Anti-sense oligonucleotide labeled with technetium-99m using hydrazinonictinamide derivative and N-hydroxysuccinimidyl S-acetylmercaptoacetyltriglycline: a comparison of radiochemical behaviors and biological properties.

Aim: To explore and compare the radiochemical behavior and biological property of anti-sense oligonuc-leotide (ASON) labeled with technetium-99m using N-hydroxysuccinimidyl S-acetylmercaptoacetyltriglycline (NHS-MAG(3)) and hydrazinonictinamide derivative (HYNIC).

Methods: After HYNIC and NHS-MAG(3) were synthesized, ASON was labeled with technetium-99m using HYNIC and NHS-MAG(3) as a bifunctional chelator. The in vivo and in vitro stability, binding rates of labeled compounds to serum albumen, biodistribution of (99m)Tc-MAG(3)-ASON and (99m)Tc-HYNIC-ASON in BALB/C mouse and its HT29 tumor cellular uptake were compared.

Targeting radioimmunotherapy of hepatocellular carcinoma with iodine (131I) metuximab injection: clinical phase I/II trials.

Purpose: HAb18G/CD147 is a hepatocellular carcinoma (HCC)-associated antigen. We developed iodine (131I) metuximab injection (Licartin), a novel 131I-labeled HAb18G/CD147-specific monoclonal antibody Fab'2 fragment, and evaluated its safety, pharmacokinetics, and clinical efficacy on HCC in Phase I/II trials.

Methods And Materials: In a Phase I trial, 28 patients were randomly assigned to receive the injection in 9.

[Preparation and biodistribution of VIP-125I-ASON].

Objective: To prepare VIP-125I-ASON and investigate the possibility of using it as an agent for diagnostic imaging and therapy of colon carcinoma.

Methods: The iodination of a 15-base single-stranded antisense oligonucleotide (ASON) complementary to C-myc oncogene mRNA was carried out in the presence of TICl3. The radiolabeled oligonucleotide was complexed with a VIP-polylysine conjugate under certain condition.

Antisense imaging of colon cancer-bearing nude mice with liposome-entrapped 99m-technetium-labeled antisense oligonucleotides of c-myc mRNA.

Aim: To investigate the feasibility for antisense imaging of the colon cancer with liposome-entrapped 99 m-technetium labeled antisense oligonucleotides as tracers.

Methods: Fifteen mer single-stranded aminolinked phosphorothioate antisense oligonucleotides of c-myc mRNA were labeled with 99mTc-pertechnetate, then purified and finally entrapped with liposomes to form the labeling compounds, liposome-entrapped 99mTc-labeled antisense oligonucleotides. The LS-174-T cells (colon of adenocarcinoma cell line) were incubated with the labeling compounds to test the uptake rates of LS-174-T cells.

131I-recombinant human EGF has antitumor effects against MCF-7 human breast cancer xenografts with low levels of EGFR.

This study investigated the inhibitory action of (131)I-recombinant human EGF ((131)I-rhEGF) on MCF-7 human breast cancer tumor development in nude mice. The activity and tumor uptake of (131)I-rhEGF was measured by tissue distribution assay, and its effect on tumor growth was measured by monitoring tumor size after treatment with (131)I-rhEGF. Changes in tumor cell ultrastructure were observed by transmission electron microscopy (TEM), and pathological changes in tumor tissue were observed by light microscopy.

[The radiolabeling property of oligonucleotide with 99mTc using NHS-MAG3 as a chelator].

Objective: To explore the radiolabeling property of oligonucleotide with 99mTc using NHS-MAG3 as a bifunctional chelator.

Methods: Three 15-base single-stranded amine-derivitized oligonucleotides, which were antisense(ASON), sense(SON) and mismatched oligonucleotides(MON) of c-myc oncogene mRNA, were coupled with NHS-MAG3 and labeled with 99mTc. The labeled oligonucleotide was purified by Sephadex G25 column chromatogram, then the stability was evaluated.