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Microsoft word - alm i - wi - wi – skin health, ageing & cosmoceuticals.doc

ALM I – Dermatology
WI – Skin Health, Ageing & Cosmoceuticals
Please read the following article titled “Efficacy and safety of innovativecosmeceuticals” Clinics in Dermatology (2008) 26, 367–374 Efficacy and safety of innovative cosmeceuticals☆ Xing-Hua Gao, MDa, Li Zhang, MDa, Huachen Wei, MDb, Hong-Duo Chen, MDa, aDepartment of Dermatology, No. 1 Hospital of China Medical University, Shenyang, ChinabDepartment of Dermatology, The Mount Sinai Medical Center, New York, USA Abstract The research and development of cosmeceuticals is booming in recent years. Many substances,either from botanical, animal, or chemically synthesized sources, are tested or investigated as the activeingredients in cosmeceuticals. The interactions between cosmeceuticals and skin are complex,depending on the specific composites in cosmeceutical products, condition of the skin or general healthstatus of a subject, and the environment where the action occurs. As such, careful preclinical or clinicalevaluation of efficacy and safety is a prerequisite for the development of a specific cosmeceuticalproduct. This article reviews some of the ingredients that are currently in use or might be potentialcandidates in cosmeceuticals of different categories.
2008 Elsevier Inc. All rights reserved.
are irritability to the skin, contact dermatitis, photosensitiv-ity, comedogenicity, hair and nail damage, hyper- or The term cosmeceutical was first introduced by Albert hypopigmentation, infectivity, carcinogenicity, and even during a meeting about 20 years ago. It is a systemic adverse effects. The research and development of category of cosmetic products claimed to have biologically cosmeceuticals, especially the composite active ingredients, active ingredients with medicinal or druglike benefits.
should be based on their clarified sources, structures, Furthermore, they satisfy the needs of beauty and health.
interactive mechanisms with the skin, and, most importantly, Many substances, either chemically synthesized or extracted their efficacy and safety on the targeted components of skin.
from plants or animals, can be used as functional ingredients.
Here we review some of the cosmeceuticals with different Nowadays, many cosmetic products with biologically active categories of functions, with special focuses on their ingredients have been developed and marketed, though there are discrepancies about their regulations and approvals bythe government.
Cosmeceuticals are intended to carry out their functions as protection, whitening, tanning, antiwrinkling, deodorants,antiaging, and nail and hair care. Cosmeceuticals may, however, cause some unwanted problems. The common ones The number and amount of melanocytes, as well as the type and distribution of melanin in the skin, are the main ☆ This article was supported by the Program for New Century Excellent factors to determine the color of skin. The synthesis of Talents in University (NCEP-04-0287).
melanin pigment is completed by a series of oxidative Corresponding author. Tel.: +86 24 83282642; fax: +86 24 83282633.
reactions, along which tyrosinase is the key enzyme.
0738-081X/$ – see front matter 2008 Elsevier Inc. All rights reserved.
Tyrosinase converts tyrosine to dihydroxyphenylalanine citric acid, mixed fruit acid, triple fruit acid, sugar cane (DOPA) and then to dopaquinone; dopaquinone autooxidates extract, and so on. Primarily, lactic acid and glycolic acid are to dopachrome and, finally, to dihydroxyindole or dihydrox- the most widely studied forms of AHAs because they have a yindole-2-carboxylic acid to form eumelanin (black-brown molecular size that allows effective penetration into the top pigment). Dopaquinone can also be converted to cysteinyl layers of skin. α Hydroxy acids have been used for years in DOPA or glutathione DOPA and subsequently form chemical peels. It is generally assumed that AHAs at pheomelanin (yellow-red pigment). The etiology of hyper- concentrations of 4% to 15% are not effective for inhibiting pigmentation includes postinflammatory hyperpigmentation, melanin production. Rather, it is believed that they can pregnancy, drugs, photosensitizing agents, UV light, or accelerate cell turnover rates and exfoliate the stratum systemic diseases (eg, Addison's disease, liver disease, corneum. Other research, however, has shown that lactic and pituitary tumors). There are many pigmentary disorders that glycolic acids can indeed inhibit melanin production in pose cosmetic problems in humans. Melasma, freckles, and addition to their actions as an exfoliant on skin.There are aging spots are among the most common ones.
