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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

What do diamonds, chocolates, bugs and almost 30 Nobel Prizes have in common? Crystallography
2014-10-15

 

Some of the keynote speakers and chairpersons at the third world summit in the International Year of Crystallography (in Africa) were, from the left, front: Profs Abdelmalek Thalal (Morocco), Prosper Kanyankogote (University of Kinshasa, Democratic Republic of the Congo); Habib Bougzala (Tunisia), Santiago Garcia-Granda (IUCr, University Oviedo, Spain), Michele Zema (IYCr 2014, Italy/UK) and Dr Jean-Paul Ngome-Abiaga (UNESCO, Paris, France); back: Dr Thomas Auf der Heyde (Acting Director-general, South African Department of Science and Technology); Dr Petrie Steynberg (SASOL) and Prof André Roodt (UFS, host).

Photo: Marija Zbacnik
The third world summit in the International Year of Crystallography (in Africa) was hosted by Prof André Roodt, Head of the Department of Chemistry and President of the European Crystallographic Association,  at the University of the Free State in Bloemfontein.

A declaration with and appeal to support crystallography and science across Africa, was signed.

When one mentions 'Crystallography', or more simply 'crystals', what comes to mind? Diamonds? Perhaps jewellery in general? When thinking of crystals and Crystallography, you will need to think much bigger. And further – even to Mars and back.

Crystallography refers to the branch of science that is concerned with structure and properties of crystals. The obvious examples would include cut diamonds, gemstones such as amethysts, and ‘simple’ crystals such as selenite and quartz.

But have you thought about the irritating brown scales at the bottom of your kettle? The sand in your shoes? The salt over your lamb chops or the sugar in your coffee? All crystals. From egg shells to glucose, from bugs and insecticides to additives in food – even the compounds in chocolate – all fall under the close scrutiny of Crystallography.

The breakthroughs this field of science has produced have led to almost 30 Nobel Prizes over the years.

Determining the structure of DNA by crystallography was arguably one of the most significant scientific events of the 20th century. Different diseases have been cured or slowed by medicines obtained based on crystallographic studies. These include certain cancers, HIV/Aids, Tuberculosis and Malaria. Biological Crystallography enables the development of anti-viral drugs and vaccines.

This field of science influences our daily lives in virtually immeasurable ways. Here are but a few areas of study and development Crystallography contributes to:

•    LCD displays;
•    cellular smartphones;
•    insects and insecticides;
•    additives and products in foods;
•    improved effectiveness and security of credit cards;
•    new materials to preserve energy;
•    better gasoline with less by-products;
•    identify colour pigments used in paintings from the old masters, indicating if it’s an original or an imitation; and
•    beauty products such as nail polish, sun-block, mascara and eye shadow.

Crystallography is also currently used by the Curiosity Rover to analyse the substances and minerals on Mars.

Crystals and Crystallography form an integrated part of our daily lives – from bones and teeth to medicines and viruses, from chocolates to the blades in airplane turbines. Even down to the humble snowflake.


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