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The Use of Serenoa Repens (Saw Palmetto) in Hair Care Products

Authors:
1/4
Volume 5- Issue 4: 2018
ISSN: 2574-1241
DOI: 10.26717/BJSTR.2019.13.002348
Joanna Igielska Kalwat.
Biomed J Sci & Tech Res
Review Article
Biomedical Journal of


Serenoa Repens


Faculty of Cosmetology and Educational Sciences, Poland
 : December 21, 2018;  : January 11, 2019
 Joanna Igielska Kalwat, Faculty of Cosmetology and Educational Sciences, Poland
Introduction
Saw palmetto it is a plant that growns in the United States,
Central, North and South America and West Indies. In the USA, it can
be found in the marshy areas of Florida, North Carolina, Alabama and
Texas. Palm fruit is characterized by purple-black coloring. It grows
in clusters, and the fruiting period falls in October - December. Ripe
and partially dried fruits are used to prepare extracts. In traditional
medicine, the interest in saw palmetto goes back to the beginning
of the 19th century. Native Americans consumed this plant to
overcome the problems associated with prostatic hyperplasia, or

introduced into the pharmaceutical market, but around 1950 it

Studies on the plant were relaunched in the 1980s.

Serenoa repens (W. Bartram) Small plant belongs to the
Arecaceae family. It is a monoicous palm tree with thin bark. This
species is long-lived and can grow for 500-700 years. It has an
underground rhizome from which 3 to 7 leaves grow every year.
The leaves are leathery, green or white-green in color, characterized
by both palmoid and fan shape. The petioles are spiny, longer than
the leaf blade, and covered with sharp spines, which is why the
   
are small, white and gathered in panicles growing from the leaf
angles. The palm is pollinated by insects and blooms from April
 
blue-black color. They have an ellipsoidal shape [1]. The healing
raw material consists of the dried, mature fruit - Sabalis serrulatae
fructus of Serenoa repens. The fruit must contain at least 11% of
fatty acids. The raw material is sourced exclusively from the wild.
The fruit can be eaten raw, or in the form of an extract enclosed in a
capsule, tincture or tablet [2].
The main components of the fruit and extract obtained from
them is the lipid-sterol fraction. This fraction includes triglycerides,
phytosterols (beta-sitosterol, stigminerol, campesterol, cycloarte-
nol), fatty acids (capric, caproic and caprylic, lauric, myristic, ole-
ic and palmitic), their ethyl esters and triglycerides. Saw palmetto
also contains kaempferol, quercetin, isoquercitrin, roifolin, farne-
sol, lupeol, lupenone, uronic acids, arabinose, galactose, polysac-
charides, resins and tannins. Biological active monoacylglycerides
(1-monolaurine and 1-monomyristin) with cytotoxic activity on
human prostate cells were isolated from the raw material [3]. Due
     
in the food, pharmaceutical, medical and cosmetics industries. The
Maya used Serenoe repens as a tonic. In Florida, Native Americans
         
an expectorant and antiseptic. Extract from saw palmetto contrib-
utes to the reduction in the activity level of enzyme responsible
      
a hormone whose elevated level causes numerous ailments of the
urinary tract. This can be manifested by among others infertility,

The following paper describes saw palmetto, a plant that found its use already in the 19th century. Nowadays, it is still used in medicine,

         
     
times.
 Serenoa Repens

Joanna Igielska Kalwat. The Use of Serenoa RepensBiomed J Sci & Tech Res 13(1)-2019.
BJSTR. MS.ID.002348. DOI: 10.26717/ BJSTR.2019.13.002348.
Volume 13- Issue 1: 2019
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hormonal failure of male or female reproductive organs, testicular
tumors and polycystic ovary syndrome [4].
        
which is manifested by abdominal pain and problems with passing
urine [1]. The consequence of prostatic hypertrophy may be
complete urinary retention in the body. Phytosterols contained
in the saw palmetto limit the cholesterol absorption process.
         