reports that glycolic acid, or glycolic acid with hydroqui- Hydroquinone, with a phenol structure, is well known for none, is highly effective in reducing the pigment in melasma its suppressive effect on melanin synthesis. Topical hydro- There have been, however, accumulating reports quinone in 2% to 4% concentrations, alone or in combination on adverse effects of cosmetics containing AHA. They with tretinoin 0.05% to 0.1%, has been successfully used for include severe redness, swelling, blistering, burning, itching, years in treating melasma.The problem with hydroquinone discoloration, and increased photosensitivity. The side use is that it can be a skin irritant causing contact dermatitis, effects are related to the pH and concentration of AHA, particularly in higher concentrations of 4% or greater, or vehicles used, and frequency of application.
when combined with tretinoin. Hydroquinone is also an Kojic acid (5-hydroxy-4-pyran-4-one-2-methyl), a natural unstable and easily oxidized ingredient in cosmetic formula- substance produced by fungi or bacteria, such as Aspergillus, tions. It is, therefore, essential to package it in a Penicillium, or Acetobacter spp, is present in traditional nontransparent and airtight container to avoid light and air Japanese fermented foods. There is convincing evidence, in exposure. An uncommon adverse effect is exogenous vitro and in vivo, showing kojic acid to be effective for ochronosis, characterized by progressive sooty darkening inhibiting melanin production.Kojic acid is highly of the skin area exposed to hydroquinone. Derivatives of effective in reducing the pigment in melasma The hydroquinone have also shown some promises for lightening problem with kojic acid is that it is an extremely unstable skin. For example, arbutin contains a form of hydroquinone ingredient in cosmetic formulations. Upon exposure to air or (β-D-glucopyranoside) derived from the leaves of bearberry, sunlight, it can turn to a strange shade of brown and lose its cranberry, mulberry, or blueberry shrubs, and in most types efficacy. Furthermore, some controversial studies have of pears. Pure forms of arbutin derivatives, such as α-arbutin, shown that kojic acid has some mutagenic properties, at β-arbutin, and deoxyarbutin, are considered more potent for least in some strains of bacteria.A stable derivative of lightening skin. It was reported that deoxyarbutin effectively kojic acid, 5-[(3-aminopropyl)phosphinooxy]-2-(hydroxy- inhibits mushroom tyrosinase in vitro with a Ki that is methyl)-4H-pyran-4-one (Kojyl-APPA), was synthesized.
10-fold lower than hydroquinone and 350-fold lower than Kojyl-APPA significantly inhibited tyrosinase activity at arbutin. In a human clinical trial, topical treatment of 24 hours after treatment in normal human melanocytes. In deoxyarbutin for 12 weeks resulted in a significant or slight addition, Kojyl-APPA decreased melanin content to 75% of reduction in overall skin lightness and improvement of solar control in melanoma cells and decreased the newly lentigines in a population of light skin or dark skin synthesized melanin to 43% of control in normal human individuals, respectivelyArbutin inhibits melanin synth- melanocytes. Its permeation through skin increased by about esis in a dose-dependent mannerSo far, most of the 8 times as compared with kojic acid.Again, there have research describing arbutin's effectiveness has been done in been no reports on its clinical usefulness and safety issues.
vitro. Clinical studies are needed to test at what concentra- Azelaic acid is a naturally occurring saturated dicar- tion or in what vehicle arbutin is more effective to lighten boxylic acid originally isolated from Pityrosporum ovale. It the skin, and what possible hazards it may pose to skin.
