Derivatives of addicted nuts can help smokers break the habit of nicotine
In Southeast Asia, as many as 600 million people chew betel nuts with betel leaves and sometimes add tobacco leaves. Many users are addicted to this harmful "betel" preparation, which can create a sense of euphoria and alertness. However, researchers have now found that compounds extracted from nuts can help smokers - as well as betel nut chews - to relieve their habits.
Researchers will present their work today at the 253th National Conference of Chemical Society (ACS) National Conference and Expo. The world's largest scientific association ACS will meet on Thursday. It contains more than 14,000 speeches on a wide range of scientific topics.
"These two addictions have a commonality, so we think we can develop drugs for both," said Dr. Roger L. Papke, one of the project's main researchers. Principal Investigator Nicole A. Horenstein, Ph.D. And Papke, as well as Dr. Clare Stokes and Marta Quadri, are studying the betel nut compounds to create new molecules that are better than existing smoking cessation drugs. As Chantix® (Vanicline).
According to the US Centers for Disease Control and Prevention, more than 480,000 people die each year from smoking in the United States. Prescription smoking cessation drugs currently on the market work well, but can also have harmful side effects. For example, some patients taking varenicline have reported suicidal thoughts, sleepwalking and cardiovascular problems.
Researchers such as Papke and Horenstein are studying alternatives at the University of Florida due to the side effects of varenicline. Varenicline reduces the desire for nicotine by binding to the same receptor that binds nicotine molecules to brain cells, but it activates these receptors to a lesser extent. Papke explained that the adverse reaction occurred because the drug also binds to other nicotine receptors that are not involved in addiction. "The molecules we are developing are more specific - they don't target those other receptors at all, so our compounds should be safer," he said.
When Papke got a headhunting sword from Borneo, the idea of studying betel nut appeared. He learned that the strange carvings on the hilt might have been made by people who used betel nuts. It is prepared by mixing sliced betel nut with slaked lime (calcium hydroxide), flavor or candy, mixing the tobacco in some cases, and wrapping the mixture in the leaves of betel nut. Quid chews the user's teeth into a bright red color and forces them to spit out a lot of red saliva, which can tarnish local sidewalks and buildings. To make matters worse, using quid can cause serious health effects, including oral cancer and cardiovascular problems.
In previous work, Papke and Horenstein studied a psychoactive alkaloid in betel nut, betel nut. They found that arecoline stimulated the same brain cell receptors responsible for nicotine addiction, but did not stimulate other types of nicotine receptors.
Now, Horenstein is synthesizing a series of compounds whose structure is slightly different from arecoline. The researchers found that some of these new compounds also bind to addiction-related receptors, while other receptors exist alone. This means that these betel nut analogs may be able to treat addiction to cigarettes or betel nut without side effects. The next step for Horenstein and Papke is to seek funding so they can test these potential new drugs in animal tests.
Abstract
The Areca nut is well known in southeastern Asia as the source of muscarinic active alkaloids that constitute a popular addictive drug known as the betel quid, in which limed extracts of the nut are rolled in betel vine leaves and in some cases, include tobacco. Of the four known alkaloids in Areca, arecoline is the most active muscarinic agonist while guvacoline is less potent. Arecaidine is an M2 selective agonist. Muscarinic activity has not been reported for guvacine, a GABA transport inhibitor.
