Effect of the Lipidosterolic Extract of Serenoa repens (Permixon&lt;sup&gt;&amp;reg;&lt;/sup&gt;) and Its Major Components on Basic Fibroblast Growth Factor-Induced Proliferation of Cultures of Human Prostate Biopsies

Paubert-Braquet, Monique; Cousse, Henri; Raynaud, Jean‐Pierre; Mencia‐Huerta, Jean Michel; Braquet, P.

doi:10.1159/000019570

Cited by 68 publications

(35 citation statements)

References 15 publications

(13 reference statements)

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“…One interesting possibility comes from the recent observation that geraniol activates TRPM8 (18). The PP i ester of geraniol is an intermediate in cholesterol synthesis (26), and geraniol enhances cell proliferation in prostate epithelium (27). Thus, it is possible that in prostate epithelial cells, TRPM8 is involved in the regulation of cell proliferation and responds to geraniol as an intracellular messenger.…”

Section: Discussionmentioning

confidence: 99%

Evidence that TRPM8 Is an Androgen-Dependent Ca2+ Channel Required for the Survival of Prostate Cancer Cells

2004

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The Ca 2؉ -permeable channel TRPM8 is thought to play an important role in the pathophysiology of prostate cancer. We have investigated the intracellular location of TRPM8 and its role as a Ca 2؉ -permeable channel in an androgen-responsive and an androgen-insensitive prostate cancer cell line. We report evidence from immunofluorescence experiments that in the androgen-responsive LNCaP cell line, the TRPM8 protein is expressed in the endoplasmic reticulum and plasma membrane, acts as a Ca 2؉ -permeable channel (assessed using Fura-2 to measure increases in the cytoplasmic Ca 2؉ concentration) in each of these membranes, and is regulated by androgen. Although TRPM8 was detected in the androgeninsensitive PC-3 cell line, no evidence was obtained for regulation of its expression by androgen. The results of experiments using LNCaP cells, the TRPM8 antagonist capsazepine, and small interference RNA targeted to TRPM8 indicate that TRPM8 is required for cell survival. These results indicate that TRPM8 is an important determinator of Ca 2؉ homeostasis in prostate epithelial cells and may be a potential target for the action of drugs in the management of prostate cancer.

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Section: Discussionmentioning

confidence: 99%

Evidence that TRPM8 Is an Androgen-Dependent Ca2+ Channel Required for the Survival of Prostate Cancer Cells

2004

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“…One interesting possibility comes from the recent observation that geraniol activates TRPM8 (Behrendt et al 2004). The pyrophosphate ester of geraniol is an intermediate in cholesterol synthesis (Voet & Voet 1990), and geraniol enhances cell proliferation in prostate epithelium (Paubert-Braquet et al 1998). Thus it is possible that, in prostate epithelial cells, TRPM8 is involved in the regulation of cell proliferation and responds to geraniol as an intracellular messenger (Zhang & Barritt 2004).…”

Section: Physiological Functions Of Trpm8 In Prostate Cancer Cellsmentioning

confidence: 99%

TRPM8 in prostate cancer cells: a potential diagnostic and prognostic marker with a secretory function?

Zhang

Barritt

2006

Endocr Relat Cancer

130

108

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During the past 5 years it has emerged that the transient receptor potential (TRP) family of Ca 2+ -and Na + -permeable channels plays a diverse and important role in cell biology and in pathology. One member of this family, TRPM8, is highly expressed in prostate cancer cells but the physiological and pathological functions of TRPM8 in these cells are not known. Here we address these questions, and the issue of whether or not TRPM8 is an effective diagnostic and prognostic marker in prostate cancer. TRPM8 is known to be activated by cool stimuli (17-25 C) and cooling compounds such as menthol. The activation mechanism(s) involves voltage sensing of membrane potential, phosphatidylinositol 4,5-bisphosphate and Ca 2+. In addition to prostate cancer cells, TRPM8 is expressed in sensory neurons where it acts as a sensor of cold. In prostate epithelial cells, expression of TRPM8 is regulated by androgen and is elevated in androgen-sensitive cancerous cells compared with normal cells. While there is some evidence that in prostate cancer cells Ca 2+ and Na + inflow through TRPM8 is necessary for survival and function, including secretion at the apical membrane, the function of TRPM8 in these cells is not really known. It may well differ from the role of TRPM8 as a cool sensor in sensory nerve cells. Androgen unresponsive prostate cancer is difficult to treat effectively and there are limited diagnostic and prognostic markers available. TRPM8 is a potential tissue marker in differential diagnosis and a potential prognostic marker for androgen-unresponsive and metastatic prostate cancer. As a consequence of its ability to convey Ca 2+ and Na + and its expression in only a limited number of cell types, TRPM8 is considered to be a promising target for pharmaceutical, immunological and genetic interventions for the treatment of prostate cancer.

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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%).…”

mentioning

confidence: 99%

mentioning

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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Effect of the Lipidosterolic Extract of Serenoa repens (Permixon<sup>®</sup>) and Its Major Components on Basic Fibroblast Growth Factor-Induced Proliferation of Cultures of Human Prostate Biopsies

Cited by 68 publications

References 15 publications

Evidence that TRPM8 Is an Androgen-Dependent Ca2+ Channel Required for the Survival of Prostate Cancer Cells

Evidence that TRPM8 Is an Androgen-Dependent Ca2+ Channel Required for the Survival of Prostate Cancer Cells

TRPM8 in prostate cancer cells: a potential diagnostic and prognostic marker with a secretory function?

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

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