity 99mTc-Digoxin in a yield of about 98%. The optimal conditions for labelling were as follows: 100µg of Digoxin, 2µg of SnCl2•2H2O, room temperature (25±1°C), reaction retention time of 30 min at pH 7. Under these conditions, the radiochemical yield of 99mTc-Digoxin reaches 98%. In vivo bio distribution was performed in normal Swiss Albino mice at different time intervals after administration of 99mTc-Digoxin.Scintigraphic study of 99mTc-Digoxin was performed in rabbits. The heart uptake of 99mTc-Digoxin was sufficiently high and thus may be a potential myocardial imaging radiopharmaceutical applicable in cardiology.

Synthesis, quality control, and bio-evaluation of 99m Tc-cyclophosphamide.

Cancer is found to be the leading cause of death worldwide characterized by uncontrolled cell division. Nuclear medicines imaging using radiopharmaceuticals have pronounced potential for the diagnosis and treatment of cancers. Cyclophosphamide (CPH) is an antineoplastic drug which targets selectively cancer cells. In the present work, labeling of CPH with Tc-99m is performed for diagnostic purpose, which gave labeling yield as high as 99% using 20 µg SnCl2 ·2H2 O, 200 µg of ligand at pH 7 for 10 min reaction time at room temperature. The characterization of the prepared complex was performed using ITLC, electrophoresis, and HPLC. In vitro stability was analyzed in the presence of human serum at 37°C which has maximum value of 94 ± 0.5. The biodistribution studies of 99m Tc-CPH were performed in normal and tumor bearing Swiss Webster mice. The high accumulation of 99m Tc-CPH was observed in liver and tumours respectively at 4 hr after injection. Biodistribution results revealed that 99m Tc-CPH may be a potential tumour diagnostic agent simultaneously with chemotherapy.

Radiolabeling, quality control, and biological characterization of 177 Lu-labeled kanamycin.

Kanamycin is an antibiotic, isolated from Streptomyces kanamyceticus, which is used to treat serious bacterial infections. The fact that the present radioligand 99m Tc-kanamycin used for diagnosis is short-lived, raised a need to label and study kanamycin with one of the most important beta (ß) radiation emitting isotope 177 Lu. Labeling yield of 177 Lu-kanamycin was confirmed by different chromatography techniques such as paper chromatography, TLC, HPLC. Several experiments were performed to optimize labeling with changing reaction conditions such as pH, temperature, amount of ligand, and reaction time. In vitro stability analysis was performed incubation with human serum. Electrophoresis analysis was also conducted to determine the charge on 177 Lu-kanamycin. The biodistribution and scintigraphy were performed in normal mice and rabbit, respectively, at different time intervals of postinjection. 177 Lu-kanamycin was prepared with very high yield (~100%), with excellent stability in vivo and in vitro (>99% 6 hr postprep.), at pH 7. Maximum labeling was achieved at less reaction time (15 min), with maximum conjugation of the ligand (12.5 mg) with 177 Lu. Electrophoresis analysis showed net neutral charge. The radioligand showed rapid clearance from body in biodistribution and scintigraphy studies. The preparation 177 Lu-kanamycin could be used as a radio-pharmaceutical for infection imaging purpose, especially when transporting the radioligand to long-range distances.

Preparation, biodistribution and scintigraphic evaluation of (99m)Tc-lincomycin.

A complex of lincomycin was synthesized with technetium-99m. The synthesis was carried out by using SnCl2.2H2O as reducing agent and ascorbic acid as stabilizer. The effect of various parameters such as amount of ligand/reducing agent, pH value and reaction time on radio labeling process was studied. The characterization of the (99m)Tc-Lincomycin was performed by HPLC and electrophoresis Biodistribution studies were carried out by analyzing the model of bacterial infectious rats (Sprague-Dawley). The uptake of infectious lesions at different time interval was also studied by using scintigraphic technique. The complex showed effective target to non-target ratio for various inflammatory or infectious lesions. The (99m)Tc-Lincomycin effective binding to living bacteria and could be used successfully as an infection imaging agent.

