Guggul in Hypercholesterolemia: Recent research has thrown light on the possible lipid lowering mechanism of guggulipid. Cholesterol levels are controlled in a number of ways including intestinal uptake, endogenous biosynthesis, transport and elimination. Guggulipid probably works by the last-mentioned mechanism – elimination.
 Bile acids are the end products of cholesterol catabolism. In addition to their critical roles in lipid and vitamin absorption, bile acids are ligands for the nuclear receptor farnesol X receptor (FXR) and regulate expression of genes whose producta are critically important in bile acid and cholesterol homeostasis. Cholesterol 7- α - hydroxylase (Cyp7 α ) catalyzes the first rate-limiting step in the conversion of cholesterol to bile acids, a quantitatively important route for the elimination of excess cholesterol. This conversion is regulated by the liver oxysterol-activated receptor (LXR) and FXR. Cross-talk between LXR feed-forward and FXR feed-back regulation permits fine tuning of hepatic cholesterol homeostasis. A number of recent studies have shown that guggulsterone can act as an antagonist ligand for FXR. At the same time, guggulsterone has the ability to enhance the action of agonists on the bile salt export pump (BSEP), a major hepatic bile acid transporter. Guggulsterone treatment decreases hepatic cholesterol in wild-type mice fed a high-cholesterol diet, but is ineffective in FXR-null mice.
Guggul in Inflammation: The effectiveness of guggul in knee osteoarthritis has been studied. Thirty participants entered the study. Guggul was administered in capsule form (500 mg concentrated extract delivered TID) along with food. Overall data indicate significant improvement during the trial in both primary and secondary scales and objective measurements for assessment purposes. No side effects were reported during the trial. Guggul significantly inhibited both the maximal edema response and total edema response during 6 h of carrageenan-induced rat paw edema. One study showed that guggulsterone suppressed inflammation by inhibiting inducible nitric oxide synthetase expression induced by lipopolysaccharides in macropahges.
Guggul in Cancer: Of the 121 prescription drugs in use today for cancer treatment, 90 are derived from plant sources. About 75% of these were discovered by investigating folk medicines. These phytochemicals may fight cancer through suppression of the inflammatory response. Most inflammatory diseases are mediated through the activation of NF κ B, a nuclear transcription factor. It was indeed shown that guggulsterone suppresses NF κ B and NF κ B-regulated gene products. Various tumor cell types express constitutively NF κ B and is critical for their proliferation. Thus, guggulsterone, which is a pharmacologically safe agent, could be used as an anticancer agent on its own, a preventive agent, or an enhancer of chemotherapy/radiotherapy activity. Guggulsterone can suppress NF κ B activation induced by various carcinogens, inflammatory agents and tumor promoters.
Hepatoprotective action of guggul as well as its use in hypothyroidism have been demonstrated in experimental animals
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