In vitro study of Organization for Economic Co-operation and Development (OECD) endocrine disruptor screening and testing methods- establishment of a recombinant rat androgen receptor (rrAR) binding assay.
The androgen receptor (AR) binding assay can be used to determine the ability of probable endocrine disruptors (EDs) to compete with synthetic androgen methyltrienolone (R1881) for binding to recombinant rat AR (rrAR). In this study, we assessed AR binding of various chemicals using Lexius Freyberger's method. The rank of relative binding affinity (RBA, IC(50)) on the tested chemicals was trenbolone 1.3 x 10(-8) M (RBA 138) > dihydrotesterone (DHT) 1.8 x 10(-8) M (RBA 100) > methyl testosterone 5.7 x 10(-8) M (RBA 31.6) > nonylphenol (NP) 1.3 x 10(-5) M (RBA 0.14) > bisphenol A (BPA) 1.1 x 10(-4) M (RBA 0.016) > isobutyl paraben 3.1 x 10(-4) M (RBA 0.0058) > butyl paraben 6.2 x 10(-4) M (RBA 0.0029) > propyl paraben 9.7 x 10(-4) M (RBA 0.0019). However, di(n-butyl) phthalate (DBP) and di(2-ethylhexyl) phthalate (DEHP), known anti-androgenic chemicals, did not show any significant AR binding activity. Our data suggests that in vitro AR binding assay may be useful as a screening tool for potential EDs.
Kim
Tae Sung
TS
Yoon
Chang Yong
CY
Jung
Ki Kyung
KK
Kim
Soon Sun
SS
Kang
Il Hyun
IH
Baek
Jung Hee
JH
Jo
Min Soo
MS
Kim
Hyung Sik
HS
Kang
Tae Seok
TS
D000818:Animals; D003993:Dibutyl Phthalate / Q000378:metabolism; D013196:Dihydrotestosterone / Q000378:metabolism; D052244:Endocrine Disruptors / Q000378:metabolism*; D015741:Metribolone / Q000378:metabolism; D051381:Rats; D011944:Receptors, Androgen / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism
D052244:Endocrine Disruptors; D011944:Receptors, Androgen; D011994:Recombinant Proteins; D013196:Dihydrotestosterone; D003993:Dibutyl Phthalate; D015741:Metribolone