Natural cholesterol-lowerer shows the way

Houston, Texas-- (May 2, 2002) -- Baylor College of Medicine scientists studying a natural product used in Indian traditional medicine for more than 2,500 years have unlocked the secret to its cholesterol-lowering success and possibly opened the door to production of more potent medicines. Dr. David D. Moore, professor of molecular and cell biology, and fourth-year Ph.D. student Nancy L. Urizar discovered that an extract of the resin of the guggul tree - approved as a cholesterol-fighter in India - actually targets the Farnesoid X Receptor (FXR). FXR is involved in regulation of the cholesterol by monitoring levels of bile acids, which are produced from cholesterol and released by the liver. The steroid guggulsterone, the active agent in the extract, blocks the activity of FXR.

The study results are reported in this week's issue of the journal Science.

"It really does lower cholesterol in a number of clinical studies in the Indian literature," said Moore. The only report in the western medical literature combined the extract, called guggulipid, with a cholesterol-lowering diet that reduced cholesterol 10 percent. The addition of guggulipid added another 10 percent reduction.

This study identifies FXR as a target for companies developing drugs to affect cholesterol metabolism, he said. He and Urizar want to study guggulsterone further to determine the biochemical reasons for the cholesterol-lowering effect, what genes are involved and how they affect the cell. Guggulipid is available in health food stores in the United States. When Moore tried it, he found that it did add to the effect of the statins he already took, but he stopped when further work indicated that guggulsterone might decrease the effectiveness of other drugs. Other claims for guggulipid are that it increases metabolism, resulting in weight loss. "I was disappointed there," said Moore, "It did not affect my weight."

Urizar said her cholesterol is normal, and she has not tried the drug. Her tests confirmed the lack of effect on metabolism by showing that guggulsterone did not affect the receptor for thyroid hormone, an important metabolic regulator.

"While we have seen promising results concerning the drug's cholesterol-reducing ability, there is a lot out there on the Web that we can't support," said Urizar.

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