Why grapefruit interferes with taking medicine and what to do about it

Why grapefruit interferes with taking medicine and what to do about it

Written by Charlotte Hu Edited by Tanya Lewis

Unfortunately for grapefruit lovers, mixing the appealingly bitter citrus fruit with certain medications can have dangerous side effects. According to the National Capital Poison Center, a nonprofit poison control organization, At least 85 drugsCommonly prescribed antidepressants, statins, antibiotics, etc. Known or suspected interactions With grapefruit or grapefruit juice. But plant researchers are now working on possible solutions. The idea is to genetically modify a variety of fruits that are safe to use with medication.

Over the past few decades, scientists have zeroed in on a class of chemicals known as the main culprit for grapefruit’s notorious sabotaging effects. Furanocoumarin. These molecules can bind to and inactivate an enzyme called CYP3A4 in the intestine. metabolize certain drugs. This can lead to excessive concentrations of the drug in the bloodstream, creating a risk of a harmful overdose. (Grapefruit may have an adverse effect on some medications, such as certain antihistamines, through another mechanism.) Many popular citrus fruits, such as grapefruit, limes, and pomelo, contain It contains coumarins, but some orange varieties such as Valencia, navel, and mandarin contain furanocoumarins. Oranges have low or negligible levels of these chemicals.

In a recently published study, new botanist, Researchers at Israel’s Institute of Volcanology have discovered a gene in grapefruit that plays a key role in the production of furanocoumarins. According to the study authors, editing this gene could result in a variety of grapefruit that does not interfere with drug therapy in this way.

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“there was chemical efforts Removes furanocoumarins from juice. People too Cross-bred mandarin and pomelo“We got a grapefruit-like product,” says Yoram Eyal, professor at the Volcano Center and co-author of the paper. “However, commercial production of grapefruit juice is extremely difficult. [regulated]Therefore, something that resembles a grapefruit cannot be sold as “grapefruit juice.” ”

Eyal and his colleagues had wanted to try a new approach by engineering grapefruit without furanocoumarins, but “now we know which genes to target,” he says.

Researchers discovered the gene by crossing grapefruit and mandarin oranges and examining the genetics of the resulting plants. “We found that 50 percent of the offspring produced furanocoumarins and 50 percent did not. This indicates that there is probably only one gene involved in this pathway of furanocoumarin biosynthesis.” said Livnat Goldenberg, a postdoctoral researcher at the Institute of Volcanology and lead author of the study. “We then examined its activity and found that it did indeed produce the first component of the furanocoumarin pathway.”

Paul Watkins, director of the Watkins Institute for Drug Safety Sciences at the University of North Carolina at Chapel Hill, previously worked with stakeholders in the Florida citrus industry to understand how grapefruit interferes with drug administration. I’ve done it before. him and his colleagues conducted an experiment They found that after removing furanocoumarins from grapefruit juice, the main known grapefruit-drug interactions did not occur.

However, removing these chemicals from the juice using a process similar to that used to make lactose-free milk was expensive and affected the taste.

“Unfortunately, during the process of extracting the furanocoumarins, the juice also lost its vigor. [it] They took a lot of other things with them,” said Watkins, who was not involved in the incident. new botanist study. “If we could use technology like CRISPR, [a method of editing genes] And we’ve created a whole line of grapefruit products with no potential for drug interactions…which has great value economically, commercially, and for people who really like grapefruit juice. ”

Identifying common genes for furanocoumarin synthesis is only the first step, and the Volcani team is currently using CRISPR to create a set of real-world trees. “We are developing this type of grapefruit,” Eyal says. But he points out that it could take about four years for the edited plants to become fruit-bearing trees.

The researchers’ ultimate goal is to produce viable grapefruit trees that can be classified as genome-edited, but not as genetically modified organisms (GMOs). In some countries, including Israel and the United States, crops that have been CRISPR edited but do not have the new genes are Designated Non-GMO. Additionally, the lack of furanocoumarin genes does not seem to make citrus fruits such as mandarins more susceptible to disease or pests, leading Eyal and colleagues to discuss any significant health implications for grapefruit trees. says he is not worried. He also doesn’t expect it to have a major impact on grapefruit’s nutritional benefits. “Furanocoumarins are considered antioxidants,” he added. “But there are many other antioxidants, too. [such as] Vitamin C and flavonoids. ”

If the genome editing efforts bear fruit, Volcani’s team will work with researchers in the medical field to test modified fruit juices, first in the lab and eventually in human studies.

“Our long-term goal is to develop grapefruit varieties that are free of furanocoumarins and make them available to grapefruit growers,” Eyal says.