About the Author(s)


J. Ackermann Email
Department of Chemistry, University of Johannesburg, South Africa

Radiochemistry, Department of Applied Chemistry, Nesca, South African Nuclear Energy Corporation Limited, South Africa

D. Jansen
Radiochemistry, Department of Applied Chemistry, Nesca, South African Nuclear Energy Corporation Limited, South Africa

N. Jarvis
Radiochemistry, Department of Applied Chemistry, Nesca, South African Nuclear Energy Corporation Limited, South Africa

A. Muller
Department of Chemistry, University of Johannesburg, South Africa

J-R. Zeevaart
Radiochemistry, Department of Applied Chemistry, Nesca, South African Nuclear Energy Corporation Limited, South Africa

Citation


Ackermann, J., Jansen, D., Jarvis, N., Muller, A. & Zeevaart, J-R., 2016, ‘223Ra calix[4]areen-krooneterverbindings met teenligaampies as radiofarmaseutiese middels vir die behandeling van kanker’, Suid-Afrikaanse Tydskrif vir Natuurwetenskap en Tegnologie 35(1), a1406. http://dx.doi.org/10.4102/satnt.v35i1.1406

Note: A selection of conference proceedings: Student Symposium in Science, 29–30 October 2015, University of the Free State, South Africa. Organising committee: Mr Rudi Pretorius and Ms Andrea Lombard (Department of Geography, University of South Africa); Dr Hertzog Bisset (South African Nuclear Energy Corporation (NECSA); Dr Ernie Langner and Prof Jeanet Conradie (Department of Chemistry, University of the Free State).

Referaatopsomming

223Ra calix[4]areen-krooneterverbindings met teenligaampies as radiofarmaseutiese middels vir die behandeling van kanker

J. Ackermann, D. Jansen, N. Jarvis, A. Muller, J-R. Zeevaart

Copyright: © 2016. The Author(s). Licensee: AOSIS.
This is an Open Access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

223Ra calix[4]arene-crown ether antibody conjugates as potential radiopharmaceuticals for the treatment of cancer. Radium possesses a self-directing capability to accumulate in bones for treatment of bone cancer. The treatment of other cancers requires a method that will shield the Ra from bone absorption and direct it towards specific cancers. This study investigates the probability of tailored Ra/Ba-calixarene systems for such purposes.

Radioïmmunoterapie (RIT) is ’n metode van kankerbehandeling wat gebruik maak van ’n kankerspesifieke teenliggaampie, gemerk met ’n gekonjugeerde radio-isotoop. Aangesien RIT geteiken is, kan ’n hoë dosis bestraling toegedien word op kankerselle terwyl normale selle gespaar word.

223Ra het die gepaste radiochemiese en radiobiologiese eienskappe om effektief te wees in die gebruik van geteikende radioterapie. In biologiese stelsels boots radium die gedrag van kalsium na en hoop dit dus in die skelet op. Dit is hierdie eienskap wat gelei het tot die gebruik van 223Ra-dichloried in die behandeling van beenmetastases. Dit is onlangs as radioterapeutiese middel goedgekeur en word tans vervaardig onder die handelsnaam Xofigo (Kim & Brechbiel 2012). Radium se natuurlike affiniteit vir been is ook ’n nadeel, aangesien dit nie gebruik kan word in die behandeling van ander kankertipes nie. Die suksesvolle gebruik van radium in die behandeling van kanker verg, anders as met beenkanker, ’n metode wat radium teen die chemiese interaksies in die liggaam beskerm en op spesifieke kankerselle sal rig, en dus opeenhoping in die bene sal vermy.

Calix[4]areen-krooneterverbindings het die vermoë om radium selektief te bind in verskeie toepassings, byvoorbeeld in radioterapie en die ekstraksie van radium uit industriële afval (Chen et al. 1999; Van Leeuwen et al. 2005a, 2005b). Die doel van hierdie studie is om die stabiliteit van Ba/Ra-komplekse met die calix[4]arene-krooneterverbindings onder fisiologiese toestande te toets en hierdie verbindings aan nuut ontwikkelde teenliggaampies te koppel om spesifieke tipes kanker te teiken. Omrede alle isotope van radium radioaktief is, behels die aanvanklike studies die gebruik van barium om die hantering van die verbindings in standaardlaboratoriums te vergemaklik. Die chemiese eienskappe van barium en radium stem grootliks ooreen, en dus kan enige positiewe evalueringsresultate met barium oorgedra word na die kompleksingreaksies met radium.

Literatuurverwysings

Chen, X., Ji, M., Fisher, D.R. & Wai, C.M., (1999), ‘Ionizable calixarene-crown ethers with high selectivity for radium over light alkaline earth metal ions’, Inorganic chemistry, 38(23), 5449–5452. http://dx.doi.org/10.1021/ic990135

Kim, Y. & Brechbiel, M.W., (2012), ‘An overview of targeted alpha therapy’, Tumor biology, 33(3), 573–590. http://dx.doi.org/10.1007/s13277-011-0286-y

Van Leeuwen, F.W., Beijleveld, H., Miermans, C.J., Huskens, J., Verboom, W. & Reinhoudt, D.N., (2005a), ‘Ionizable (thia) calix[4]crowns as highly selective 226Ra2 ionophores’, Analytical chemistry, 77(14), 4611–4617. http://dx.doi.org/10.1021/ac050524n

Van Leeuwen, F.W., Beijleveld, H., Velders, A.H., Huskens, J., Verboom, W. & Reinhoudt, D.N., (2005b), ‘Thiacalix [4] arene derivatives as radium ionophores: A study on the requirements for Ra2 extraction’, Organic & Biomolecular Chemistry, 3(10), 1993–2001. http://dx.doi.org/10.1039/b501587a