5-Androstenediol Ameliorates Pleurisy, Septic Shock, and Experimental Autoimmune Encephalomyelitis in Mice

Table 2

Transactivation EC₅₀ values for dihydrotestosterone (DHT), estradiol (E₂) and androstenediol (5-AED) for AR, ER𝛼 and ER𝛽.

Ligand	Experimental System*
	MDA-kb2^(a)	T47D-kBluc^(b)	ER𝛽-HEK293^(c)
DHT	0.06 nM ± 0.01 (9)	112 nM (1)	409 nM ± 92 (6)
E2	851 nM ± 172 (6)	0.001 nM ± 0.0003 (5)	0.06 nM ± 0.02 (9)
5-AED	2969 nM ± 790 (7)	2.5 nM ± 0.76 (4)	1.7 nM ± 0.26 (7)**

^∗Results are expressed as EC₅₀ values in nM units, representing the statistical mean ± SEM. The numbers in parenthesis represent the number of independent experiments performed (𝑛 value).
^(a)MDA-kb2 cells are stably transfected with a promoter/ reporter construct sensitive to sex steroid receptor stimulation fused upstream of (MMTV promoter) a luciferase reporter gene. These cells endogenously express both AR and glucocorticoid receptors.
^(b)T47D-kBluc cells are stably transfected with a synthetic promoter/ reporter construct sensitive to estrogenic stimulation, consisting of 3 copies of the estrogen response element- (ERE-) fused upstream of a luciferase reporter gene. These cells express endogenously both ER𝛼 and ER𝛽.
^(c)ER𝛽-HEK293 cells are transiently cotransfected with an ERE/luciferase promoter/reporter construct and a cDNA expression vector encoding the full length human ER𝛽. These cells exhibit virtually undetectable levels of endogenous sex steroid receptors.
^∗∗Although a total of 9 experiments were initially conducted, results from two experiments were discarded as clear outliers on the basis that their values fell >1.5 times the interquartile range above the third quartile of the entire dataset (standard statistical criterion for defining outlier values for a normally distributed population).