MELSCREEN® COFFEE
DESCRIPTION
Coffee Oil extracted from Coffea arabica green coffee beans, specially obtained
through a very careful cold pressing technique.
COMPOSITION
INCI NAME
CAS N°
EINECS (I)/ELINCS (L)
Coffea Arabica (Coffee) Seed Oil
8001-67-0
283-481-1 (I)
Figure 1: Coffea arabica coffee seed
It presents triacylglycerols (40% in linoleic acid, an essential fatty acid) and diterpenic
esthers, more specifically cafestol palmitate.
FATTY ACID COMPOSITION
FATTY ACID
%
Palmitic acid (C16:0)
25.0 - 40.0
Stearic acid (C18:0)
7.0 – 15.0
Oleic acid (C18:1)
8.0 – 15.0
Linoleic acid (C18:2)
35.0 – 48.0
Linolenic acid (C18:3)
0.1 – 3.0
Arachidic acid (C20:0)
2.0 – 5.0
Behenic acid (C22:0)
1.5 max.
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BOTANICAL DESCRIPTION
Coffee is the Coffea arabica Linne or C. liberica Hiern (Pharm. Rubiaceae) ripe and
dried seed lacking most of its coating.
Coffee beans are composed by 1% to 2% of caffeine, about 2.5% of trigonelline (Nmethylbeatine of nicotinic acid), from 3% to 5% of tannin, about 15% of glucose and
dextrin, from 10% to 13% of fatty oils and from 10% to 13% of protein.
MELSCREEN® COFFEE derives from green seeds of some types of Rubiaceae genus
Coffea shrubs. There are more than 30 species of coffee, and according to their
commercial value, the two most important types of coffee are the Arabian (Coffea arabica)
and the Robusta (Coffea liberica). Our coffee, as manufactured by CHEMYUNION, derives
exclusively from Arabica species, which is considered the finest and highest quality coffee
in the world.
MELSCREEN® COFFEE is cold press extracted and presents a special composition of
fatty acids. It is very rich in essential fatty acids; for instance, it includes around 40% of
linoleic acid (omega 6).
Even more interesting is the MELSCREEN® COFFEE ability to decrease the skin
damage from UV radiation, particularly UVB that causes erythema.
More than just water channels – roles of Aquaporins
Aquaporins (AQPs) are a family of membrane proteins that forms water channels
across cell membranes. Some AQPs can also transport small solutes like glycerol or urea.
Aquaporins are expressed in many fluid-transporting tissues, such as kidney tubules and
glandular epithelia, as well as in non-fluid transporting tissues, such as epidermis.
There are several kinds of aquaporins, including the one expressed in the
skin/epidermis, called AQP3, playing an important role transporting water and solutes as
glycerol (aquaglyceroporins).
Epidermal hydration and biosynthesis
The most superficial layer of skin is the stratum corneum (SC), which consists of
terminally
differentiated
corneocytes
that
originate
from
actively
proliferating
keratinocytes in the underlying epidermis.
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Hydration of SC is an important determinant of the appearance and physical
properties of the skin, and depends on several factors, including the external humidity,
skin structure, lipid/protein composition, barrier properties, and the concentration of
water-retaining “humectants” such as free amino acids, ions and other small solutes.
Figure 2: Schematic showing stratum epidermal layers and the natural movement of water
Aquaporins are strongly expressed in the basal layer of keratinocytes in mammalian
skin. Some references about skin analyses showed that lacking of Aquaporins exhibit
reduced SC hydration. In addition, they have reduced skin elasticity, delayed biosynthesis
of the SC and delayed wound healing.
Aquaporins in the skin are also responsible for glycerol transport. The reduced SC
hydration and elasticity is likely to be related to the water retaining property of glycerol
and the delayed barrier recovery and wound healing to the biosynthetic role of glycerol.
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/Water
/Water
Figure 3: Mechanism of action of skin Aquaporins
MELSCREEN® COFFEE according to our in vitro studies showed the ability to
increase aquaporin expression in keratinocytes cell culture. We conclude that it can be
used as an active that can help skin hydration improvement through the repair of the
water channels expression in the epidermis.
TESTS
Safety Tests
1. Assessment of the skin compatibility and absence of allergenic potential of a
cosmetic body cream with 5% of MELSCREEN® COFFEE after repeated application under
patch in human. (Methodology described by Marzulli and Maibach: Human Repeated Insult
Patch Test for Delayed Contact Hypersensitivity: HRIPT).
