Article ID Journal Published Year Pages File Type
2028788 Steroids 2011 11 Pages PDF
Abstract

Two natural 5-androstene steroid tetrols, androst-5-ene-3β,7β,16α,17β-tetrol (HE3177) and androst-5-ene-3α,7β,16α,17β-tetrol (HE3413), were discovered in human plasma and urine. These compounds had significant aqueous solubility, did not bind or transactivate steroid-binding nuclear hormone receptors, and were not immunosuppressive in murine mixed-lymphocyte studies. Both compounds appear to be metabolic end products, as they were resistant to primary and secondary metabolism. Both were orally bioavailable, and were very well tolerated in a two-week dose-intensive toxicity study in mice. Anti-inflammatory properties were found with exogenous administration of these compounds in rodent disease models of multiple sclerosis, lung injury, chronic prostatitis, and colitis.

Research highlights▶ 5-Androstene tetrols are DHEA metabolites found naturally in human plasma. ▶ Tetrols are orally bioavailable and resistant to primary and secondary metabolism. ▶ Tetrols do not bind or transactivate steroid binding nuclear hormone receptors. ▶ Exogenous tetrols are very well tolerated in murine toxicity studies. ▶ Exogenous tetrols have anti-inflammatory activity in rodent models.

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Life Sciences Biochemistry, Genetics and Molecular Biology Biochemistry
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