Extracts of saw palmetto fruit treat voiding disorders in patients
with prostatic hypertrophy, reduce urinary retention in the bladder

of prostatic mucous membranes and muscles, as well as cause the
disappearance of burning and pain during urination or urgent need

  
      
and have immunostimulatory effect (polysaccharides). Flavonoids
      
and they also improve blood circulation. Saw palmetto extract
also act as antiaggregatives and stimulate epithelial and muscle
regeneration [6-7].
Extract of saw palmetto fruit contributes to inhibiting the
       
inhibiting the arachidonic acid cascade (reduction of 5-lipoxygenase
activity). Blocking of androgen activity by saw palmetto extract, as
 
in vivo experiments, it was found that the administration of extract
together with hormones (testosterone and estradiol) results in
inhibited prostate weight gain in castrated rats [8]. Palm fruit
(Serenoa repens) extract is a preparation that has an effective and
safe effect on human health. It is well tolerated by the majority of
patients. The best therapeutic effects can be achieved when using
extract of dried fruit that has been obtained by extracting the raw
material (using CO2, in supercritical conditions, with preservation
       
        
[9]. Appropriate doses of Serenoa repens extract range from
800 to 1200mg per day. Therapy should last at least 4-6 months.
Preparations of saw palmetto fruit bring effective effects also in
      
disorders (psoriasis, urticaria, pemphigus and atopic dermatitis),
  
pain.
The sabal palm is also used as a sedative and to increase sex
drive (aphrodisiac). It is utilized in the treatment of chronic migraine
headaches. Serenoe repens can be used in patients with asthma,
       
pertussis. It is very useful with excessive secretion of mucus from
the sinuses and the nose [10,11]. In the cosmetics industry, saw
palmetto fruit have found application in preparations intended for
scalp and hair care. The plant in question is antiandrogenic, and
therefore can be used in the treatment of androgenetic alopecia [12].
Excessive hair loss is caused by many environmental factors such as
inadequate diet, irritating cosmetics and stress. In approximately
95% of cases, baldness are caused by hormones - androgens.
Androgenetic alopecia is an increased or rapid hair loss without
simultaneous physical changes on the skin. The type of baldness
discussed here is one of the most severe problems affecting mainly
men. The progressive process of baldness contributes to the lack of
acceptance towards one’s appearance. Therefore, manufacturers of
scalp and hair care cosmetics make every effort to isolate the active
substance that will effectively combat the problem.

which is a stronger and more active testosterone derivative.
    
reaction catalysed by 5-alpha-reductase catalysed enzyme (5-AR)
[13]. Serenoa extract is a potent 5-AR inhibitor, the use of which
        
        
and nuclear androgen receptors. The already mentioned

alopecia. Sebaceous glands contain also 5-alpha-reductase - an
       
             
generally believed) that causes hair loss. This hormone contributes
to the miniaturization of hair follicles, which leads to a shortening
of the hair’s lifespan and its incorrect production. The hair becomes
thinner, lighter and shorter. This type of baldness mainly affects
men and is manifested by the loss of hair on the top of the head

with endocrine disorders or with a fall in female hormones after
pregnancy or during menopause [14,15]. Treatment of androgenetic
alopecia involves the inhibition of 5-alpha-reductase activity. This
      

doses than in the treatment of prostatic hypertrophy. An alternative
to synthetic drugs in the prevention of androgenetic alopecia are
preparations containing saw palmetto extract.
In the market of dietary supplements, several preparations
containing this raw material may be found. They are recommended
to people struggling with not so much with androgenic alopecia, as
with worsened condition of hair and skin. Typically, such products
contain also vitamins A, E, C and silicone. Saw palmetto extract can
also be found in hair care products: shampoos (e.g. Ducray Sabal),

a vast array of preparations containing sabal palmetto extract, but
the vast majority belong to the category of dietary supplements.
These preparations do not have medicinal properties. In Poland,
only two drugs are available containing a standardized extract from
saw palmetto: Prostamol Uno and Sterko. Their advantage over
other preparations with this raw material results from the rigorous
procedure of introducing and controlling medicinal products
that are subject to the Chief Pharmaceutical Inspector. Dietary
supplements are controlled by the Sanitary and Epidemiological
       
only, and their true qualitative and quantitative composition does
not always coincide with the manufacturers’ declarations.
 Volume 13- Issue 1: 2019
Joanna Igielska Kalwat. The Use of Serenoa RepensBiomed J Sci & Tech Res 13(1)-2019.
BJSTR. MS.ID.002348. DOI: 10.26717/ BJSTR.2019.13.002348.3/4
Both drugs alleviate ailments associated with the initial stage
of benign prostatic hyperplasia. In addition to the aforementioned
medicines based on saw palmetto extract, supplements with this
ingredient may also be found on the market (Table 1) [19]. Saw
palmetto is a potential therapeutic in androgenetic alopecia affecting
both women and men. In addition to the oral application, there is
a much less invasive form, not affecting the hormonal balance of
the whole organism - a direct application to the scalp in the form
          
