Anthraquinone glycoside Overview
Anthraquinone glycosides are a class of naturally occurring compounds found in several medicinal plants such as senna, cascara sagrada, frangula (buckthorn), aloe vera, and rhubarb. They are not themselves a receptor or enzyme but rather plant-derived stimulant laxatives whose pharmacological effect is mediated after metabolic activation in the intestine. Upon ingestion and hydrolysis by gut bacteria, they release anthraquinone aglycones that act locally on the colon to increase smooth muscle tone and stimulate peristaltic contractions. This results in increased bowel motility and enhanced secretion of water/electrolytes into the lumen—softening stool and promoting defecation. Their mechanism involves inhibition of sodium/potassium ATPase activity in colonic epithelial cells as well as direct stimulation of enteric nerves within the myenteric plexus. Chronic or high-dose use can lead to significant safety concerns including electrolyte imbalances (notably hypokalemia), dehydration, nephrotoxicity, melanosis coli (pigmentation changes), potential inflammatory changes to colonic mucosa with apoptosis induction at high doses or prolonged exposure. They also interact with cardiac glycosides due to their effect on potassium levels.[1][3][4] **Note:** "Gastrointestinal motility via anthraquinone glycosides" is not itself a canonical molecular target but describes a pharmacological process mediated by this compound class acting through multiple mechanisms on intestinal tissue; thus it should be flagged as an incorrect entry if used as a drug target name.[1]
Mechanism of Action
Hydrolyzed in the gut to active aglycones by intestinal bacteria; aglycones stimulate colonic smooth muscle contraction and inhibit water/sodium reabsorption by inhibiting Na⁺/K⁺ ATPase activity in epithelial cells
Biological Functions
Disease Associations
Safety Considerations
- Electrolyte disturbances, especially hypokalemia
- Risk of dehydration
- Long-term use may cause albuminuria, hematuria, nephropathy, arrhythmias, bone deterioration
- Not recommended for pregnant women or children
Gosset