Ancient elixir passes the test

A traditional Indian remedy for lowering cholesterol does work, and in a new way that might lead to the development of improved drugs.

The resin of the guggul tree has been used in Indian traditional medicine for more than 2500 years, and more recently has been enlisted to fight high cholesterol.

David Moore, of the Baylor College of Medicine in Houston, found the guggul extract lived up to its reputation.

"It really does lower cholesterol in a number of clinical studies in the Indian literature," Mr Moore said.

Writing in the journal Science, he said it had been used in Indian Ayurvedic medicine since at least 600 BC to treat obesity and other disorders.

Moore's team found the steroid guggulsterone, the active agent in the guggul extract, blocks the activity of the farnesoid X receptor (FXR) on cells.

FXR helps regulate cholesterol by affecting levels of bile acids, which are produced from cholesterol and released by the liver.

"Bile acids are the only way that cholesterol has to get out of the body," Moore said in a telephone interview. "We knew that FXR was a key regulator of cholesterol metabolism."

Moore wanted to study FXR more, so he looked for compounds known to lower cholesterol in ways not understood.

"I spent quite a lot of time clicking around the internet," he said. He found guggulsterone, with niacin - a B vitamin often prescribed for cholesterol patients - and red wine.

Red wine and niacin were not strongly enough involved with FXR to interest him, but guggulipid, available in American health food stores, was.

Tests in mice showed guggul extract lowered cholesterol by blocking the effects of FXR.

"We put mice on a high-cholesterol diet for a week and measured cholesterol levels in the liver," said Moore.

"In normal mice you feed them cholesterol and the cholesterol level in the liver goes up. But if you feed them cholesterol and give them guggulsterone at the same time, the cholesterol levels stay the same."

Moore, who with colleagues has set up a small biotechnology company called X-Ceptor Therapeutics in San Diego, California, said it might be possible to more specifically target FXR with a drug. The company has patented FXR.

"As a pharmaceutical company you are not going to be interested in producing something that is already available, but you are going to be interested in producing something that is better," Moore said.

Moore, who takes statin drugs to control his own cholesterol, tried guggul. "I was curious about whether it would work with statins ... It dropped my total serum cholesterol by 10 per cent," he said.

"But we had some evidence that it might have effects on the activity of other drugs and I stopped taking it."

Other claims for guggulipid are that it can promote weight-loss by raising metabolism.

"I was disappointed there," said Moore. "It did not affect my weight."

- REUTERS

nzherald.co.nz/health