Phenolphthalein Metabolite Inhibits Catechol-O-methyltransferase-Mediated Metabolism of Catechol Estrogens: A Possible Mechanism for Carcinogenicity

Ovarian cancer risk and use of phenolphthalein‐containing laxatives

“…12,13 Mechanisms through which phenolphthalein could affect ovarian cancer include interaction with the estrogen-receptor 14 and its potential influence on estrogen metabolism. In in vitro and in vivo studies in mice, Garner et al 15 recently reported that a metabolite of phenolphthalein, hydroxyphenolphthalein, inhibited O-methylation of catechol estrogens by catechol-O-methyltransferase.…”

Impact of ADAM17 Expression as a Potential Prognostic Biomarker and Target for Therapy in Node-negative Breast Carcinoma

“…These polluatnts are designated xeno-estrogens, which include pesticides, dyes, food preservatives and other polluatnts and can play a role in the etiology of breast cancer,since they interfere with the activity of endogenous estrogens (Garner et al, 2000).…”

Constipation Treatment in Neurological Disorders

“…Phenolphthalein is absorbed and can be undergone to an enterohepatic circulation which may prolong its effect. It has been withdrawn from sale in the United States because some studies in rodents suggested it may be carcinogenic (Garner et al, 2000;Josefson et al, 1997). Adverse reactions of derivatives of diphenylmethane are cramping and abdominal pain; high doses induce severe diarrhea, electrolyte depletion, damage to enterocytes, skin allergies and Stevens-Johnson syndrome (phenolphthalein).…”