PATTERN OF CONSANGUINITY AND INBREEDING COEFFICIENT IN SARGODHA DISTRICT, PUNJAB, PAKISTAN.

Consanguinity is widespread in Pakistan. The majority of studies on consanguinity in Pakistan have been carried out in urban metropolitan areas, and data on rural populations are scarce. The present cross-sectional study was conducted in Sargodha district, upper Punjab, Pakistan where the majority of the population reside in rural areas. A random sample of 1800 married females belonging to six tehsils of Sargodha district was obtained and differentials in consanguinity rates and inbreeding coefficient (F) were investigated. The consanguinity rate was calculated to be 56.72% and the inbreeding coefficient was 0.0348. First cousin unions had the highest representation (49.11% of all marriages), and marriages up to distantly related/Biradari constituted 67.94% of all marriages. Among the six tehsils, consanguinity rates ranged from 50.38% in Bhalwal to 62.88% in Sillanwali. A high rate of consanguinity was observed in subjects speaking the Punjabi language, those with self-arranged/arranged-love marriages and those engaged in professional jobs. With respect to the occupation of husbands the highest consanguinity rate was found among landowners (77.59%; F=0.0539) and businessmen (62.62%; F=0.0377). However, consanguinity did not appear to be associated with rural/urban origin or literacy level. The data showed a wide variation in consanguinity rate and inbreeding coefficient across socio-demographic strata in the Sargodha district population. A comparison of Sargodha with other populations of Punjab also showed regional heterogeneity in the pattern of consanguinity, warranting further studies.

Preparation, biodistribution, and scintigraphic evaluation of (99m)Tc-clindamycin: an infection imaging agent.

Bacterial infection is found to be the cause of death throughout the world. Nuclear medicine imaging with the help of radiopharmaceuticals has great potential for treating infections. In the present work, clindamycin, a lincosamide antibiotic, was labeled with technetium-99 m (~380 MBq). Clindamycin has been proven to be efficient for treating serious infections caused by bacteria such as Staphylococcus aureus. Quality control, characterization, biodistribution, and scintigraphy of radiolabeled clindamycin were done, and labeling efficiency was determined by ascending paper chromatography. More than 95 % labeling efficiency with technetium-99 m ((99m)Tc) was achieved at pH 6-7 while using 2.5-3 µg SnCl2 · H2O as a reducing agent and 100 µg of ligand at room temperature. The characterization of the compound was performed by using electrophoresis, HPLC and shake flask assay. Electrophoresis indicates the neutral behavior of (99m)Tc-clindamycin. HPLC analysis confirms the single specie of the labeled compound, while shake flask assay confirms high lipophilicity. The biodistribution studies of (99m)Tc-clindamycin were performed Sprague Dawley rats bearing bacterial infection. Scintigraphy and biodistribution studies showed a high uptake of (99m)Tc-clindamycin in the liver, heart, lung, and stomach as well as at S. aureus-infected sites in rabbits.

6-(1-Adamant-yl)-3-(2-chloro-phen-yl)-1,2,4-triazolo[3,4-b][1,3,4]thia-diazole.

In the title compound, C(19)H(19)ClN(4)S, the 2-chloro-phenyl and [1,2,4]triazolo[3,4-b] [1,3,4]thia-diazole fragments (r.m.s. deviations of 0.015 and 0.017 Å, respectively) are oriented at a dihedral angle of 55.76 (6)°. The adamantane group exhibits extensive rotational disorder about the single C-C bond to the thia-diazole ring, which was modelled as occupying four orientations each with 0.25 occupancy. In the crystal, the chloro-phenyl rings exhibit π-π stacking inter-actions with centroid-centroid distances of 3.9526 (18) Å.