Herbal cholesterol-lowering drug accelerates breakdown of numerous drugs including anti-AIDS and cancer chemotherapeutic agents

The herbal cholesterol-lowering drug guggulsterone, the active ingredient in the herbal drug gugulipid, accelerates the breakdown of almost 60 percent of current prescription drugs, including statin agents, anti-AIDS drugs, and cancer chemotherapeutic agents, according to an article in the August issue of the Journal of Pharmacology and Experimental Therapeutics.

Experiments showed that guggulsterone activates a cell receptor called PXR, which results in stimulation of the CYP3A family of liver enzymes, which are responsible for degradation of almost 60 percent of the prescription drugs on the market.
Drugs affected by guggulsterone include the anti-AIDS drug AZT, chemotherapeutic agents, and statins. The liver enzyme also can turn some chemicals that do not cause cancer into carcinogens, senior author Dr. Jeffrey Staudinger said.

The PXR cell receptor is one of three stimulated by guggulsterone stimulates. Estrogen and progesterone receptors are also stimulated.

Earlier studies had shown that guggulsterone lowers cholesterol by turning down the activity of a receptor known as FXR. Brobst, Staudinger and their collaborators decided to experiment with the herbal gugulipid, which they bought at a health-food store, and with the pure form, guggulsterone, to see whether other receptors also were implicated in its effect on the body.

"This country's diet is atrocious, so there are plenty of people walking around with high cholesterol," Staudinger said. "They'll get on the Web and see that gugulipid herbal therapy lowers cholesterol and is available without a prescription. They may then begin self-medicating with gugulipid in addition to other drugs prescribed by their physician. In this study, we've shown that, when they do, they have a high likelihood of causing herb-drug interactions."



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