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Currying skin health with
multifunctional curcuminoids |
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ABSTRACT |
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The healthful spice turmeric, has traditionally been
used in skin care since ancient times in South Asia.
Recent scientific research has validated its inherent
beneficial effects, both nutritional and topical.
Technological innovation in ingredients enables
imparting the goodness of curcuminoids from "curry",
(turmeric) into skin, hair and nails without being
hampered by the yellow color. Tetrahydrocurcuminoids
(a) are patented colorless derivatives of the yellow
"bioprotectant" curcuminoids (b) with multifaceted
benefits in anti-aging and skin protectant compositions.
This article discusses innovative applications of the
natural compositions of Curcuminoids and
Tetrahydrocurcuminoids, as well as a single
component Tetrahydrocurcumin. |
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INTRODUCTION: SKIN AGING AND ANTIOXIDANTS |
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Aging is attributed to the effects of collective damage
to connective tissues, that overpowers the body's
natural ability to repair them. The perceptible signs of
skin aging include discoloration, wrinkles, and texture
loss. These effects result from structural and metabolic
changes effected by biochemical reactions in the
connective tissues, that are accelerated by free
radicals. Environmental agents such as UV rays
exacerbate the effects of free radical reactions and
oxidative stress. These reactions to time and the
environment are rooted in the metabolic processes in
the body, and the ability of the internal machinery to
combat stress and adapt to the environment (1, 2).
About 25 percent of the lipids in the skin surface are
unsaturated, and therefore more prone to attack by
free radicals. These reactions in turn promote the
action of inherent enzymes such as collagenase and
elastase, facilitating the proliferation of inflammatory
mediators. Apparent deteriorative oxidative changes
triggered by free radicals include wrinkling,
hyperpigmentation (excessive tanning) and
inflammation (sunburn). Free radicals attack the skin's
fibroblasts, leading to loss of collagen and elastin; and
cause cross-linkage of connective tissue fiber. The
result is dry, leathery skin, with wrinkled appearance
and poor skin tone. Aged skin may be manifested in
the form of discoloration, actinic keratosis (rough,
reddish warts on sun-exposed areas, a precursor to
"squamous cell carcinoma"), seborrehic keratosis
(non-cancerous brown or black raised spots), cherry
angiomas (small, bright red domes due to dilated blood
vessels), and broken capillaries (bruising due to dilated
blood vessels and loss of subcutaneous fat), as well.
"Anti-aging" cosmetic products, potentially inhibit or
delay the visible signs of chronoaging and photoaging,
such as wrinkles, lines, sagging, hyperpigmentation
and age spots. Recent trends favor attacking the root
causes of aging from the inside and the outside for
consolidated benefits. Nutricosmetics in the form of
dietary interventions work with externally applied
cosmeceuticals to slow down the aging process.
Natural antioxidants that quench free radicals are an
essential component of anti-aging formulations. They
potentially offer protection against damage to the
tissues by environmental and other agents.
Biochemical reactions that accelerate the progression
of skin aging have their roots in inflammatory
processes. Inflammation generates microscars which
mature into blemishes or wrinkles. Various types of
inflammatory mediators such as leukotrienes and
prostaglandins, cytokines and growth factors may
influence melanin synthesis by affecting the
proliferation and functioning of melanocytes. Protein
kinase C, the enzyme, that phosphorylates proteins,
may also influence the growth and differentiation of
melanocytes. Cytokines such as endothelins (also
known as vasoconstrictive peptides) are also reported
to accelerate melanogenesis. Natural antiinflammatory
agents are therefore included in antiaging
formulations, and serve to soothe, heal and
protect skin tone and integrity. Lipids play an important
role in maintaining the barrier functions of the skin. In
general, unsaturated fatty acids reinforce the skin's
barrier function, prevent moisture loss through the
epidermis, provide structural integrity to the skin
damaged by external influences and are antiinflammatory.
They also help to soften and smoothen
the skin by inhibiting the formation of corneous cells.
Lipid compounds that provide an occlusive effect to
prevent water loss, repair lipid layers and restore
barrier functions are therefore an integral part of antiaging
formulations. |
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CURCUMINOIDS: ANTIOXIDANT
PHYTONUTRIENTS FROM TURMERIC |
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Curcuminoids-rich extract from turmeric rhizomes is
well known for its antioxidant properties, antimicrobial
effects, and beneficial effects on inflammation.
Turmeric has been traditionally used by South Asian
women in skin care since ancient times. However, its
yellow color may not blend well with cosmetic
formulations. An innovative colorless (white to very
light tan) derivative, Tetrahydrocurcuminoids,
addresses this drawback, and offers effective
protection against sun damage. Its antioxidant action is
of a comprehensive "bioprotectant" nature, efficiently
preventing the formation of free radicals, while
quenching pre-formed ones as well, thereby protecting
the skin cells from damage by UV radiation and the
resultant inflammation and injury. This in turn has far
reached beneficial effects on overall health and well
being, rendering a healthy glow to the skin.
