Preparation of 125I-celecoxib with high purity as a possible tumor agent

被引:36
作者
El-Azony, K. M. [1 ]
机构
[1] Atom Energy Author, Hot Lab Ctr, Radioact Isotope & Generators Dept, Cairo, Egypt
关键词
Radioiodination; Celecoxib; Labeling; Tumor agent; CYCLOOXYGENASE-2; INHIBITORS; COX-2; CELECOXIB; OSTEOARTHRITIS; APOPTOSIS; ARTHRITIS;
D O I
10.1007/s10967-010-0583-8
中图分类号
O65 [分析化学];
学科分类号
070302 ; 081704 ;
摘要
A preparation of I-125-celecoxib is carried out via an electrophilic substitution reaction. The reaction parameters studied were celecoxib concentration, reaction temperature, pH of the reaction mixture and kinds of oxidizing agents in order to obtain a high radiochemical yield of the I-125-celecoxib. Using 3.7 MBq of (NaI)-I-125, 150 mu g (3.9 mM (mmol/L)) of celecoxib, and 1.6 mM (mmol/L) of chloramine-T (CAT) as oxidant at pH 4 and 60 A degrees C for 15 min a maximum radiochemical yield of I-125-celecoxib (65%) was obtained. The labeled compound was separated and purified by means of high pressure liquid chromatography (HPLC). The biological distribution in infected mice indicates the suitability of radioiodinated celecoxib as imaging of tumor.
引用
收藏
页码:315 / 320
页数:6
相关论文
共 23 条
[1]  
Abu-Zeid M, 2000, BIOL PHARM BULL, V23, P195
[2]   A MONTE-CARLO TREATMENT OF THE DECAY OF I-125 [J].
CHARLTON, DE ;
BOOZ, J .
RADIATION RESEARCH, 1981, 87 (01) :10-23
[3]   An investigation of the 125I-radioiodination of colchicine for medical purposes [J].
El-Azony, K. M. ;
El-Mohty, A. A. ;
Killa, H. M. ;
Seddik, U. ;
Khater, S. I. .
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2009, 52 (1-2) :1-5
[4]  
El-Azony K. M., 2004, ARAB J NUCL SCI APPL, V37, P81
[5]  
Geis GS, 1999, J RHEUMATOL, V26, P31
[6]  
Goldstein JL, 2001, AM J GASTROENTEROL, V96, P1019
[7]   Cyclooxygenase-2 (COX-2)-independent anticarcinogenic effects of selective COX-2 inhibitors [J].
Groesch, Sabine ;
Maier, Thorsten Juergen ;
Schiffmann, Susanne ;
Geisslinger, Gerd .
JNCI-JOURNAL OF THE NATIONAL CANCER INSTITUTE, 2006, 98 (11) :736-747
[8]   The cyclooxygenase-2 inhibitor celecoxib induces apoptosis by blocking Akt activation in human prostate cancer cells independently of Bcl-2 [J].
Hsu, AL ;
Ching, TT ;
Wang, DS ;
Song, XQ ;
Rangnekar, VM ;
Chen, CS .
JOURNAL OF BIOLOGICAL CHEMISTRY, 2000, 275 (15) :11397-11403
[9]   RADIOPHARMACEUTICAL PREPARATION OF 3-123-I-ALPHA-METHYLTYROSINE FOR NUCLEAR-MEDICAL APPLICATIONS [J].
KNUST, EJ ;
DUTSCHKA, K ;
MACHULLA, HJ .
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY-LETTERS, 1990, 144 (02) :107-113
[10]  
Koki Alane T, 2002, Cancer Control, V9, P28