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Scientists invent a way to synthesize potential brain-protecting compound

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Posted June 18, 2015

The researchers at the Scripps Research Institute have created a new way to synthesize jiadifenolide, a plant-derived molecule that may have powerful brain-protecting properties. Scientists were trying to achieve this since the discovery of the compound in 2009. The method is practical and scalable, which should allow producing bigger quantities of the compound.

Illicium henryi – plant related to Illicium jiadifengpi, both growing in china. Illicium plants were used in traditional Chinese medicine for a long time and now scientists managed to effectively synthesize the compound that may have powerful brain-protecting properties. Image credit: Scott Zona via Wikimedia, CC-BY-2.0

Illicium henryi – plant related to Illicium jiadifengpi, both growing in china. Illicium plants were used in traditional Chinese medicine for a long time and now scientists managed to effectively synthesize the compound that may have powerful brain-protecting properties. Image credit: Scott Zona via Wikimedia, CC-BY-2.0

Jiadifenolide was studied since its discovery. First studies have hinted that it might be useful in protecting brain cells from number of neurodegenerative diseases, such as Alzheimer’s and perhaps other neurological conditions including stroke and even traumatic brain injury. That is why synthesizing jiadifenolide has been a major task, especially having in mind that obtaining useful quantities of the compound from plants is very difficult.

Previously tested methods did not achieve any significant results and were only useful for yielding a few milligrams for cell-culture experiments. However, new method is much more advanced and can produce gram to kilogram quantities needed for tests in animals and humans.

All of this research is aimed at making a jiadifenolide-derived drug, even though it is still many years ahead. Research also demonstrated the increasing power of synthetic chemistry to produce the potentially valuable molecules found in nature on large scale at low cost. Science now can find useful compounds in nature and use them for our health benefits easier than ever before, because of scientific and technological advancements.

Jiadifenolide is found in trace quantities in the fruit of the star anise-related shrub Illicium jiadifengpi, which grows in southern China. This and other related plants have been used in traditional Chinese medicine for a long time. Most parts of the plant are poisonous if eaten, but root extracts applied to the skin have been used to treat arthritis.

Back in 2009, when jiadifenolide was discovered, a team of Japanese and Chinese scientists reported isolating tiny quantities of jiadifenolide from Illicium jiadifengpi. They noticed that the compound is not toxic, and strongly promotes the growth of axons and dendrites (output and input branches) from rat neurons in a culture dish.

Further research has showed that jiadifenolide works by enhancing the activity of natural brain growth factors, known as neurotrophins. Ryan A. Shenvi, associate professor who led the study, said that “neurotrophin levels are depressed in diseases like Alzheimer’s, so researchers have long sought compounds that behave like neurotrophins or that amplify their activity, especially those that could be taken in a pill”. Neurotrophins are large molecules and cannot be used as drugs, because they are rapidly broken down by enzymes in the digestive tract and bloodstream and also don’t cross the blood-brain barrier easily. Jiadifenolide, on the other hand, is a small molecule, and thus has more potential to be developed into an oral drug.

Scientists were aware of previous attempts to synthesize jiadifenolide that yielded small amounts of compound. Therefore, they took a completely different approach. The new method is very practical and scalable. Eight-step synthesis involves merging two simple molecules, called butenolides, via a process called the Michael reaction (double version of it) to make a compound very close to jiadifenolide itself.

Scientists say that luck was involved too, as very few scientists would have predicted that this process will work as needed. However, after developing the method, scientists soon realised that they can obtain more than a gram from one batch.

Now that method is developed and scientists can produce significant amounts of the compound, they will look for companies to do further research and tests in animal models. Funny thing is that therapeutic potential of the compound was not the only thing that stimulated the research. Professor Shenvi said that he was also inspired by structural beauty as well.

Source: Scripps

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