New frontier radioiodinated probe based on in silico resveratrol repositioning for microtubules dynamic targeting
| Autor: | Ashgan F. Mahmoud, Mohamed H. Aboumanei, Walaa Hamada Abd-Allah, Mohamed M. Swidan, Tamer M. Sakr |
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| Rok vydání: | 2022 |
| Předmět: | |
| Zdroj: | International Journal of Radiation Biology. 99:281-291 |
| ISSN: | 1362-3095 0955-3002 |
| Popis: | As the 'Resveratrol was radiolabeled with radioactive iodine where the radioiodination efficiency was enlightened and the computational approaches were employed to investigate the affinity and specificity with tubulins. Furthermore, the in-vivo distribution and pharmacokinetic studies in normal and tumor induced mice were investigated.The maximum radioiodination yield (94.6 ± 1.66) was achieved at optimum preparation parameters stated as 100 μg/mL of oxidizing agent, 100 μg/ml of resveratrol, reaction time of 30 min and reaction pH 5. The in silico studies showed that di-iodinated resveratrol (compound 6) exhibited the best binding score (-34.46) and interaction with the β-tubulin binding site. The in vivo distribution in tumor models revealed a significant accumulation (4.02% ID/g) in tumor lesion at 60 min p.i. The rate of drug elimination demonstrated a mono-exponential decline of radioactivity versus time in the blood.Radioiodinated resveratrol revealed good microtubules targeting which render it as a novel theranostic probe for cancer management. |
| Databáze: | OpenAIRE |
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