androgenetic alopecia, the most effective are shampoos, masks
and rub-in compounds with extract of saw palmetto fruit. They
can also be used in prevention of hair loss [22]. Extract from saw
palmetto has also found application in the treatment of androgenic
acne, hirsutism (virilism in women) and hyperandrogenism.
Saw palmetto is a component of anti-acne preparations as well
as shampoos and hair masks regulating the secretion of sebum
[23]. In rare cases, the researchers observed side effects such as
mild dizziness and headache, nausea, vomiting, constipation or
diarrhea. Using palmetto extract may reduce blood coagulation as
well as increase the tendency to bruises and bleedings. Therefore,
people who have a planned surgical procedure should stop using
saw palmetto at least two weeks before. The preparation is not
recommended during pregnancy and breastfeeding or when using
contraceptives. This plant may cause irreversible damage to the
fetus or lead to a miscarriage [24,25].
Table 1: Examples of preparations containing saw palmetto extract, available in Polish pharmacies [19-21].
   
Prostamol Uno Treatment of mild prostate hypertrophy Medicinal product Berlin Chemie
Sterko Treatment of mild prostate hypertrophy Medicinal product Glenmark
Saw Palmetto Supporting the treatment of mild prostatic
hypertrophy Dietary supplement Solgar
MultiProsti Supporting the treatment of mild prostatic
hypertrophy Dietary supplement +Pharma Arzneimittel
Gold-Vit for men Vitamin supplement for men Dietary supplement 
Rutiver Vitamin supplement for men Dietary supplement Biovena
Profolan  Dietary supplement Profolan
Prostatan Proper prostate function, hair growth stimulation Dietary supplement 
Prostenal Perfect Support of prostate function and health of the
genitourinary and urinary tract Dietary supplement Walmarkt
 Weak hair needing reinforcement Cosmetic Elfa Pharm

Weak
hair needing reinforcement
Cosmetic Elfa Pharm
 Weak hair needing reinforcement Cosmetic Elfa Pharm
Ducray Sabal Shampoo for oily hair Cosmetic Ducra
Conclusion
The development of technology, cosmetology, medicine and
consumer awareness forces the manufacturers to search for new
active substances of both plant and synthetic origin. They are
   
health and beautiful appearance. One controversial plant that has

described in the above paper.
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11. Marderosian A (2000) Saw palmetto in the review of natural products.


Joanna Igielska Kalwat. The Use of Serenoa RepensBiomed J Sci & Tech Res 13(1)-2019.
BJSTR. MS.ID.002348. DOI: 10.26717/ BJSTR.2019.13.002348.
Volume 13- Issue 1: 2019
4/4
12. 
Evidence that Serenoa repens extract displays an antiestrogenic activity
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14. 
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15. 
of medicinal herbs. In Duke JA, Bogenschutz Godwin MJ, Cellier J, Duke
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16.       ania niepo.
Przegld Urologiczny 5: 23.
17.        
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18. Farmakopea Polska VIII (I, II, III) (2008) Urzd Rejestracji Produktów
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19. 

      
Association, Naples (USA).
20. 
leki ro
21.           
of Pygeum africanum and Serenoa repens. Urology Res 28(3): 201-210.
22. Prager N, Bickett K, French N, Marcovici G (2002) A randomized,
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botanically derived inhibitors of 5-alpha-reductase in the treatment of
androgenetic alopecia. J Altern Complement Med 8(2): 143-152.
23. 
In Schaffner W (Eds.) Wyd. Multico, Warszawa, Poland.
24.         
acylglycerides from the berries of Saw-Palmetto (Serenoa repens). J Nat
Prod 60(4): 417-418.
25.              

