Radiolabeling, biological distribution, docking and ADME studies of 99mTc-Ros as a promising natural tumor tracer

Dina M El-Sharawy; S I Khater; Marwa S El Refaye; Hossam M Hassan; Asmaa M AboulMagd; Mahmmoud A Aboseada

doi:10.1016/j.apradiso.2022.110196

Radiolabeling, biological distribution, docking and ADME studies of ^99mTc-Ros as a promising natural tumor tracer

Appl Radiat Isot. 2022 Jun:184:110196. doi: 10.1016/j.apradiso.2022.110196. Epub 2022 Mar 30.

Authors

Dina M El-Sharawy¹, S I Khater², Marwa S El Refaye², Hossam M Hassan³, Asmaa M AboulMagd⁴, Mahmmoud A Aboseada⁵

Affiliations

¹ Labeled Compound Department,Hot Lab.Center, Egyptian Atomic Energy Authority, 13759, Cairo, Egypt; Cyclotron Project, Nuclear Research Center, Cairo Egypt, Egyptian Atomic Energy Authority (EAEA), 13759, Cairo, Egypt. Electronic address: dina.sharawy@nub.edu.eg.
² Cyclotron Project, Nuclear Research Center, Cairo Egypt, Egyptian Atomic Energy Authority (EAEA), 13759, Cairo, Egypt; Radioactive Isotopes and Generators Department, Hot Lab. Center, Egyptian Atomic Energy Authority (EAEA), 13759, Cairo, Egypt.
³ Department of Pharmacognosy, Faculty of Pharmacy, Nahda University, Beni-Suef, 62513, Egypt; Department of Pharmacognosy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, 62511, Egypt.
⁴ Pharmaceutical Chemistry Department, Faculty of Pharmacy, Nahda University, Beni Suef, Egypt.
⁵ Department of Pharmacognosy, Faculty of Pharmacy, Nahda University, Beni-Suef, 62513, Egypt.

PMID: 35390625
DOI: 10.1016/j.apradiso.2022.110196

Abstract

Rosmarinic acid (Ros) is one of phenolic metabolites with powerful potency as an anticancer agent, with different mechanisms to diminish the cancer cells. This current study represents radiolabeling of Ros with ^99mTc using SnCl₂ in pH4 for 15 min at 60 °C, The yield up to 92.2%. Biological evaluation in normal and cancer mice revealed the localization of the tracer in tumor tissue. Furthermore, docking and ADME (Absorption, Distribution, Metabolism, and Excretion) studies were performed, The resulted data clarifies the use of Ros as a promissing natural tracer.

Keywords: ADME; Molecular docking; Radiolabeling; Rosmarinic acid.

MeSH terms

Animals
Cinnamates
Depsides*
Mice
Neoplasms*
Rosmarinic Acid
Technetium
Tissue Distribution

Substances

Cinnamates
Depsides
Technetium