is an effective therapeutic agent in treatment of a number of Another study screened several phenolic derivatives using skin disorders (eg, acne and rosacea) when applied in a B16 melanoma cells and found that a biphenyl derivative, cream or gel at concentrations of 15% to 20%. It can also 2,2′-dihydroxy-5,5′-dipropyl-biphenyl (DDB), down-regu- inhibit melanin production. A double-blind study with lated melanin synthesis effectively. DDB down-regulates 329 women showed that 20% azelaic acid cream in melanin synthesis by inhibiting the maturation of tyrosinase, conjunction with a broad-spectrum sunscreen yielded 65% leading to acceleration of tyrosinase degradation.DDB, good or excellent results against melasma. Over the treatment thus, might be a potential depigmenting candidate as a period of 24 weeks, the azelaic acid cream had comparable cosmeceutical, given careful and sufficient testing and trials.
effects to 4% hydroquinone cream with regard to overall There are many forms and various sources of α hydroxy rating, reduction in lesion size, and pigment intensity. Severe acids (AHAs), such as lactic acid, glycolic acid, malic acid, side effects such as allergic sensitization were not observed Efficacy and safety of innovative cosmeceuticals with azelaic Additional research, however, suggests Magnesium-L-ascorbyl-2-phosphate (MAP) is a stable that azelaic acid is more irritating than hydroquinone mixed derivative of ascorbic acid. When used as a 10% cream, with glycolic acid (source, eMedicine Journal, MAP showed significant lightening effect in more than half of patients with melasma and solar lentigines. Furthermore, acid is an optional candidate for skin lightening if a patient MAP has been shown to have a protective effect against skin has acne and postinflammatory hyperpigmentation or has allergic reaction with hydroquinone.
Alkyl esters of the natural product gentisic acid are also Retinoids are compounds that have the basic core structure tyrosinase inhibitors. The smaller esters (eg, methyl and of vitamin A and its oxidized metabolites, or synthetic ethyl) were more effeSphingosylphosphorylcholine compounds that share similar mechanisms of action as is emerging as a potent signaling-lipid mediator. It naturally occurring retinoids.Topical retinoids such as all- significantly inhibits melanin synthesis in a concentration- trans-retinoic acid (RA), 13-cis-retinoic acid (isotretinoin), dependent manner, and further, that it reduces the activity retinol, retinaldehyde, tazarotene, and adapalene have been shown to improve dyspigmentation of photodamaged skin, Some amides obtained from coupling p-hydroxycinnamic including mottling and actinic lentigines. All-trans-retinoic acid derivatives with phenylalkylamines were also very acid has been demonstrated to improve melasma and potent in inhibiting melanin synthesis. The most active postinflammatory hypermelanosis. Furthermore, RA, in amides were trans-N-caffeoyltyramine, N-dihydrocaffeoyl- combination with hydroquinone or 4-hydroxyanisole, or tyramine, and trans-N-dihydro-p-hydroxycinnamoyltyra- azelaic acid increases the potency of depigmenting agents for mine.There have been no studies on what other effects the treatment of melasma, actinic lentigines, and postin- these amides have on melanocytes, apart from their strong flammatory hypermelanosis. There are several possible mechanisms underlying these effects. All-trans-retinoic acid Melanin content of the cells was significantly decreased inhibits melanin synthesis through down-regulation of by C(2)-ceramide. The tyrosinase activity of cell extracts was tyrosinase and tyrosinase-related protein 1 expression in reduced by C(2)-ceramide treatment. In the cell-free system, melanocytes. All-trans-retinoic acid could also act as a however, C(2)-ceramide could not suppress tyrosinase, selective melanocytotoxin in relatively high doses. In whereas kojic acid directly inhibited tyrosinase. These addition, RA increases keratinocyte turnover and augments results suggest that C(2)-ceramide decreases the pigmenta- melanin loss from the epidermis. The inhibition of glutathione tion of melanocytes indirectly by regulating tyrosinase.
S-transferase by RA explains its synergistic depigmenting Furthermore, C(2)-ceramide decreased the protein expres- action with other melanocytotoxins such as hydroquinone.
sion of microphthalmia-associated transcription factor, Topical retinoids could irritate the skin causing redness, dryness, swelling, desquamation, and subjective feelings Zinc α-2-glycoprotein inhibits melanin production by B16 melanoma cells via posttranscriptional effects on A pomegranate extract (PE) from the rind containing 90% tyrosinase protein. Because zinc α-2-glycoprotein is nor- ellagic acid showed inhibitory activity against mushroom mally produced by epidermal keratinocytes, these studies tyrosinase in vitro, and the inhibition by the extract was raise the possibility that epidermal-derived zinc α-2- comparable with that of arbutin. Orally taken PE also glycoprotein may play a part in normal regulation of melanin inhibited UV-induced skin pigmentation on the back of production in vivo.It is interesting to note that endogenous brownish guinea pigs. The intensity of the skin-whitening substances might be a potential candidate in a cosmeceutical.
effect was similar between guinea pigs fed with PE and thosefed with L-ascorbic acid. Pomegranate extract reduced thenumber of DOPA-positive melanocytes in the epidermis ofUV-irradiated guinea pigs, but L-ascorbic acid did not. These results suggest that the skin-whitening effect of PE wasprobably due to inhibition of the proliferation of melanocytes The stratum corneum is composed mainly of lipids, and melanin synthesis by tyrosinase. Further clinical studies proteins, enzymes, and water. The extracellular lipid are needed to test its efficacy and safety membrane of the stratum corneum is composed mainly of Glabridin was extracted from licorice. It could inhibit ceramides and its derivatives (40%), cholesterol (25%), and tyrosinase activity of melanocytes without cytotoxicity, and free fatty acids (10%-15%), followed by smaller amounts of it also inhibited UV-B–induced pigmentation and erythema triglycerides, stearyl esters, and cholesterol sulfate. These by topical application in a 0.5% There are lipids are synthesized throughout the epidermis where they also more potent ingredients extracted from licorice that may are packaged in lamellar granules and subsequently undergo become potential depigmenting agents. They include differentiation and constitute the water barrier. Many factors glabrene, isoliquiritigenin, glycyrrhisoflavone, and glyas- could disturb their synthesis pathway, such as essential fatty perin; all of them could inhibit tyrosinase activity with acid deficiency, enzyme inhibitors, defective enzymes, enzyme deficiency, environmental constituents, topically applied agents, or water content of the stratum corneum.
petrolatum did not show any significant effect, though High amounts of cholesteryl sulfate, the intercellular cement, nicotinamide and white petrolatum increased stratum have been shown to inhibit desquamation. Cornified cell corneum hydration.Another study showed that a niacina- envelope, a structure synthesized at late stages of keratino- mide-containing facial moisturizer improved the stratum cyte differentiation, is composed of structural proteins, corneum barrier and, thus, provided a clinical benefit to including involucrin, loricrin, and the small proline-rich proteins. The stratum corneum possesses approximately 30% In xerotic skin, the proteolysis of desmosomes is reduced, water, which is mainly associated with its elasticity. A leading to the accumulation of corneocytes on the surface of healthy stratum corneum contains about 10% tightly held the skin. Soap-induced xerosis could be ameliorated by the water. The tightly bound water is closely dependent on the topical application of exogenous protease, such as bovine presence of natural moisturizing factor. Natural moisturizing pancreatic chymotrypsin, papain, and a bacterial protease factor is composed of amino acids and their metabolites, from Bacillus licheniformis. Alcalase and optimase, both which are byproducts formed from the breakdown of broad specificity alkaline bacterial proteases, were the most filaggrin. Natural moisturizing factor is found exclusively efficient ones. Morphological and immunologic analysis of inside the cells.Perturbation of the aforementioned bacterial enzyme-treated skin revealed that topically applied composites in stratum corneum might cause functional protease specifically induced the degradation of the desmo- defect and clinical symptoms. Dry skin is one of the common problems due to defective stratum corneum. It is acondition featured by some subjective or objective denomi-nators, including sensory characteristics with dry, uncomfor-table, itchy, stinging, and tingling sensation; tactile characteristics with a rough, uneven, and sandlike feeling;and visible characteristics with redness, lackluster surface, Wrinkle is one of the key features of aging skin, including dry, white patches, flaky appearance, cracks, and even photoaging and chronological aging.The exact pathogen- fissures.In addition, several skin diseases are also esis of wrinkle is not fully understood yet. Changes in the featured by dry skin, including atopic dermatitis, ichthyosis, dermis are most prominent in aged skin. Aged dermis has and the like. Moisturizers are agents designed to repair the fragmented elastic fibers, decreased collagen, and dispropor- damaged stratum corneum to make the stratum corneum tionate types I and III collagens. At the bottom of a wrinkle, softer and more pliant by increasing its hydration, resulting type IV collagen is decreased. Glycosaminoglycans, espe- in smooth, more supple, and healthier looking skin. More- cially hyaluronic acid, are decreased. Collagen damage is over, moisturizers are also designed to act as adjuvant attributed to several types of collagen-degrading enzymes treatment option for some dermatologic diseases with feature known as matrix metalloproteinases (MMPs). Metallopro- of dry skin. From the view of safety, therapeutic moisturizers teinases activation can result in production of collagenase, should be noncomedogenic, devoid of irritant ingredients, gelatinase, and stromelysin. The degradation of elastins and compatible with many other therapeutic regimens.