        
1005.
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ISSN: 2574-1241
DOI: 10.26717/BJSTR.2019.13.002348
Joanna Igielska Kalwat.
Biomed J Sci & Tech Res
... It is also used for benign prostatic hyperplasia and prostatic cancer treatment (17)(18)(19)(20)(21). The plants or extracts can be used in natural product creation such as hair supplements for hair growth improvement and hair loss reduction, given the better absorption and improved activity for the treatment of alopecia in shampoos and hair serums (22)(23)(24). In this regard Polygonum multiform and saw palmetto (Serenoa repens) have been used in hair care products (23). ...
... The plants or extracts can be used in natural product creation such as hair supplements for hair growth improvement and hair loss reduction, given the better absorption and improved activity for the treatment of alopecia in shampoos and hair serums (22)(23)(24). In this regard Polygonum multiform and saw palmetto (Serenoa repens) have been used in hair care products (23). In addition to the β-sitosterol substance contained in the Dillenia species, there were high quantities of oleamide percentage-wise as elucidated by the GC-MS method. ...
Article
Introduction: Plants containing β-sitosterol and oleamide are important for various diseases. So, Dillenia indica, D. obovata, and D. pentagyna were investigated for phytochemicals, cytotoxicity, and genotoxicity levels on peripheral blood mononuclear cells (PBMCs) and Hela cells. The protective effect of D. pentagyna extract on a HepG2 cell line was also investigated. Methods: Gas chromatography-mass spectrometry (GC-MS) and high-performance liquid chromatography (HPLC) were used for phytochemical analysis. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) tetrazolium reduction (MTT) and comet assays were performed for toxicity testing and protective effects against DNA oxidative damage. Results: The major components were oleamide and β-sitosterol at 38.464-58.247% and 5.585-6.887% with concentration and quantity of β-sitosterol at 0.2-0.37 mg/mL and 0.42-0.964 mg/g leaf. The D. indica, D. obovata, and D. pentagyna toxicities on PBMCs showed IC50 values at >430, >430, and 350 μg/mL respectively, with no significant DNA damage (P > 0.05) compared to the negative control group. All plant extracts showed toxic activity on Hela cell with IC50 values at <0.43 μg/mL and induced significant DNA damage (P < 0.05) compared to the negative control group. Conversely, the activity of the D. pentagyna extract indicated low cytotoxic activity against HepG2 (IC50>430 μg/mL), no significant (P > 0.05) DNA damage induction, significantly (P < 0.05) decreased DNA damage level, and tremendous antioxidant effect. Additionally, a combined mixture of all plants in an equal proportion revealed no IC50 value and insignificant DNA damage. Conclusion: All the studied species contained oleamide and β-sitosterol, with toxicity on Hela cells without toxicity on PBMC. The D. pentagyna species showed high antioxidant effects and no toxicity on HepG2.
... Another highly recommended compound is vitamin B 2 , also known as riboflavin. Moreover, two approved drugs, finasteride, and dutasteride, were chosen as positive controls to be compared with the aforementioned natural compounds (17)(18)(19)(20)(21). ...
Article
Full-text available
Background: Dihydrotestosterone (DHT), the most critical pathogenic androgen in hair loss, is identified as an etiologic factor of androgenetic alopecia (AGA). The AGA is a genetically common disorder among men and is characterized by the progressive conversion of hair follicles into small vellus hair. Steroid 5 alpha-reductase type 1 (5AR1) is a crucial target responsible for this gradual replacement. The 5AR1 function is determined by converting testosterone to DHT. The inhibitors of 5AR1 play their role by blocking the DHT production pathway. Objectives: This study focused on the potent inhibitors of the 5AR1 enzyme to suggest effective synthetic drugs for restoring hair loss with fewer side effects. Methods: The three-dimensional structure of 5AR1 was created using homology modeling methods. Then, the inhibitory effects of some significant compounds from natural sources were examined on the 5AR1 protein using molecular docking approaches. Results: The obtained results suggest that two natural compounds isolated from Serenoa repens, including beta-sitosterol and stigmasterol, could inhibit the regular activity of 5AR1 and can be recommended as safe and novel AGA medicines for hair restoration.
... The active ingredient of Serenoa repens (SR) is saw palmetto, which is a palm tree berry extract that inhibits the 5-alpha-reductase and was advertised as a regimen for benign prostatic hyperplasia and AGA. [140][141][142] In a study with 10 male subjects with AGA, improvement was noted in 60% of the participants. 143 Another study applying topical SR extract in lotion and shampoo for 3 months led to 35% increase in hair density. ...
Article
Full-text available
