HairGenesis™, a proprietary formulation of botanically derived
components, combines the power of known 5AR inhibitors
(anti-androgenic substances) into a powerful hair loss
treatment regimen. The individual substances used in the
formulations comprising the HairGenesis™ treatment line were
selected for inclusion after meticulous research. A great deal
of basic science as well as independent clinical research
supports the efficacy of certain botanicals as known inhibitors of
5AR. A small compilation of this independently derived data
has been gathered below in support of the safety, efficacy, and
value of HairGenesis™.
Saw palmetto berry extract, or
LSESr
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. 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
action.
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
"Among 1,098 patients with BPH (benign prostatic hyperplasia)
in that study, the general safety profile of saw palmetto compared
favorably with that of finasteride, and sexual side effects
were less common with the extract than with the drug. In particular,
the use of extract has not been associated with erectile
dysfunction, ejaculatory disturbance, or altered libido."
Carraro et al. Prostate vol. 29 pp.231-240 1996
"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
5aReductase than finasteride when comparing the recommended
therapeutic dose by the manufacturers for the treatment of BPH.
(5mg per day vs. 320mg per day LSESr Note: 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 5aReductase, whereas LSESr markedly inhibited both type one
and type two isoforms of 5aReductase" (Type one
5aReductase 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
Research abstract on LSESr
Human prostatic steroid 5 alpha-reductase isoforms--a comparative
study of selective inhibitors.
Author
Lehlé C; Délos S; Guirou O; Tate R; Raynaud JP; Martin PM
Journal
J Steroid Biochem Mol Biol, 54: 5-6, 1995 Sep, 273-9
Abstract
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 LSES 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.
ßetaSitosterol
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
sitosterol.
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 oestrogen, 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.
Research abstract on
BetaSitosterol
Title
Beta-sitosterol for the treatment of benign prostatic hyperplasia: a
systematic review.
Author
Wilt TJ; MacDonald R; Ishani A
Address
The VA Coordinating Center of the Cochrane Collaborative Review
Group in Prostatic Diseases and Urologic Malignancies,
13/Minneapolis, VA, USA.
Source
BJU Int, 83(9): 976-83 1999 Jun
Abstract
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.
Biotin
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.
Research abstract on
Biotin
Title
Vitamin and dermatology
Author
Yoshikawa K Address Department of Dermatology, Osaka University
Graduate School of Medicine
Source
Nippon Rinsho, 57(10): 2385-9 1999 Oct
Abstract
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.
Essential Fatty Acids
GLA, ALA, Linoleic Acid and
Palmitoleic Acid
Gamma 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
Gamma-linolenic Acid
AUTHOR
Liang T; Liao S
JOURNAL
Journal of Investigational Dermatology: 1997 Aug; 109 (2): 152-7
ABSTRACT
Certain 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
acid.
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 5-alpha-reductase
AUTHOR
Liang T; Liao S
JOURNAL
Journal of Biochemistry, 1992 Jul 15, 285 (Pt 2): 557-62
ABSTRACT
Human or rat microsomal 5 alpha-reductase 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 reductase, is 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
Title
Enhancement of propylene glycol distribution in the skin by high
purity cis-unsaturated fatty acids with different alkyl chain
lengths having different double bond position.
Author
Taguchi K; Fukushima S; Yamaoka Y; Takeuchi Y; Suzuki M
Address
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences,
Kobe Gakuin University, Japan.
Source
Biol Pharm Bull, 22(4): 407-11 1999 Apr
Abstract
Enhancement 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 enhancers.
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
Title
Procyanidin Oligomers selectively and intensively promote
proliferation of mouse hair epithelial cells in vitro and
activate hair follicle growth in vivo.
Source
J Invest Dermatol 1999 Mar; 112 (3): 310-6
Author
Takahashi T, Kamiya T, Hasegawa A, Yokoo Y Tsukuba Research
Laboratories, Kyowa Hakko Kogyo, Ibaraki, Japan.
Abstract
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 microM). 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
Therapeutic
Dosage
Peer-Reviewed
Medical Journal Publishes positive results from HairGenesis
Placebo-Controlled, Double-Blind Clinical Study:
