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 |
|---|---|
| Pages (from-to) | 343-351 |
| Number of pages | 9 |
| Journal | Steroids |
| Volume | 71 |
| Issue number | 5 |
| DOIs | |
| State | Published - May 2006 |
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All Science Journal Classification (ASJC) codes
- Biochemistry
- Endocrinology
- Molecular Biology
Cite this
Sulfation of tibolone metabolites by human postmenopausal liver and small intestinal sulfotransferases (SULTs). / Wang, Min; Ebmeier, Christopher C.; Olin, John R.; Anderson, Robert J.
In: Steroids, Vol. 71, No. 5, 05.2006, p. 343-351.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Sulfation of tibolone metabolites by human postmenopausal liver and small intestinal sulfotransferases (SULTs)
AU - Wang, Min
AU - Ebmeier, Christopher C.
AU - Olin, John R.
AU - Anderson, Robert J.
PY - 2006/5
Y1 - 2006/5
N2 - 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 (
AB - 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 (
UR - http://www.scopus.com/inward/record.url?scp=33646074319&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=33646074319&partnerID=8YFLogxK
U2 - 10.1016/j.steroids.2005.11.003
DO - 10.1016/j.steroids.2005.11.003
M3 - Article
C2 - 16360722
AN - SCOPUS:33646074319
VL - 71
SP - 343
EP - 351
JO - Steroids
JF - Steroids
SN - 0039-128X
IS - 5
ER -