Result:
MELSCREEN®
COFFEE
used
in
the
suggested
concentrations
for
dermatological cosmetic formulations, presented excellent compatibility with the skin.
MELSCREEN® COFFEE was tested in a cream (code CCR033A00 – Excipient formulation
previously tested and considered safe according to dermatological standards). After
repeated applications in the skin, neither irritation nor allergic reaction was observed.
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Efficacy Tests
1. Clinical assessment of the sun protection factor of a sunscreen product with
addition of 5% of MELSCREEN® COFFEE, according to the “Sun Protection Measurement
Protocol” issued by the COLIPA in 1994.
Result: Under the experimental conditions adopted and according to the results
obtained the sun protection product with addition of 5% of MELSCREEN® COFFEE showed
an SPF increased of about 25% (graph 1).
MELSCREEN® COFFEE also reduced the erythema caused by solar radiation.
16
14
12
10
8
6
4
2
0
FPS PLACEBO
FPS PLACEBO +
MELSCREEN COFFEE
5%
Graph 1- Effects of the addition of MELSCREEN® COFFEE 5% in a sun protection product.
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2.
Evaluation of TGF-beta and GM-CSF release in a human fibroblast
culture:
204.43%
TGF-beta (pg/mL)
1400
*
1200
1000
800
600
400
200
0
Control
Control
MELSCREEN
COFFEE
MELSCREEN
COFFEE
2,5% ORG
(2,5%)
Graph 2: Evaluation of TGF-beta production in human fibroblasts culture after 48 hours of incubation with 2.5%
of MELSCREEN
®
COFFEE. *P<0.001, related to the control (ANOVA, Tukey).
834.47%
*
GM-CSF (pg/mL)
320
280
240
200
160
120
80
40
0
Control
Control
MELSCREEN COFFEE ORG
(2,5%)
MELSCREEN COFFEE 2,5%
Graph 3: Evaluation of GM-CSF production in human fibroblasts culture after 48 hours of incubation with 2.5% of
MELSCREEN
®
COFFEE. *P<0.001, related to the control (ANOVA, Tukey).
According to the results showed in the graph above, MELSCREEN® COFFEE
increased in a very significant way TGF-beta and GM-CSF production in a human fibroblast
culture. Taking account the fundamental role of these tissue growth factors on the cell
metabolism and also on the synthesis of extracellular matrix components, we could
conclude that MELSCREEN® COFFEE has an important activity on damaged tissue repair.
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3. Quantification of extracellular matrix (ECM) components: collagen,
elastin and glycosaminoglycans.
The extracellular matrix (ECM), also known as the connective tissue, is a complex
structure that involves and gives support to all tissues in the body. It is composed by 3
main classes of biomolecules:
• Structural proteins: collagen and elastin;
• Specialized proteins: fibrilin, fibronectin and laminin;
• Proteoglycans: glycosaminoglycans
3.1. Evaluation of collagen production:
+ 76%
Colagen (µ
µ g/mL)
180
*
150
120
90
60
30
0
Control
Control
MELSCREEN
COFFEE ORG
®
COFFEE 2,5%
(2,5%)
MELSCREEN
Graph 4: Evaluation of collagen production in human fibroblasts culture after 48 hours of incubation with 2.5%
of MELSCREEN® COFFEE . *P<0.001, related to the control (ANOVA, Tukey).
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3.2. Evaluation of elastin production:
52,24%
60
Elastin (µ
µ g/mL)
*
50
40
30
20
10
0
Control
Control
MELSCREEN
COFFEE
MELSCREEN
COFFEE
2,5% ORG
(2,5%)
Graph 5: Evaluation of Elastin production in human fibroblasts culture after 48 hours of incubation with 2.5% of
MELSCREEN
®
COFFEE . *P<0.001, related to the control (ANOVA, Tukey).
Glycosaminoglycans (µ
µ g/mL)
3.3. Evaluation of glycosaminoglycans production:
>100%
3
*
2,5
2
1,5
1
0,5
0
Control
Control
MELSCREEN COFFEE ORK
(2,5%)
MELSCREEN COFFEE 2,5%
Graph 6: Evaluation of Glycosaminoglycans production in human fibroblasts culture after 48 hours of incubation
with 2.5% of MELSCREEN
®
COFFEE . *P<0.001, related to the control (ANOVA, Tukey).
