- study ingredients testing
(original generation 3 hairloss products)
saw palmetto berry extract
the saw palmetto
is a small shrubby palm native to florida and has a
long folk history as an aphrodisiac and sexual
rejuvenator. recent studies have implicated saw palmetto
as an effective treatment for benign prostatic
hyperplasia (bph). investigators have found that the
fatty and sterolic extracts (fatty acids: capric,
caprylic, caproic, lauric, palmitic, and oleic; sterols:
beta-sitosterol, stigmasterol, cycloartenol, luepol,
lupenone and 24 methyl-cycloartenol) are the active
molecular components responsible for its therapeutic
scientific research shows that:
"in a large european study, one in which a
pharmaceutical clinical trial model was closely
followed, a saw palmetto product (permixon) was
found to cause no change in standard blood tests
and no change in serum prostate specific anagen
levels (psa) during a six month treatment period."
carraro et al. prostate vol. 29 pp.231-240 1996
1,098 patients with bph (benign prostatic hyperplasia)
in that study, the general safety profile of saw
palmetto compared favorably with that of
finasteride (the chemical used in the drugs propecia
[for hairloss treatment] and proscar [for prostate
treatment] ), and sexual side effects were less common
with the extract than with the drug finasteride. in
particular, the use of extract has not been associated
with erectile dysfunction, ejaculatory disturbance, or
altered libido." carraro et al. prostate vol. 29
extract serenoa repens (lsesr)
"aside from an occasional instance of gi upset, side effects of saw palmetto extract have not been reported" bach et al. phytomedicine pp. 105-111, 1996.
"pharmaceutical style evaluations have not yet been performed in the united states, partly
because they are not required by law, and partly because the cost of such evaluations would be difficult to recoup with
non-patentable products." marks and tyler, urology, vol. 53, 457-461, 1999
"lsesr was found to be a three fold more potent competitor of
5ar (5-alpha-reductase) than finasteride when comparing the recommended therapeutic dose by the
manufacturers for the treatment of bph. (5mg per day vs. 320mg per day lsesr
the hairloss treatment drug propecia = 1mg per day
finasteride." (this suggests a fifteen-fold greater efficacy dose for dose in favor of
lsesr) delos et al., j. steroid biochem. molec. biol., vol. 48, pp 347-352, 1994
"finasteride is a selective inhibitor of the type two isoform of
5ar (5-alpha-reductase), whereas lsesr markedly inhibited both type one and type two isoforms of
5-alpha-reductase." (type one
5-alpha-reductase predominates in tissue specific to the hair follicle morphology, whereas with type two there is evidence for the
expression of both) lehle et al., j. steroid biochem.
molec. biol., vol 54, 273-279, 1995
"naturopathic physicians have used lsesr as a tonic to naturally support the body in the treatment of genital/urinary tract disturbances, in men
to increase testicle function, and in women with mammary gland disorders."
murray, vital comm. 1990 pp 1-14
abstract on lesr
human prostatic steroid 5 alpha-reductase isoforms--a comparative study
of selective inhibitors.
lehlé c; délos s; guirou o; tate r; raynaud jp; martin pm
j steroid biochem mol
biol, 54: 5-6, 1995 sep, 273-9
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.
one of the most profoundly significant developments in the past few years is the discovery of the action in the body of the plant sterols and
sterolins. these are potent phytochemicals found in a variety of botanical sources. there are a number of different
sterols and these include the principal phytosterol, which is known as
in addition to sitosterol the most common sterols include
campesterol, sitostanol and stigmasterol. the glucoside of sitosterol is known as sitosterolin and in plants it is always found together with the sterol. the ratio of sterol
to sterolin varies in the plant kingdom ranging from 5% to 10% but in some
cases being higher as in the case of potatoes.
sterols are essential cell membrane components and the maintenance of adequate serum levels in humans seems to be necessary for an efficient immune system. seeds are the richest source of the sterols and sterolins and yet, the refining
processes applied by the food industry render the staple foods useless, because
they remove the sterols and sterolins to make the product more appealing to the eye.
for instance, in order to prevent precipitation of the fats in so-called "cold pressed oils," the oil is heated and refined to remove the sterols /
sterolins. sterols and sterolins have been shown to modulate the functions
of the t-cells both in vitro and in vivo by enhancing their cellular division.
