Terasaki, Masanori; Kamata, Ryo; Shiraishi, Fujio; Makino, Masakazu published the artcile< Evaluation of estrogenic activity of parabens and their chlorinated derivatives by using the yeast two-hybrid assay and the enzyme-linked immunosorbent assay>, Application In Synthesis of 3964-57-6, the main research area is estrogenicity chlorinated paraben derivative estrogen receptor.
We assessed the estrogen agonist activities of 21 parabens and their chlorinated derivatives by using yeast two-hybrid assays incorporating either the human or medaka (Oryzias latipes) estrogen receptor α (hERα and medERα, resp.), and by using hERα competitive ELISA (ER-ELISA). In the two-hybrid assay with hERα, five parabens and three chlorinated derivatives exhibited estrogenic activity, and their relative activity (17β-estradiol [E2] = 1) ranged from 2.0 × 10-5 to 2.0 × 10-4, with the highest activity observed in i-butylparaben. In the medERα assay, six parabens and six chlorinated derivatives exhibited estrogenic activity and their relative activity ranged from 2.7 × 10-5 to 3.5 × 10-3, with the highest activity observed in benzylparaben, its monochlorinated derivative, i-butylparaben, and n-butylparaben. Although medERα demonstrated an activity to E2 that was three times lower than that demonstrated by hERα, medERα has a higher sensitivity to parabens than hERα (1.3-8.9 times). Five parabens and two chlorinated derivatives exhibited a binding affinity to ERα in the ER-ELISA; of the parabens, i-butylparaben exhibited the strongest binding affinity. The yeast two-hybrid assay and the ER-ELISA also revealed that many of the assayed chlorinated parabens were much weaker than the parent compound In addition, the results mainly showed that parabens with a bulk substituent (e.g., i-Bu and benzyl groups) had a higher activity than those with a sterically small substituent. It is considered that derivatization masks the apparent estrogenic activity of parabens, but the resulting chlorinated compounds may represent a potential hazard and therefore other toxicity tests should be performed to determine the toxicity of the chlorinated derivatives
Environmental Toxicology and Chemistry published new progress about Estrogen receptor α Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 3964-57-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, Application In Synthesis of 3964-57-6.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics