Molecular docking and preliminary bioevaluation of 99m Tc-Thiadiazuron as a novel potential agent for cervical cancer im
- PDF / 2,682,152 Bytes
- 7 Pages / 595.276 x 790.866 pts Page_size
- 80 Downloads / 148 Views
Molecular docking and preliminary bioevaluation of 99mTcThiadiazuron as a novel potential agent for cervical cancer imaging Hesham A. Shamsel‑Din1,2 · Mohamed A. Gizawy1,2 · Gamal Abdelaziz1 Received: 25 July 2020 / Accepted: 10 September 2020 © Akadémiai Kiadó, Budapest, Hungary 2020
Abstract Thidiazuron (TDZ) was reported to possess anti-cancer activity against Human cervical carcinoma cell line, so that this study has been conducted for the radiolabeling of TDZ with Technetium-99m. The conditions of the radiolabeling process were optimized and a high radiochemical yield of 93.1 ± 0.35% has been obtained. Molecular docking study illustrated that [99mTc]technetium bisthiadiazuron (99mTc-TDZ) complex has the ability to bind with Caspase-3 protein that over expressed in cancers. Its in-vivo biodistribution on solid tumor bearing mice showed comparatively high T/NT ratio of 6.87 ± 0.14 at 60 min post injection. These promising characteristics make our new designed labeled conjugate a very suitable candidate for molecular imaging of solid tumors, particularly in the cervix. Keywords Thidiazuron · Technetium-99m · Molecular docking · Cervical cancer · Sodium dithionite
Introduction Cervical cancer is one of the world’s most common gynecological diseases. It’s rated to be the fourth prevalent cancer in women after breast, colorectal, and lung cancers. On the other hand, it’s considered the second widespread carcinoma among females in underdeveloped countries. [1, 2] While cervical cancer mortality decreased, it remains one of the leading causes of cancer death [3]. In order to help assess tumor distribution and metastatic cancer, diagnostic imaging during primary diagnostics is very important and highly recommended. So that, the National Cancer Comprehensive Network (NCCN) guidelines prescribe the use of pelvic magnetic resonance imaging (MRI), chest radiography and/or chest/abdominal/ pelvic computed tomography (CT), or whole-body positron emission tomography-CT (PET-CT) in the primary diagnostic work-up [4]. Radiography is one of the most successful methods used to diagnose many cancers in their early * Hesham A. Shamsel‑Din [email protected] 1
Labeled Compounds Department, Hot Labs Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt
Radioisotopes Production Facility (RPF), Egyptian Second Research Reactor (ETRR‑2), Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt
2
stages. Many challenges face researchers upon developing new diagnostic tool for tumor radio-imaging. Among these; (a) selectivity, (b) safety and (c) clearance from the body. Thiadiazole and its products are pharmacologically important scaffolds due to their broad and potent anticancer activity against different cancer cell lines including: lung cancer (HOP 92), colon cancer (HCC-2998), prostate cancer (PC-3) and cervical cancer (Hela) [5–7]. Thidiazuron (TDZ); chemically known as 1-phenyl-3-(1, 2, 3-thiadiazol5-yl) urea (Fig. 1) is one of the most important thiadiazole derivative. It’s a synthetic plant hormone and it has
Data Loading...