Tetrahydrocurcuminoids are therefore useful in
brightening and lightening skin tone, and offer
protection against the development of melanoma (1, 8,
9). The bioprotectant effect of curcuminoids (4) and
tetrahydrocurcuminoids is further validated in welldocumented
experiments related to anti-tumor activity.
The addition of 0.5 to 10 micromoles of curcumin to an
in vitro skin cell culture inhibited the activity of the
enzyme ornithine decarboxylase which has been
linked to the promotion of tumor cell growth. Thus
curcumin has the capability to inhibit genetic change
(mutation) in the cells, that often initiates the aging
process, and contributes to cancer development.
Traditionally, turmeric from which curcuminoids and
tetrahydrocurcuminoids are derived, has been used in
the ancient system of Indian medicine, Ayurveda in a
variety of internal and topical uses. Documented
traditional topical uses include application to the ear in
chronic otorrhea, as a cooling eyewash to relieve
purulent opthalmia, as a topical treatment for
pemphigus (an allergic and inflammatory skin
condition), in viral conditions such as shingles and
chickenpox to facilitate the process of healing, and as
a dressing applied to bruises, sprains, found that
curcuminoids can be effectively applied in the
treatment of precancerous lesion called leukoplakia
(usually affecting oral mucosa).
Based on their history of traditional use in Ayurvedic
medicine, and the relatively recent research findings
on their safety and efficacy, the multifunctional
curcuminoids, and their metabolite
tetrahydrocurcuminoids, deserve a special place
among natural cosmeceuticals. |
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CURCUMINOIDS EXERT BENEFITS AT THE
MOLECULAR LEVEL |
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At the fundamental level, phytonutrients such as
curcumin have been shown to up regulate antioxidant
gene expression in animal models. The multifunctional
health benefits of the curcuminoids are well
researched and these antioxidant compounds are
potentially useful in preventing inflammation and
several types of cancer. A common spice used in
South Asian cooking, turmeric and more appropriately
the curcuminoids have been preclinically and/or
clinically validated for beneficial effects in a number of
disease conditions ranging from Alzheimer's disease to
cystic fibrosis. The antioxidant effects of curcuminoids
combined with their known inhibitory effects on
cyclooxygenase 2 (COX-2) render them useful as
ingredients in anti-aging formulations, and in topical
formulations designed to maintain general skin health
and integrity. Oxidative stress and inflammation are
major players in the aging process. The antiinflammatory
role of curcuminoids is well established.
Curcuminoids have been shown to inhibit nuclear
factor kappaB (NF B) a transcription factor that triggers
inflammatory mediators. NF B has been implicated in a
variety of chronic disease conditions ranging from
cardiovascular diseases to cancer (3). A recent study
postulates that curcumin can potentially slow down the
aging process, delaying senescence and the onset or
progression of many age-related diseases.
Curcuminoids offer antioxidant support, antiinflammatory
support, support a healthy immune
system, prevent connective tissue break down through
inhibiting destructive enzymes (such as collagenase,
elastase, hyaluronidase) (8). |
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TETRAHYDROCURCUMINOIDS: THE "WHITE"
CURCUMINOIDS |
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This composition (5, 6) is a colorless hydrogenated
derivative of the natural yellow curcuminoids
(curcumin, demethoxycurcumin,
bisdemethoxycurcumin, from Curcuma longa
(Turmeric)). The components Tetrahydrocurcumin
(INCI: Tetrahydrodiferuloylmethane),
Tetrahydrodemethoxycurcumin (INCI:
Tetrahydrodemethoxydiferuloylmethane), and
Tetrahydrobisdemethoxycurcumin (INCI:
Tetrahydrobisdemethoxydiferuloylmethane) are
reported to be major metabolites of curcuminoids in
vivo. For example, Curcumin the major curcuminoid in
the natural extract is biotransformed in the body
through reduction to Tetrahydrocurcumin and other
reduced forms (8, 9).
Several independent studies reported the significant
antioxidant effects of Tetrahydrocurcuminoids and their
utility in achromatic food and cosmetic applications that
currently employ conventional synthetic antioxidants.
Tetrahydrocurcuminoids was shown to be a more
efficient antioxidant than the curcuminoids, curcumin,
and vitamin E in laboratory studies. The concentration
of Tetrahydrocurcuminoids needed to scavenge free
radicals (IC50) was 2.3, 2.7 and 5.8 times lower than
that of Curcuminoids, Curcumin and vitamin E,
respectively (8).
Tetrahydrocurcuminoids inhibit cross linking of
proteins, supporting healthy aging. Described as a
"crossregulin" composition, this natural ingredient is
effective in skin lightening, and offers protection
against UVB rays, melanoma, and age spots.
