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Anthraquinone glycosides are a major class of naturally occurring phenolic compounds found in medicinal plants such as Senna, Aloe, Rhubarb, and Cascara. These molecules serve as pro-drugs that are pharmacologically inactive until they reach the colon, where they are hydrolyzed by gut microbiota into active aglycones like rhein-anthrone and emodin. These active forms exert a potent stimulant laxative effect by irritating the colonic mucosa, stimulating the myenteric plexus to increase peristalsis, and inhibiting the Na+/K+-ATPase pump to promote fluid accumulation in the intestinal lumen. Beyond their established use as cathartics for the treatment of acute constipation, anthraquinone glycosides and their derivatives are extensively studied for potential anti-inflammatory, antimicrobial, and anticancer properties. They have been shown to modulate signaling pathways such as MAPK/ERK and interact with molecular targets like topoisomerases and kinases. However, their clinical application is frequently balanced against safety concerns including electrolyte imbalances, dehydration, and the development of melanosis coli following chronic exposure.
Bacterial hydrolysis to active aglycones followed by stimulation of enteric nerves and inhibition of colonic Na+/K+-ATPase, leading to increased motility and fluid secretion.
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