The results showed that MELSCREEN® COFFEE promote increases up to 76% and
52.24% in the production of collagen and elastin, respectively. MELSCREEN® COFFEE
also increases Glycosaminoglycans synthesis up to 100%. These results support a better
performance in the production of extracellular matrix components, thus increasing the
production of these essential biomolecules of dermis.
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4. In vitro efficacy of the lipolytic activity of MELSCREEN™ COFFEEQuantification of free fatty acid release (NEFA)
213.33%
0,6
*
NEFA (mEq/L)
0,5
0,4
0,3
0,2
0,1
0
Control
Control
MELSCREEN
COFFEE
MELSCREEN
COFFEE
2,5% ORG
(2,5%)
Graph 7: Evaluation of NEFA production in human adipocytes culture after 48 hours of incubation with 2.5% of
MELSCREEN
®
COFFEE. * P<0.001, related to the control group (ANOVA, Tukey).
The graph above demonstrates the effects of MELSCREEN® COFFEE showing a
considerable lipolytic action, inducing in vitro lipolysis. NEFA quantification is an accurate
indicator to evaluate lipolysis rate once intracellular fat is given in the form of
tryacylglycerols (TAG), formed by a process called lipogenesis, which occurs from the
union of three (3) free fatty acids (NEFA) molecules and one glycerol molecule. In
addition, during lipolysis occurs the breakdown of intracellular TAG with a consequent
release of NEFA to extracellular.
5. Relative expression of gene that codifies Aquaporin 3 protein – Treatment
with MELSCREEN® COFFEE:
Keratinocytes cell culture was incubated with MELSCREEN® COFFEE and the
evaluation of AQUAPORIN 3 expression was measured after 3 and 6 hours in comparison
to cell culture without treatment (control).
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6.88x
3
6.93x
Time (h)
6
0
1,5
3
4,5
6
7,5
9
Relative AQP-3 mRNA expression
(in relation to control group)
The assessment of AQP3 expression in a cell culture of human keratinocytes
incubated with 2.5% of MELSCREEN® COFFEE demonstrated that after both time, 3 and
6 hours of incubation, MELSCREEN® COFFEE increased the AQP3 expression almost 7fold in relation to control group.
WHY TO USE IT?
Human skin provides a barrier between the body and the environment to protect
against damages from outside (e.g. UV-radiation, chemicals, microbes). The skin consists
of hypodermis, dermis and epidermis. The outermost layer of the epidermis, the stratum
corneum (SC), is mainly responsible for the barrier function of the skin. The cells of the
SC, called corneocytes, are continuously replaced and are derived from keratinocytes.
During the differentiation process, these keratinocytes produce lipids among other things,
which are extruded in the intercellular matrix just before reaching the SC. The intercellular
lipids comprise ceramides (CER), cholesterol (CHOL), and free fatty acids (FFA).
Sebaceous glands, mainly found in hair-covered areas, secrete an oily substance
called sebum, presenting a diverse composition (triglycerides, free fatty acids, cholesterol,
squalane, waxes). The sebum and the products secreted by sudoriferous glands form the
most important “Natural Cosmetic”: the epicutaneous emulsion. Although the sebum slows
water evaporation from the surface of the skin, it cannot prevent dryness if skin lacks
moisture.
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Other factors that can dry skin include wind and sun exposure, using alkaline soaps,
dietary deficiencies, stress and pollution. These factors damage the hydrolipidic barrier by
leading it to a higher Trans-Epidermic Water Loss (TEWL), consequently, a drier skin.
MELSCREEN® COFFEE is rich in fatty acids. It can help to restore the lipids present
in the corneum layer by restructuring those protective lipids and giving the skin a healthier
appearance since it promotes the skin hydration.
In addition, it contains a very convenient percentage of linoleic acid (omega 6) that
is an essential fatty acid. It is an essential skin lubricant, which works as a true skin
treatment.
The poly-unsaturated fatty acids (linoleic, linolenic and arachidonic) are just as
essential as vitamins. They are basic substances from which not only skin lipids
(ceramides)
and
cell
membrane
lipids
(phospholipids)
but
also
hormones
and
prostaglandins are synthesized.
These fatty acids are very interesting when used in cosmetic products. Studies have
shown that a fatty acid deficiency generated different kinds of disturbances and, above all,
a break up in the keratinization process. This results in a visible remarkable skin
desquamation.
