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25 April 2022 | Story Elsabé Brits
Andre Roodt and Alice Brink
Prof Andreas Roodt and Prof Alice Brink are two of the inventors of the ‘Multinuclear complexes and their preparation patent.

According to the World Health Organisation (WHO), cancer is a leading cause of death worldwide, accounting for nearly 10 million deaths in 2020, or nearly one in six. The most common cancers are breast, lung, colon, rectum, and prostate cancers. There is a constant need to provide methods to diagnose and treat cancer-related tumours.  Current research strategies focus on eliminating cancer cells with the minimum damage to surrounding healthy cells.

A limitation of current technologies is that they are mostly based on the separate identification of cancer (diagnostic), followed by treatment (therapy) using chemotherapy and/or radiotherapy. To fit both needs at the same time and with similar or identical compounds, the principle of theranostic medicine was identified. This concept employs both diagnosing (by imaging) cancer and delivering therapy (treatment) simultaneously, which has been receiving increased attention internationally.

Collaborating with the University of Zurich
A University of the Free State (UFS) team, together with a team from the University of Zürich, conducted exciting research in this area and filed a patent titled ‘Multinuclear complexes and their preparation’. The patent was granted in South Africa and by the European Patent Office. It is being validated in selected European countries. The patent is pending in the USA, Japan, Hong Kong, and India. The inventors from the UFS are Prof Andreas Roodt, Prof Alice Brink, Dr Pennie Mokolokolo, and Dr Vincent Dumisani Kama. The approach that their technology takes is to enable the synthesis of a multinuclear compound/s, which may contain different pre-selected radioisotopes, to allow both imaging and therapy to the cancer site(s) with one and the same metal-organic complex.

So far, high-yield production of compounds has been successfully innovated, which contain both an imaging (in particular the widely utilised imaging isotope Technetium-99m) and therapeutic (typically the therapeutic isotope Rhenium-186) radioactive isotope(s), optionally carrying an additional cytotoxic agent. (Chemotherapy uses anti-cancer [cytotoxic] drugs to destroy cancer cells.)

Nuclear medicine technologies
In the next phase of the research, a lead compound portfolio of four to five model pharmaceuticals containing these metal nuclides with appropriate directing groups to target cancer sites will be designed and constructed. A number of these entities are known and can be introduced through different techniques. These will then undergo full characterisation and efficacy evaluation in biological models (in vitro), followed by extensive animal and human trials.

The technology will be delivered as a product or service in the way that current nuclear medicine technologies are delivered.

The fact that this product(s) contains both imaging and therapeutic radionuclides or cytotoxic modalities, enables detailed tracking of the pharmaceutical and monitoring of the tumours' response to the therapy. Not directly related to the patent, but an asset to it, is the fact that the incorporation of rhenium with a high atomic number (Z = 75) opens the additional opportunity to utilise the multinuclear compounds also as radiosensitisers. Synergistic effects, enhancing the therapeutic efficacy, can thus be expected in combination with radiotherapy.

The UFS would like to partner with a pharmaceutical company working in the field of nuclear medicine to commercialise this technology. Interested parties can contact Ravini Moodley at MoodleyR5@ufs.ac.za

News Archive

New world-class Chemistry facilities at UFS
2011-11-22

 

A world-class research centre was introduced on Friday 18 November 2011 when the new Chemistry building on the Bloemfontein Campus of the University of the Free State (UFS) was officially opened.
The upgrading of the building, which has taken place over a period of five years, is the UFS’s largest single financial investment in a long time. The building itself has been renovated at a cost of R60 million and, together with the new equipment acquired, the total investment exceeds R110 million. The university has provided the major part of this, with valuable contributions from Sasol and the South African Research Foundation (NRF), which each contributed more than R20 million for different facets and projects.
The senior management of Sasol, NECSA (The South African Nuclear Energy Corporation), PETLabs Pharmaceuticals, and visitors from Sweden attended the opening.

Prof. Andreas Roodt, Head of the Department of Chemistry, states the department’s specialist research areas includes X-ray crystallography, electrochemistry, synthesis of new molecules, the development of new methods to determine rare elements, water purification, as well as the measurement of energy and temperatures responsible for phase changes in molecules, the development of agents to detect cancer and other defects in the body, and many more.

“We have top expertise in various fields, with some of the best equipment and currently competing with the best laboratories in the world. We have collaborative agreements with more than twenty national and international chemistry research groups of note.

“Currently we are providing inputs about technical aspects of the acid mine water in Johannesburg and vicinity, as well as the fracking in the Karoo in order to release shale gas.”

New equipment installed during the upgrading action comprises:

  • X-ray diffractometers (R5 million) for crystal research. Crystals with unknown compounds are researched on an X-ray diffractometer, which determines the distances in angstroms (1 angstrom is a ten-billionth of a metre) and corners between atoms, as well as the arrangement of the atoms in the crystal, and the precise composition of the molecules in the crystal.
  • Differential scanning calorimeter (DSC) for thermographic analyses (R4 million). Heat transfer and the accompanying changes, as in volcanoes, and catalytic reactions for new motor petrol are researched. Temperature changes, coupled with the phase switchover of fluid crystals (liquid crystals -watches, TV screens) of solid matter to fluids, are measured.
  • Nuclear-magnetic resonance (NMR: Bruker 600 MHz; R12 million, one of the most advanced systems in Africa). A NMR apparatus is closely linked with the apparatus for magnetic resonance imaging, which is commonly used in hospitals. NMR is also used to determine the structure of unknown compounds, as well as the purity of the sample. Important structural characteristics of molecules can also be identified, which is extremely important if this molecule is to be used as medication, as well as to predict any possible side effects of it.
  • High-performance Computing Centre (HPC, R5 million). The UFS’ HPC consists of approximately 900 computer cores (equal to 900 ordinary personal computers) encapsulated in one compact system handling calculations at a billion-datapoint level It is used to calculate the geometry and spatial arrangements, energy and characteristics of molecules. The bigger the molecule that is worked with, the more powerful the computers must be doing the calculations. Computing chemistry is particularly useful to calculate molecular characteristics in the absence of X-ray crystallographic or other structural information. Some reactions are so quick that the intermediary products cannot be characterised and computing chemistry is of invaluable value in that case.
  • Catalytic and high-pressure equipment (R6 million; some of the most advanced equipment in the world). The pressures reached (in comparison with those in car tyres) are in gases (100 times bigger) and in fluids (1 500 times) in order to study very special reactions. The research is undertaken, some of which are in collaboration with Sasol, to develop new petrol and petrol additives and add value to local chemicals.
  • Reaction speed equipment (Kinetics: R5 million; some of the most advanced equipment in the world). The tempo and reactions can be studied in the ultraviolet, visible and infrared area at millisecond level; if combined with the NMR, up to a microsecond level (one millionth of a second.

Typical reactions are, for example, the human respiratory system, the absorption of agents in the brain, decomposition of nanomaterials and protein, acid and basis polymerisation reactions (shaping of water-bottle plastic) and many more.

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