Saw palmetto extract: A dermatologist's perspective

Abstract

Saw palmetto extract is believed to have antiandrogenic properties and has been used widely for the treatment of androgenic alopecia. It is claimed to have much less side effects as compared to finasteride. Along with its use for androgenic alopecia, it has also been tried for other conditions associated with increased androgen levels in dermatology. This article will review a dermatologist's perspective of this traditional herb.

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© 2017 Indian Journal of Drugs in Dermatology | Published by Wolters Kluwer - Medknow 11
Review Article
introduction
Saw palmetto or serenoa repens (SR) is a small palm tree
native to eastern regions of the United States. Its extract is
believed to be a highly effective antiandrogen as it contains
phytoesterols and fatty acids as its major ingredient.[1] SR is
used in several forms of traditional herbal medicine. American
Indians used the fruit for food and to treat a variety of urinary
and reproductive system problems. The Mayans drank it as a
tonic, and the Seminoles used the berries as an expectorant
and antiseptic. Crude SR extract was used by the European
and American medical practitioners for at least 200 years
for various conditions, including asthenia, recovery from
major illness and urogenital problems. SR is currently being
commercially marketed for the treatment of benign prostatic
hyperplasia.[2] Of late SR has gained popularity as a magical
remedy for androgenetic alopecia (AGA).[3] Being a naturally
occurring 5 alpha reductase inhibitor, it has also been used for
other dermatologic indications. This article will review the
dermatologic perspective of SR.
mechanism oF action
Like finasteride, SR is believed to block the enzyme 5
alpha reductase. Whether SR inhibits 5 alpha reductase 1
or both the isoenzymes of 5 alpha reductase is not clear.
This action thereby blocks the conversion of testosterone to
dihydrotestosterone (DHT).[4] This is its primary mode of
action for most dermatologic conditions. Other mechanisms of
therapeutic benet by SR will be elaborated under the specic
conditions of its usage in dermatology.
dermatologic indications oF serenoa repens
There is no Food and Drug Administration (FDA) approved
indications of SR in dermatology. All are off-label indications.
Androgenetic alopecia
SR has proved to be effective in the management of
AGA. Apart from the primary mechanism of action of
5 alpha-reductase blockade,[4] SR is thought to decrease the
uptake of DHT by the hair follicles[3] and decrease its binding
to androgenic receptors. Another possible effect of SR in
AGA seen with its liposterolic extract is suppression of
lipopolysaccharide-activated gene expression of chemokines,
including CCL 17, CXCL 6, and LT B 4 associated inammatory
and apoptotic pathways.[5] Hence, its anti-inflammatory
properties are of value in AGA. With SR growth of hair is
prevalently seen over the frontal and temporal regions of the
scalp.[6]
Hirsuitism
The safety and efcacy of SR in treating hirsuitism have not
been sufciently investigated. Studies show that it inhibits
5 alpha reductase and as a result prevents the conversion
of testosterone to DHT.[7] Further SR strongly inhibits
3 ketosteroid reductase-mediated conversion of DHT to
5-alpha androstane-3 alpha and 17 beta-diol which may
Saw Palmetto Extract: ADermatologist’s Perspective
Varshini Reddy, Aditya Kumar Bubna, Mahalakshmi Veeraraghavan, Sudha Rangarajan
Department of Dermatology, Sri Ramachandra University, Chennai, Tamil Nadu, India
Saw palmetto extract is believed to have antiandrogenic properties and has been used widely for the treatment of androgenic alopecia. It is
claimed to have much less side effects as compared to nasteride. Along with its use for androgenic alopecia, it has also been tried for other
conditions associated with increased androgen levels in dermatology. This article will review a dermatologist’s perspective of this traditional herb.
Keywords: 5-alph reductase inhibitor, anti-androgen, serenoa repens
Address for correspondence: Dr.Varshini Reddy,
No.13/7, 7thMain Road, RA Puram, Chennai‑600028, Tamil Nadu, India.
E‑mail:r.varshini91@gmail.com
Abstract
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DOI:
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How to cite this article: Reddy V, Bubna AK, Veeraraghavan M,
Rangarajan S. Saw palmetto extract: A dermatologist's perspective. Indian
J Drugs Dermatol 2017;3:11-3.
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Reddy, et al.: Saw Palmetto: Dermatologist’s perspective
Indian Journal of Drugs in Dermatology ¦ Volume 3 ¦ Issue 1 ¦ January‑June 2017
12
help as therapy for hirsuitism.[8] A study done using a cream
containing SR extract (Nela Depil) twice a day for 2 months
in 31 women with idiopathic facial hirsuitism showed a
