From folk medicine to cuisine, jambu is traditional in the northern region of Brazil. The country's native plant is found in cachaça and typical dishes such as Tacacá and Pato no Tucupi. The aphrodisiac herb that numbs the mouth, heals wounds and relieves pain has drawn the attention of science for a long time. And now, the spilanthol molecule, which is the substance responsible for the medicinal effects of jambu, was obtained synthetically by researchers from the Institute of Chemistry (IQ) at Unicamp.
The technology is an unprecedented production route, more concise, efficient and does not depend on the planting of jambu, as it is completely synthetic. With great potential for application, as the bioactive compound is recognized as being largely responsible for the antioxidant, anti-inflammatory and anesthetic effects of jambu, the process was the subject of a patent application made by Inova, the Unicamp Innovation Agency, which It also dealt with licensing for a spin-off company, created especially to develop products from synthetic spilanthol.
“The difference in the process developed at Unicamp is the number of steps. It is a very short process, one of the shortest in relation to what is found in scientific literature”, explains Julio Cezar Pastre, professor at the IQ Organic Synthesis Laboratory and one of the inventors of the technology.
A gram of purified spilanthol costs an average of US$60 – despite jambu extract being commercially available at a lower price. Initial research shows that the proposed new route could reduce this amount by up to ten times.
The technology developed at Unicamp allows spilanthol to be obtained using a five-step route, in a faster and cheaper process. The researchers start with substrates derived from petroleum and commercially available. They then carry out controlled chemical reactions, transforming the structure and increasing the complexity of these molecules until they reach spilanthol.
According to researchers, the closest route, patented by a Japanese company, suggests processes of seven to nine steps. However, the material is composed of three isomers, only 79% of which corresponds to spilanthol and there is no possibility of separation between them. Brazilian technology achieved purity of 98% and also employs, in the five stages, two catalytic reactions that are more selective and suitable for industrial scale.
With small modifications to the proposed route, the researchers believe they can also synthesize other natural and non-natural analogues of spilanthol, increasing supply and economic viability.
Biosíntese, a spin-off company that licensed the patent, is betting on synthetic spilanthol as a substitute for morphine, for the treatment of chronic and acute pain. The company will work, in parallel, with another startup incubated at Incamp, the Unicamp Technology-Based Business Incubator. Especiarias Amazônia has already launched products on the market with Jambu extract, such as a painless depilatory wax and a pre-tattoo anesthetic ointment.
Startups founder and CEO Danúbio Martins explains that the synthesis of bioactive compounds found in plants provides easier methods of obtaining them with greater control when compared to extraction from natural sources, which is limited. “We noticed that some companies have difficulty working with a natural product, because it does not have a precise standard: sometimes the harvest comes with one percentage of the asset and at other times it comes with another. The synthetic can solve this”, reveals Martins.
Danúbio estimates that the first products with synthetic spilanthol will reach the market within a year. “Today we are still finalizing the bench studies, improving the route so that it has better commercial viability”, he concludes. In Brazil, the synthetic version of spilantol still needs approval from Anvisa.
One molecule, many uses
The study also resulted in a second patent application for a biofilm containing synthetic spilanthol and an analogue. The anesthetic activity of the compounds was evaluated in a study with mice and confirmed values similar to those of jambu extract, described in previous research carried out by the university. The analogue also showed better results than a commercial anesthetic cream, considered the highest standard in topical anesthesia, which was used as a control.
In the cosmetics industry, spilanthol is compared to botulinum toxin for its anti-wrinkle effect, being included in the formulation of high-value-added creams. With synthetic production at a high level of purity, the startup hopes to meet market demand for the development of new applications. One of the proposals is to include spilanthol in intimate lubricating gels. And the startup says it already has the green light from a health and hygiene products company that would enable distribution in 128 countries.
Other ongoing research is analyzing the performance of spilantol as a tick killer, food preservative and even a weight loss aid. In the area of security, the bioactive compound can also be used as a personal defense weapon, with fewer side effects compared to traditional pepper spray.
Published article originally on the Unicamp Innovation Agency website.
