| Pygeum Africanum,
Urtica Dioica, Sabal serrulata, Curcurbitae pepo, Serenoa Repens. AT MIDNIGHT
***********************************
PYGEUM AFRICANUM, URTICA DIOICA,
SABAL SERRULATA, CURCURBITAE PEPO,
SERENOA REPENS
*************************************
****** DERMAGIC-EXPRESS No.61 *******
****** 17 JUNIO DE 1.999 ***********
17 JUNE 1.999
**************************************
***************************************
EDITORIAL ESPAÑOL
=================
Hola amigos de la Red,,, a la MEDIANOCHE, de esta semana navegue por el cyber, buscando alternativas terapeuticas para la hiperplasia prostatica benigna y encontré estas 31 interesantes referencias.
Estos extractos vegetales estudiados cientificamente han demostrado ser altamente efectivos en dicha enfermedad, de modo pues que este DERMAGIC no DERMATOLOGICO,,, espero les sea bastante util
En Venezuela se consiguen 2 de estos productos,,, el PROSTATONIN,,, combinacion de Urtica dioica y Pygeum africanum (una maravilla de producto) de origen Suizo, y el PERMIXON (Serenoa Repens) inhibidor de la alfa 5 reductasa y por lo tanto una alternativa para loas personas que no toleran el finasteride.
Espero las disfruten...
Saludos a todos !!!
Dr. Jose Lapenta R.,,,
EDITORIAL ENGLISH
=================
Hello friends of the Net, at MIDNIGHT, of this week i navigate for the cyber, looking for therapeutic alternatives for the benign prostatic hyperplasia and I found these 31 interesting references.
These vegetable extracts studied scientifically have demonstrated to be highly effective in this illness, I Think that this DERMAGIC non DERMATOLOGIC, will be quite useful for all.
In Venezuela 2 of these products are available, the PROSTATONIN, combination of Urtica dioica and Pygeum africanum (a marvel product) of Swiss origin, and the PERMIXON (Serenoa Repens) 5 alpha-reductase inhibitor, and therefore an alternative for people that don't tolerate the finasteride.
I hope enjoy it....
Greetings to ALL, !!
Dr. Jose Lapenta R.,,,
=====================================================================
A LA MEDIANOCHE / AT MIDNIGHT
*********************************************************************
PYGEUM AFRICANUM, URTICA DIOICA, SABAL SERRULATA,
CURCURBITAE PEPO,SERENOA REPENS
=====================================================================
1.) Efficacy and acceptability of tadenan (Pygeum africanum extract) in the treatment of benign prostatic hyperplasia (BPH): a multicentre trial in central Europe.
2.) Antiproliferative effect of Pygeum africanum extract on rat prostatic fibroblasts.
3.) Cellular and molecular aspects of bladder hypertrophy.
4.) Effect of Pygeum africanum extract on A23187-stimulated production of lipoxygenase metabolites from human polymorphonuclear cells.
5.) Combined extracts of Urtica dioica and Pygeum africanum in the treatment of benign prostatic hyperplasia: double-blind comparison of two doses.
6.) [Urological and sexual evaluation of treatment of benign prostatic disease using Pygeum africanum at high doses].
7.) [Efficacy of Pygeum africanum extract in the medical therapy of urination disorders due to benign prostatic hyperplasia: evaluation of objective and subjective parameters. A placebo-controlled double-blind multicenter study].
8.) [Controlled study of the effects of Pygeum africanum extract on the functional symptoms of prostatic adenoma].
9.) Treatment of benign prostatic hyperplasia with phytosterols.
10.) [Sabal serrulata extract in the management of symptoms of prostatic hypertrophy].
11.) Enzyme activities in tissue of human benign prostatic hyperplasia after three months' treatment with the Sabal serrulata extract IDS 89 (Strogen) or placebo.
12.) Drug therapy of benign prostatic hyperplasia].
13.) Effects of the sabal serrulata extract IDS 89 and its subfractions on 5 alpha-reductase activity in human benign prostatic hyperplasia.
14.) Sabal serrulata extract (Strogen forte) in the treatment of symptomatic benign prostatic hyperplasia.
15.) In vitro inhibition of testicular delta 5-3 beta-hydroxysteroid dehydrogenase and prostatic 5 alpha-reductase activities in rats and humans by strogen forte extract.
16.) Mechanisms involved in the spasmolytic effect of extracts from Sabal serrulata fruit on smooth muscle.
17.) [Benign prostatic hyperplasia--treatment with sabal fruit extract. A treatment study of 1,334 patients].
18.) Experience in treating benign prostatic hypertrophy with Sabal serrulata for one year.
19.) [Anti-inflammatory activity of sabal fruit extracts prepared with supercritical carbon dioxide. In vitro antagonists of cyclooxygenase and 5-lipoxygenase metabolism].
20.) [Immunostimulant action of polysaccharides (heteroglycans) from higher plants. Preliminary communication].
21.) Lignans from the roots of Urtica dioica and their metabolites bind to human sex hormone binding globulin (SHBG).
22.) The inhibiting effects of Urtica dioica root extracts on experimentally induced prostatic hyperplasia in the mouse.
23.) [Cytokine secretion in whole blood of healthy subjects following oral administration of Urtica dioica L. plant extract].
24.) Ex-vivo in-vitro inhibition of lipopolysaccharide stimulated tumor necrosis factor-alpha and interleukin-1 beta secretion in human whole blood by extractum urticae dioicae foliorum.
25.) [Anti-inflammatory effect of Urtica dioica folia extract in comparison to caffeic malic acid].
26.) The effect of extracts of the roots of the stinging nettle (Urtica dioica) on the interaction of SHBG with its receptor on human prostatic membranes.
27.) Effects of stinging nettle root extracts and their steroidal components on the Na+,K(+)-ATPase of the benign prostatic hyperplasia.
28.) Testosterone metabolism in primary cultures of human prostate
epithelial cells and fibroblasts.
29.) Human prostatic steroid 5 alpha-reductase isoforms--a comparative study of selective inhibitors.
30.) Serenoa repens (Permixon). A review of its pharmacology and therapeutic efficacy in benign prostatic hyperplasia.
31.) Effect of Serenoa repens extract (Permixon) on estradiol/testosterone-induced experimental prostate enlargement in the rat.
======================================================================
1.) Efficacy and acceptability of tadenan (Pygeum africanum extract) in the treatment of benign prostatic hyperplasia (BPH): a multicentre trial in central Europe.
======================================================================
Curr Med Res Opin 1998;14(3):127-39
Breza J, Dzurny O, Borowka A, Hanus T, Petrik R, Blane G, Chadha-Boreham H
Department of Urology, University Hospital, Bratislava, Slovak Republic.