Background Androgenetic alopecia (AGA) is the most common form of hair loss consisting of a characteristic receding frontal hairline in men and diffuse hair thinning in women, with frontal hairline retention, and can impact an individual's quality of life. The condition is primarily mediated by 5-alpha-reductase and dihydrotestosterone (DHT) which causes hair follicles to undergo miniaturization and shortening of successive anagen cycles. Although a variety of medical, surgical, light-based and nutraceutical treatment options are available to slow or reverse the progression of AGA, it can be challenging to select appropriate therapies for this chronic condition. Aims To highlight treatment options for androgenetic alopecia taking into consideration the efficacy, side effect profiles, practicality of treatment (compliance), and costs to help clinicians offer ethically appropriate treatment regimens to their patients. Materials and Methods A literature search was conducted using electronic databases (Medline, PubMed, Embase, CINAHL, EBSCO) and textbooks, in addition to the authors' and other practitioners' clinical experiences in treating androgenetic alopecia, and the findings are presented here. Results Although topical minoxidil, oral finasteride, and low-level light therapy are the only FDA-approved therapies to treat AGA, they are just a fraction of the treatment options available, including other oral and topical modalities, hormonal therapies, nutraceuticals, PRP and exosome treatments, and hair transplantation. Discussion Androgenetic alopecia therapy remains challenging as treatment selection involves ethical, evidence-based decision-making and consideration of each individual patient's needs, compliance, budget, extent of hair loss, and aesthetic goals, independent of potential financial benefits to the practitioners.
Article
Background: Dihydrotestosterone (DHT), the most critical pathogenic androgen in hair loss, is identified as an etiologic factor of androgenetic alopecia (AGA). The AGA is a genetically common disorder among men and is characterized by the progressive conversion of hair follicles into small vellus hair. Steroid 5 alpha-reductase type 1 (5AR1) is a crucial target responsible for this gradual replacement. The 5AR1 function is determined by converting testosterone to DHT. The inhibitors of 5AR1 play their role by blocking the DHT production pathway. Objectives: This study focused on the potent inhibitors of the 5AR1 enzyme to suggest effective synthetic drugs for restoring hair loss with fewer side effects. Methods: The three-dimensional structure of 5AR1 was created using homology modeling methods. Then, the inhibitory effects of some significant compounds from natural sources were examined on the 5AR1 protein using molecular docking approaches. Results: The obtained results suggest that two natural compounds isolated from Serenoa repens, including beta-sitosterol and stigmasterol, could inhibit the regular activity of 5AR1 and can be recommended as safe and novel AGA medicines for hair restoration.
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Polycystic ovary syndrome (PCOS) is characterized by gynaecological endocrine and metabolic abnormality of women at reproductive ages. It is established that hyperandrogenism, insulin resistance, menstrual abnormalities, and chronic absence of ovulation of polycystic ovary are commonly associated with symptoms. It might indicate the multidisciplinary approach for the therapeutic management of PCOS. Conventional medical management concentrated single symptom, is often associated with the side effect, maybe contraindicated and ineffective in some conditions. So far women with PCOS have expressed a desire for alternative medicine. Ayurvedic medicine has been emerging as one of the commonly practised medicines for different health problems, including PCOS. In this review, an attempt has been made to study the use and mode of action of potential Ayurvedic drugs for the treatment of PCOS. This review is mainly based on the scientific literature search. The first search on plant possesses multiple effects against PCOS reproductive and metabolic complications. Selected plants from the first search were used as a keyword for the second search. They include Cinnamomum zeylanium, Gymnema sylvestre, Mentha spicata, Pergularia daemia, Saraka indica, Saw palmetto, Tribulus terrestis, and Withania somnifera. The second search sought the reproductive endocrinal and metabolic demonstrated mechanism of the selected plants.This review supports the alternative Ayurvedic medication as a standard effective and safe drug in the management of PCOS.
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Saw palmetto [Serenoa repens (Bartr.) Small] is the most common native palm in the U.S. and, possibly, the most useful. Cattle and wildlife, especially black bears and white-tailed deer, consume the fruits. The flowers are a favorite nectar source for honey bees, and the sprawling, shrubby palm provides excellent cover for birds, reptiles, and small animals. Saw palmetto's edible fruits were a staple in the diet of Florida's pre-contact inhabitants. Vegetative parts of the plant supply fiber, wax, and roof thatch. Current interest in saw palmetto stems from its use in the treatment of benign prostatic hyperplasia. An estimated 6 800 000 kg of the fruit are shipped to Europe each year. Preliminary data suggest that the economic value of saw palmetto harvesting may exceed that of cattle grazing, the common use of much saw palmetto habitat.