Tetrahydrocurcuminoids also support skin texture
through inhibitory effects on enzymes that help to
break down connective tissues. The composition also
effects skin lightening effects through tyrosinase
inhibition. A branded Tetrahydrocurcumin product
(patents pending) was found to be several fold more
effective as a skin lightener than other natural skin
lightening agents including glabridin (licorice extract)
and kojic acid. The comparative tyrosinase inhibitory
activity of these natural materials is summarized in
Table 1 (7): |
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APPLICATIONS IN COSMETICS |
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Some of the cosmeceutical applications of
Tetrahydrocurcuminoids are as below. The suggested
level of use in such formulations is 0.5 percent to 2
percent w/w.
- Dyschromia management support
- Skin tone lightener
- Protection against UVB (sun care,
after-sun care)
- Antiaging Support
- Antioxidant (both as functional
antioxidant to prevent fat oxidation in
the formulation and as a
"cosmeceutical" antioxidant)
From the safety point of view, the
bioprotectant role of
Tetrahydrocurcuminoids is further
enhanced by its very low toxicity, (oral
LD50 is 5000 mg/kg) with a 0.00 irritation score in a
skin patch test. It does not sensitize the skin. Turmeric
root, the source of Tetrahydrocurcuminoids, is listed by
the US Food and Drug Administration (FDA) as an
herb generally recognized as safe (GRAS) for its
intended use as a spice, seasoning and flavoring agent
(21 CFR 100.0, 182.10, 182.20).
Sample formulations for cosmetic and nutricosmetic
applications are presented here.
MUHAMMED MAJEED,
LAKSHMI PRAKASH
Sabinsa Corporation
70 Ethel Road West, Unit 6
Piscataway, NJ 08904
USA |
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Cosmetic formulation: skin lightening "Antiaging"
formula |
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| Ingredient Function |
% Wt. |
| Phase A |
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| Deionized water Solvent |
82.10 |
| Xanthan gum Stabilizer |
0.60 |
| Phase B |
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| Caprylic/capric triglyceride Emollient/Solvent |
3.00 |
| Myristyl myristate Emollient |
3.00 |
| Cetyl alcohol Emollient/solvent |
1.50 |
| Emulsifying wax NF Emulsifying agent |
2.50 |
| Sodium methylparaben Preservative |
0.2 |
| Sodium propylparaben Preservative |
0.1 |
| Tetrahydropiperine
(Cosmoperine® Active Sabinsa Corp) |
0.01 |
| Phase C |
|
Tetrahydrodiferuloylmethane Active
(SabiWhite®, Sabinsa Corp)
| 0.5 |
Oxyresveratrol Active
(OxyResvenoxTM, Sabinsa Corp)
Rosmarinus Officinalis (Rosemary) |
0.1 |
Leaf Extract Active
(Rosemary CG , Sabinsa Corp) |
0.5 |
| Cyclomethicone Antistatic agent |
3.00 |
|
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Heat water from phase A to 50°C and sprinkle in
xanthan gum, mixing well, and then heat mixture to
75°C. Combine ingredients of phase B with mixing and
heat to 75°C. Add B to A using agitation, at this
temperature, mix for 20 minutes and maintain
temperature at 70-75°C. Cool to 40°C, add phase C
with mixing and cool to desired fill temperature. |
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Sample nutricosmetic dietary supplement
formulation: Sun protection/After- sun care |
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Formulate as tablet or capsule with permitted carriers
and other inactive ingredients Suggested use level: 1
tablet or capsule twice daily. |
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REFERENCES AND NOTES |
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a. US Patent #6,653,327, EP1171144 and pending International
patents
b. US Patent #5,861,415; EP0839037
1. V. Badmaev, M. Majeed, "Tetrahydrocurcuminoids (THC) as a
Skin Bioprotectant", Agro-Food-Hi-Tech, Jan.-Feb, pp.25-27
(2000).
2. H. Black, "Potential involvement of free radical reactions in
ultraviolet light-mediated cutaneous damage", Photochem.
Photobiol., 46, pp. 213-22 (1987).
3. A. Kumar et al., "Nuclear factor-kappaB: its role in health and
disease", Journal of Molecular Medicine, 82, pp. 434-48 (2004).
4. M. Majeed et al., US Patent 5,861,415 Bioprotectant composition,
method of use and extraction process of Curcuminoids.
5. M. Majeed et al., US Patent No. 6,653,327. Cross regulin
composition of turmeric-derived tetrahydrocurcuminoids for skin
lightening and protection against UVB rays.
6. L. Prakash et al., "Multifunctional Ingredients: The Novel Face of
Natural", Cosmetics & Toiletries Magazine, 118, No. 11/
November, pp. 41-46 (2003).
7. Research Report, Sami Labs Ltd., 2002.
8. www.curcuminoids.com
9. www.tetrahydrocurcuminoids.com |
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