Abstract:
:Androgens' metabolism and activity are gaining a more and more important role in human physiology particularly referring to aging and to neurodegenerative diseases. Androgen treatment is often required for long-lasting disorders. In order to improve their duration and effects, androgens can be administered as esters of carboxylic acids. The novelty of our research is the use of esters of androgens with specific unsaturated fatty acids, in order to reduce possible side effects particularly related to chronic pathologies with altered lipid homeostasis such as X-linked adrenoleukodystrophy and cardiovascular disorders. Thus the esters of the main androgenic substances testosterone, dihydrotestosterone (DHT) and their metabolite 5α-androstan-3α,17β-diol were chemically obtained by coupling with different unsaturated fatty acids. To this aim, fatty acids with various degree of unsaturation and belonging to different series were selected. Specifically, oleic acid (18:1, n-9), linoleic acid (18:2, n-6), and the n-3 fatty acids, α-linolenic acid (18:3), eicosapentaenoic acid (EPA, 20:5), and docosahexaenoic acid (DHA, 22:6) were used obtaining corresponding esters with acceptable yields and good degree of purity. All the synthesized compounds were tested for their cytotoxic activities in mouse NIH3T3 and human astrocyte cell lines. The esters demonstrated good tolerability and no in vitro cytotoxic effect in both cell cultures. After these promising preliminary results, the esters will be suitable for in vivo studies in order to ascertain their pharmacokinetic characteristics and their biological effects.
journal_name
J Endocrinol Investjournal_title
Journal of endocrinological investigationauthors
Aiello F,Garofalo A,Aloisi AM,Lamponi S,Magnani A,Petroni Adoi
10.3275/8655subject
Has Abstractpub_date
2013-06-01 00:00:00pages
390-5issue
6eissn
0391-4097issn
1720-8386pii
8655journal_volume
36pub_type
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journal_title:Journal of endocrinological investigation
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journal_title:Journal of endocrinological investigation
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journal_title:Journal of endocrinological investigation
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journal_title:Journal of endocrinological investigation
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journal_title:Journal of endocrinological investigation
pub_type: 杂志文章
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journal_title:Journal of endocrinological investigation
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journal_title:Journal of endocrinological investigation
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journal_title:Journal of endocrinological investigation
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