Article
From the fruits of S. repens some extracts have been prepared with a procedure involving CO2 in hypercritical conditions at different sets of temperature and pressure. The obtained oils showed in castrated prepuberal rats a significant anti-androgenic activity, in agreement with what reported in the literature for other lipophilic extracts. The best results were observed with the extract arising from hypercritical CO2 at 45°C and 220 bar.
Article
S. repens is a low shrubby palm native to the southern regions of North America. Preparations from the fruit have been used in traditional American medicine in the treatment of bladder, urethra and prostate irritations. Today, lipophilic extracts of the S. repens fruit are widely used in the therapy of urological symptoms associated with BPH. The clinical efficacy of these extracts and their good tolerability have been demonstrated in numerous clinical trials, including double-blind studies. Inhibition of 5α-reductase activity, antagonism of dihydrotestosterone binding to androgen receptors, double blocking of cycloxygenase and lipoxygenase pathways are the main mechanisms involved in the antiprostatic effect of the S. repens extracts.
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A Practical, Authoritative CompendiumThis handbook catalogs 365 species of herbs having medicinal or folk medicinal uses, presenting whatever useful information has been documented on their toxicity and utility in humans and ani-mals. Plants from all over the world - from common cultivars to rare species - are included in these 700 pages. The toxicity of these species varies, but the safety of each has been formally or informally questioned by the Food and Drug Administration, National Cancer Institute, Department of Agriculture, Drug Enforcement Administra-tion, or Herb Trade Association. Easy-to-Locate Facts and FiguresDesigned to enable fast access to important information, this hand-book presents information in both catalog and tabular forms. In the catalog section, plants are presented alphabetically by scientific name. (The index permits you to locate an herb by its common name.) A detailed sketch of the chief identifying features accompa-nies most catalog entries. For each species the following information, as available, is presented and referenced: Family and colloquial namesChemical contentUses and applications - present and historicalProcessing, distribution, and economic potentialToxicological agents and degree of toxicityPoison symptoms in humans and animalsTreatment and antidotes References to original literature Five Tables of Accessible DataGiven a plant species, you can easily determine its toxins; or, given a toxin, you can discover which plants contain it. These and other data are presented in convenient tabular formats as appendixes to the handbook. Other information contained in these tables include toxicity ranking and other toxicity data (as applicable), such as mode of contact, organs affected, and lethal dose; and proximate analyses of selected foods. These tables are titled: Medicinal Herbs: Toxicity Ranking and PricelistToxins: Their Toxicity and Distribution in Plant GeneraHigh Plant Genera and Their ToxinsPharmacologically Active PhytochemicalsProximate Analyses of Conventional Plant Foods
Article
Within the group of botanical products there is a large range of variation with regard to their properties. Some products are identical to foods while others come close to or are medicines. Botanical products are regulated differently within the different member states of the European Union (EU) and globally. They are regulated either as food or as medicinal products, and in the latter case often with simplified registration procedures. These differences are caused by differences in traditional use, in cultural and historical background, in scientific substantiation and in enforcement of current legislation. One may expect that in the future differences will remain, unless EU legislation is enacted with sufficient room for different approaches. The strengths and weaknesses of the different regulatory procedures have been reviewed and evaluated as well as the current methods for quality, efficacy and safety evaluation. Criteria to categorize botanical products have been defined, such that botanical products can be regulated under the current food and medicinal regulations. Furthermore, a decision tree has been developed as a tool to distinguish herbal medicinal products from botanical health products and vice versa, and to provide a stepwise framework for the assessment of safety and efficacy.
Article
