Estrogenic activity of 37 components of commercial sunscreen lotions evaluated by in vitro assays.
Thirty-seven chemical components of commercial sunscreen lotions were evaluated for estrogen agonistic and/or antagonistic activity using two in vitro assays, (1) an ELISA-based estrogen receptor competitive binding assay (ER-ELISA) and (2) a modified yeast two-hybrid estrogen assay, with and without addition of a rat liver preparation, S9 mix. Eleven compounds, most of which were benzophenone derivatives and parabens, showed binding affinity to ER by ER-ELISA without S9 mix. Although the activities of almost all of the compounds were attenuated by addition of S9 mix, 4-octylphenylsalicylate and 2,2'-dihydroxy-4,4'-dimethoxybenzophenone acquired estrogenic activity, suggesting metabolic activation of these compounds. Two benzophenones showed agonistic activity in the yeast two-hybrid assay without S9 mix. The activity of one of these was reduced by S9 treatment and a further two benzophenones was activated. Eight parabens were active in this assay without S9 exposure, but their activities were eliminated by S9 treatment. Benzophenones with para-phenolic hydroxyl groups and parabens with branched and/or longer linear chains were generally more potent in both bioassays. In addition, weak antagonistic activity of 4-t-butylphenyl-salicylate, 2-ethylhexyl 4-dimethylaminobenzoate and (+/-)-alpha-tocopherolacetate was observed with S9 treatment. In vivo testing of the compounds reported here to have estrogen agonistic and antagonistic activities is required to confirm their effects at an organismal level.
Morohoshi
K
K
National Institute for Environmental Studies, Endocrine Disruptors and Dioxin Research Project, 16-2 Onogawa, Tsukuba, Ibaraki 305-8506, Japan.
Yamamoto
H
H
Kamata
R
R
Shiraishi
F
F
Koda
T
T
Morita
M
M
D000818:Animals; D000975:Antioxidants / Q000494:pharmacology; D001565:Benzoates / Q000494:pharmacology; D001577:Benzophenones / Q000494:pharmacology; D004797:Enzyme-Linked Immunosorbent Assay; D004965:Estrogen Antagonists / Q000494:pharmacology; D047628:Estrogen Receptor alpha / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism; D004968:Estrogens, Non-Steroidal; D066298:In Vitro Techniques; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D010226:Parabens / Q000494:pharmacology; D011310:Preservatives, Pharmaceutical / Q000494:pharmacology; D051381:Rats; D012441:Saccharomyces cerevisiae / Q000187:drug effects / Q000378:metabolism; D012459:Salicylates / Q000494:pharmacology; D013347:Subcellular Fractions / Q000187:drug effects / Q000378:metabolism; D013473:Sunscreening Agents / Q000494:pharmacology*; D014230:Triazoles / Q000494:pharmacology; D014466:Ultraviolet Rays
D000975:Antioxidants; D001565:Benzoates; D001577:Benzophenones; D004965:Estrogen Antagonists; D047628:Estrogen Receptor alpha; D004968:Estrogens, Non-Steroidal; D010226:Parabens; D011310:Preservatives, Pharmaceutical; D012459:Salicylates; D013473:Sunscreening Agents; D014230:Triazoles