A formulation of lactic acid 12% neutralized with Paeoniflorin (PF), partially purified from roots of Paeo- ammonium hydroxide and pramoxine hydrochloride 1% nia lactiflora, protected cells from DNA damage induced by was tested on dry itchy skin for 7 days. Patients had UV-B irradiation in cultured normal human keratinocytes statistically significant improvement in skin surface hydra- and hairless mouse keratinocytes. It was also revealed that tion by day 3, with further improvement by day 7, as 0.5% PF-containing formulation reduced facial wrinkles during an 8-week clinical trial. These results suggest that Pantothenic acid, a component of coenzyme A, serves as a the partially purified PF has potent antiaging and anti- cofactor for a variety of enzyme-catalyzed reactions that are wrinkle activities, and should be a useful ingredient for important in the metabolism of carbohydrates, fatty acids, proteins, sterols, steroid hormones, and porphyrins. The It was found that Morinda citrifolia fruit extract up- topical use of dexpanthenol, the stable alcoholic analog of regulated biosynthesis of type I collagen and glycosamino- pantothenic acid, improved stratum corneum hydration, glycans in primary cultures of normal human fibroblasts. 1,4- reduced transepidermal water loss, and maintained skin Dihydroxy-2-methoxy-7-methylanthraquinone, an active ingredient with a type I collagen–stimulating effect, was A ceramide-dominant physiologic lipid-based emollient isolated and identified from M. citrifolia fruit. It was showed satisfactory results in the treatment of childhood revealed that anthraquinone showed significantly increased atopic dermatitis, which is featured by dry skin.A elaboration of type I procollagen C-terminal peptide and nicotinamide cream containing 2% nicotinamide was tested glycosaminoglycans, and reduced expression of the collage- on atopic dry skin over 4 or 8 weeks; white petrolatum was nase MMP-1 dose dependently in human dermal fibroblasts.
used as control. The results showed that nicotinamide Furthermore, a nanoemulsion containing anthraquinone significantly decreased transepidermal water loss, but white predominantly increased the dermal type I procollagen in Efficacy and safety of innovative cosmeceuticals nude mouse skin. These results suggest that anthraquinone There are 2 distinct types of aging. One is intrinsic aging, derived from M. citrifolia fruit extract is a good candidate for which is the natural aging process. The other is extrinsic aging, which is caused by environmental factors such as The inner shell of the chestnut has been used as an repetitive facial expressions, gravity, sleeping positions, antiwrinkle or skin-firming agent in East Asia. A 70% smoking, and, above all, exposure to the sunlight. The ethanol extract from this plant can prevent cell detachment of commonly seen features of intrinsic aging are fine wrinkles, skin fibroblasts from culture plates, possibly through thin and transparent skin, hollowed cheeks and eye sockets, enhancing the expression of the cell-associated fibronectin loss of firmness on the hands and neck, sagging, dry skin that and vitronectin. Scoparone (6,7-dimethoxycoumarin), iso- may itch, inability to sweat sufficiently, graying hair that lated from the extract of inner shell of the chestnut, possessed eventually turns white, and hair loss. Extrinsic factors, similar properties. These findings underline the usefulness of especially sun exposure, often act together with the normal these substances as antiwrinkle/skin-firming agents.