Pygeum africanum extract is available as Tadenan in many countries, including those in central and eastern Europe, for the treatment of mild to moderate BPH. Its efficacy and acceptability have been demonstrated in numerous open and placebo-controlled studies in large populations. The present open three-centre efficacy and safety study was conducted according to common protocol at urology clinics in the Czech and Slovak Republics and in Poland, in order to confirm the therapeutic profile of Pygeum africanum in conditions of daily practice, using International Prostate Symptom Score (IPSS) and flowmetry assessments. Men aged 50-75 years and in compliance with the selection criteria (including IPSS > or = 12, quality of life (QoL) score > or = 3, and maximum urinary flow < or = 15 ml/s) were first examined then recalled after two weeks during which no treatment was provided (washout and check of stability). If still compliant, they were entered at this point into a two-month period of treatment with Pygeum africanum extract 50 mg twice daily. There followed a further one-month period without treatment, the objective being to evaluate the persistence of any effects observed during the previous two months of Pygeum africanum administration. The primary efficacy parameter investigated was IPSS; the other efficacy parameters were QoL, nocturnal frequency, maximum urinary flow, average urinary flow, post-voiding residual volume and prostatic volume, after one and two months of Pygeum africanum treatment and one month after stopping treatment. A total of 85 patients were evenly distributed between the three centres and completed the entire study. At inclusion their mean IPSS was 16.17, QoL was 3.60 and nocturia was 2.6 times per night. The changes in subjective scores, IPSS and QoL after the two-month treatment period were highly statistically significant with mean improvements of 40% and 31%, respectively. Nocturnal frequency was reduced by 32% and the mean reduction was again highly statistically significant. Mean maximum urinary flow, average urinary flow and urine volume were also statistically significantly improved, but the modest improvement in post-voiding volume did not reach statistical significance. The improvements, which exceeded those observed with placebo in earlier studies, were maintained after one month without treatment indicating an interesting persistence of clinically useful activity. Prostatic volume and quality of sexual life remained unchanged throughout. No treatment-related adverse effects were observed. In conclusion, under conditions of daily practice, Pygeum africanum extract induces significant improvement in IPSS and uroflowmetry parameters. These positive effects are accompanied by a very satisfactory safety profile with the overall result of a substantial improvement in QoL.
======================================================================
2.) Antiproliferative effect of Pygeum africanum extract on rat prostatic fibroblasts.
======================================================================
J Urol 1997 Jun;157(6):2381-7
Published erratum appears in J Urol 1997 Sep;158(3 Pt 1):889
Yablonsky F, Nicolas V, Riffaud JP, Bellamy F
Laboratoires Debat, groupe Fournier, Garches, France.
The effect of a Pygeum africanum extract (Tadenan) (Pa), used in the treatment of micturition disorders associated with BPH, has been examined on the proliferation of rat prostatic stromal cells stimulated by different growth factors. EGF, bFGF, and IGF-I but not KGF are mitogenic for prostatic fibroblasts in culture. Pygeum africanum inhibits both basal and stimulated growth with IC50 values of 4.5, 7.7 and 12.6 micrograms./ml. for EGF, IGF-I and bFGF, respectively, compared to 14.4 micrograms./ml. for untreated cells, the inhibition being stronger towards EGF. Pygeum africanum inhibited the proliferation induced by TPA or PDBu in a concentration-dependent manner with IC50 values of 12.4 and 8.1 micrograms./ml. respectively. The antiproliferative effects of Pa were not ascribed to cytotoxicity. These results show that Pygeum africanum is a potent inhibitor of rat prostatic fibroblast proliferation in response to direct activators of protein kinase C, the defined growth factors bFGF, EGF and IGF-I, and the complex mixture of mitogens in serum depending on the concentration used. PKC activation appears to be an important growth factor-mediated signal transduction for this agent. These data suggest that therapeutic effect of Pygeum africanum may be due at least in part to the inhibition of growth factors responsible for the prostatic overgrowth in man.
======================================================================
3.) Cellular and molecular aspects of bladder hypertrophy.
======================================================================
Eur Urol 1997;32 Suppl 1:15-21
Levin RM, Levin SS, Zhao Y, Buttyan R
Albany College of Pharmacy, N.Y., USA.
Bladder dysfunction secondary to benign prostatic hyperplasia (BPH) is a major affliction associated with ageing. As the disease slowly progresses, the bladder changes from a state of compensation to decompensation, in which there are severe, irreversible alterations in bladder function. Using a rabbit model of partial outlet obstruction we have identified three major cellular changes in the bladder which result from such obstruction. These include progressive denervation, mitochondrial dysfunction and disturbances of calcium storage and release from the sarcoplasmic reticulum. Our hypothesis is that outlet obstruction results in bladder hypertrophy which induces ischaemia. This leads to a release of intracellular calcium, leading to activation of specific enzymes and generation of free radicals. These then attack the membranes of nerves, sarcoplasmic reticulum and mitochondria. We have demonstrated that pretreatment of rabbits with Pygeum africanum extract (Tadenan) significantly reduced the severity of both the contractile and metabolic dysfunctions induced by partial outlet obstruction. Our current hypothesis is that Tadenan may either prevent the activation of degradative enzymes (or generation of free radicals), or protect the intracellular membranes against the destructive effects of free radicals or degredative enzymes. In conclusion, identifying cellular mechanisms responsible for bladder dysfunction induced by partial outlet obstruction provides new possibilities for non-surgical treatment of BPH. Our studies on Tadenan support this concept that the bladder provides a novel target for therapeutic intervention.
======================================================================
4.) Effect of Pygeum africanum extract on A23187-stimulated production of lipoxygenase metabolites from human polymorphonuclear cells.
======================================================================
J Lipid Mediat Cell Signal 1994 May;9(3):285-90
Paubert-Braquet M, Cave A, Hocquemiller R, Delacroix D, Dupont C, Hedef N, Borgeat P
Laboratories BIO-INOVA, Plaisir, France.
Pygeum africanum extract has been used for more than 20 years in France in patients suffering from benign prostatic hypertrophy (BPH). The extract displays anti-inflammatory activity and inhibits bladder hyperreactivity during the above conditions. However, the mechanism of action of P. africanum extract has never been clearly resolved. It has been recently demonstrated that infiltration by inflammatory cells may be involved in the development of BPH. Certain of these cell types, such as macrophages, are known to produce chemotactic mediators including leukotrienes, and thus may contribute to the development of the disease. In order to investigate the potential effect of P. africanum extract on arachidonate metabolism, we examined its effect in vitro on leukotriene (LT) synthesis in human polymorphonuclear cells stimulated with the calcium ionophore A23187. Two formulations of the extract were tested, one dissolved in DMSO and one aqueous solution obtained after alkalinization (0.1 N; NaOH/acidification (0.1 N; HCl). Neither formulation had any effect on cell viability which was above 95% in both cases. P. africanum extract dissolved in DMSO significantly inhibited the production of 5-lipoxygenase metabolites (5-HETE, 20-COOH LTB4, LTB4 and 20-OH LTB4) at concentrations as low as 3 micrograms/ml (p < 0.01), while the same extract dissolved in NaOH/HCl only exhibited an inhibitory effect at 10 micrograms/ml (p < 0.01). This difference apparently reflects the greater solubility of the active components in the extract in DMSO. The ability of P. africanum to antagonize 5-lipoxygenase metabolite production may contribute, at least in part, to its therapeutic activity in inflammatory component of BPH.