recent research conducted by professor patrick bouic and his research team at the university of stellenbosch medical faculty and published in the international
journal of immunopharmacology is providing an entirely new medical approach to the treatment of autoimmune diseases and other chronic diseases that
only manifest themselves when the afflicted individuals are at cause. international medical and scientific interest on this breakthrough has been overwhelming.
sitosterol assists in the conversion of linoleic acid to polyunsaturated fatty acids. this process is essential for the conversion of the omega 6 fatty acids to prostaglandins and
leukotrienes. prostaglandins and leukotrienes are hormone like substances that are involved in immune support; they assist in the reduction of
thrombo-embolic disorders by reducing platelet aggregation
and they also assist in the reduction of inflammatory metabolites.
sitosterol can be metabolized to pregnenolone and therefore to dhea and
the other hormones derived from pregnenolone and its analogues. in the human body there is a steady decline with age in the production of
dhea, which is the master hormone responsible for the synthesis of
estrogen, progesterone, testosterone, cortisol and others.
by the age of 70 the dhea production can be down to 10% or 20% of the levels found in a twenty year old, thus sitosterol supplements have an enormous potential for supporting the endocrine system in elderly people and, by implication, increasing their longevity.
abstract on beta sitosterol
beta-sitosterol for the treatment of benign prostatic hyperplasia: a systematic
wilt tj; macdonald r; ishani a
the va coordinating center of the cochrane collaborative review group in prostatic diseases and urologic malignancies, 13/minneapolis, va, usa.
int, 83(9): 976-83 1999 jun
objectives: to conduct a systematic review of the evidence for the efficacy of
beta-sitosterol in men with symptomatic benign prostatic hyperplasia
(bph). methods: studies were identified through medlinetrade mark (1966-98), embasetrade mark,
phytodok, the cochrane library, bibliographies of identified trials and review articles, and contact with
study authors and pharmaceutical companies. randomized trials were included
if: men had symptomatic bph; plant extract preparations contained
beta-sitosterols; a control group received placebo or a pharmacological therapy; and treatment duration was >/=30 days. study characteristics, demographic information, enrolment criteria and outcomes were extracted.
results: four trials comprising a total of 519 men met the inclusion criteria. all were double blind and lasted 4-26 weeks. three studies used
nonglucosidic beta-sitosterols and one used a preparation that contained only
beta-sitosterol-beta-d-glucoside. compared with placebo,
beta-sitosterol improved urinary symptom scores and flow measures. for the two studies reporting
the international prostate symptom score (ipss), the weighted mean difference
(wmd) against placebo was -4.9 ipss points (95% confidence interval, ci, -6.3 to-3.5). the wmd for peak urinary flow rate was 3.91
ml/s (95% ci 0.91 to 6.90, four studies) and for residual volume the wmd was -28.62 ml (95% ci-41.42 to-15.83, four studies).
beta-sitosterol did not reduce prostate size.the trial using pure
beta-sitosterol-beta-d-glucoside (wa184) showed no improvement in urinary flow measures. withdrawal rates
for men assigned to beta-sitosterol and placebo were 7.8% and 8.0% (not
significant), respectively. conclusion: beta-sitosterol improves urological
symptoms and flow measures. however, the existing studies are limited by
short treatment duration and lack of standardized beta-sitosterol preparations. their long-term effectiveness, safety and ability to prevent the complications
of bph are unknown.
essential fatty acids (efa)
gla, ala, linoleic acid and palmitoleic acid
linolenic acid (gla), alpha linolenic acid (ala),
linoleic and oleic acid are essential fatty acids found
in plant oils. these fatty acids have been individually
proven to inhibit 5-alpha reductase. the essential fatty
acids are among the most powerful inhibitors of 5-alpha
reductase known today. they have been demonstrated
to inhibit both type 1 and type 2 isoforms of the
enzyme 5ar. this is in marked contrast to finasteride,
which has been shown efficacious only in the inhibition
of type 2 5ar. importantly for the purposes of
considering value in combating pattern hair loss; the
type 1 isoenzyme is present in high concentrations in
the scalp, sebaceous glands, and the skin. it has also
been shown that gla, ala and oleic acid have
potent anti-inflammatory properties.
