Linked Life Data

12477490

Source:http://linkedlifedata.com/resource/pubmed/id/12477490

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2-3
pubmed:dateCreated
2002-12-12
pubmed:abstractText
In different cell systems, the lipido-sterolic extract of Serenoa repens (LSESr, Permixon inhibits both type 1 and type 2 5alpha-reductase activity (5alphaR1 and 5alphaR2). LSESr is mainly constituted of fatty acids (90+/-5%) essentially as free fatty acids (80%). Among these free fatty acids, the main components are oleic and lauric acids which represent 65% and linoleic and myristic acids 15%. To evaluate the inhibitory effect of the different components of LSESr on 5alphaR1 or 5alphaR2 activity, the corresponding type 1 and type 2 human genes have been cloned and expressed in the baculovirus-directed insect cell expression system Sf9. The cells were incubated at pH 5.5 (5alphaR2) and pH 7.4 (5alphaR1) with 1 or 3nM testosterone in presence or absence of various concentrations of LSESr or of its different components. Dihydrotestosterone formation was measured with an automatic system combining HPLC and an on-line radiodetector. The inhibition of 5alphaR1 and 5alphaR2 activity was only observed with free fatty acids: esterified fatty acids, alcohols as well as sterols assayed were inactive. A specificity of the fatty acids in 5alphaR1 or 5alphaR2 inhibition has been found. Long unsaturated chains (oleic and linolenic) were active (IC(50)=4+/-2 and 13+/-3 microg/ml, respectively) on 5alphaR1 but to a much lesser extent (IC(50)>100 and 35+/-21 microg/ml, respectively) on 5alphaR2. Palmitic and stearic acids were inactive on the two isoforms. Lauric acid was active on 5alphaR1 (IC(50)=17+/-3 microg/ml) and 5alphaR2 (IC(50)=19+/-9 microg/ml). The inhibitory activity of myristic acid was evaluated on 5alphaR2 only and found active on this isoform (IC(50)=4+/-2 microg/ml). The dual inhibitory activity of LSESr on 5alpha-reductase type 1 and type 2 can be attributed to its high content in free fatty acids.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
http://linkedlifedata.com/resource/pubmed/chemical/Androgen Antagonists, http://linkedlifedata.com/resource/pubmed/chemical/Cholestenone 5 alpha-Reductase, http://linkedlifedata.com/resource/pubmed/chemical/Fatty Acids, Nonesterified, http://linkedlifedata.com/resource/pubmed/chemical/Fatty Alcohols, http://linkedlifedata.com/resource/pubmed/chemical/Hypolipidemic Agents, http://linkedlifedata.com/resource/pubmed/chemical/Isoenzymes, http://linkedlifedata.com/resource/pubmed/chemical/Oxidoreductases, http://linkedlifedata.com/resource/pubmed/chemical/Permixon, http://linkedlifedata.com/resource/pubmed/chemical/Plant Extracts, http://linkedlifedata.com/resource/pubmed/chemical/Sitosterols, http://linkedlifedata.com/resource/pubmed/chemical/Tocopherols, http://linkedlifedata.com/resource/pubmed/chemical/docosanol, http://linkedlifedata.com/resource/pubmed/chemical/sitosterol
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0960-0760
pubmed:author
pubmed:issnType
Print
pubmed:volume
82
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
233-9
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed:year
2002
pubmed:articleTitle
Inhibition of type 1 and type 2 5alpha-reductase activity by free fatty acids, active ingredients of Permixon.
pubmed:affiliation
D.R.I.T.T., Université Pierre et Marie Curie, 4 Place Jussieu, Paris, France. jean-pierre.raynaud@admp6.jussieu.fr
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't