SNAP-8

(ACETYL OCTAPEPTIDE-3)

SMALL PEPTIDES AS
ANTI-WRINKLE PRODUCTS
NA DISTRIBUTOR * CENTERCHEM, INC
PH:203-822-9800;FAX: 203-822-9820
COSMETICS@CENTERCHEM.COM

V.5

WHAT IS THE MAIN CAUSE

OF SKIN TENSION?

The excessive release of chemical signals

overstimulates facial muscles
The excess tension can be eliminated, for a
relaxed face with no wrinkles

NEURONAL EXOCYTOSIS

Neurotransmitters are released from vesicles

in a process called neuronal exocytosis

NEUROMUSCULAR JUNCTION

EXOCYTOSIS INVOLVES A
PROTEIN COMPLEX

SNARE complex is formed by 3 proteins: SNAP-25, VAMP and SYNTAXIN

Exocytosis is a reversible process

STRUCTURE OF THE ASSEMBLED

SNARE COMPLEX

The SNARE complex mediates the final steps of exocytosis

SNARE COMPLEX MODULATION

R30=E145

R31=E206
E38-H213
I209

S28-E206
V153

I157 L160

F216

L205

L212
E206-R210

Small mimetic peptides modulate the formation

and stability of the SNARE complex

BONTOMIMETIC PEPTIDES EXHIBIT

IN VIVO ACTIVITY AND ARE A SAFE
ALTERNATIVE TO BOTULINUM
NEUROTOXINS

SNAP-8 - Acetyl Octapeptide-3

What is it? SNAP-8 is an octapeptide

What is an octapeptide?
A combination of 8 natural amino acids
What does it do?
Reduces wrinkle depth
Prevents skin aging

SNAP-8 - Synthesis
SNAP-8 is synthesized at our facilities in Gav under GMP standards
It is synthesized using solid synthesis by Fmoc protocols
The heptapeptide is built sequentially on a solid polymer resin, adding
one by one all the amino acids, up to 8
After the synthesis is complete, the peptide is cleaved off the resin and
analysed for purity

ARGIRELINE-BASED PEPTIDES REGULATE THE

FORMATION OF THE SNARE COMPLEX

SNARE
complex

8
SN
A
P-

H
EA
T

SN
A
R
E

SNAP-25

9We examine the effect of small peptides (3 mM) on the stability of the SNARE
complex
9The in vitro method allows us to follow the formation and thermal stability of the
reconstituted protein complex.
9We can evaluate the antagonistic competitive efficacy of small peptides versus the
wild type protein on its capacity to assemble with syntaxin and synaptobrevin
forming the SNARE complex

SNAP-8 ATTENUATES RELEASE

OF NEUROTRANSMITTER
Inhibition of cate cholamine re le ase by
pe ptide s (100 M ) de riv e d from SNAP-25

80
RELEASE (%)

CATECHOLAMINE

100

60
40
20
0

l
t ro
n
Co

e
6
8
lin
TA
P11
e
2
A
G
r
0
E
gi
SN
Ar
DD

Due to the
differences in activity
and concentration, a
relative unit must be
defined for
comparison: the
antiwrinkle activity
unit (AAU)

Chromaffin cells are often used as models for study of neural properties and processes, for
instance, exocytosis. Chromaffin cells secrete catecholamine which is used in this study as a
model for acetylcholine, the real neurotransmitter directly involved in muscle contraction.
(Chromaffin cells as models of endocrine cells and neurons, Tischler AS, Ann N Y Acad Sci, 2002,
971: 366 70)

ANTIWRINKLE ACTIVITY UNITS - AAUs

Dose-response curves from the catecholamine release tests yield IC50 values for the different
peptides.
We can quantify the exocytosis-blocking activity, which is related to the antiwrinkle power.
ESUP E is the most potent exocytosis-blocking synthetic peptide known, so it is chosen as
reference for AAUs.
AAUs are defined in Int.Journal Cosm Sci, 2002, 24, 303 310.

