Active

ingredients

MELANOSTATINE5
Focusing on Whitening
Peptide antagonist of a-MSH
Reduces melanin synthesis for
a better control over skin tone

Melanostatine5 is a biomimetic peptide derived from a-msh that

blocks melanin synthesis allowing a better control over skin tone.

Variations in skin colour are caused by different levels of melanin in the skin. Regular
exposure to the sun causes brown spots known as sunspots and their occurrence
increases with age. Classic descriptions of these troubles refer to hyperactivity of the
melanocytes, which synthesize abnormal amounts of melanin.
The skin pigmentation process

DOPA quinone

Alpha Melanocyte Stimulating Hormone also named Melanotropin (a-MSH) is the

natural substance produced by our body which is responsible for several physiological
activities like pigmentation. Tyrosinase is stimulated by the bonding of a-MSH on
its specific receptor MC1-R. The stimulation of the tyrosinase activity, induces the
hydroxylation of the amino acid tyrosine to DOPA (dihydroxyphenylalanine) and
catalyses its oxidation to dopaquinone. The final step is the synthesis of melanin in
organelles called melanosomes, in melanocytes.
The ideal skin lightening agent for cosmetic products is one that inhibits melanogenesis
without cytotoxicity .

Mechanism of action

Melanostatine5

Epidermis

MC1-R

Melanin

Keratinocyte

Binding of a-MSH to the MC1-Receptor on melanocytes is the first step in melanogenesis

and the pigment formation. By binding and blocking the MC1-R, we can block the
intracellular melanogenesis pathway and decrease the synthesis or the over expression
of melanin produced by melanocytes.

Dermis

Melanocyte
DOPA
quinone

Inhibition of the melanin production

Melanostatine5 is an oligopeptide with an high affinity for MC1-R. Melanostatine5 is a

biomimetic peptide antagonist specific of the a-MSH (Alpha Melanocyte Stimulating
Hormone). As an antagonist, Melanostatine5 competes against the natural ligand
(a-MSH) on its specific receptor (MC1-R) by preventing any further activation of the
tyrosinase, and thus blocking melanin synthesis. Tyrosinase inhibition reduces the
formation of unwanted pigmentation allowing for the control over skin tone and brown
spots.

Inhibiting tyrosinase
The tyrosinase activity is detected with a Western Blot. Tyrosine is labelled by specific
anti-tyrosinase monoclonal antibody.

Tyrosinase

Control

a-MSH Melanostatine5 0.1%

10-6M
+ a-MSH 10-6M

Melanostatine5 blocks the melanogenesis pathway and inhibits tyrosinase activity

and melanin synthesis.

Improving hyper-pigmentation
The melanin synthesis is determined by Pierce BCA Bicinchoninic Acid Protein Assay.
Melanostatine5 inhibits the synthesis of melanin induced by a-MSH by 33%.

synthesis by melanocytes

Melanin synthesis (%)

Inhibiting hyper-stimulation of melanin

Effect of melanostatine5 on melanin

-33%

100
90
80
70
60
50
40
30
20
10
0
-MSH 10-7M

Reversing hyper-pigmentation
The stimulation of melanocytes by a-MSH is accompanied by structural modifications
of the cell. Melanisation of the epidermis involves several types of cells and keratinocytes
plays a regulating role in this effect. The co-culture model used in this study brings out
the microscopic phenomena connected with the physiological process of pigmentation.
In presence of a-MSH, melanocytes are more spread out and dendritic than in the control
culture. Moreover, they are strongly DOPA positive. In presence of Melanostatine5,
melanocytes are comparable of those observed in the control culture. When a-MSH
and Melanostatine5 are combined in the culture medium, melanocytes are less spread
out and are weakly DOPA positive in comparison with cells stimulated by the hormone
alone.

-MSH 10-7M +
Melanostatine 5 0.01%

Microscope images of
melanocyte/keratinocyte co-culture
Control

a-MSH
DOPA
negative
cell
DOPA
positive
cell

Melanostatine5

a-MSH +
Melanostatine5

These microscope images demonstrate that Melanostatine5 does not interfere

with the melanocytes functions. However when melanocytes are stimulated,
Melanostatine5 opposes the hyperproduction of melanin.