aging process to cause skin aging prematurely. Photoaging is Dimethylaminoethanol (DMAE) is an analog of the B the term especially reserved to describe extrinsic aging vitamin choline and is a precursor of acetylcholine. In a caused by sun exposure. Photoaging is often featured by age randomized clinical study, 3% DMAE facial gel applied spots, spider veins on the face, rough and leathery skin, fine daily for 16 weeks has been shown to be safe and efficacious wrinkles that disappear when stretched, loose skin, a blotchy in the mitigation of forehead lines and periorbital fine complexion, solar elastosis, actinic keratoses, and skin wrinkles, and in improving lip shape and fullness and the cancer. In photoaged skin, the epidermis has thinning of overall appearance of aging skin. Application was well stratum spinosum and flattening of the dermoepidermal tolerated; an open-label extension of the trial showed that the junction. Decrease in the numbers of melanocytes and long-term application of DMAE gel for up to 1 year was dysregulation of melanocyte density result in guttate hypo- associated with a good safety profile. The benefits of DMAE or hypermelanosis and a blotchy complexion. The number of may include a potential anti-inflammatory effect and an Langerhans cells also decreases, and the cells have less increase in skin firmness with possible improvement in dendrites. There are thickened, tangled, and degraded nonfunctional fibers in the The interaction between Ubiquinone (coenzyme 10) is present in almost all collagen fibers and fibroblast is also decreased.In an living cells, excluding some bacteria and fungi. It is a experimental study, chronic UV-A irradiation of normal strong antioxidant in cells. Ubiquinone can suppress UV- human fibroblasts induced shortening of the cellular life span A–induced production of collagenase in fibroblasts and, and an increase of cellular diameter; MMP-1 was over- thus, protect from the UV-A–induced degradation of collagen. It can also retard loss of hyaluronic acid, increase Photoaged skin has variable manifestations produced by levels of glycosaminoglycan, and slowdown cell division.
changes of different cellular or noncellular components of Ubiquinone can penetrate into the viable layers of the the skin and caused by different mechanisms. It is difficult to epidermis. Topical use of ubiquinone could reduce the invent a cosmeceutical with multifunctions to meet all the needs. Some of the aforementioned cosmeceuticals, such asdepigmenting, moisturizing, and antiwrinkle cosmeceuticals,have the potency to relieve part of photoaging signs. Thefollowing describes some agents that might be of potential Sunscreens and antiphotoaging cosmeceuticals Sesamol is a highly acclaimed antioxidant. An experiment Exposure of skin to UV irradiation can cause acute on mouse skin showed that it has a good effect on prevention inflammatory changes, such as erythema, edema, and subse- of photodamage, observed on biochemical and histopatho- quently pigmentation or tanning, and chronic changes, such as photoaging, immunosuppression, or photocarcinogenesis.
Several topically applied retinoids, such as tretinoin, Sunscreens are intended to counteract these detrimental effects isotretinoin, retinaldehyde, and tazarotene, have been proven of UV through direct blocking of light or by absorbing UV clinically and histologically effective for treating the radiation. Many substances are commonly used in cosmetics, appearance of photoaging. Adverse effects are also docu- such as para-aminobenzoic acid derivatives, cinnamates, mented as irritant reaction of variable intensity presenting salicylates, octocrylene, and ensulizole as UV-B filter, and with dryness, scaling, and Alitretinoin (9-cis- benzophenones, butyl methoxydibenzoyl, and meradimate as retinoic acid) is a naturally occurring endogenous retinoid. It UV-A filter. Still, many other ingredients from different has the ability to bind and activate all known intracellular sources are tested as candidates in a cosmeceutical, including retinoic acid receptors, which might promote the repair calcitriol, caffeic acid, polyphenols compound, isoflavones, mechanisms in damaged skin. A small-scale clinical trial and so on, as excellently reviewed by Kullavanijaya and showed that topical alitretinoin gel 0.1% was well tolerated LimThe common adverse effects of sunscreens are irritant by participants and showed improvement of benign skin or allergic dermatitis and comedogenicity.