======================================================================
5.) Combined extracts of Urtica dioica and Pygeum africanum in the treatment of benign prostatic hyperplasia: double-blind comparison of two doses.
======================================================================
Clin Ther 1993 Nov-Dec;15(6):1011-20
Krzeski T, Kazon M, Borkowski A, Witeska A, Kuczera J
Warsaw School of Medicine, Poland.
The 134 patients (aged 53 to 84 years) with symptoms of benign prostatic hyperplasia were drawn from two medical centers in Warsaw. The patients were randomly assigned to receive two capsules of the standard dose of an urtica/pygeum preparation (300 mg of Urtica dioica root extract combined with 25 mg of Pygeum africanum bark extract) or two capsules containing half the standard dose twice daily for 8 weeks. After 28 days' treatment, urine flow, residual urine, and nycturia were significantly reduced in both treatment groups. After 56 days' treatment, further significant decreases were found in residual urine (half-dose group) and in nycturia (both groups). There were no between-group differences in these measures of efficacy. Five patients reported adverse effects of treatment; treatment was not discontinued in any patient because of side effects. It is concluded that half doses of the urtica/pygeum extract are as safe and effective as the recommended full doses.
======================================================================
6.) [Urological and sexual evaluation of treatment of benign prostatic disease using Pygeum africanum at high doses].
======================================================================
Arch Ital Urol Nefrol Androl 1991 Sep;63(3):341-5
Carani C, Salvioli V, Scuteri A, Borelli A, Baldini A, Granata AR, Marrama P
Cattedra di Endocrinologia, Universita degli Studi di Modena.
This clinical study has been designed to evaluate the efficacy of an extract of Pygeum Africanum (Tadenan) (Roussel-Pharma) in patients suffering from prostatic hypertrophy or chronic prostatitis. The drug has been administrated to 18 patients, for 60 days, as double of standard dosage (200 mg/die per os, instead of 100 mg/die). Because of the high frequency of association of sexual disorders with those two pathologies, we have extended the study also to sexual disorders selecting patients suffering from prostatic hypertrophy or chronic prostatitis and, simultaneously, from sexual disturbances. No side effects have been observed during the treatment. The urinary disturbances have been evaluated by anamnesis and prostatic transrectal echography; sexual disorders have been evaluated by anamnesis and nocturnal penile tumescence and rigidity (NPTR) monitoring. Furthermore, dosage of serum levels of the hormones LH, FSH, Prolactin, 17 beta-Estradiol and Testosterone has been performed before and after therapy. Pygeum Africanum extract administration improved all the urinary parameters we investigated; prostatic echography relieved reduction of peri-urethral edema. Also an improvement of sexual behaviour has been obtained; but we have not found significant differences between serum hormonal levels before and after therapy, as well as for NPTR.
======================================================================
7.) [Efficacy of Pygeum africanum extract in the medical therapy of urination disorders due to benign prostatic hyperplasia: evaluation of objective and subjective parameters. A placebo-controlled double-blind multicenter study].
======================================================================
Wien Klin Wochenschr 1990 Nov 23;102(22):667-73
Barlet A, Albrecht J, Aubert A, Fischer M, Grof F, Grothuesmann HG, Masson JC, Mazeman E, Mermon R, Reichelt H, et al
Laboratoires Debat, Paris, Frankreich.
The efficacy of an extract of Pygeum africanum in the treatment of micturitional disorders due to benign prostatic hyperplasia was tested in a multicentre double-blind trial versus placebo. Capsules containing 50 mg of Pygeum africanum extract or placebo were administered at a dosage of 1 capsule in the morning and 1 capsule in the evening over a period of 60 days. 263 patients were included in this study, which was carried out in 8 centres in Germany, France, and Austria. Evaluation was mainly based on quantitative parameters such as residual urine, uroflowmetry and the precise monitoring of diurnal and nocturnal pollakiuria. Treatment with the Pygeum africanum extract led to a marked clinical improvement: a comparison of the quantitative parameters showed a significant difference between the Pygeum africanum group and the placebo group with respect to therapeutic response. The characteristic subjective symptoms of micturitional disorders, which were evaluated by the patients in a qualitative manner, were also significantly improved by administration of Pygeum africanum extract. Overall assessment at the end of therapy, showed that micturition improved in 66% of the patients treated with Pygeum africanum extract, as compared with an improvement of 31% in the placebo group. The difference was significant at the statistical level of p less than 0.001. During therapy with Pygeum africanum extract, gastrointestinal side effects occurred in 5 patients. Treatment was discontinued in three of those cases.
======================================================================
8.) [Controlled study of the effects of Pygeum africanum extract on the functional symptoms of prostatic adenoma].
======================================================================
Ann Urol (Paris) 1984 May;18(3):193-5
Dufour B, Choquenet C, Revol M, Faure G, Jorest R
Two random groups of sixty patients each were given an extract of pygeum africanum in one group, and a placebo in the other. The results highlight the placebo effect (50 per cent of cases), and that the extract provided an overall improvement in the functional symptoms. The differences between the two treatments were statistically significant for nocturnal frequency, difficulty in starting micturition, and incomplete emptying of the bladder.
======================================================================
9.) Treatment of benign prostatic hyperplasia with phytosterols.
======================================================================
Br J Urol 1990 Dec;66(6):639-41
Carbin BE, Larsson B, Lindahl O
Department of Urology, Karolinska Hospital, Stockholm, Sweden.
In a randomised, double-blind study, the preparation Curbicin, obtained from pumpkin seeds and dwarf palm plants (Cucurbita pepo L. and Sabal serrulata), was compared with a placebo in the treatment of symptoms caused by prostatic hyperplasia; 53 patients took part in the study, which was carried out over a 3-month period. Urinary flow, micturition time, residual urine, frequency of micturition and a subjective assessment of the effect of treatment were all significantly improved in the treatment group. No untoward side effects were noted.
======================================================================
10.) [Sabal serrulata extract in the management of symptoms of prostatic hypertrophy].
======================================================================
Orv Hetil 1997 Feb 16;138(7):419-21
[Article in Hungarian]
Kondas J, Philipp V, Dioszeghy G
Fovarosi Onkormanyzat Peterfy Sandor utcai Korhaz-Rendelointezet, Urologiai-sebeszeti Osztaly, Budapest.
