Natural synthetic: Analgesic unearthed

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  • Published: Nov 1, 2013
  • Author: David Bradley
  • Channels: NMR Knowledge Base
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Getting to the root of painkiller

Occurrence of the Synthetic Analgesic Tramadol in an African Medicinal Plant

The African pin cushion plant produces large quantities of analgesic compounds...now NMR has demonstrated that one of the primary components is chemically identical to the well-known, synthetic opioid painkiller Tramadol. The discovery should serve as a warning to the potential problems of dependency and addiction that might occur with use of so-called natural and herbal medicinal products.

Michel De Waard, Inserm Research Director at the Grenoble Institute of Neurosciences and colleagues report that this is the first time that what was considered to be an entirely synthetic pharmaceutical product is present naturally at high concentration in a plant or other biological source.

Herbal analgesic

Writing in Angewandte Chemie, the team discusses the chemistry of Nauclea latifolia, a small shrub that is widespread across Sub-Saharan Africa. It has been used extensively in traditional medicine, particularly in Cameroon, where the plant has been used to apparently treat various health problems including, pain, fever and epilepsy. De Waard and colleagues worked with chemist Ahcène Boumendjel and Germain Sotoing Taiwe of the University of Buea to isolate and investigate the active components of the root bark of the pin cushion plant.

De Waard and colleagues were rather surprised to find that one of those components is the opiate painkiller Tramadol. This medication was developed in the 1970s and is a widely used analgesic with a chemical structure related to morphine, although is far less addictive than the parent compound. Confirmation of the presence of the opiate in the plant root bark samples was confirmed by three laboratories independently testing three different samples collected at different times of the year to ensure that there was no cross contamination or error in the analyses.

Synthetically natural

"All results converge and confirm the presence of Tramadol in the root bark of N. latifolia. On the other hand, no trace of this molecule was detected in the aerial part of the shrub (leaves, trunk or branches)," the researchers say. Moreover, samples were retrieved from the interior of the roots too where substantial concentrations of the compound were also shown to be present and thus precluding contamination.

From a quantitative point of view, the concentration of Tramadol in the dried bark extracts was recorded at 0.4% and 3.9%. These are extremely high levels for any active substance in a plant and thus opens up the possibility of exploiting this local natural resource more efficiently by decoction of the roots for use in a more controlled herbal remedy product. "There are over 10 different varieties of this shrub in Africa, so we can envisage repeating the tests in order to determine which varieties contain Tramadol," De Waard adds.

There are countless plants that have physiologically and medically active natural products, including morphine in opium poppies caffeine in coffee plants and the metabolite of aspirin salicylic acid which is present in willow bark and was well known as a source of natural painkiller. Indeed around 40 percent of pharmaceutical drugs that have been used during the last century have a natural origin. However, this is the first time that what is a synthetic drug has been found natively in a natural source.

"The next step is looking for other compounds in this plant, to explain how it can be used to treat epilepsy and see how we can start a business on this issue," de Waard told SpectroscopyNOW. "I hope to convince scientists and the population that ethnopharmacology has a lot of value."

Related Links

Angew Chem, 2013, 52, 11780-11784: "Occurrence of the Synthetic Analgesic Tramadol in an African Medicinal Plant"

Article by David Bradley

The views represented in this article are solely those of the author and do not necessarily represent those of John Wiley and Sons, Ltd.

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