Two natural 5-androstene steroid tetrols, androst-5-ene-3 beta,7 beta,16 alpha,17 beta-tetrol (HE3177) and androst-5-ene-3 alpha,7 beta,16 alpha,17 beta-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. (C) 2010 Elsevier Inc. All rights reserved.
Two natural 5-androstene steroid tetrols, androst-5-ene-3 beta,7 beta,16 alpha,17 beta-tetrol (HE3177) and androst-5-ene-3 alpha,7 beta,16 alpha,17 beta-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. (C) 2010 Elsevier Inc. All rights reserved.
Novel components of the human metabolome: The identification, characterization and anti-inflammatory activity of two 5-androstene tetrols
MANGANO, KATIA DOMENICA;NICOLETTI, FERDINANDO;
2011-01-01
Abstract
Two natural 5-androstene steroid tetrols, androst-5-ene-3 beta,7 beta,16 alpha,17 beta-tetrol (HE3177) and androst-5-ene-3 alpha,7 beta,16 alpha,17 beta-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. (C) 2010 Elsevier Inc. All rights reserved.File | Dimensione | Formato | |
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