Lethality Assay of Radiopharmaceutical bis-Thiosemicarbazones Using Brine Shrimp (Artemia salina) Test Toxicity of bis-thiosemicarbazones
Iranian Journal of Pharmaceutical Sciences,
Vol. 8 No. 3 (2012),
1 July 2012
,
Page 197-201
https://doi.org/10.22037/ijps.v8.40942
Abstract
In the present study, aqueous solutions of some copper-complexing ligands were screened for their cytotoxicity using brine shrimp lethality test. Among the ligands tested, diacetyl-bis(N4- methylthiosemicarbazones) (ATSM) proved to be the most safe and non-toxic compound (2% lethality at 10 ppm), while pyruvaldehyde Bis(N4-methyl)thiosemicarbazone (PTSM) was shown to possess low toxicity (7% lethality at 10 ppm) and glyoxal-bis-thiosemicarbazone (GTS) proved to be a toxic compound even at 1 ppm (20% lethality). An interesting structure-toxicity relationship was observed for the ligands based on their water solubility leading to more toxicity which can be related to polysaccharide crustae of the shrimps. Considering the 1-10 ppm to be the maximum possible concentration of the ligands in the final
pharmaceutical samples, the safety of these ligands are ATSM>PTSM>GTS.
- Brine shrimp
- Cytotoxicity
- Radiopharmaceutical
- bis-Thiosemicar bazones
How to Cite
References
[2] Tadamura E, Tamaki N, Okazawa H, Fujibayashi Y, Kudoh T, Yonokura Y. Generator-produced copper-62-PTSM as a myocardial PET perfusion tracer compared with nitrogen-13-ammonia. J Nucl Med 1996; 37: 729-33.
[3] Fujibayashi Y, Cutler CS, Anderson CJ, McCarthy DW, Jones LA, Sharp T, Yonekura Y, Welch MJ. Comparative studies of Cu-64-ATSM and C-11-acetate in an acute myocardial infarction model:ex vivo imaging of hypoxia in rats. Nucl Med Biol 1999; 26: 117-21.
[4] Fujibayashi Y, Taniuchi H, Yonekura Y, Ohtani H, Konishi J, Yokoyama A. Copper-62-ATSM: a new hypoxia imaging agent with high membrane permeability and low redox potential. J Nucl Med 1997; 38: 1155-60.
[5] Höckel M, Knoop C, Schlenger K, Vorndran B, Baussmann E, Mitze M, Knapstein PG, Vaupel. Intratumoral pO2 predicts survival in advanced cancer of the uterine cervix. Radiother Oncol 1993; 26: 45-50.
[6] Michael AS, Thompson CG, Abramovitz M. Artemia salina as a test organism for a bioassay. Science 1956; 123: 464.
[7] Vanhaecke P, Persoone G, Claus C, Sorgeloos P. Proposal for a short-term toxicity test with Artemia nauplii. Ecotoxicol Environment Safety 1981; 5:382-7.
[8] McLaughlin JL, Chang CJ, Smith DL. Bench-top bioassays for the discovery of bioactive natural products: an update. In: Studies in Natural Products Chemistry. Rhaman, A.U. (Ed.), Elsevier, 1991; pp. 383-409.
[9] Jalilian AR, Sattari S, Bineshmarvasti M, Shafiee A, Daneshtalab M. Synthesis and in vitro antifungal and cytotoxicity evaluation of thiazolo-4H-1,2,4-triazoles and 1,2,3-thiadiazolo-4H-1,2,4-triazoles. Archiv Der Pharmazie 2000; 333:347-354.
[10] Gingras BA, Suprunchuk T, Bayley CH. The preparation of some thiosemicarbazones and their copper complexes. Can J Chem 1956; 40: 1053-7.
[11] Jalilian AR, Rowshanfarzad P, Sabet M.Preparation of [61Cu]Pyruvaldehyde-bis (N4-methylthiosemicarbazone) complex as a possible PET radiopharmaceutical. Radiochim Acta 2006;94: 113-7.
[12] Jalilian AR, Sabet M, Rowshanfarzad P, Kamalidehghan M, Akhlaghi M, Mirzaii M. Optimization of the production of [61Cu]Diacetyl-bis(N4-methylthiosemicarbazone) for PET studies. J Radioanal Nucl Chem 2006; 269: 147-54.
- Abstract Viewed: 293 times
- IJPS_Volume 8_Issue 3_Pages 197-201 Downloaded: 218 times