research abstract on
liang t; liao s
journal of investigational dermatology: 1997 aug; 109 (2): 152-7
unsaturated aliphatic fatty acids, such as gamma-linolenic
acid, inhibit 5alpha-reductase activity in vitro and in
vivo. hamster flank organ growth, as measured by
the increase in the area of pigmented macule, is
dependent on androgen. when one of the paired flank
organs of a castrated hamster was treated
topically with testosterone, the treated organ, but
not the contralateral flank organ, became larger and
darker. topical application of gamma-linolenic acid to
the testosterone-treated flank organ suppressed this testosterone effect. other fatty acids that were
not inhibitors of 5alpha-reductases were not active.
topical treatment of hamster flank organs with
5alpha-dihydrotestosterone also stimulated the growth of
the organ. this 5alpha-dihydrotestosterone-dependent
activity, however, was not significantly affected
by gamma-linolenic acid, suggesting that flank organ
growth was dependent on 5alpha-dihydrotestosterone and
that gamma-linolenic acid acted by inhibiting
5alpha-reductase. with intact male hamsters, the
endogenous androgen-dependent growth of flank organs is
also suppressed by topical treatment with gamma-linolenic
the effect of gamma-linolenic acid is
localized at the site of its application; topical
application of gamma-linolenic acid did not affect the
androgen-dependent growth of other organs such as
testis, epididymis, seminal vesicle, and prostate.
gamma-linolenic acid, with low toxicity and absence of
systemic effect, may be potentially useful for
treatment of androgen-dependent skin disorders.
research abstract examining
gamma-linolenic acid against other fatty acids in the inhibition of
liang t; liao s
journal of biochemistry, 1992 jul 15, 285 (pt 2): 557-62
or rat microsomal 5-alpha-reductase (5ar) activity, as
measured by enzymatic conversion of testosterone into 5
alpha-dihydrotestosterone or by binding of a
competitive inhibitor, [3h] 17
beta-nn-diethulcarbamoyl-4-methyl-4-aza-5 alpha-androstan-3-one ([3h] 4-ma) to the
inhibited by low concentrations (less than 10
microm) of certain polyunsaturated fatty acids. the relative inhibitory potencies of unsaturated fatty
acids are, in decreasing order: gamma-linolenic
acid greater than cis-4, 7,10,13,16,19-docosahexaenoic
acid = cis-6, 9,12,15-octatetraenoic acid = arachidonic
acid = alpha-linolenic acid greater than linoleic
acid greater than palmitoleic acid greater than oleic acid greater than myristoleic acid. other
unsaturated fatty acids such as undecylenic acid, erucic
acid and nervonic acid, are inactive. the methyl esters
and alcohol analogues of these compounds, glycerols,
phospholipids, saturated fatty acids, retinoids and
carotenes were inactive even at 0.2 mm.
the results of
the binding assay and the enzymatic assay correlated
well except for elaidic acid and linolelaidic acid, the
trans isomers of oleic acid and linoleic acid
respectively, which were much less active than their cis
isomers in the binding assay but were as potent in the
enzymatic assay. gamma-linolenic acid had no effect on
the activities of two other rat liver microsomal
enzymes: nadh: menadione reductase and glucuronosyl
transferase. gamma-linolenic acid, the most potent
inhibitor tested, decreased the vmax. and
increased km values of substrates, nadph and
testosterone, and promoted dissociation of [3h]
4-ma from the microsomal reductase. gamma-linolenic
acid, but not the corresponding saturated fatty acid (stearic
acid), inhibited the 5 alpha-reductase activity, but not
the 17 beta-dehydrogenase activity, of human prostate
cancer cells in culture. these results suggest that
unsaturated fatty acids may play an important role in
regulating androgen action in target cells.
research abstract on palmitoleic acid
of propylene glycol distribution in the skin by high
purity cis-unsaturated fatty acids with different
alkyl chain lengths having different double bond
taguchi k; fukushima
s; yamaoka y; takeuchi y; suzuki m
of pharmaceutics, faculty of pharmaceutical sciences,
kobe gakuin university, japan.
pharm bull, 22(4): 407-11 1999 apr
of skin distribution of propylene glycol (pg) in the
skin by high purity cis-unsaturated fatty acids with
different alkyl chain lengths was studied in the rat
using fourier transform/attenuated total reflection (ft-ir/atr)
analysis. two fatty acids with the double bond at the
delta9 position, palmitoleic acid (omega7, delta9) and
oleic acid (omega9, delta9), enhanced pg flux into the
dermis and increased the dermal steady state level of
pg. in contrast, myristoleic acid (omega5, delta9) was
extremely weak in its action. a positional effect of the
omega chain was observed. the rate of skin structural
alteration increased in proportion to omega chain length.
