Inhibition of androgen metabolism and binding by a liposterolic extract of “serenoa repens B” in human foreskin fibroblasts

Sultan, Charles; Terraza, Annie; Devillier, Claude; Carilla, Elisabeth; Briley, Mike; Loire, Corinne; Descomps, Bernard

doi:10.1016/0022-4731(84)90264-4

Cited by 130 publications

(61 citation statements)

References 15 publications

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“…SPE is constituted of both saturated and unsaturated fatty acids by more than 90%, which are present in mixture of free and esterified forms. 4 SPE has an ability to inhibit type 1 and 2 isozymes of 5a-reductase, 5,6 and other biological functions of SPE were found to stimulate the a1-adrenoceptor, 7 and produce anti-androgenic, 8 anti-proliferative, 9 and anti-inflammatory effects. 10 Recently, our group demonstrated that SPE could inhibit specific bindings of radioligands for muscarinic and 1,4-dihydropyridine calcium channel (1,4-DHP) receptors.…”

Section: Introductionmentioning

confidence: 99%

Isolation and Pharmacological Characterization of Fatty Acids from Saw Palmetto Extract

Abe

Ito

Suzuki³

et al. 2009

ANAL. SCI.

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Saw palmetto extract (SPE) has been widely used for the treatment of lower urinary-tract symptoms secondary to benign prostatic hyperplasia. The mechanisms of pharmacological effects of SPE include the inhibition of 5a-reductase, antiandrogenic effects, anti-proliferative effects, and anti-inflammatory effects. Previously, we showed that SPE bound actively to a1-adrenergic, muscarinic and 1,4-dihydropyridine calcium channel (1,4-DHP) receptors in the prostate and bladder of rats, whereas its active constituents have not been fully clarified. The present investigation is aimed to identify the main active components contained in hexane and diethyl ether extracts of SPE with the use of column chromatography and preparative HPLC. Based on the binding activity with a1-adrenergic, muscarinic, and 1,4-DHP receptors, both isolated oleic and lauric acids were deduced to be active components. Authentic samples of oleic and lauric acids also exhibited similar binding activities to these receptors as the fatty acids isolated from SPE, consistent with our findings. In addition, oleic and lauric acids inhibited 5a-reductase, possibly leading to therapeutic effects against benign prostatic hyperplasia and related lower urinary-tract symptoms.

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Section: Introductionmentioning

confidence: 99%

Isolation and Pharmacological Characterization of Fatty Acids from Saw Palmetto Extract

Abe

Ito

Suzuki³

et al. 2009

ANAL. SCI.

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“…Only the extract obtained from Serenoa repens (Permixon®) has been tested in vitro (isolated prostate tis sues) and was reported to have 5a-reductase inhibitory activity [13].Recent data provided by Rhodes et al [14] have shown that Permixon has very weak antiandrogen or 5a-reductase inhibitory activity in castrated rats that were stimulated with T or DHT. The purpose of this open, comparative, randomized, placebo-controlled study was to investigate in humans the inhibitory effect of Permixon on 5a-reductase in comparison with finasteride, a known potent 5a-reductase inhibitor.…”

Section: Radioimmunoassaymentioning

confidence: 99%

Comparison of Finasteride (Proscar®) and Serenoa repens (Permixon®) in the Inhibition of 5-Alpha Reductase in Healthy Male Volunteers

Strauch¹,

Perles²,

Vergult³

et al. 1994

Eur Urol

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“…4,5) Other pharmacodynamic mechanisms of SPE have also been proposed, including anti-androgenic effects, anti-proliferative effects and anti-inflammatory effects. [6][7][8] Our recent study has shown that the intraduodenal administration of SPE in the rat cystometry resulted in a significant and dose-related increase in micturition interval as well as a decrease in micturition volume and bladder capacity caused by the infusion of 0.1% acetic acid.9) Furthermore, we have reported that SPE inhibited the specific binding of radioligands to a 1 -adrenergic, muscarinic and 1,4-dihydropyridine (1,4-DHP) calcium channel antagonist receptors in the lower urinary tract of rats.9-11) However, the exact active constituents of SPE remain to be identified. SPE contains mainly saturated and unsaturated fatty acids (90%).…”

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confidence: 99%

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confidence: 99%

Pharmacologically Relevant Receptor Binding Characteristics and 5.ALPHA.-Reductase Inhibitory Activity of Free Fatty Acids Contained in Saw Palmetto Extract

Abe

Ito

Oyunzul

et al. 2009

Biological & Pharmaceutical Bulletin

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Benign prostatic hyperplasia (BPH) and related lower urinary tract symptoms (LUTS) are common disorders in aging men. Plant extracts are widely used in the treatment of BPH and related LUTS. In fact, phytotherapeutic agents, including saw palmetto extract (SPE), are very popular in many European countries as herbal remedies, representing up to 80% of all drugs prescribed for these disorders.1,2) An analysis of many clinical trials showed mild to moderate improvements in symptom scores and urinary flow in patients with BPH.3)The most widely known effect of SPE is the inhibition of type 1 and 2 isozymes of 5a-reductase. 4,5) Other pharmacodynamic mechanisms of SPE have also been proposed, including anti-androgenic effects, anti-proliferative effects and anti-inflammatory effects. [6][7][8] Our recent study has shown that the intraduodenal administration of SPE in the rat cystometry resulted in a significant and dose-related increase in micturition interval as well as a decrease in micturition volume and bladder capacity caused by the infusion of 0.1% acetic acid.9) Furthermore, we have reported that SPE inhibited the specific binding of radioligands to a 1 -adrenergic, muscarinic and 1,4-dihydropyridine (1,4-DHP) calcium channel antagonist receptors in the lower urinary tract of rats.9-11) However, the exact active constituents of SPE remain to be identified. SPE contains mainly saturated and unsaturated fatty acids (90%). Among these fatty acids, the major constituents are oleic acid and lauric acid, which together compose more than 50% of SPE.12) The aim of this study is to investigate binding activities for pharmacologically relevant (a 1 -adrenergic, muscarinic, 1,4-DHP calcium channel antagonist) receptors of major fatty acids contained in SPE. In addition, with a newly developed method using LC/MS, the effects of SPE and its fatty acids on 5a-reductase activity in the rat liver were also examined. MATERIALS AND METHODSMaterials SPE (Serenoa repens purified extract) was kindly provided by Indena Japan (Tokyo, Japan). SPE was obtained with hypercritical CO 2 (SABAL SELECT, Indena S.p.A., Milan, Italy). The constituents contained in SPE are presented elsewhere.12) Oleic acid, lauric acid, myristic acid, palmitic acid and linoleic acid were purchased from Tokyo Chemical Industry (Tokyo, Japan), Nacalai Tesque (Kyoto, Japan), Sigma-Aldrich (St. Louis, MO, U.S.A.) and Wako Pure Chemicals (Osaka, Japan), respectively. [ Animals Male and female Sprague-Dawley rats at 8-10 weeks of age (Japan SLC Inc., Shizuoka, Japan) were housed in the laboratory with free access to a normal diet (CE-2, CREA Japan Inc., Tokyo, Japan) and water, and maintained on a 12-h light-dark cycle in a room with controlled temperature and humidity. The study was conducted in accordance with the guidelines of the Experimental Ani- to bind a a 1 -adrenergic, muscarinic and 1,4-dihydropyridine (1,4-DHP The results suggest that lauric acid and oleic acid bind noncompetitively to a a 1 -adrenergic, muscarinic and 1,4-DHP calcium channel antagonist...

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Inhibition of androgen metabolism and binding by a liposterolic extract of “serenoa repens B” in human foreskin fibroblasts

Cited by 130 publications

References 15 publications

Isolation and Pharmacological Characterization of Fatty Acids from Saw Palmetto Extract

Isolation and Pharmacological Characterization of Fatty Acids from Saw Palmetto Extract

Comparison of Finasteride (Proscar®) and Serenoa repens (Permixon®) in the Inhibition of 5-Alpha Reductase in Healthy Male Volunteers

Pharmacologically Relevant Receptor Binding Characteristics and 5.ALPHA.-Reductase Inhibitory Activity of Free Fatty Acids Contained in Saw Palmetto Extract

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