The effectiveness of Sabal serrulata (dwarf palm) extract was evaluated in the treatment of 38 patients with symptomatic prostatic hyperplasia. During a 12-month treatment controlled by investigations the subjective symptoms decreased in nearly three fourth of the patients. Side effects were not observed. According to uroflowmetric investigations the average peak flow value increased from 10.36 ml/sec to 14.44 ml/sec (p < 0.0001) and the average mean flow value from 0.02 ml/sec to 7.45 ml/sec (p < 0.001). After treatment residual urine volume decreased or was nil in more than 9/10 of the cases. The average decrease of residue was 47 ml (p < 0.001). The average decrease in prostatic volume was 10.6% (p < 0.02). On the basis of their favorable experience the authors recommend the administration of Sabal serrulata extract in the treatment of patients with mild or moderate symptoms of prostatic hyperplasia.
======================================================================
11.) Enzyme activities in tissue of human benign prostatic hyperplasia after three months' treatment with the Sabal serrulata extract IDS 89 (Strogen) or placebo.
======================================================================
Eur Urol 1997;31(1):97-101
Weisser H, Behnke B, Helpap B, Bach D, Krieg M
Institute of Clinical Chemistry, Transfusion and Laboratory Medicine, University Clinic Bergmannsheil, Bochum, Germany.
OBJECTIVE: The mechanism of action of plant extracts used for the medical treatment of human benign prostatic hyperplasia (BPH) is still unknown. In this prospective, randomized, double-blind trial, we investigated the possible influence of the Sabal serrulata extract IDS 89 (Strogen) on epithelial and stromal enzyme activities of BPH tissue. METHODS: 18 patients with BPH were randomly assigned to receive 3 x 2 capsules Strogen uno (320 mg/capsule) (n = 8) or placebo (n = 10) daily for 3 months. The activity (Vmax and Km) of 5 alpha-reductase. 3 alpha-HSORred, 3 beta-HSORred, and creatine kinase was determined in mechanically separated epithelium and stroma of human BPH. RESULTS: The multivariate correlation analysis revealed a positive correlation between therapy and the following enzyme alterations: (1) In epithelium, the substrate affinity of the 5 alpha-reductase decreased slightly (increase of Km value). (2) In stroma, the Vmax value of the 3 alpha-HSORred increased statistically distinctly, leading to a moderate increase of Vmax/Km. (3) In stroma, the Vmax value of the 3 beta-HSORred increased moderately, but not statistically significant. (4) In stroma, the Vmax value of creatine kinase increased significantly, leading to a statistically distinct increase of Vmax/Km. CONCLUSION: This double-blind, placebo-controlled clinical trial with the S. serrulata extract IDS 89 revealed significant biochemical changes at the cellular level of BPH tissue. However, the alterations are merely moderate, their biochemical causes and consequences regarding the pathophysiology of BPH rather uncertain. Therefore, more studies are needed before plant extracts like IDS 89 become valid candidates likewise synthetic substances already used for medical treatment of human BPH.
======================================================================
12.) Drug therapy of benign prostatic hyperplasia].
======================================================================
Fortschr Med 1996 Nov 10;114(31):407-11
Vahlensieck W Jr, Fabricius PG, Hell U
BPH patients with Vahlensieck stage II or III disease are suitable for drug treatment. The points of attack are reduction of testosterone, conversion of testosterone to dihydrotestosterone, conversion of testosterone to estrogen using GnRH analogues, antiandrogens and alpha reductase inhibitors or aromatose inhibitors. Furthermore a reduction in obstruction is achieved through the use of phytopharmaceuticals containing 5-lipoxygenase and cyclooxygenase inhibitors. At present, Curcurbitae pepo seeds, Urtica dioica root, Pollinis siccae extract and Sabal serrulata seed extract are approved for the treatment of prostatic diseases in Germany. The use of alpha-1-sympathicolytic treatment may reduce muscular tone in the prostate. Combination of the various modes of action may also offer an effective form of treatment.
======================================================================
13.) Effects of the sabal serrulata extract IDS 89 and its subfractions on 5 alpha-reductase activity in human benign prostatic hyperplasia.
======================================================================
Prostate 1996 May;28(5):300-6
Weisser H, Tunn S, Behnke B, Krieg M
Institute of Clinical Chemistry, Transfusion and Laboratory Medicine, University Clinic Bergmannsheil, Bochum, Federal Republic of Germany.
Extract from fruit of Sabal serrulata are used in the treatment of human benign prostate hyperplasia (BPH). Therefore, it is of interest whether this phytopharmacon has any influence on the androgen metabolism in the human prostate. It was found that the extract IDS 89 of Sabal serrulata inhibited dose dependently 5 alpha-reductase activity in the epithelium and stroma of human BPH, the mean inhibition being 29% and 45%, respectively. This inhibitory effect is mainly due to the saponifiable subfraction of IDS 89 showing a mean 5 alpha-reductase inhibition of 39% and 38% in epithelium and stroma, respectively. The inhibition was dose dependent and noncompetitive. At a testosterone concentration of 580 nM as substrate for 5 alpha-reductase, the main fatty acids of the extract IDS 89 gave rise to a percentual enzyme inhibition in the epithelium and stroma as follows: 51% and 42% (lauric acid), 5% and 0% (oleic acid), 43% and 34% (myristic acid), 2% and 0% (palmitic acid), respectively. The inhibitory effect of lauric acid was noncompetitive and dose dependent up to a concentration of 0.2 nM, the maximal inhibition in the epithelium and stroma being 52% and 45%, respectively. The nonsaponifiable subfraction, consisting mainly of phytosterols, showed a mean inhibition of 5 alpha-reductase in the epithelium and stroma of 15% and 10%, respectively. Finally, the hydrophilic subfraction, containing carbohydrates, amino acids, and polysaccharides, showed no inhibitory effect. The present in vitro studies suggest that the Sabal serrulata extract IDS 89 has an inhibitory effect on 5 alpha-reductase in the epithelium and stroma of human BPH. This inhibition is mainly due to the fatty acids of the saponifiable subfraction.
======================================================================
14.) Sabal serrulata extract (Strogen forte) in the treatment of symptomatic benign prostatic hyperplasia.
======================================================================
Int Urol Nephrol 1996;28(6):767-72
Kondas J, Philipp V, Dioszeghy G
Department of Urological Surgery, Municipal Peterfy Sandor Street Hospital, Budapest, Hungary.
The effectivity of Sabal serrulata extract in the treatment of symptomatic prostatic hyperplasia was scrutinized in 38 patients. In the course of the 12-month treatment followed up by examinations, the subjective complaints abated in almost 3/4 of the cases. Adverse effects were not encountered. According to uroflowmetry, the average peak flow rate increased from 10.36 ml/s to 14.44 ml/s (p < 0.0001), while the average middle stream increased from 6.02 ml/s to 7.45 ml/s (p < 0.001). Urinary retention decreased or disappeared in more than 9/10 of the cases. The average amount of the residue decreased by 47 ml (p < 0.001). The average volume of the prostate was reduced by 10.6% (p < 0.02). On the basis of the favourable results, Sabal serrulata extract is recommended in the treatment of prostatic hyperplasia producing symptoms of mild and moderate severity.