Lightening improvement in Asian skin

Test protocol
50 Asian (female) volunteers applied a whitening cream containing 2% TyrostatTM-11
and 4% Melanostatine5, 2x/day for 4 weeks.
Positive opinion

Benefits

Dull complexion is reduced

Yellowish appearance is reduced
The appearance of age spots is reduced
Evenness of the skin tone
The skin looks more translucent
The skin is lighter/whiter
The skin looks brighter
The skin looks moisturized
The skin is suppler
The skin is smoother
The skin texture looks more refined
The product leaves a healthy looking skin

After 1 week
of use

After 4 weeks
of use

86%
80%
62%
74%
66%
76%
66%
66%
80%
76%
80%
68%

92%
86%
78%
88%
90%
80%
86%
80%
90%
90%
88%
84%

With complementary and synergic pathways, TyrostatTM-11 and Melanostatine5

reduce sun spots, freckles and uneven pigmentation allowing a lighter and luminous
skin tone.

Melanostatine5 reverses the pigmentation process for

an overall better control over skin tone.

Features and benefits

inci name
Water (1) (and) Dextran (2) (and)
Nonapeptide-1 (3)
CAS
7732-18-5 (1), 9004-54-0 (2),
158563-45-2 (3)
EINECS
231-791-2 (1), 232-677-5 (2), - (3)

Features

Benefits

Peptide

Stable, easy to work with

a-MSH antagonist mechanism of

action

Reverses pigmentation without toxicity

Clinical efficacy on Asian skin

Significant lightening effect after only 28 days

After hours hand cream

Appearance
Aqueous limpid solution, odorless,
colorless
Formulation
Melanostatine5 should be
incorporated at the end of the
formulation at a temperature of
35/40C.
DOsage
4-8%
optimum ph
5-7
applications
- Lightening care
- Skin tone equalizer care
- Aging spot corrective care
- Skin illumination-brilliance
(foundation-powder)
- Photoaging
- Ethnic skin care
- Hand cream
China-compliant

Ingredients

INCI Names

A Water

Water

qsp

Xanthan Gum

0.30

Glycerine

Glycerin

2.00

Glucam E-10TM

Methyl Gluceth-10

1.00

Eastman AQ 38S

Polyester-5

1.00

Glyceryl Stearate Citrate

3.00

Akoline SL

Sodium Stearoyl Lactylate

0.30

Akoline MG-P

Glyceryl Stearate

1.00

Rhodicare T

B Akoline GC

Diisostearyl Dimer Dilinoleate

10.00

Boroneige 901

Boron Nitride

0.50

TiO2 MP100

Titanium Dioxide (and) Aluminum Hydroxide

(and) Zinc Oxide

1.00

d-Delta-Rich
Tocopherols Concentrate

Tocopherol

0.05

Phenoxyethanol (and) Methylparaben (and)

Ethylparaben (and) Butylparaben (and)
Propylparaben (and) Isobutylparaben

1.00

Schercemol

TM

DISM

C Neomekkins M-16

Tinogard Q
D TyrostatTM-11
Melanostatine5
E Tinovis ADE

Tris (Tetramethylhydoxypiperidinol) Citrate

0.05

Water (and) Glycerin (and) Rumex Occidentalis

Extract (and) Ascorbic Acid

2.00

Water (and) Dextran (and) Nonapeptide-1

4.00

Sodium Acrylates Copolymer (and) Hydrogenated

Polydecene (and) PPG-1 Trideceth-6

0.80

RoRe SF 100

Dimethicone

2.00

Parfum Amnesio

Fragrance

0.50

NaOH (solution 5%)

Sodium Hydroxide

qsq

This brochure is not intended for consumers and neither this brochure nor any extract thereof shall be used in order to commercialize products to consumers. No
drawing, photograph or other extract derived from this brochure shall be used by any person without our prior written approval. As well, no claim with respect to the
ingredient referred to in this brochure shall be made by any person without our prior written approval, even though the claim is set forth in this brochure. The person
using the ingredient referred to in this brochure in the formulation of finished products is solely responsible for ensuring that the use made of the ingredient, the finished
products marketed to consumers, their packaging, labelling and advertising materials and the claims made with respect to the finished products and the ingredient
comply with all applicable laws and regulations. We hereby disclaim any warranty of suitability of the ingredient referred to in this brochure for any purpose. Any
prospective user of the ingredient shall himself determine the suitability of the ingredient for his intended use and, as the case may be, obtain the required regulatory
approvals for the commercialization of his finished products.

Lucas Meyer Cosmetics S.A.S.

Lucas Meyer Cosmetics Canada Inc.

ZA les Belles Fontaines

99 route de Versailles
91160 Champlan - France
T: +33 (0)1 69 10 69 69 - F: +33 (0)1 69 10 69 70

Place de la Cit, Tour de la Cit

2600 boul. Laurier, #900
Qubec (Qubec) G1V 4W2 Canada
T: +1 418 653-6888 - F: +1 418 653-6005

www.lucasmeyercosmetics.com
info@lucasmeyercosmetics.com

Litho Canada | 2013-03 3K

Product
description