Antiandrogenic properties of parabens and other phenolic containing small molecules in personal care products

Jiangang Chen, Ki Chang Ahn, Nancy A. Gee, Shirley J. Gee, Bruce D. Hammock, Bill L. Lasley

Research output: Contribution to journalArticle

144 Citations (Scopus)

Abstract

To identify the androgenic potency of commonly used antimicrobials, an in vitro androgen receptor-mediated transcriptional activity assay was employed to evaluate the androgenic/antiandrogenic activity of parabens and selected other antimicrobials containing a phenolic moiety. This cell-based assay utilizes a stably transfected cell line that lacks critical steroid metabolizing enzymes and is formatted in a 96-well format. At a concentration of 10 μM, methyl-, propyl- and butyl-4-hydroxybenzoate (parabens) inhibited testosterone (T)-induced transcriptional activity by 40%, 33% and 19%, respectively (P < 0.05), while 4-hydroxybenzoic acid, the major metabolite of parabens, had no effect on T-induced transcriptional activity. Triclosan inhibited transcriptional activity induced by T by more than 92% at a concentration of 10 μM, and 38.8% at a concentration of 1.0 μM (P < 0.05). Thirty-four percent of T-induced transcriptional activity was inhibited by thymol at 10 μM (P < 0.05). Cell proliferation and/or cytotoxicity were not observed in any of the treatments. None of the compounds appeared to be androgenic when tested individually without T. The data presented in this report demonstrate that some widely used antimicrobial compounds have antiandrogenic properties and warrant further investigation to fully understand their potential impact on human reproductive health.

Original languageEnglish (US)
Pages (from-to)278-284
Number of pages7
JournalToxicology and Applied Pharmacology
Volume221
Issue number3
DOIs
StatePublished - Jun 15 2007

Fingerprint

Parabens
Molecules
Assays
Triclosan
Thymol
Reproductive Health
Cell proliferation
Androgen Receptors
Cytotoxicity
Metabolites
Testosterone
Steroids
Cells
Cell Proliferation
Health
Cell Line
Enzymes
4-hydroxybenzoic acid

Keywords

  • Androgen receptor
  • Bioassay
  • Parabens
  • Phenolic moiety
  • Thymol
  • Triclosan

ASJC Scopus subject areas

  • Pharmacology
  • Toxicology

Cite this

Antiandrogenic properties of parabens and other phenolic containing small molecules in personal care products. / Chen, Jiangang; Ahn, Ki Chang; Gee, Nancy A.; Gee, Shirley J.; Hammock, Bruce D.; Lasley, Bill L.

In: Toxicology and Applied Pharmacology, Vol. 221, No. 3, 15.06.2007, p. 278-284.

Research output: Contribution to journalArticle

Chen, Jiangang ; Ahn, Ki Chang ; Gee, Nancy A. ; Gee, Shirley J. ; Hammock, Bruce D. ; Lasley, Bill L. / Antiandrogenic properties of parabens and other phenolic containing small molecules in personal care products. In: Toxicology and Applied Pharmacology. 2007 ; Vol. 221, No. 3. pp. 278-284.
@article{2cbf97800c6b45a1a1410bcbc8eb48de,
title = "Antiandrogenic properties of parabens and other phenolic containing small molecules in personal care products",
abstract = "To identify the androgenic potency of commonly used antimicrobials, an in vitro androgen receptor-mediated transcriptional activity assay was employed to evaluate the androgenic/antiandrogenic activity of parabens and selected other antimicrobials containing a phenolic moiety. This cell-based assay utilizes a stably transfected cell line that lacks critical steroid metabolizing enzymes and is formatted in a 96-well format. At a concentration of 10 μM, methyl-, propyl- and butyl-4-hydroxybenzoate (parabens) inhibited testosterone (T)-induced transcriptional activity by 40{\%}, 33{\%} and 19{\%}, respectively (P < 0.05), while 4-hydroxybenzoic acid, the major metabolite of parabens, had no effect on T-induced transcriptional activity. Triclosan inhibited transcriptional activity induced by T by more than 92{\%} at a concentration of 10 μM, and 38.8{\%} at a concentration of 1.0 μM (P < 0.05). Thirty-four percent of T-induced transcriptional activity was inhibited by thymol at 10 μM (P < 0.05). Cell proliferation and/or cytotoxicity were not observed in any of the treatments. None of the compounds appeared to be androgenic when tested individually without T. The data presented in this report demonstrate that some widely used antimicrobial compounds have antiandrogenic properties and warrant further investigation to fully understand their potential impact on human reproductive health.",
keywords = "Androgen receptor, Bioassay, Parabens, Phenolic moiety, Thymol, Triclosan",
author = "Jiangang Chen and Ahn, {Ki Chang} and Gee, {Nancy A.} and Gee, {Shirley J.} and Hammock, {Bruce D.} and Lasley, {Bill L.}",
year = "2007",
month = "6",
day = "15",
doi = "10.1016/j.taap.2007.03.015",
language = "English (US)",
volume = "221",
pages = "278--284",
journal = "Toxicology and Applied Pharmacology",
issn = "0041-008X",
publisher = "Academic Press Inc.",
number = "3",