======================================================================
15.) In vitro inhibition of testicular delta 5-3 beta-hydroxysteroid dehydrogenase and prostatic 5 alpha-reductase activities in rats and humans by strogen forte extract.
======================================================================
Int Urol Nephrol 1996;28(3):337-48
Toth I, Szecsi M, Julesz J, Faredin I, Behnke B
Endocrine Unit, Szent-Gyorgyi Albert Medical University, Szeged, Hungary.
Clinical findings indicate that Strogen forte (a standardized extract of the plant Sabalis serrulata) can be use successfully in the medical treatment of benign prostatic hyperplasia. The aim of the present study was to investigate the possible inhibitory effects of the Strogen forte extract on rat and human testicular delta 5-3 beta-hydroxysteroid dehydrogenase (delta 5-3 beta-HSD) and prostatic 5 alpha-reductase (5 alpha-R). Strogen forte proved to be a direct inhibitor of medium effectivity, with similar IC50 values for rat testicular delta 5-3 beta-HSD (400 +/- 23 micrograms/ml) and human testicular delta 5-3 beta-HSD (212 +/- 8.6 micrograms/ml). 5 alpha-R activities were analysed by in vitro incubation of rat and human prostatic tissue homogenates with 14C-labelled testosterone as substrate in KRPG-DTT medium (pH = 7.4) with NADPH coenzyme, in air, at 37 degrees C, in the presence of Strogen forte extract. The results clearly demonstrate that Strogen forte is a potent inhibitor of prostatic 5 alpha-R, with IC50 values of 385 +/- 35.6 micrograms/ml for rat and 245 +/- 64.6 micrograms/ml for human prostatic 5 alpha-R. The present study has revealed that this plant extract inhibits not only prostatic 5 alpha-R, but also testicular delta 5-3 beta-HSD.
======================================================================
16.) Mechanisms involved in the spasmolytic effect of extracts from Sabal serrulata fruit on smooth muscle.
======================================================================
Gen Pharmacol 1996 Jan;27(1):171-6
Gutierrez M, Garcia de Boto MJ, Cantabrana B, Hidalgo A
Departamento de Medicina, Laboratorio de Farmacologia, Oviedo, Spain.
1. The effects of two extracts from Sabal serrulata fruits [total lipidic (L) and saponifiable (S)] on smooth muscle contractions have been assayed. 2. Both extracts (0.1-1 mg/ml) relaxed the tonic contraction induced by norepinefrine (30 nM) on rat aorta [EC50, 0.53 +/- 0.05 mg/ml (L) and 0.5 +/- 0.04 mg/ml (S)] and by KCl (60 mM) on rat uterus. The Sabal extracts (0.3-1 mg/ml) also antagonized the dose-response curve of contractions induced by acetylcholine (0.1-100 microM) on urinary bladder. 3. dL-Propranolol (1 microM) but not the inactive (R)-(+)-propranolol(1 microM) potentiated the Sabal extracts relaxant effect by lowering the EC50 (0.35 +/- 0.2 vs 0.20 +/- 0.01 mg/ml for L and 0.43 +/- 0.02 vs 0.19 +/- 0.02 mg/ml, P < 0.01, for S extract). 4. Cycloheximide (10 micrograms/ml) antagonized the effect of extracts from Sabal. However, actinomycin D (5 micrograms/ml) significantly (P < or = 0.01) antagonized the effect of the total lipidic extract without modifying that of the saponifiable extract. 5. The relaxant effect of both extracts was not modified by the tyrosine kinase inhibitor genistein (10 microM) or the ornithine decarboxylase inhibitor alpha-difluoromethyl-ornithine (10 mM).
======================================================================
17.) [Benign prostatic hyperplasia--treatment with sabal fruit extract. A treatment study of 1,334 patients].
======================================================================
Fortschr Med 1993 Jun 30;111(18):323-6
Vahlensieck W Jr, Volp A, Lubos W, Kuntze M
Urologische Klinik und Poliklinik, Klinikum Grosshadern der Universitat Munchen.
METHOD: In a drug monitoring study, 1,334 outpatients with benign prostatic hyperplasia (BPH) were treated for 12 weeks with an extract from the fruits of Sabal serrulata. RESULTS: Under this treatment, the volume of residual urine decreased by 50%, pollakisuria decreased on average by 37%, and nocturia by 54%. The percentage of patients with dysuric pain decreased from 75% to 37%. The efficacy of the drug was rated good to excellent in more than 80% of the cases, and good to excellent tolerability was reported by more than 95% of the patients. CONCLUSION: The improvement in the irritative symptoms may be considered relevant in terms of improvement in the quality of the life of the patients, and justifies this form of treatment.
======================================================================
18.) Experience in treating benign prostatic hypertrophy with Sabal serrulata for one year.
======================================================================
Int Urol Nephrol 1993;25(6):565-9
Romics I, Schmitz H, Frang D
Department of Urology, Semmelweis University Medical School, Budapest, Hungary.
The authors treated 42 BPH patients with the Sabal extract Strogen forte for 12 months. The obstructive symptoms, residual volume, mean and maximum flow rates improved significantly by the 6th therapeutic month at the latest. The results seem to prove the effectiveness of the drug. Side effects have not been observed.
======================================================================
19.) [Anti-inflammatory activity of sabal fruit extracts prepared with supercritical carbon dioxide. In vitro antagonists of cyclooxygenase and 5-lipoxygenase metabolism].
======================================================================
Arzneimittelforschung 1992 Apr;42(4):547-51
Breu W, Hagenlocher M, Redl K, Tittel G, Stadler F, Wagner H
Institut fur Pharmazeutische Biologie, Ludwig-Maximilians-Universitat Munchen.
The extract SG 291 (Talso, Talso uno) from the fruits of Sabal serrulata (syn.: Serenoa repens) prepared by supercritical fluid extraction with carbon dioxide is used for the treatment of benign prostatic hyperplasia (BPH) and non bacterial prostatitis. In the present work, the Sabal extract SG 291 was analyzed by gas chromatography and investigated for its inhibitory influence on the biosynthesis of inflammatory arachidonic acid metabolites. The extract SG 291 was found in vitro to be a dual inhibitor of the cyclooxygenase (IC50-value: 28.1 micrograms/ml) and 5-lipoxygenase pathway (IC50-value: 18.0 micrograms/ml). By alkaline hydrolysis, ether extraction and preparative thin layer chromatography the extract SG 291 was separated in three fractions containing acid lipophilic compounds (A), fatty alcohols (B) and sterols (C) as main components. Fraction A inhibited the biosynthesis of cyclooxygenase (CO) and 5-lipoxygenase (5-LO) metabolites in the same intensity as the native extract SG 291, while the fractions B, C and beta-sitosterol showed no inhibitory effect on both enzymes of the arachidonic acid pathways. Therefore, the CO and 5-LO inhibiting principle of Sabal serrulata extract SG 291 must be localized in the acidic lipophilic fraction (SLF). The CO and 5-LO inhibitory effects may give an explanation for the in vivo observed antiphlogistic and antiedematous activity of the lipophilic Sabal serrulata extract SG 291.