AAU SAMPLE = [IC50] ESUP E / [IC50] SAMPLE

COMPOUND

IC50

AAUs

BoNT A

~0.0260 M

12

ESUP E

0.310 M

1 (dy definition)

SNAP-8

55 M

0.0056

ARGIRELINE

110 M

0.0028

SNAP-8 ATTENUATES RELEASE

OF NEUROTRANSMITTER (II)
9The release of glutamate from the neurons is measured in order to compare the in vitro
activities of the anti expression-wrinkle peptides SNAP-8 and Leuphasyl
9Glutamate is the most common neurotransmitter in the brain and its release is used as
an estimate for acetylcholine release
9Values obtained are the average of 6 determinations

100%

0%

80%

20%

60%

40%

40%

60%

20%

0%

38%

7%

47%

43%

15 %

57%

Leuphasyl 1.5mM

BoNTA 50nM

0%

80%

100%
Control

SNAP-8 0.75mM Leuphasyl 0.75mM SNAP-8 0.75mM + SNAP-8 1.5mM

Leuphasyl 0.75mM

Inhibition glutamate release (%)

Glutamate Release (%)

9The combination of SNAP-8 with LEUPHASYL show a SYNERGISTIC effect in vitro,

their mechanisms are independent and their effects can be added

IN VIVO TEST: 10% SNAP-8

SOLUTION (0.05%)
Sample 1:

Sample 2:

T= 0

n=17

Mean value: -34.98%

T= 4 weeks

Maximum reduction: -63.13%

IN VIVO TEST: 10% SNAP-8

SOLUTION (0.05%)
Anti Expression Wrinkle Peptides
10% Peptide Solutions (0.05%)

Wrinkle Reduction %

-2,99

-5
-10
-15
-20
-27,05

-25
-30

-34,98

-35
Placebo

n=17

Argireline

Mean value: -34.98%

SNAP-8

Maximum reduction: -63.23%

SNAP-8: HOW DOES IT WORK?

This

revolutionary anti-ageing peptide works by

modulating the formation of the SNARE complex.
This

complex is involved in muscle stimulation.

SNAP-8 mimics

one of the proteins of the complex

(SNAP-25), and by competing with it for a place in the
complex, it moderately affects its formation and stability.
VAMP
VAMP

SNAP

STXN

SNAP-8

S8
STXN

SNAP-8: IS IT LIKE
BOTULINUM TOXIN?
Botulinum neurotoxin Type A (BoNT/A) was first purified
in 1946 and is now available for medical and cosmetic
use under the trade name BOTOX (Allergan).
Botulinum toxins paralyse by selectively blocking
acetylcholine release at the neuromuscular junction.
This is achieved by cleaving a protein called SNAP-25.

SNAP-8: IS IT LIKE
BOTULINUM TOXIN?
BOTULINUM TOXIN

BoNT/A is thought to be the most lethal

substance on a weight basis: 1 g of toxin
would kill one million people
LD50 estimations:
9 1ng/kg parenterally;
9 3 ng/kg by inhalation
Cosmetic use requires facial injections,
which are uncomfortable and can be
painful
Cost is around 300 US$ per injection (it
must pay for clinics, doctors, equipment)

SNAP-8
SNAP-8 is a harmless octapeptide
composed of natural amino acids
LD50 determination
>2000 mg/kg orally (rat)
Cosmetic use is via topical application,
applied in creams, lotions, serums, body
milks, etc.
Average price is 25 - 50 US$* for 50mL of
final product enough for 30 days of
treatment
*Final product price depends on many factors

such as concentration of actives, parfums,

packaging, marketing, etc.

SNAP-8: A CHEAPER, SAFER,

TOPICAL ALTERNATIVE TO BoNT/A
It targets the same protein complex as Botox, but in a completely different way
VAMP
VAMP

BOTOX
SNARE complex broken =

STXN

SNAP

muscle paralysis

VAMP
STXN
SNARE complex
assembled =
muscle contraction

SNAP-8

S8
STXN

SNARE complex captured =

muscle relaxed

SNAP-8 FINAL PRODUCTS

INCI: ACETYL GLUTAMYL HEPTAPEPTIDE-1
All tradenames, trademarks, copyrights and images used
herein belong to their respective and lawful owners

www.lipotec.com

V.5

Product

Lotion Akinsine Neuropeptides

Company

Anna Pegova (Brazil)

Lipotec active

Antarcticine, SNAP-8, Leuphasyl,

Aldenine, IDB-Light (for skin
lightening)

INCI Active

Acetyl Glutamyl Heptapeptide-1,

Pentapeptide-3,
Pseudoalteromonas Ferment
Extract, Tripeptide-1, Hydrolyzed
Soy Protein, Hydrolyzed Wheat
Protein, Hydroxydecyl
Ubiquinone

Product

Inhibit

Company

Natura Bisse (Spain)

Lipotec active

SNAP-8

INCI Active

Acetyl Glutamyl Heptapeptide-1,

Product

Inhibit Dermafill

Company

Natura Bisse (Spain)

Lipotec active

SNAP-8

INCI Active

Acetyl Glutamyl Heptapeptide-1,