the application of three fatty acids with the
double bond at the omega9 position, oleic acid (omega9,
delta9), gondoic acid, (omega9, delta11), erucic
acid (omega9, delta13) enhanced pg distribution in the
skin. while nervonic acid (omega9, delta15) did
not increase pg distribution in the skin, the
relationship of the delta/omega ratio to parameters
characterizing the action of enhancers (pg (peak
area max), t (max alteration), and the slope) suggest
that skin distribution increases as the position of the
double bond is shifted toward the hydrophilic end. it is
therefore likely that the ratio of the delta/omega
chain length of the cis-unsaturated fatty acid
determines the efficacy of these compounds as skin
penetration enhancers. an adequate molecular volume may
be required for cis-unsaturated fatty acids to act as
biotin, also known as vitamin h, aids in the utilization of protein, folic acid, pantothenic acid, and vitamin b-12, and has also been shown to promote healthy hair. a deficiency of biotin may lead to extreme exhaustion, drowsiness,
muscle pain, loss of appetite, depression, loss of skin tone, and hair loss.
abstract on biotin
vitamin and dermatology
yoshikawa k address department of dermatology, osaka university graduate school of medicine
rinsho, 57(10): 2385-9 1999 oct
vitamin a, b1, b2, b6, b12, biotin, nicotinic acid, panthotenic acid, vitamin
c, e and k has been used for various skin disorders. the use is mostly based
on the similarity of the skin manifestations seen in their deficiencies,
except for the rare cases of clear deficiency like pellagra. recent introduction
of vitamin a and d analogues for psoriasis and keratinization disorders resulted in significant progress in clinical dermatology. application of vitamin c, e and beta-carotene++ for uv-induced skin damages are being studied, and the vitamins will be more important in dermatology in the future.
proanthocyanidins (procyanidin oligomers)
procyanidin oligomers (also known as
proanthocyanidin) are naturally derived ingredients that have shown to stimulate hair growth with a mechanism of action thought by some investigators to be similar to that of minoxidil
(rogaine). recent studies have shown that procyanidin oligomers promote growth stimulation activity of hair epithelial cells in vitro and stimulate
anagen induction in hair follicles in vivo.
research abstract on
procyanidin oligomers selectively and intensively promote proliferation
of mouse hair epithelial cells in vitro and activate hair follicle growth in vivo.
j invest dermatol 1999 mar; 112 (3): 310-6
takahashi t, kamiya t, hasegawa a, yokoo y tsukuba research laboratories,
kyowa hakko kogyo, ibaraki, japan.
we have previously reported that proanthocyanidins extracted from grape
seeds possess growth-promoting activity toward murine hair epithelial cells in vitro and stimulate anagen induction in hair cycle progression in vivo.
this report constitutes a comparison of the growth-promoting activity of
procyanidin oligomers and the target cells of procyanidins in the skin.
results show that procyanidin dimer and trimer exhibit higher growth-promoting activity than the monomer. the maximum growth-promoting activity for hair
epithelial cells with procyanidin b-2, an epicatechin
dimer, reached about 300% (30 microm) relative to controls (=100%) in a 5 d culture. optimum
concentration of procyanidin c-1, an epicatechin trimer, was lower than
that of procyanidin b-2; the maximum growth-promoting activity of procyanidin c-1 was about 220% (3
no other flavonoid compounds examined exhibit
higher proliferative activities than the procyanidins. in skin constituent
cells, only epithelial cells such as hair keratinocytes or epidermal keratinocytes
respond to procyanidin oligomers. topical application of 1% procyanidin
oligomers on shaven c3h mice in the telogen phase led to significant hair regeneration
[procyanidin b-2, 69.6% +/- 21.8% (mean +/- sd); procyanidin b-3, 80.9% +/- 13.0%; procyanidin c-1, 78.3% +/- 7.6%] on the basis of the
shaven area; application of vehicle only led to regeneration of 41.7% (sd
= 16.3%). in this paper, we demonstrate the hair-growing activity of procyanidin oligomers both in vitro and in vivo, and their potential for use as agents
to induce hair growth.
pmid: 10084307, ui: 99181798
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