Xantalgosil C PDF

EX
SY
M
OL
XANTALGOSIL C
INCI name : ACEFYLLINE METHYLSILANOL MANNURONATE
CAS number : 162030-43-5
Origin
XANTALGOSIL C is a silanol obtained by condensation of a silicon derivative on acefylline and
alginic acid. The silicon derivative and acefylline are obtained by synthesis, no derivative of animal
origin is used. Alginic acid is obtained after extraction from brown algae, no derivative of animal origin.
All silanols are endowed with some particular biological activities ; XANTALGOSIL C has been
specially designed for lipolysis.
Technical characteristics
Analytical composition
Monomethylsilanetriol
in wich silicon
Acefylline
Alginic acid
Water sq
limpid to slightly opalescent liquid,

colorless to slightly yellow
pH : around 5.5
density, 20 C : around 1.0
miscible with water at room temperature,
not miscible with concentrated alcohols
0.34%
0.1%
0.87%
0.1%
100%
Availability
5, 30 or 60 kg drums
Uses
Body contour ( LIPOLYTIC, ANTI-CELLULITE )
Body and face firming
Bags under the eyes / puffy eyes
Body and face moisturization
BIOLOGICAL ACTIVITIES
cAMP AND LIPOLYSIS
CLINICAL TEST : ACTIVITY OF XANTALGOSIL C ON LIPIDIC OVERLOADS
Phosphodiesterase
5 AMP
Inactive triglyceride lipase Active triglyceride lipase
Triglycerides
Free fatty acids
Results: centimeters lost around the waist
Hypothesis of a stimulative action on cAMP is advanced ; it

can be due to silicon.
The lipolytic activity could be the answer to an activation of
the membrane system, leading to adenylate cyclase
formation, thus to cAMP synthesis which activates, by a
series of reactions, the hormono-sensitive lipase.
RESULTS ON XANTALGOSIL C
AND ALGISIUM C FOR
GLYCEROL PRODUCTION
n Mole of glycerol/g of lipid
Reference
5
ALGISIUM C
XANTALGOSIL C
(60mg/lSi)
Theophylline
1.8 g/l
50
50
40
40
30
30
Average % of
cm lost
20
-6 cm
10
cm
-2
-4
-8
Results: centimeters lost around the thighs
Results : centimeters lost around the knees
50
40
40
30
30
20
10
SLIMMING ACTIVITY
XANTALGOSIL C and A LGISIUM C have been tested for
glycerol production due to their activity on adenylate cyclase,
promoting lipolysis.
In vitro study has shown that the lipolytic activity induced by
XANTALGOSIL C was higher than the lipolytic activity of
ALGISIUM C and theophylline.
This slimming activity comes along with the regeneration of the
surrounding connective tissue, leading to a better
microcirculation which normalizes cellular exchanges and
improves the skin aspect.
SIMPLIFIED OUTLINE OF LIPOLYSIS MECHANISMS

Glycerol production for human
adipose tissue with Xantalgosil C
-4
-7
y = -1.023x + 0.558 r = 0.759
0.5
XANTIC
BASES
PDE
0.25
cAMP
Triglyceride lipase
-4
As other compounds of the same family (caffeine and theophylline

derivatives), results show that acefylline inhibits the activity of LPL in a
dose dependent manner.
Lipoprotein-lipase
Fatty Acids
-2
XANTALGOSIL C is obtained from acefylline. This compound is well

known to inhibit phosphodiesterases and enhance the cAMP
concentration in the cells. Cosmetic application of this pharmacologic
activity is the cAMP dependent lipolysis. Concerning its activity on fatty
acids metabolism, acefylline inhibits the lipoprotein lipase (LPL). Inhibition
of LPL by acefylline was studied in vitro. The graph on the left shows the
activity level of the lipoprotein lipase depending on the concentration in
acefylline (XANTALGOSIL C is obtained from 0.87 % of acefylline).
LPL (activity)
speeds 10-2 DO / minute
CAFFEINE
5 AMP
cm
-1
EFFECTS OF ACEFYLLINE
ON THE LIPOPROTEIN LIPASE
Adenylate cyclase
XANTALGOSIL C has remarkable effects on :