lesions (eg, seborrheic keratoses) and precancerous lesions (eg, actinic keratoses).Large, blinded, controlled trials are ascorbate (lipid soluble) in an anhydrous polysilicone gel needed to investigate the role of this novel retinoid in the base was tested to one half of the face and the inactive polysilicone gel base to the opposite side. The effects were Genistein is a soybean isoflavone with diverse biologic evaluated clinically and histologically. A statistically activities. It substantially inhibits skin carcinogenesis and significant improvement of the vitamin C–treated side cutaneous aging induced by UV light in mice and photo- was seen in the decreased photoaging scores of the cheeks damage in humans. The mechanisms of action involve and the perioral area. Biopsies showed increased Grenz protection of oxidatively and photodynamically damaged zone collagen, as well as increased staining for messenger DNA, down-regulation of UV-B–activated signal transduc- RNA for type I collagen. No patients were found to have tion cascades, and antioxidant Clinical trials are any evidence of irritation and inflammation during the required to further substantiate its clinical applications.
A newly formulated vitamin C complex having 10% Green tea polyphenol inhibits the activity of collagenase ascorbic acid (water soluble) and 7% tetrahexyldecyl and increases collagen biosynthesis rate of human fibroblasts.
Examples of some cosmeceutical ingredients (in alphabetical order) Fruit acids (glycolic acid, lactic acid,citric acid, titanic acid, pyruvic acid,maleic acid, etc) Skin conditioning, increasing collagen production, Smoothening, moisturizing, and protection Linoleic, linolenic, and arachidonic acids Antioxidants, smoothing, rejuvenation of skin Supporting blood circulation, wound healing, Skin whitening, antioxidant, antimicrobial, Antioxidant, improving texture and integrity of skin Smoothing, promoting cell renewal, and improving compounds with similar mechanismsof action Efficacy and safety of innovative cosmeceuticals It can also inhibit tyrosinase activity. It was interesting to note 2. Dureja H, Kaushik D, Gupta M, et al. Cosmeceutical: an emerging that after irradiation at 40 kGy by γ-ray, the abovementioned concept. Indian J Pharmacol 2005;37:155-9.
3. Lee ES, Kim JH, Sungbin IM, et al. Application of computerized image effects were all Green tea polyphenol or green analysis in pigmentary skin diseases. Int J Dermatol 2001;40:45-9.
tea could protect UV-induced DNA damage in a variety of 4. Yoshimura K, Sato K, Aiba-Kojima E, et al. Repeated treatment cell types, including skin fibroblasts and keratinocytes. When protocols for melasma and acquired dermal melanocytosis. Dermatol green tea was taken orally, it also showed photoprotective effects manifested as low DNA damage of peripheral blood 5. Boissy RE, Visscher M, DeLong MA. DeoxyArbutin: a novel reversible tyrosinase inhibitor with effective in vivo skin lightening potency. Exp Orally taken green tea or green tea polyphenols have mild adverse effects, such as excess gas, upset stomach, 6. Chakraborty AK, Funasaka Y, Komoto M, et al. Effect of arbutin on nausea, heartburn, abdominal pain, dizziness, headache, and melanogenic proteins in human melanocytes. Pigment Cell Res 1998; muscle pain.Though it looks likely that green tea might be a suitable candidate for antiaging, so far, there have been no 7. Maeda K, Fukuda M. Arbutin: mechanism of its depigmenting action in human melanocyte culture. J Pharmacol Exp Ther 1996;276:765-9.
convincing reports on the evaluation of topical use of green 8. Nakamura K, Yoshida M, Uchiwa H. Down-regulation of melanin tea or its derivatives on skin. It should be kept in mind that synthesis by a biphenyl derivative and its mechanism. Pigment Cell Res green tea polyphenols are highly unstable and easily oxidized in ambient environment. Formulary of green tea polyphenols 9. Usuki A, Ohashi A, Sato H, et al. The inhibitory effect of glycolic acid as active ingredients in topicals, therefore, remains a and lactic acid on melanin synthesis in melanoma cells. Exp Dermatol2003;12(Suppl 2):43-50.
challenge in the cosmeceutical industries.