A double-blind placebo-controlled study was performed in 35 benign prostatic hypertrophy (BPH) patients never treated before. The patients were randomized into two groups, the 1st (18 cases) receiving Serenoa repens extract (160 mg t.d.) for 3 months up to the day before the operation of transvesical adenomectomy and the 2nd (17 cases) receiving placebo. Steroid receptors were evaluated in the nuclear (n) and cytosolic (c) fraction using the saturation analysis technique (Scatchard analysis or single saturating-dose assay) for androgen (AR) and estrogen (ER) receptors and the enzyme immunoassay (EIA) for ER and progesterone receptors (PgR). Scatchard analysis of ERc and ERn revealed the presence of two classes of binding sites, one with high-affinity low-capacity binding and the other with low-affinity high-capacity binding. In the untreated BPH group, ER were higher in the n than in the c fraction: ERn were positive in 14 cases and ERc in 12 of 17 cases. In the BPH group treated with S. repens extract on the contrary, ERn were negative for both binding classes in 17 cases and ERc in 6 of 18 cases. Using EIA, ERn and ERc were detected in all 15 samples examined, but in the treated group, ERn were significantly (p less than 0.01) lower than in the untreated group, whilst ERc remained almost unchanged. Similar results were obtained measuring PgR: the n fraction of the treated group prostatic samples was significantly (p less than 0.01) lower than that of the untreated group.(ABSTRACT TRUNCATED AT 250 WORDS)
Article
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.
Article
In Italy plant extracts represent 8.6% of all pharmacological prescriptions for Benign Prostatic Hyperplasia (data from 1991). This review evaluates all the suggested mechanisms of action for plant extracts. Recently we demonstrated an antiestrogenic effect of Serenoa Repens in BPH patients. Clinical trials with plant extracts have yielded conflicting results. In a recent review by Dreikorn and Richter, only five placebo controlled studies were found. Moreover, as opposed to chemically defined drugs, it is possible that for these extracts the active ingredients are not known; consequently pharmacodynamic and pharmacokinetic data are often missing. The International Consultation of Benign Prostatic Hyperplasia (Paris, June 1991) concluded that, to date, phytotherapeutic agents must be considered as a symptomatic treatment. Now more adequate pharmacological and clinical studies, placebo controlled, should determine the exact role of these drugs in the treatment of BPH.
Article
Brine shrimp lethality-directed fractionation of the 95% EtOH extract of the powdered, dried berries of Serenoa repens (Bart.) Small (saw-palmetto) (Palmae) led to the isolation of two monoacylglycerides, 1-monolaurin (1) and 1-monomyristin (2). Compounds 1 and 2 showed moderate biological activities in the brine shrimp lethality test and against renal (A-498) and pancreatic (PACA-2) human tumor cells; borderline cytotoxicity was exhibited against human prostatic (PC-3) cells. The fruits and extracts of saw-palmetto are taken orally as an herbal medicine to prevent prostatic hyperplasias.
Article
In Europe, phytotherapeutic preparations have been prescribed for the treatment of symptomatic benign prostatic hyperplasia (BPH) for over 20 years [l–4]. In these countries, phytotherapeutic preparations represent approximately l/3 of total sales of all therapeutic agents sold for the treatment of BPH. In France, and other countries, phytotherapeutic preparations are the most widely used drugs for the treatment of BPH. In Asia, Africa, and India, phytotherapy is considered a first-line treatment for BPH and has been utilized effectively for centuries. In the United States, the multi-million dollar sales of phytotherapeutic preparations for “the health of the prostate and bladder” attests to the widespread utilization of these agents [3, 4]. Two of the most popular phytotherapeutic agents that have undergone both clinical studies to determine their efficacy, and have been the subject of basic science studies to identify the mechanism(s) of action are Pygeum africanum (Tadenan), an extract from the bark of the African plum tree, and Serenoa repens (Permixon), a lipido-sterol extract of dwarf palm. Tadenan and Permixon are registered therapeutic agents of Debat Pharmaceuticals, and Pierre Fabre Medicament, respectively. Manufacture of both preparations are tightly controlled and subjected to strict quality control for stability of component composition. In regard to phytotherapeutic agents, each individual preparation (even from the same plant source) must be considered individually because of differences in the extraction techniques, preparation of products, composition, and biological activities. Thus, the clinical and biological activities of one preparation cannot be extrapolated to other preparations of the same plant source. Thus, studies described in this review which utilize the preparations that are manufactured by DEBAT (Pygeum africanum) or Pierre Fabre Medicament (Serenoa repens) are referred to by their trade names, Tadenan and Permixon, to differentiate them from other nonstandardized preparations of the same plants.