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Saturday, May 28, 2011

Indian jasmine may be next-generation painkiller

New Delhi: Familiar garden plant crepe jasmine, whose flowers are widely used as offerings in poojas and other religious ceremonies, harbours a compound in its stem that has the potential to turn the medical world around.

A team of US scientists has artificially synthesised a compound in bulk quantity originally isolated from the bark of crepe jasmine in 2004.

Preliminary analysis carried out in the laboratory showed that the plant-derived compound, conolidine, has significant pain-relieving properties, which are as good as morphine but without its adverse effects.

The initial results are very encouraging. However, elaborate clinical evaluation spanning over 10-15 years is required before the molecule enters the drug market. “We are actively pursuing seasoned pharmaceutical partners to begin the process,” Glenn C Micalizio, one of the lead scientists from The Scripps Research Institute, Florida, told Deccan Herald.

If the molecule lives up to its potential in clinical evaluations and trials over time, it can turn out to be a blockbuster drug as pain treatments represent a huge slice of the global pharmaceutical market with annual sales running into billions of dollars. A new pain-killer would certainly become a big player.

Even though crape jasmine is used in traditional Chinese, Ayurvedic and Thai medicines, this is for the first time scientists are able to produce it in bulk quantity by a chemical process. The availability would ensure detailed testing of its biological properties, the team reported in the latest issue of Nature Chemistry.

In various models of pain studied in the laboratory using mouse, the synthetic compound performed spectacularly, suppressing acute pain and inflammatory-derived pain, two key measures of efficacy.

The synthetic molecule passed easily through the blood-brain barrier, and stay at relatively high concentrations up to four hours after injection in the brain and blood, which is a testimony to its potency.

While Morphine and its derivatives (opioid analgesics) remain the most widely used pain-killers, they are clinically problematic because of their side effects, ranging from addiction, tolerance, depression of breathing, nausea and chronic constipation.
The absence of side effects, however, is acting as a double-edged sword.
"The lack of side effects makes it a very good candidate for development. If there were side effects, they might provide additional clues as to how the compound works at the molecular level," said Scripps professor Laura Bohn who did pharmacological evaluation.
Because of the side-effects, identification of effective non-opioid analgesics to replace the existing drugs remains an active area of scientific pursuit.

“We are at the very beginning of analysing the potential value of conolidine as a therapeutic. Further studies will be needed to evaluate its broad profile as a potential therapeutic agent,” Micalizio said.

Source: Decan Herald, 29-05-2011

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