| Comparison of 7α-methyl-19-nortestosterone effectiveness alone or combined with progestins on androgen receptor mediated transactivation. | |
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MedLine Citation:
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PMID: 22065861 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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7α-Methyl-19-nortestosterone (MENT) is an androgen with potent gonadotropin inhibitory activity and prostate-sparing effects. These attributes give MENT advantages over testosterone (T) as a male contraceptive, but, as in the case of T, a partial dose-dependent suppression of spermatogenesis has been observed. Combination of T or MENT with synthetic progestins improves the rate of azoospermia; however, it is unknown whether these combinations affect hormone androgenicity or exert synergistic effects via progestational or androgenic interaction. Herein, using transactivation assays, we examined the ability of MENT alone or combined with several 19-nor derived synthetic progestins to activate androgen receptor (AR)-dependent gene transcription. In addition, the capability of 7α-methyl-E2, an aromatized metabolite of MENT, to transactivate gene transcription via estrogen receptor α (ERα) or ERβ was also investigated. As expected, MENT induced gene transactivation through either the progesterone receptor (PR) or the AR. MENT showed a similar efficiency as P to activate PR-mediated reporter gene expression, but it was ten times more potent than T and DHT in activation of AR-driven gene expression. Addition of increasing concentrations of other 19-nortestosterone derivatives (NET or LNG) did not affect, in a significant manner, the ability of MENT to activate AR-dependent reporter gene transcription, the same results were obtained with different cell lines. 7α-methyl-E2 resulted in potent estrogen activity via both ER subtypes with efficiency similar to natural E2. These results suggest that addition of 19-nortestosterone derived progestins, as a hormonal adjuvant in male fertility strategies for effective spermatogenic suppression, does not display any detrimental effect that would interfere with MENT androgenic transcriptional activity. |
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Authors:
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Rocio Becerra-Garcia; David Ordaz-Rosado; Gabriela Noé; Bertha Chávez; Austin J Cooney; Fernando Larrea |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-11-7 |
Journal Detail:
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Title: Reproduction (Cambridge, England) Volume: - ISSN: 1741-7899 ISO Abbreviation: - Publication Date: 2011 Nov |
Date Detail:
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Created Date: 2011-11-8 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 100966036 Medline TA: Reproduction Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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R Becerra-Garcia, Reproductive Biology, National Institute of Nutrition, Mexico, Mexico. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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