In this situation the physiological water regulation of the skin is impaired, leading to
high TEWL (Trans Epidermal Water loss).
When this deficiency is severe, skin crack is visible and wound healing process is
delayed. Irregularities in the keratin structure and unorganized epidermal layers can
happen.
EFAs (Essential Fatty Acids), especially linoleic acid, restore the skin barrier. After
being treated with MELSCREEN® COFFEE, the skin will present a silky touch and velvety
softness.
Omega 6 present in MELSCREEN® COFFEE maintains the normal functions of
hydrolipidic barrier, its integrity and results in a normal skin balance.
Another important MELSCREEN® COFFEE function is its capacity to decrease the
skin damage from UV radiation, particularly UVB that causes erythema.
Also MELSCREEN® COFFEE can help to hydrate epidermis for increasing aquaporins
expressions.
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APPLICATION/USE
MELSCREEN® COFFEE should be used in cosmetics formulations, mainly tanning
and sunscreen lotions intended to:
•
Lubricate the skin and regenerate the hydrolipid barrier that is constantly subject
to aggressions, mainly from the sun.
•
Protect the skin damage from UV radiation, by reducing erythema due to an
anti-oxidant action. SPF boosting effect clinically tested.
•
Skin care products, anti-aging products
•
Sun care products and after sun products, including children’s products.
SUGGESTED CONCENTRATION
From 1.0% to 5.0%.
REFERENCES
•
James E. Robbers; Marilyn K. Speedie; Varro E. Tyler, “Farmacognosia/
Biotecnologia”, Editorial Premier, pág. 204 a 208.
•
WC Evans, “Trease and Evans Pharmacognosy”, 14th Edition, Sauders, pag. 403.
•
Peter T. Pugliese, MD; Physiology of the Skin, page 21 a 24.
•
Urgert R, Weustenvander Wouw MPME, Hovenier R, et al.; Diterpenes from coffee
beans decrease serum levels of
lipoprotein(a) in human: Results from four
randomized controlled trials., EUR J CLIN NUTR 51: (7) 431- JUL 1997.
•
AlKanhal MA, Lipid analysis of Coffea arabica Linn beans and their possible
hypercholesterolemic effects INT FOOD SCI NUTR 48: (2) 135-139 MAR 1997.
•
Thompson GL, Thore S, Exchanging heterogeneous goods via sealed bid auctions
and transportation systems ANN OPER RES 68: 181-208 1996.
•
QUARMBY J, FORSTER CF, An examination of the structure of usab granules
WATER RES 29: (11) 2449-2454
•
Terpstra
Ahm, Katan
NOV 1995.
MB, Weustenvanderwouw
MPME,
et. al, Coffee oil
consumption does not affect serum-cholesterol in Rhesus and Cebus Monkeys, J
NUTR 125: (9) 2301-2306 SEP 1995
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•
Mensink RP, Lebbink WJ, Lobbezoo IE, et al., Diterpene composition of oil from
arabica and robusta coffee beans and their effects on serum-lipids in man, J
INTERN MED 237: (6) 543-549 JUN 1995
•
Vanrooij J, Vanderstegen GHD, Schoemaker RC, et al., A placebo-controlled
parallel study of the effect of 2 types of Coffee Oil on serum-lipids and
transaminases - identification of chemical-substances involved in the cholesterol raising effect of coffee, AM J CLIN NUTR 61: (6) 1277-1283 JUN 1995
•
Gershbein LL, Action of dietary trypsin, pressed Coffee oil, silymarin and iron salt
on 1,2 - dimethylhydrazine tumorigenesis by gavage ANTICANCER RES 14: (3A)
11130-1116 MAY - JUN 1994
•
Weustenvanderwouw MPME, Katan MB, Viani R, et al., Identity of the cholesterolraising factor from boiled coffee and its effects on liver-function enzymes, J LIPID
RES 35: (4) 721-733 APR 1994
Documento
Elaborated by:
Revised by:
Approved by:
Controlled by:
R&D Dept.
Mkt. Dept.
R&D. Board
QA Dept.
The information contained in this Literature is provided in good faith. We recommend the test of our products in order to verify the
convenience of their use before adopting them at industrial level. Such information shall not be understood as concession or
permission to use the methods or compositions covered by any patent. This material reproduction is prohibited without the
CHEMYUNION QUÍMICA LTDA authorization.
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