======================================================================
20.) [Immunostimulant action of polysaccharides (heteroglycans) from higher plants. Preliminary communication].
======================================================================
Arzneimittelforschung 1984;34(6):659-61
Wagner H, Proksch A, Riess-Maurer I, Vollmar A, Odenthal S, Stuppner H, Jurcic K, Le Turdu M, Heur YH
From the water or alcaline-water extracts of Echinacea purpurea (L.) Moench and -angustifolia DC., Eupatorium cannabinum L. and -perfoliatum L., Chamomilla recutita (L.) (Rauscher), Calendula officinalis L., Baptisia tinctoria (L.) R.B., Achyrocline satureoides DC., Arnica montana L., Sabal serrulata Roem et Schult. and Eleutherococcus senticosus Maxim. polysaccharide fractions with molecular weights in the range of 25 000 to 500 000 and higher have been isolated, which, according to the granulocytes- and carbon clearance tests, showed significant immunostimulating activities. The isolated compounds belong to the group of water-soluble, acidic heteroglycanes. The linkages in the different polysaccharides do not represent a uniform structure type.
======================================================================
21.) Lignans from the roots of Urtica dioica and their metabolites bind to human sex hormone binding globulin (SHBG).
======================================================================
Planta Med 1997 Dec;63(6):529-32
Schottner M, Gansser D, Spiteller G
Lehrstuhl Organische Chemie I, Universitat Bayreuth, Germany.
Polar extracts of the stinging nettle (Urtica dioica L.) roots contain the ligans (+)-neoolivil, (-)-secoisolariciresinol, dehydrodiconiferyl alcohol, isolariciresinol, pinoresinol, and 3,4-divanillyltetrahydrofuran. These compounds were either isolated from Urtica roots, or obtained semisynthetically. Their affinity to human sex hormone binding globulin (SHBG) was tested in an in vitro assay. In addition, the main intestinal transformation products of plant lignans in humans, enterodiol and enterolactone, together with enterofuran were checked for their activity. All lignans except (-)-pinoresinol developed a binding affinity to SHBG in the in vitro assay. The affinity of (-)-3,4-divanillyltetrahydrofuran was outstandingly high. These findings are discussed with respect to potential beneficial effects of plant lignans on benign prostatic hyperplasia (BPH).
======================================================================
22.) The inhibiting effects of Urtica dioica root extracts on experimentally induced prostatic hyperplasia in the mouse.
======================================================================
Planta Med 1997 Aug;63(4):307-10
Lichius JJ, Muth C
Institut fur Pharmazeutische Biologie, Philipps-Universitat, Marburg, Germany.
Extracts of stinging nettle roots (Urtica dioica L. Urticaceae) are used in the treatment of benign prostatic hyperplasia (BPH). We established a BPH-model by directly implanting an urogenital sinus (UGS) into the ventral prostate gland of an adult mouse. Five differently prepared stinging nettle root extracts were tested in this model. The 20% methanolic extract was the most effective with a 51.4% inhibition of induced growth.
======================================================================
23.) [Cytokine secretion in whole blood of healthy subjects following oral administration of Urtica dioica L. plant extract].
======================================================================
Arzneimittelforschung 1996 Sep;46(9):906-10
Teucher T, Obertreis B, Ruttkowski T, Schmitz H
Strathmann AG & Co., Hamburg.
Twenty healthy volunteers ingested for 21 days 2 capsules b.i.d. of an IDS 23/1 containing nettle leaf extract (Rheuma-Hek). Before and after 7 and 21 days the basal and the lipopolysaccharide (LPS) stimulated tumor necrosis factor-alpha (TNF-alpha), interleukin-1 beta (IL-1 beta) and interleukin-6 (IL-6) concentrations were measured ex vivo. In vitro the effects of IDS 23/1 on the release of these cytokines were determined. Additionally basal interleukin-4 (IL-4) and interleukin-10 (IL-10) levels were recorded. Orally taken the test drug has ex vivo no effect on basal levels of TNF-alpha, IL-1 beta, IL-4, IL-6 or IL-10 which were always below detection limits. After 7 and 21 days ingestion ex vivo a decrease of LPS stimulated TNF-alpha release of 14.6 and 24.0%, respectively, was observed. IL-1 beta was reduced for 19.2 and 39.3%. In vitro IDS 23/1 added to whole blood resulted in an exceeded inhibition of LPS stimulated TNF-alpha and IL-1 beta secretion which correlated with the duration of the drug ingestion. Using the highest tested IDS 23/1 concentration the inhibition reached 50.5 (day 0) to 79.5% (day 21) for TNF-alpha and 90.0 (day 0) to 99.2% (day 21) for IL-1 beta, respectively. IDS 23/1 induced a pronounced release of IL-6 in absence of LPS only in vitro. The detected IL-6 concentrations were comparable to those after LPS stimulation, additive effects could not be observed. The absence of detectable IL-6 concentrations in whole blood ex vivo after oral ingestion of the tested drug as well as the differences in the inhibition patterns for TNF-alpha and IL-1 beta ex vivo and ex vivo in vitro suggest that the extract contains different pharmacological effective compounds with varying bioavailabilities.
======================================================================
24.) Ex-vivo in-vitro inhibition of lipopolysaccharide stimulated tumor necrosis factor-alpha and interleukin-1 beta secretion in human whole blood by extractum urticae dioicae foliorum.
======================================================================
Arzneimittelforschung 1996 Apr;46(4):389-94
Published erratum appears in Arzneimittelforschung 1996 Sep;46(9):936
Obertreis B, Ruttkowski T, Teucher T, Behnke B, Schmitz H
Strathmann AG & Co., Hamburg, Germany.
An extract of Urtica dioica folium (IDS 23, Rheuma-Hek), monographed positively for adjuvant therapy of rheumatic diseases and with known effects in partial inhibition of prostaglandin and leukotriene synthesis in vitro, was investigated with respect to effects of the extract on the lipopolysaccharide (LPS) stimulated secretion of proinflammatory cytokines in human whole blood of healthy volunteers. In the assay system used, LPS stimulated human whole blood showed a straight increase of tumor necrosis factor-alpha (TNF-alpha) and interleukin-1 beta (IL-1 beta) secretion reaching maximum concentrations within 24 h following a plateau and slight decrease up to 65 h, respectively. The concentrations of these cytokines was strongly positively correlated with the number of monocytes/macrophages of each volunteer. TNF-alpha and IL-1 beta concentration after LPS stimulation was significantly reduced by simultaneously given IDS 23 in a strictly dose dependent manner. At time 24 h these cytokine concentrations were reduced by 50.8% and 99.7%, respectively, using the highest test IDS 23 assay concentration of 5 mg/ml (p < 0.001). After 65 h the corresponding inhibition was 38.9% and 99.9%, respectively (p < 0.001). On the other hand IDS 23 showed no inhibition but stimulated IL-6 secretion in absence of LPS alone. Simultaneously given LPS and IDS 23 resulted in no further increase. In contrast to described effects on arachidonic acid cascade in vitro, tested Urtica dioica phenol carbon acid derivates and flavonoides such as caffeic malic acid, caffeic acid, chlorogenic acid, quercetin and rutin did not influence LPS stimulated TNF-alpha, IL-1 beta and IL-6 secretion in tested concentrations up to 5 x 10(-5) mol/l. These further findings on the pharmacological mechanism of action of Urticae dioica folia may explain the positive effects of this extract in the treatment of rheumatic diseases.
