Drug intelligence / Profile preview

Rheinanthrone

Development stage
Discontinued
Modality
Small Molecules
Administration
Oral
01

Overview

Rheinanthrone is a naturally occurring anthraquinone compound and the major active metabolite of sennosides A and B, which are found in plants such as Senna and Rheum species. It is primarily known for its laxative effect, which results from stimulating peristalsis and increasing fecal water content in the large intestine. Mechanistically, rheinanthrone activates macrophages to increase cyclooxygenase 2 (COX2) expression, leading to elevated prostaglandin E2 (PGE2) production. The rise in PGE2 subsequently decreases aquaporin 3 expression in colonic epithelial cells, reducing water reabsorption and promoting laxation. About 10% of orally administered rheinanthrone is absorbed from the gut; most is excreted unchanged in feces with minor urinary elimination. Rheinanthrone has no approved medical indications but has been studied for its biological activities including potential anticancer effects[1][2][4][5][6].

Other names
rhein-9-anthronerhein9-anthronerhein 9-anthronerheinanthrone
02

Targets

AQP3 (Aquaporin-3 channel protein)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PTGES (Microsomal prostaglandin E synthase-1)

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