- lipolysis in the adipocytes which confirms the results of the experiment on adipocytes in vitro.
- the trophicity and degeneration of the proteoglycans or acid mucopolysaccharides in elastic
fibres and collagen.
- on tissular permeability and thus the resorption of local oedema.
0.75
Mean +/- S.E.M.
10
cm
-2
Average % of
cm lost
20
Average % of
cm lost
-3 cm
20
10
Blood
Results: centimeters lost around the hips
Glycerol
After treating adipose tissue with XANTALGOSIL C ,

intracellular cyclic AMP concentration is increased in a
significant way.
The lipolytic activity obtained with XANTALGOSIL C ,
compared with results obtained with phosphodiesterase
inhibitors, can not be only linked to this cAMP increase in
concentration.
cAMP
25 volunteers with different types of cellulite were selected for this study.
After twice applications per day during 30 days, the centimeters lost were measured for waist, hips, thighs and knees.
The results evaluated on centimeters-loss are summarized in the graphs below :
ATP
XANTALGOSIL C has a notable lipolytic activity. This

activity is directly linked to silicon content; liberated glycerol
content increases with silicon content.
Adenylate cyclase
0
0
0.1
0.2
0.3
0.4
0.5
acefylline (%)
Glycerol
Triglycerides
Glycerol
ADIPOCYTE
EXSYMOL
Fatty Acids
EXSYMOL
Tolerance study
The product is neither toxic nor irritant.
Tolerance has been studied in vitro by alternative methods on both cell culture and
reconstituted epidermis. Ocular tolerance is evaluated by studying cytotoxicity on cornea
isolated fibroblasts culture. Cutaneous tolerance is evaluated on reconstituted epidermis by
valuation of cells viability after a contact period of 24 hours with the product.
Formulation
XANTALGOSIL C is stable for pH included between 3,5 and 6,5. On average, the
recommended concentration is 3 to 6%.
Important remark : XANTALGOSIL C must not be stored at temperature inferior to 0C
otherwise an irreversible polymerization might occur.
Existing studies
EXSYMOL S.A.M. - 4 avenue du Prince Hrditaire Albert - MC 98000 MONACO

Tl. : +377 92 05 66 77 - Fax : +377 92 05 25 02
E-mail : exsymol@exsymol.com - Internet : http://www.exsymol.com
A3_0595GB0301B.pdf
Technical document
*
Lipolytic activity in vitro : adipocytes
*
Tolerances investigations
*
Activity on lipidic overloads clinical test
*
Toxicity Tolerance - alternative methods

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EX

limpid to slightly opalescent liquid,

CLINICAL TEST : ACTIVITY OF XANTALGOSIL C ON LIPIDIC OVERLOADS

Inactive triglyceride lipase Active triglyceride lipase

Free fatty acids

Results: centimeters lost around the waist

Hypothesis of a stimulative action on cAMP is advanced ; it

n Mole of glycerol/g of lipid

Results: centimeters lost around the thighs

Results : centimeters lost around the knees

SIMPLIFIED OUTLINE OF LIPOLYSIS MECHANISMS

y = -1.023x + 0.558 r = 0.759

As other compounds of the same family (caffeine and theophylline

XANTALGOSIL C is obtained from acefylline. This compound is well

XANTALGOSIL C has remarkable effects on :

Mean +/- S.E.M.

Results: centimeters lost around the hips

After treating adipose tissue with XANTALGOSIL C ,

XANTALGOSIL C has a notable lipolytic activity. This

EXSYMOL S.A.M. - 4 avenue du Prince Hrditaire Albert - MC 98000 MONACO

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