======================================================================
25.) [Anti-inflammatory effect of Urtica dioica folia extract in comparison to caffeic malic acid].
======================================================================
Obertreis B, Giller K, Teucher T, Behnke B, Schmitz H
Strathmann AG, Hamburg.
Urtica dioica extract is a traditionary used adjuvant therapeutic in rheumatoid arthritis. The antiphlogistic effects of the urtica dioica folia extract IDS 23 (Extractum Urticae dioicae foliorum) and the main phenolic ingredient caffeic malic acid were tested concerning the inhibitory potential on biosynthesis of arachidonic acid metabolites in vitro. The caffeic malic acid was isolated from Urtica folia extract using gel exclusion- and high performance liquid chromatography and identified by mass spectroscopy and nuclear magnetic resonance. Concerning the 5-lipoxygenase products IDS 23 showed a partial inhibitory effect. The isolated phenolic acid inhibited the synthesis of the leukotriene B4 in a concentration dependent manner. The concentration for halfmaximal inhibition (IC50) was 83 microns/ml in the used assay. IDS 23 showed a strong concentration dependent inhibition of the synthesis of cyclooxygenase derived reactions. The IC50 were 92 micrograms/ml for IDS 23 and 38 micrograms/ml for the caffeic malic acid. Calculating the content in IDS 23 the caffeic malic acid is a possible but not the only active ingredient of the plant extract in the tested assay systems. It is demonstrated that the phenolic component showed a different enzymatic target compared with IDS 23. The antiphlogistic effects observed in vitro may give an explanation for the pharmacological and clinical effects of IDS 23 in therapie of rheumatoid diseases.
======================================================================
26.) The effect of extracts of the roots of the stinging nettle (Urtica dioica) on the interaction of SHBG with its receptor on human prostatic membranes.
======================================================================
Planta Med 1995 Feb;61(1):31-2
Hryb DJ, Khan MS, Romas NA, Rosner W
Department of Medicine, St. Luke's/Roosevelt Hospital Center, New York, N.Y. 10019.
Extracts from the roots of the stinging nettle (Urtica dioica) are used in the treatment of benign prostatic hyperplasia. The mechanisms underlying this treatment have not been elucidated. We set out to determine whether specific extracts from U. dioica had the ability to modulate the binding of sex hormone-binding globulin to its receptor on human prostatic membranes. Four substances contained in U. dioica were examined: an aqueous extract; an alcoholic extract; U. dioica agglutinin, and stigmasta-4-en-3-one. Of these, only the aqueous extract was active. It inhibited the binding of 125I-SHBG to its receptor. The inhibition was dose related, starting at about 0.6 mg/ml and completely inhibited binding at 10 mg/ml.
======================================================================
27.) Effects of stinging nettle root extracts and their steroidal components on the Na+,K(+)-ATPase of the benign prostatic hyperplasia.
======================================================================
Planta Med 1994 Feb;60(1):30-3
Hirano T, Homma M, Oka K
Department of Clinical Pharmacology, Tokyo College of Pharmacy, Japan.
The effects of organic-solvent extracts of Urtica dioica (Urticaceae) on the Na+,K(+)-ATPase of the tissue of benign prostatic hyperplasia (BPH) were investigated. The membrane Na+,K(+)-ATPase fraction was prepared from a patient with BPH by a differential centrifugation of the tissue homogenate. The enzyme activity was inhibited by 10(-4)-10(-5) M of ouabain. The hexane extract, the ether extract, the ethyl acetate extract, and the butanol extract of the roots caused 27.6-81.5% inhibition of the enzyme activity at 0.1 mg/ml. In addition, a column extraction of stinging nettle roots using benzene as an eluent afforded efficient enzyme inhibiting activity. Steroidal components in stinging nettle roots, such as stigmast-4-en-3-one, stigmasterol, and campesterol inhibited the enzyme activity by 23.0-67.0% at concentrations ranging from 10(-3)-10(-6) M. These results suggest that some hydrophobic constituents such as steroids in the stinging nettle roots inhibited the membrane Na+,K(+)-ATPase activity of the prostate, which may subsequently suppress prostate-cell metabolism and growth.
======================================================================
28.) Testosterone metabolism in primary cultures of human prostate
epithelial cells and fibroblasts.
======================================================================
AU: Delos-S; Carsol-JL; Ghazarossian-E; Raynaud-JP; Martin-PM
AD: Laboratoire de Cancerologie Experimentale, Faculte de Medecine Secteur Nord, Marseille, France.
SO: J-Steroid-Biochem-Mol-Biol. 1995 Dec; 55(3-4): 375-83
ISSN: 0960-0760
PY: 1995
LA: ENGLISH
CP: ENGLAND
AB: We compare testosterone (T) metabolism in primary cultures of epithelial cells and fibroblasts separated from benign prostate hypertrophy (BPH) and prostate cancer tissues. In all cultures, androstenedione (delta 4) formed by oxidation of T by 17 beta-hydroxysteroid dehydrogenase (17 beta-HSD) represented 80% of the metabolites recovered. The amounts of 5 alpha-dihydrotestosterone (DHT), formed by reduction of T by 5 alpha-reductase (5 alpha-R), were small: 5 and 2% (BPH) and 8 and 15% (adenocarcinoma) for epithelial cells and fibroblasts, respectively. Northern blot analysis of total RNA from epithelial cells (BPH or adenocarcinoma) attributed the reductive activity to the 5 alpha-reductase type 1 isozyme and oxidative activity to the 17 beta-HSD type 2. In cancer fibroblasts, only little 17 beta-HSD type 2 mRNA was detected. The 5 alpha-reductase inhibitors, 4-MA (17 beta-(N,N-diethyl)carbamoyl-4-methyl-4-aza-5 alpha-androstan-3-one) and finasteride, inhibited DHT formation with a preferential action of 4-MA on epithelial cells (BPH or adenocarcinoma) and of finasteride on fibroblasts from adenocarcinoma. Neither inhibitor acted on delta 4 formation. On the other hand, the lipido-sterol extract of Serenoa repens (LSESr, Permixon) inhibited the formation of all the T metabolites studied [IC50 S = 40 and 200 micrograms/ml (BPH) and 90 and 70 micrograms/ml (adenocarcinoma) in epithelial cells and fibroblasts, respectively]. These results have important therapeutic implications when selecting appropriate treatment options for BPH.
