nikkol vc-ip - ProdottiGianni

Innovative Vitamin C derivative Prevent
Skin Troubles From Free Radicals
NIKKOL VC-IP
(Ascorbyl Tetra Isopalmitate)
Nikko Chemicals Co., LTD.
Hiro Onoue
International Division
Development of New Oil Soluble
Vitamin C Derivative
HO
OH
+
CHCH2- OH
O
O
H
Isopalmitic Acid
OH
OCO-C15 H31
C15 H31 -COO
CHCH2 OCO-C15 H31
O
O
OCO-C15 H31
INCI Name : Ascorbyl Tetraisopalmitate
The Properties of VC-IP
• Excellent percutaneous absorption
• Prevention of lipid peroxidation
• Scavenging Free Radicals
• Inhibition of melanogenesis and Tyrosinase
Activity
• Prevention of cell (Keratinocytes) damage
• Cell (Fibroblast) activation
• Prevention of cell (Fibroblast) damage and
inhibition of Gelatinase activity
Amount of Ascorbic Acid
Penetrated into the Epidermis
VC-PMG
VC-IP
-Molecular Weight
289.5
1129.8
-Ascorbic acid moiety
in the molecule
59.4%
15.2%
-Skin penetration
0.7%
(amount in the epidermis)
11.6%
-Ascorbic acid penetrated 0.42%
into the epidermis
1.76%
Preventive Effect against Lipid Peroxidation
(SOD-like Activity)
SOD-like Activity
Placebo
VC-IP
0%
40.0 %
0.1ml of VC-IP or placebo with 1ml of 0.4mM of Xanthin and
Xanthin oxidase with 0.24mM of NBT, at 37℃ for 10min
Singlet oxygen reducing activity (%)
Preventive Effect against Lipid Peroxidation
(Quenching Singlet Oxygen)
100
80
60
40
20
0
Ascorbic Acid
VC-IP
Preventive Effect against Lipid Peroxidation
(UV-B Photo-oxidation of Human Sebum)
Placebo(Mineral Oil)
10% VC-IP in Mineral Oil
6
Hydroperoxide (%)
Concentration of Squalene
7
5
4
3
2
1
0
1
2
3
Subjects
4
Average
100
80
60
(%)
Stable radical reducing activity
Stable Radical Reducing Activity
40
Ascorbic Acid
VC-IP
20
0
0
10
20
30
40
50
Incubating Time (hours)
DPPH Method
Inhibitory Effect on Melanogenesis
in Cultured Human Melanoma Cell
Amount of Melanin (%)
100
80
60
40
20
0
0
0.005
0.01
0.05
0.1
Concentration of VC-IP (%)
0.2
Inhibitory Effect on Tyrosinase Activity in
Cultured Melanoma Cell
Tyrosinase Activity (%)
100
80
60
40
20
0
0
0.02
0.05
Concentration of VC-IP (%)
0.1
12
(nmol/106 cells)
Ascorbic Acid content
in the test cell
Uptaken Content of Intracellular
(Keratinocytes) Ascorbic Acid
VC-IP
Ascorbic Acid
10
8
6
4
2
0
5
10
20
50
Concentration (μM)
500
Cytoprotective Effect against Cell Mortality
of UV-B Irradiated Skin Keratinocytes
100
VC-IP
Cell Viability (%)
Ascorbic Acid
80
60
40
20
0
0
20
40
Amount of UV-B irradiation (J/cm2)
Concentration: 10μM
Prevention effect of DNA damage against
VC-IP （-）
VC-IP （＋）
0ｈｒ
2ｈｒ 0ｈｒ
2ｈｒ
0.5ｈｒ
4ｈｒ0.5ｈｒ
4ｈｒ
1ｈｒ
8ｈｒ 1ｈｒ
8ｈｒ
Cell：HaCat
UVA：100J/cm2
VC-IP：80μM
TUNEL analysis
Prevention Effect of Cell damage against UVA
UVA
No Treatment
Cell Survival rate （％）
Cell：HaCat
UVA：100J/cm2
VC-IP：80μM
100
VC-IP（-）
VC-IP（＋）
19.74
51.32
Intracellular AsA Content
(nmol/106 cells)
The intracellular intake and
conversion to AsA
12
10
8
6
4
2
0
0
10
20
VC-IP
50
20
50
AsA
（μM）
Cell Activation in Fibroblast
200
Cell Viability (%)
150
100
50
0
0
0.025
Concentration of VC-IP (%)
0.1
(104 dpm / 106cells)
Collagen Synthesis
The Comparison of Ability for Collagen
Synthesis
4
3
2
1
0
μ M
No
Additive
20
50
AsA
10
20
VC-IP
50
The Ability of Inhibition of Gelatinase
Activity
Gelatinase-Activity(%)
■MMP-2(72KDa)　■ MMP-9(92KDa)
120
100
80
60
40
20
0
No
Additive
10
20
VC-IP
50
20
50
AsA
The inhibitory effect on DNA damage
induced by UVB (p53 expression analysis)
p53 Expression
(% of control)
100
80
60
40
20
0
0
0.005
VC-IP (%)
0.01
Approach for Various Properties of VC-IP
Sebum
Keratinocyte
VC-IP
Melanocyte
Fibroblast
The Efficacy of Oil Soluble
Vitamin C (VC-IP) Against Acne
This study examined the efficacy of fat soluble
vitamin C derivative, NIKKOL VC-IP, which has
active oxygen scavenging ability, when applied by
patients with acne.
Active oxygen plays important role at comedo
formation and inflammation induction phase of acne
<Sample was prepared with 10% of VC-IP>
•
Tokyo Metropolitan Police Hospital
Test result - Acne Treatment by 10 % VC-IP Gel
No Change
Good
Excellent
Before　After 12 weeks
Before
After 9 weeks
Before
After 11 weeks
Before
After 11 weeks
Before
After 16 weeks
Before
After 12 weeks
Before
After 16 weeks
In Conclusion
‹Inhibit Melanogenesis and tyrosinase
Activity
Skin Lightning
‹Eliminate Free Radicals
‹SOD like Activity
Anti-Aging
‹Prevent DNA damage
‹Collagen Synthesis
‹Inhibit Gelatinase Activity
Anti-Acne