}

TY - JOUR

T1 - Antiandrogenic properties of parabens and other phenolic containing small molecules in personal care products

AU - Chen, Jiangang

AU - Ahn, Ki Chang

AU - Gee, Nancy A.

AU - Gee, Shirley J.

AU - Hammock, Bruce D.

AU - Lasley, Bill L.

PY - 2007/6/15

Y1 - 2007/6/15

N2 - To identify the androgenic potency of commonly used antimicrobials, an in vitro androgen receptor-mediated transcriptional activity assay was employed to evaluate the androgenic/antiandrogenic activity of parabens and selected other antimicrobials containing a phenolic moiety. This cell-based assay utilizes a stably transfected cell line that lacks critical steroid metabolizing enzymes and is formatted in a 96-well format. At a concentration of 10 μM, methyl-, propyl- and butyl-4-hydroxybenzoate (parabens) inhibited testosterone (T)-induced transcriptional activity by 40%, 33% and 19%, respectively (P < 0.05), while 4-hydroxybenzoic acid, the major metabolite of parabens, had no effect on T-induced transcriptional activity. Triclosan inhibited transcriptional activity induced by T by more than 92% at a concentration of 10 μM, and 38.8% at a concentration of 1.0 μM (P < 0.05). Thirty-four percent of T-induced transcriptional activity was inhibited by thymol at 10 μM (P < 0.05). Cell proliferation and/or cytotoxicity were not observed in any of the treatments. None of the compounds appeared to be androgenic when tested individually without T. The data presented in this report demonstrate that some widely used antimicrobial compounds have antiandrogenic properties and warrant further investigation to fully understand their potential impact on human reproductive health.

AB - To identify the androgenic potency of commonly used antimicrobials, an in vitro androgen receptor-mediated transcriptional activity assay was employed to evaluate the androgenic/antiandrogenic activity of parabens and selected other antimicrobials containing a phenolic moiety. This cell-based assay utilizes a stably transfected cell line that lacks critical steroid metabolizing enzymes and is formatted in a 96-well format. At a concentration of 10 μM, methyl-, propyl- and butyl-4-hydroxybenzoate (parabens) inhibited testosterone (T)-induced transcriptional activity by 40%, 33% and 19%, respectively (P < 0.05), while 4-hydroxybenzoic acid, the major metabolite of parabens, had no effect on T-induced transcriptional activity. Triclosan inhibited transcriptional activity induced by T by more than 92% at a concentration of 10 μM, and 38.8% at a concentration of 1.0 μM (P < 0.05). Thirty-four percent of T-induced transcriptional activity was inhibited by thymol at 10 μM (P < 0.05). Cell proliferation and/or cytotoxicity were not observed in any of the treatments. None of the compounds appeared to be androgenic when tested individually without T. The data presented in this report demonstrate that some widely used antimicrobial compounds have antiandrogenic properties and warrant further investigation to fully understand their potential impact on human reproductive health.

KW - Androgen receptor

KW - Bioassay

KW - Parabens

KW - Phenolic moiety

KW - Thymol

KW - Triclosan

UR - http://www.scopus.com/inward/record.url?scp=34249791786&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=34249791786&partnerID=8YFLogxK

U2 - 10.1016/j.taap.2007.03.015

DO - 10.1016/j.taap.2007.03.015

M3 - Article

C2 - 17481686

AN - SCOPUS:34249791786

VL - 221

SP - 278

EP - 284

JO - Toxicology and Applied Pharmacology

JF - Toxicology and Applied Pharmacology

SN - 0041-008X

IS - 3

ER -