======================================================================
29.) Human prostatic steroid 5 alpha-reductase isoforms--a comparative study of selective inhibitors.
======================================================================
AU: Iehle-C; Delos-S; Guirou-O; Tate-R; Raynaud-JP; Martin-PM
AD: Laboratoire de Cancerologie Experimentale, Faculte de Medecine, Marseille, France.
SO: J-Steroid-Biochem-Mol-Biol. 1995 Sep; 54(5-6): 273-9
ISSN: 0960-0760
PY: 1995
LA: ENGLISH
CP: ENGLAND
AB: The present study describes the independent expression of the type 1 and 2 isoforms of human 5 alpha-reductase in the baculovirus-directed insect cell expression system and the selectivity of their inhibition. The catalytic properties and kinetic parameters of the recombinant isozymes were consistent with published data. The type 1 isoform displayed a neutral (range 6-8) pH optimum and the type 2 isoform an acidic (5-6) pH optimum. The type 2 isoform had higher affinity for testosterone than did the type 1 isoform (Km = 0.5 and 2.9 microM, respectively). Finasteride and turosteride were selective inhibitors of the type 2 isoform (Ki (type 2) = 7.3 and 21.7 nM compared to Ki (type 1) = 108 and 330 nM, respectively). 4-MA and the lipido-sterol extract of Serenoa repens (LSESr) markedly inhibited both isozymes (Ki (type 1) = 8.4 nM and 7.2 micrograms/ml, respectively; Ki (type 2) = 7.4 nM and 4.9 micrograms/ml, respectively). The three azasteroids were competitive inhibitors vs substrate, whereas LSESr displayed non-competitive inhibition of the type 1 isozyme and uncompetitive inhibition of the type 2 isozyme. These observations suggest that the lipid component of LSESr might be responsible for its inhibitory effect by modulating the membrane environment of 5 alpha-reductase. Partially purified recombinant 5 alpha-reductase type 1 activity was preserved by the presence of lipids indicating that lipids can exert either stimulatory or inhibitory effects on human 5 alpha-reductase.
======================================================================
30.) Serenoa repens (Permixon). A review of its pharmacology and therapeutic efficacy in benign prostatic hyperplasia.
======================================================================
Plosker GL; Brogden RN
Adis International Limited, Auckland, New Zealand.
Drugs Aging (NEW ZEALAND) Nov 1996 9 (5) p379-95 ISSN: 1170-229X
Language: ENGLISH
Document Type: JOURNAL ARTICLE; REVIEW; REVIEW, TUTORIAL
Journal Announcement: 9704
Subfile: INDEX MEDICUS
Serenoa repens (Permixon) has been available for several years for the treatment of
men with benign prostatic hyperplasia (BPH). The drug is the n-hexane lipidosterolic
extract of the dwarf American palm (also known as Serenoa repens) and is a complex
mixture of various compounds. A number of pharmacodynamic effects have been
demonstrated with the lipidosterolic extract of Serenoa repens (LSESR), suggesting
multiple mechanisms of action including in vitro inhibition of both type 1 and type 2
isoenzymes of 5 alpha-reductase and interference with binding of dihydrotestosterone
to cytosolic androgen receptors in prostate cells. In controlled clinical trials in
men with BPH, oral administration of Serenoa repens 160 mg twice daily for 1 to 3
months was generally superior to placebo in improving subjective symptoms, such as
dysuria, as well as objective parameters. The frequency of nocturia was reduced by
33 to 74%, while urinary frequency during the day decreased by 11 to 43% and peak
urinary flow rate increased by 26 to 50% with Serenoa repens. Corresponding values
for placebo were 13 to 39%, 1 to 29% and 2 to 35%. The only large comparative trial
conducted to date, in which > 1000 men with moderate BPH were randomised to receive
Serenoa repens 160 mg twice daily or finasteride 5 mg once daily for 6 months,
demonstrated similar efficacy between the two drugs. No statistically significant
difference was demonstrated between treatment groups for improvement in patient self-
rated quality-of-life scores and the primary end-point of objective symptom score;
International Prostate Symptom Score improved by 37% with Serenoa repens compared
with 39% with finasteride. In much smaller comparative trials, few significant
differences were demonstrated between Serenoa repens and alpha 1-receptor
antagonists, and larger randomised trials of adequate duration are required to better
compare the clinical efficacy of these drugs. The most frequently reported adverse
events in clinical trials with Serenoa repens have been minor gastrointestinal
problems (e.g. nausea and abdominal pain). In conclusion, Serenoa repens is well
tolerated and has greater efficacy than placebo and similar efficacy to finasteride
in improving symptoms in men with BPH. Although there is a need for further
comparative studies, particularly with alpha 2-receptor antagonists, available data
indicate that Serenoa repens is a useful alternative to alpha 1-receptor antagonists
and finasteride in the treatment of men with BPH. (86 References)
======================================================================
31.) Effect of Serenoa repens extract (Permixon) on estradiol/testosterone-induced experimental prostate enlargement in the rat.
======================================================================
Paubert-Braquet M; Richardson FO; Servent-Saez N; Gordon WC; Monge MC; Bazan NG;
Authie D; Braquet P
BIO-Inova EuroLab Research Labs, Plaisir, France.
Pharmacol Res (ENGLAND) Sep-Oct 1996 34 (3-4) p171-9 ISSN: 1043-6618
Language: ENGLISH
Document Type: JOURNAL ARTICLE
Journal Announcement: 9707
Subfile: INDEX MEDICUS
The effect of the lipidosterolic extract of Serenoa repens (LSESR) on experimental
prostate enlargement was investigated in three groups of rats: shams treated with
LSESR (sham rats), castrated animals treated with estradiol and testosterone
(castrated rats), castrated animals treated with estradiol/testosterone and treated
with LSESR (castrated and treated rats). Following three months of continuous
hormonal treatment, the weight of prostates in estradiol/testosterone-treated
castrated rats was significantly increased in comparison with sham-operated rats.
Such an increase started rapidly, reached a maximum by 30 days and remained at a
plateau or slightly declined thereafter. The increase of prostate total weight
induced by the hormone treatment was inhibited by administration of LSESR. Indeed,
the weight was significantly lower at day 60 and day 90 for the dorsal and lateral
regions of the prostate. The weight of the ventral region of the prostate was
significantly lower after 30 and 60 days treatment with LSESR. These results
demonstrate that administering LSESR to hormone-treated castrated rats inhibits the
increase in prostate wet weight. This effect of LSESR may explain the beneficial
effect of this extract in human benign prostatic hypertrophy.
====================================================================
DATA-MEDICOS/DERMAGIC-EXPRESS No (61) 17/06/99 DR. JOSE LAPENTA R.
====================================================================
|
