Ovarian cancer risk and use of phenolphthalein‐containing laxatives

Cooper, Glinda S.; Longnecker, Matthew P.; Peters, Ruth

doi:10.1002/pds.824

Cited by 17 publications

(7 citation statements)

References 11 publications

(10 reference statements)

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“…Phenolphthalein was used in certain laxatives until a 1997 FDA decision withdrew approval following findings that it caused tumors in rodents and could have estrogenic effects on human breast cancer cells in vitro [33]; however, no harmful effects in humans have yet been identified [34]. Given the known inter-species differences in NR ligands, compounds that cause toxic effects in rodents may activate NRs in humans leading to detoxification.…”

Section: Resultsmentioning

confidence: 99%

Rational quantitative structure–activity relationship (RQSAR) screen for PXR and CAR isoform-specific nuclear receptor ligands

Dring

Anderson

Qamar

et al. 2010

Chemico-Biological Interactions

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Constitutive androstane receptor (CAR) and pregnane X receptor (PXR) are closely related orphan nuclear receptor proteins that share several ligands and target overlapping sets of genes involved in homeostasis and all phases of drug metabolism. CAR and PXR are involved in the development of certain diseases, including diabetes, metabolic syndrome and obesity. Ligand screens for these receptors so far have typically focused on steroid hormone analogs with pharmacophore-based approaches, only to find relatively few new hits. Multiple CAR isoforms have been detected in human liver, with the most abundant being the constitutively active reference, CAR1, and the ligand-dependent isoform CAR3. It has been assumed that any compound that binds CAR1 should also activate CAR3, and so CAR3 can be used as a ligand-activated surrogate for CAR1 studies. The possibility of CAR3-specific ligands has not, so far, been addressed. To investigate the differences between CAR1, CAR3 and PXR, and to look for more CAR ligands that may be of use in quantitative structure-activity relationship (QSAR) studies, we performed a luciferase transactivation assay screen of 60 mostly non-steroid compounds. Known active compounds with different core chemistries were chosen as starting points and structural variants were rationally selected for screening. Distinct differences in agonist versus inverse agonist/antagonist effects were seen in 49 compounds that had some ligand effect on at least one receptor and 18 that had effects on all three receptors; eight were CAR1 ligands only, three were CAR3 only ligands and four affected PXR only. This work provides evidence for new CAR ligands, some of which have CAR3-specific effects, and provides observational data on CAR and PXR ligands with which to inform in silico strategies. Compounds that demonstrated unique activity on any one receptor are potentially valuable diagnostic tools for the investigation of in vivo molecular targets.

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Section: Resultsmentioning

confidence: 99%

Rational quantitative structure–activity relationship (RQSAR) screen for PXR and CAR isoform-specific nuclear receptor ligands

Dring

Anderson

Qamar

et al. 2010

Chemico-Biological Interactions

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“…Cooper et al . reported that phenolphthalein‐containing laxatives do not increase the risk of ovarian cancer in humans . These findings are of importance to those countries in which phenolphthalein is still used in over‐the‐counter medications.…”

Section: Biological Applications Of Phthalein Dyesmentioning

confidence: 82%

Developments in the chemistry and applications of phthalein dyes. Part 2: biological applications

Sabnis¹

2018

Coloration Technology

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This review describes the huge impact of phthalein dyes on multiple industries. Although phthalein dyes demonstrate several vital applications, there appears to be no review in the literature. Part 2 of the review focuses on developments in the chemistry and biological applications of phthalein dyes. The biological applications of phthalein dyes are grouped into agrochemical, biochemical, food, personal care, pharmaceutical and sensors applications. The importance of these dyes in various commercial products is also revealed, and patent analysis is provided in the Appendix. The uses of phthalein dyes in various fields are important but their growing popularity with fascinating colour change features is particularly notable. Part 1 of the review focused on developments in the chemistry and industrial applications of phthalein dyes. The industrial applications of phthalein dyes are grouped into building/construction applications, coatings applications, electronic/electrical applications and miscellaneous applications.

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“…Recently, using a pH meter or pH tape, several investigators have shown that salivary pH plays important roles in oral diseases [21] and systemic diseases [22], and that nasal pH becomes more alkaline in allergic rhinitis [23]. However, these measurements remain difficult to perform at frequent intervals with a pH meter, and saliva must be collected prior to the measurement of salivary pH, because the chemical components of the pH indicator tape may be carcinogenic [24]. As expected, the cotton swab ® revealed a variety of colors at different pHs due to changes of the molecular structure caused by the ionic nature of anthocyanins [1] [3].…”

Section: Discussionmentioning

confidence: 99%

Polyvinylalcohol Stabilizes Anthocyanins of Red Wine in the Solid Phase but Not in the Aqueous Phase

Sakamoto¹,

Kanehira²,

Hongou³

et al. 2015

ABC

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Monomeric anthocyanins exhibit color variations at different pH, but they are highly unstable at physiological pH. To improve the stability, the effects of polyvinylalcohol on the anthocyanins of young red wine prepared from Cambell Early grapes were examined in aqueous solution and in the solid phase on a cotton swab ® and inert materials. Cyanidin-3-glucoside and malvidin-3-glucoside represented approximately 43.6% of total anthocyanins in the red wine. The anthocyanins decreased to 11.3% of the initial amount in aqueous solution at physiological pH after storage for 60 days at room temperature. On the other hand, from 66.9% to 87.2% remained in the solid phase on a cotton swab ® and polypropylene membrane in the presence of polyvinylalcohol. The stability of the anthocyanins increased with the concentration of polyvinylalcohol in the solid phase but not in the aqueous solution. The anthocyanins were found to be condensed and immobilized in the complexes of anthocyanins and polyvinylalcohol on the polypropylene membrane by phase-contrast microscopy analysis. The anthocyanins in the cotton swab ® displayed color variations when dipped into different pH buffer solutions. These results suggest that anthocyanins from red wine stabilized in the solid phase by polyvinylalcohol can be used as a visual indicator of pH.

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Ovarian cancer risk and use of phenolphthalein‐containing laxatives

Abstract: This study provides some assurance that phenolphthalein-containing laxatives do not increase the risk of ovarian cancer in humans. These findings are of particular importance to those countries in which phenolphthalein is still used in over-the-counter medications.

Cited by 17 publications

References 11 publications

Rational quantitative structure–activity relationship (RQSAR) screen for PXR and CAR isoform-specific nuclear receptor ligands

Rational quantitative structure–activity relationship (RQSAR) screen for PXR and CAR isoform-specific nuclear receptor ligands

Developments in the chemistry and applications of phthalein dyes. Part 2: biological applications

Polyvinylalcohol Stabilizes Anthocyanins of Red Wine in the Solid Phase but Not in the Aqueous Phase

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