Natural pain relief with no opioids, no side effects?

Isolated from a tropical flowering plant, conolidine kills pain like morphine without going through any of the major neurotransmitters associated with opiates, chemists show.
Written by Janet Fang, Contributor

It’s called conolidine, and it’s been used for many years in traditional Chinese, Ayurvedic, and Thai medicines.

Originally isolated from the bark of a tropical, ornamental flowering plant Tabernaemontana divaricata (also known as crepe jasmine or pinwheel flower, pictured), the compound from the leaves and roots have been used for anti-inflammation and pain relief, respectively.

Now, a synthetic form of the rare natural product can alleviate fever and acute pain as well, according to researchers from the Scripps Research Institute.

Conolidine belongs to a larger class of natural products, called C5-nor stemmadenines, members of which have been described as opioid analgesics belonging to the same class of compounds as morphine and hydrocone.

But because conolidine is not an opioid, it might offer pain relief without complications like the development of dependence and nausea.

Although researchers are aware of the analgesic effects of similar compounds, it's been difficult to investigate conolidine since there isn't enough of it available from natural sources. It makes up just 0.00014% of the bark of T. divaricata.

So in order to conduct medicinal testing with mice, the team developed a method to rapidly synthesize the compound.

They found that conolidine’s potency was similar to morphine, but behaved differently. It doesn’t act at any of the receptors associated with opiates, missing most of the major neurotransmitter receptors completely. Nature News explains:

Morphine and other opioids increase the activity of the locomotor centers in the brain, which control the mice's movements, by raising levels of the neurotransmitter dopamine. This seems to be related to their addictive properties.

But conolidine doesn’t affect locomotor activity, suggesting that it doesn’t induce dopamine elevations.

So, it showed few, if any, of the side effects associated with opioids. According to study researcher Laura Bohn of Scripps, “the lack of side effects makes it a very good candidate for development.”

In 2009 alone, analgesics saw the sales of several tens of billions of dollars.

The study was published in Nature Chemistry today.

Image by rjackb via Flickr

This post was originally published on Smartplanet.com

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