29% decline in hair counts 2 months posttreatment which is
statistically signicant (P < 0.0001).[9] However, further studies
maybe required to determine the effectiveness of SR extract
for this condition.
Acne
As SR lowers DHT levels, it inuences the production of sebum
by reducing the excessive oils contributing to the development
of acne.[10] SR is a dual inhibitor of cyclooxygenase and
5-lipoxygenase pathways according to in vitro research.
More recently, decreased expression of COX-2 has been
identied providing a further explanation for the observed
anti-inammatory activity. Further studies would only help
in elucidating the efcacy of SR both as monotherapy or as a
combination therapy in acne.
Polycystic ovarian syndrome
In polycystic ovarian syndrome, there are increased levels of
adrenal androgens. Furthermore, the peripheral tissues such
as skin, liver, and adipose tissue also take part in androgen
synthesis by converting the weaker androgens into, the more
potent ones. Androgen receptor activation takes place only
with circulating testosterone and DHT. Twenty-ve percent
of the circulating testosterone is produced individually
by the ovaries and adrenals. The remaining 50% is by the
peripheral conversion from androstenedione.[11] SR helps as an
antiandrogen and may also have anti-inammatory effects. An
ethanol extract of SR inhibited the lipid droplet accumulation
by attenuation of protein expressions of C-EBP alpha and
PPAR gamma. Phosphorylation of Erk 1/2 and Akt 1 were
also decreased by SR ethanol extract. Hence, SR extracts
could selectively affect the adipocyte differentiation through
the modulation of several key factors that play a critical role
in adipogenesis.[12]
pharmacokinetics
As yet, there is no data available on absorption, distribution,
metabolism, and elimination for SR.
dosage
The dosage of SR for dermatologic indications has not been
clearly established. For benign prostatic hyperplasia 160 mg
twice daily of an extract standardized to contain 85%–95%
fatty acids or sterols is administered. Similarly, a single daily
dose of 320 mg may just be effective in this condition.[13,14] As
with many other herbs the quality of SR products may vary
widely,[15] owing to which a standardized dosing may pose to
be a serious problem.
adverse eFFects
Mild stomach discomfort is the most common side effect.
It can be alleviated by taking the drug after food. Hepatic
inammation is another serious problem with SR. There have
been two case reports showing this adverse reaction in patients
taking the medication for benign prostatic hyperplasia.[16,17]
Pancreatitis has been reported with SR extract. In general,
some potential mechanisms for drug-induced acute pancreatitis
include pancreatic duct constriction, cytotoxic and metabolic
effects, accumulation of a toxic metabolite or intermediary
and hypersensitivity reactions.[18] Another theory suggests that
pancreatitis may occur due to SR stimulating the estrogenic
receptors and induces a hypercoaguable state that leads to
pancreatic necrosis.[19] There is one report of SR apparently
causing excessive bleeding during surgery.[20] The signicance
of this isolated event is not clear, but it is probably prudent to
avoid SR before and just after surgery.
drug interactions
Drugs such as warfarin, heparin, aspirin, clopidogrel, and
ticlopidine should be avoided in patients taking SR, owing
to an increased tendency for bleeding. The exact mechanism
for the increased risk of hemorrhage while taking SR with the
above-mentioned drugs requires further elucidation.[21]
saFety in pregnant and nursing women
It has not been established till date.
conclusion
SR is an herbal drug which has found to be useful in the
dermatologic indications mentioned above. It has been used as
a topical formulation and also systemically. Despite the easy
availability of saw palmetto extract and it being designated as
a food product by the US FDA there still remains paucity on
its regulations with regard to efcacy and safety. Moreover, we
also need to be aware of the low quality of evidence about saw
palmetto extract with regard to most dermatologic indications
where it has been utilized. With there being a number of side
effects with the systemic route the development of more topical
formulations in the near future in the form of creams, lotions,
and gels could help in getting a good therapeutic outcome with
the risks minimized. Finally, all patients need to be adequately
counseled regarding the paucity of literature with regard to
the exact mode of action, safety, and long-term effects of SR
and therefore its use should be limited in those patients where
there is a contraindication in the usage of other conventional
modalities of management.
Financial support and sponsorship
Nil.
Conflicts of interest
There are no conicts of interest.
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