Preparation and Biological Evaluation of a [55Co]-2-Acetylpyridine Thiosemicarbazone

JALILIAN, Amir R.; ROWSHANFARZAD, Pejman; AKHLAGHI, Mehdi; SABET, Mahsheed; KAMALI-DEHGHAN, Mohsen; POULADI, Mehrban

doi:10.3797/scipharm.0907-04

Open AccessArticle

Preparation and Biological Evaluation of a [⁵⁵Co]-2-Acetylpyridine Thiosemicarbazone

by

Amir R. JALILIAN

^*,

Pejman ROWSHANFARZAD

,

Mehdi AKHLAGHI

,

Mahsheed SABET

,

Mohsen KAMALI-DEHGHAN

and

Mehrban POULADI

Agricultural, Medical and Industrial Research School (AMIRS), Nuclear Science and Technology Research Institute (NSTRI) Karaj, P.O.Box: 31485-498, Iran

^*

Author to whom correspondence should be addressed.

Sci. Pharm. 2009, 77(3), 567-578; https://doi.org/10.3797/scipharm.0907-04

Submission received: 4 July 2009 / Accepted: 3 August 2009 / Published: 5 August 2009

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Abstract

Due to the anti-proliferative properties of cobalt-thiosemicarbazone complexes, the production of [⁵⁵Co](III)-bis-(2-acetylpyridine thiosemicarbazone) ([⁵⁵Co](III)[APTS]₂) was investigated. Co-55 (T_1/2=17.53 h) was produced by 150 μA irradiation of a natural nickel target by 15 MeV protons. The ⁵⁵Co was separated from the irradiated target material using a two-step method with a radiochemical yield of >95% followed by radionuclidic and chemical purity control. [⁵⁵Co](III)chloride was mixed with 2-acetylpyridine thiosemicarbazone for 30 min at room temperature to yield [⁵⁵Co](III)[APTS]2 (radiochemical purity > 98% shown by RTLC/HPLC). A specific activity of about 10–20 Ci/mmol was obtained. The final solution was diluted in normal saline to 5% ethanolic solution for biological evaluation. The stability of the final product was checked in the absence and presence of human serum at 37°C to 24 h. The partition co-efficient of the final complex at the pH of 7 was 1.00±0.08. A significant tumor accumulation (%ID/g; 3.5%) was observed in tumoral tissue 21 h post injection in fibrosarcoma-bearing mice by biodistribution studies. Co-incidence imaging also demonstrated tumor uptake from 21–35 h however at 35 h tumor uptake is more specific and significant.

Keywords: Cobalt-55; Thiosemicarbazone; Biodistribution; Tumor imaging; Co-incidence; Fibrosarcoma

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MDPI and ACS Style

JALILIAN, A.R.; ROWSHANFARZAD, P.; AKHLAGHI, M.; SABET, M.; KAMALI-DEHGHAN, M.; POULADI, M. Preparation and Biological Evaluation of a [⁵⁵Co]-2-Acetylpyridine Thiosemicarbazone. Sci. Pharm. 2009, 77, 567-578. https://doi.org/10.3797/scipharm.0907-04

AMA Style

JALILIAN AR, ROWSHANFARZAD P, AKHLAGHI M, SABET M, KAMALI-DEHGHAN M, POULADI M. Preparation and Biological Evaluation of a [⁵⁵Co]-2-Acetylpyridine Thiosemicarbazone. Scientia Pharmaceutica. 2009; 77(3):567-578. https://doi.org/10.3797/scipharm.0907-04

Chicago/Turabian Style

JALILIAN, Amir R., Pejman ROWSHANFARZAD, Mehdi AKHLAGHI, Mahsheed SABET, Mohsen KAMALI-DEHGHAN, and Mehrban POULADI. 2009. "Preparation and Biological Evaluation of a [⁵⁵Co]-2-Acetylpyridine Thiosemicarbazone" Scientia Pharmaceutica 77, no. 3: 567-578. https://doi.org/10.3797/scipharm.0907-04

APA Style

JALILIAN, A. R., ROWSHANFARZAD, P., AKHLAGHI, M., SABET, M., KAMALI-DEHGHAN, M., & POULADI, M. (2009). Preparation and Biological Evaluation of a [⁵⁵Co]-2-Acetylpyridine Thiosemicarbazone. Scientia Pharmaceutica, 77(3), 567-578. https://doi.org/10.3797/scipharm.0907-04

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Preparation and Biological Evaluation of a [⁵⁵Co]-2-Acetylpyridine Thiosemicarbazone

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