Sulfation of tibolone metabolites by human postmenopausal liver and small intestinal sulfotransferases (SULTs)

Min Wang; Christopher C. Ebmeier; John R. Olin; Robert J. Anderson

doi:10.1016/j.steroids.2005.11.003

Sulfation of tibolone metabolites by human postmenopausal liver and small intestinal sulfotransferases (SULTs)

Min Wang, Christopher C. Ebmeier, John R. Olin, Robert J. Anderson

Department of Medicine

Research output: Contribution to journal › Article › peer-review

14 Scopus citations

Abstract

Sulfation is a major pathway in humans for the biotransformation of steroid hormones and structurally related therapeutic agents. Tibolone is a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis. Sulfation inactivates the hydroxylated metabolites, 3α-hydroxytibolone (3α-OH-tibolone) and 3β-hydroxytibolone (3β-OH-tibolone), and contributes to the regulation of tissue responses to tibolone. We detected SULT1A1, SULT1A3, SULT1E1 and SULT2A1 mRNA expression by RT-PCR in postmenopausal liver and small intestine. Liver pool (n = 5) SULT activities measured with tibolone substrates reflected COS-1 expressed SULT2A1 and SULT1E1 activities. Liver SULT2A1 activity (1.8 ± 0.3 units/mg protein, n = 8, mean ± SEM), and activities with 3α-OH-tibolone (0.6 ± 0.1, n = 8) and 3β-OH-tibolone (0.9 ± 0.2, n = 8) were higher than SULT1E1 activities (

Original language	English (US)
Pages (from-to)	343-351
Number of pages	9
Journal	Steroids
Volume	71
Issue number	5
DOIs	https://doi.org/10.1016/j.steroids.2005.11.003
State	Published - May 2006

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Biology
Endocrinology
Pharmacology
Clinical Biochemistry
Organic Chemistry

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title = "Sulfation of tibolone metabolites by human postmenopausal liver and small intestinal sulfotransferases (SULTs)",

abstract = "Sulfation is a major pathway in humans for the biotransformation of steroid hormones and structurally related therapeutic agents. Tibolone is a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis. Sulfation inactivates the hydroxylated metabolites, 3α-hydroxytibolone (3α-OH-tibolone) and 3β-hydroxytibolone (3β-OH-tibolone), and contributes to the regulation of tissue responses to tibolone. We detected SULT1A1, SULT1A3, SULT1E1 and SULT2A1 mRNA expression by RT-PCR in postmenopausal liver and small intestine. Liver pool (n = 5) SULT activities measured with tibolone substrates reflected COS-1 expressed SULT2A1 and SULT1E1 activities. Liver SULT2A1 activity (1.8 ± 0.3 units/mg protein, n = 8, mean ± SEM), and activities with 3α-OH-tibolone (0.6 ± 0.1, n = 8) and 3β-OH-tibolone (0.9 ± 0.2, n = 8) were higher than SULT1E1 activities (",

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AU - Anderson, Robert J.

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