10. Galcia A, Fulton JE. The combination of glycolic acid and N-Furfuryladenine is a cytokinin growth factor that can hydroquinone or kojic acid for the treatment of melasma and related be obtained from a variety of sources, such as plants, parts conditions. Dermatol Surg 1996;22:443-7.
of animals, and even human In the presence of 11. Moon KY, Ahn KS, Lee J, et al. Kojic acid, a potential inhibitor of NF- calcium, it could promote differentiation of human kappaB activation in transfectant human HaCaT and SCC-13 cells.
Arch Pharm Res 2001;24:307-11.
keratinocytes.It could also inhibit oxidative and glycox- 12. Nohynek GJ, Kirkland D, Marzin D, et al. An assessment of the idative protein damage in vitro, and Fenton reaction– genotoxicity and human health risk of topical use of kojic acid [5- mediated oxidative damage to DNA.Cosmetic pro- hydroxy-2-(hydroxymethyl)-4H-pyran-4-one]. Food Chem Toxicol ducts containing N(6)-F-furfuryladenine have been devel- oped and marketed for a couple of years. A randomized, 13. Wan HM, Chen CC, Chang TS, et al. Combining induced mutation and protoplasting for strain improvement of Aspergillus oryzae for kojic blinded, and controlled clinical trial is needed to evaluate its acid production. Biotechnol Lett 2004;26:1163-6.
14. Kim DH, Hwang JS, Baek HS, et al. Development of 5-[(3- aminopropyl)phosphinooxy]-2-(hydroxymethyl)-4H-pyran-4-one as anovel whitening agent. Chem Pharm Bull (Tokyo) 2003;51:113-6.
15. Balina LM, Graupe K. The treatment of melasma. 20% azelaic acid versus 4% hydroquinone cream. Int J Dermatol 1991;30:893-5.
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The essence of innovative cosmeceuticals is their 17. Ortonne JP. Retinoid therapy of pigmentary disorders. Dermatol Ther functional active ingredients. Hundreds of substances have been screened, synthesized, and tested (as exampled in 18. Gao XH, Chen HD, Kligman AM. Topical tretinoin for photoaging: the and many have been included in commercially China experience. J Appl Cosmetol 1997;15:77-82.
available products, for example, chamomile and soy. Prudent 19. Yoshimura M, Watanabe Y, Kasai K, et al. Inhibitory effect of an ellagic acid–rich pomegranate extract on tyrosinase activity and measures should be taken on clinical trials of cosmeceuticals ultraviolet-induced pigmentation. Biosci Biotechnol Biochem 2005; because the interaction between skin and cosmeceuticals could be influenced by environmental factors as temperature, 20. Yokota T, Nishio H, Kubota Y. The inhibitory effect of glabridin from humidity, pollution, microbial, light, and so on. In addition, licorice extracts on melanogenesis and inflammation. Pigment Cell Res the desired functions of a cosmeceutical might require a 21. Nerya O, Vaya J, Musa R, et al. Glabrene and isoliquiritigenin as coordinating action of multiple ingredients. Moreover, there tyrosinase inhibitors from licorice roots. J Agric Food Chem 2003;51: are problematic skin conditions that might change the interactive pattern and outcome between cosmeceuticals 22. Kim HJ, Seo SH, Lee BG, et al. Identification of tyrosinase inhibitors and skin. Scientific clinical evaluation is a must for research, from Glycyrrhiza uralensis. Planta Med 2005;71:785-7.
development, and application of cosmeceuticals.
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