Infectious diseases are a major cause of threat throughout the world which may have concern with microorganisms, specifically bacteria. Various antibiotics are synthesized and used against infectious diseases to mimic the death rate. The tetracyclines are a broad spectrum antibiotics discovered as natural products with exclusive biological and chemical properties against both gram-positive/negative bacteria. Many of members of this family also possess some non-antibacterial properties such as anti-inflammatory, immunosuppressant and inhibition of lipase. Various studies reveals structure activity relationship of the tetracycline family, which shows the bioactivity, strength and selectivity to biological target, specifically depends upon modification of lower and upper peripheral zones of tetracycline skeleton. The broad spectrum antibacterial activities of tetracyclines drag the attention toward labeling of tetracycline with radioisotopes for imaging of infectious lesions. For labeling purposes, optimization conditions, characterization, in-vivo and in-vitro studies are essential parameters to be studied. In clinical practice, tetracycline and three of its analogs were labeled with technetium-99m ( Tc-99m) used as diagnostic agents for renal and myocardial abnormalities as well as for inflammatory disorders Graphical Abstract.
The aim of this study is to develop (177) Lu-5-Flourouracil as a potential cancer therapeutic radiopharmaceutical. 5-Flourouracil (5-FU) is widely accepted as an anticancer drug of broad spectrum fame. The labeling of 5-FU was carried out at different set of experimental conditions using high specific activity of (177) LuCl3 . The optimum conditions for maximum radiochemical yield was set: 5-FU (5 mg), (177) LuCl3 (185 MBq), diethylenetriaminepentaacetic acid (10 µg), reaction volume (2 mL), pH (5.5), temperature (80°C), and reaction time (20 min). The radiochemical labeling was assessed with Whatman No. 2 paper, instant thin layer chromatographic, and radio-HPLC, which revealed >94% labeling results with sufficient stability up to 6 h. Serum stability study also showed (177) Lu-5-FU promising stability. Biodistribution study in normal rats and rabbits showed liver, stomach, kidney, and heart as area of increased tracer accumulation just after injection, which decreased to 1.4%, 0.4%, 0.2%, and 0.39% ID/g, respectively, after 72 h. Glomerular filtration rate and cytotoxicity study results of (177) Lu-5-FU showed it had no adverse effect on renal function and nontoxic to blood cells. The promising characteristics of (177) Lu-5-FU, that is, clever elimination from kidney and nontoxic nature toward blood cells make it the radiopharmaceutical for further testing in patients for therapeutic purposes.
Roxithromycin is a second‐generation macrolide antibiotic derived from erythromycin. In the current study, roxithromycin (ROX) was successfully labeled with technetium‐99m for early diagnosis of bacterial infection and discrimination between septic and aseptic inflammation. The highest radiochemical purity of ≥95% was achieved by investigating different labeling parameters such as pH, ligand/reducing agent concentration, temperature, and amount of stabilizing agent. For this purpose, 0.3–0.5 mg ligand, 2–6 μg SnCl2·2H2O as a reducing agent at basic pH (8–10 pH) and 2 mg mannitol used as a stabilizing agent, in the end, 370 MBq 99mTc added into the reaction vials and incubated for a wide range of temperature (−4 to 65°C). The percent radiochemical purity of 99mTc‐roxithromycin was assessed with the help of the radio‐thin‐layer chromatography technique. The characterization studies were carried out using electrophoresis and Radio‐HPLC techniques as well as saline stability and serum stability studies were also performed. Furthermore, biodistribution study was also performed in an inflamed animal model to discriminate between septic (heat‐killed Staphylococcus aureus) and aseptic (turpentine oil) inflammatory lesions. The results were elaborated that 99mTc‐roxithromycin (99mTc‐ROX) was clearly bounded at the septic inflammation site (T/NT ratio of 7.08 ± 1.14) at 30 min postadministration, and maximum accumulation was seen in heart, lungs, liver, stomach, kidneys, and intestine. The results were suggested that 99mTc‐ROX might be used to discriminate between septic and aseptic inflammatory lesions at an early stage.
Objective: To see the association of endometriosis with other uterine conditions in our setup. Study Design: Descriptive Retrospective study. Setting: Private Lab in Faisalabad. Period: January 2010 to December 2019. Material & Methods: A total of 297 cases were evaluated in this study. We have included all endometriosis cases with associated other conditions of the uterus. In this study paraffin blocks and previous slides along with clinical data were analyzed according to the standard protocols. All the data including age, location of endometriosis, and association with other uterine conditions were noted and reported as percentages. Results: In this study, we analyzed 297 endometriosis cases, received during ten years. The age group ranges from 15 years to 75 years. The most common age group ranges from 26-30 years, 87(29%) cases, and the least commonly affected group was 71-75 years, only one case. The most common site of endometriosis was in the ovaries, 169(57%) cases. The most common associated other condition was benign tumor leiomyoma, 65(43%) cases while only one case of endometrial carcinoma was noted. Conclusion: This study concludes that ovarian endometriosis is the most common location and there is a strong association with another co-existing benign tumor such as leiomyoma. This signifies the possibility of common risk factors such as hyperestrogenism. Thus it is important to be aware of the possibility of co-existence of other conditions so that they can be treated at once in a single surgery.
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