30 AESTHETIC DERMATOLOGY JUNE 2009 • SKIN & ALLERGY NEWS

COSMECEUTICAL CRITIQUE
Rosmarinic Acid
osmarinic acid (alpha-o-caffeoyl- istration (60% for topical administra- their bioactive constituents and proper- tration-dependent fashion, and that pro-

R 3,4-dihydroxyphenyl lactic acid) tion), with a longer lag time associated ties, as well as the distribution and levels tein kinase A was involved in and medi-
is a naturally occurring hydrox- with percutaneous administration, sug- of antioxidants. They found a strong ated the melanogenesis spurred by ros-
ylated compound and analogue of caf- gesting that rosmarinic acid is well ab- correlation between antioxidant activity marinic acid (Biochem. Pharmacol.
feic acid (3,4-dihydroxycinnamic acid). sorbed from the gastrointestinal tract as and total phenol content, with all rose- 2007;74:960-8).
Caffeic acid, which is one of the main well as the skin. mary extracts displaying significant rad- Early in 2009, Sánchez-Campillo et al.
hydroxycinnamic acids (a ma- The investigators conclud- ical scavenging activity. performed in vitro and in vivo experi-
jor class of phenolic com- ed that rosmarinic acid has A methanol extract that contained ments that showed rosmarinic acid acts
pounds), confers antioxidant potential as a therapeutic non- 30% carnosic acid, 16% carnosol, and as an exogenous photoprotective agent
activity, protects human skin steroidal anti-inflammatory 5% rosmarinic acid was substantially by scavenging free radicals. The re-
from ultraviolet C–induced agent (Methods Find. Exp. more effective as an antimicrobial agent searchers also found that rosmarinic acid
erythema, and exhibits con- Clin. Pharmacol. 1989;11:345- against gram-positive bacteria, gram- acts as an endogenous photoprotector by
siderable anticarcinogenic po- 52). negative bacteria, and yeast than was a activating the body’s defense mecha-
tential ( J. Nutr. 2001;131:66- During the ensuing 2 water extract containing 15% ros- nisms through the regulation of tyrosi-
71; Folia Biol. [Praha] 2003; decades, a variety of benefi- marinic acid. nase activity and the initiation of
49:197-202; Int. J. Pharm. cial activities were associated The investigators concluded that the melanin synthesis.
2000;199:39-47; Nutr. Cancer with rosmarinic acid, sug- antimicrobial activity of rosemary ex- In particular, in vivo experiments
1998;32:81-5). B Y L E S L I E S. gesting medical indications. tracts was linked to their phenolic com- showed that UVA-exposed mice orally
Caffeic acid and its deriv- B A U M A N N , M . D . In 2004, Osakabe et al. de- position, and that carnosic acid and ros- treated with rosmarinic acid displayed
atives, such as rosmarinic termined that oral supple- marinic acid are probably the primary only slight dysplasia (in 30% of cases),
acid, carnosol, and carnosic acid—all of mentation with the polyphenol was an antimicrobial components of rosemary whereas UVA-exposed mice fed a control
which manifest antioxidant activity— effective treatment for seasonal allergic (Free Radic. Res. 2006;40:223-31). diet exhibited severe or moderate dys-
are thought to be the key constituents rhinoconjunctivitis, due to inhibition of plasia in all cases (Food Chem. Toxicol.
of rosemary. Caffeic acid also is found the inflammatory response and the scav- Photoprotection 2009;47:386-92).
in coffee, several grains, fruits, and veg- enging of reactive oxygen species ex- Later that year, Psotova et al. examined
etables, including white grapes, olives, hibited by the compound (Biofactors the protective effects of Prunella vulgaris Atopic Dermatitis
spinach, cabbage, and asparagus, as well 2004;21:127-31). and rosmarinic acid, its primary pheno- In 2008, Lee et al. assessed the effects of
as white wine and olive oil (Phytother. lic constituent, against alterations in- rosmarinic acid on mild atopic der-
Res. 2003;17:987-1000; Indian J. Exp. Antitumorigenic Actions duced by UVA exposure in a human ker- matitis in 21 patients (14 females, 7
Biol. 1999;37:124-30). The same year, Osakabe et al. reported atinocyte cell line. For 4 hours, human males) aged 5-28 years. Twice daily, a
Notably, rosmarinic acid is a common on the antitumorigenic ef- 0.3% rosmarinic acid emulsion
component of some fern and hornwort fects of a rosmarinic Rosmarinic acid acts as an exogenous was topically applied to elbow
species, as well as species of the Boragi- acid–rich Perilla frutescens flexures for 8 weeks. Erythema
naceae family and, particularly, the Lami- extract in a two-stage photoprotective agent by scavenging free on the antecubital fossa was
aceae family (Phytochemistry 2003; murine skin cancer model. radicals and as an endogenous photoprotector significantly diminished at 4
62:121-5). The Lamiaceae family includes They noted significant sup- and 8 weeks, and transepider-
common culinary herbs such as basil, pression of tumorigenesis by activating the body’s defense mechanisms. mal water loss from the ante-
lavender, lemon balm, marjoram, as a result of the topical ap- cubital fossa was significantly
oregano, peppermint, perilla, sage, sa- plication of 2 mg/mouse of the extract keratinocytes exposed to UVA (10-30 lower at 8 weeks than at baseline, ac-
vory, thyme, and rosemary. following tumor initiation with 7,12-di- J/cm2) were treated with 1-75 mg/L of cording to local Severity Scoring of
A dimer of caffeic acid, rosmarinic methylbenz[a]anthracene (DMBA). P. vulgaris extract or 0.9-18 mg/L of ros- Atopic Dermatitis index results.
acid is well absorbed through the gas- Tumor promotion was achieved by marinic acid. Xerosis, pruritus, and general symp-
trointestinal tract and the skin, and has the use of 12-tetradecanoylphorbol 13- Both P. vulgaris extract and ros- toms all improved, according to the re-
been shown to augment prostaglandin acetate (TPA). The researchers noted marinic acid mitigated UVA-induced sults of self-administered questionnaires.
E2 production and reduce leukotriene B4 that anti-inflammatory activity 5 hours loss of cell viability and significantly in- The investigators concluded that ros-
production in human polymorphonu- after TPA treatment was equivalent be- hibited the production of free radicals marinic acid warrants consideration as a
clear leukocytes (Indian J. Exp. Biol. tween a perilla extract containing 68% engendered by UVA exposure. DNA therapeutic agent for atopic dermatitis (J.
1999;37:124-30). rosmarinic acid and a commercially avail- damage also was lessened as a result of Dermatol. 2008;35:768-71).
Rosmarinic acid is versatile, and it is able rosmarinic acid. postexposure treatment with both com- Rosmarinic acid can be obtained
used in food preservatives, cosmetics, In addition, TPA-induced increases in pounds. through the diet or as an oral supple-
and medical applications by dint of its an- myeloperoxidase activity, as well as the The investigators, who noted that P. ment pill, and it is used in cosmetic for-
timicrobial, antiviral, antioxidant, anti-in- production of certain chemokines, were vulgaris and rosmarinic acid are used in mulations with numerous other ingre-
flammatory, and immunomodulatory significantly reduced by pretreatment cosmetics, concluded that both botani- dients.
properties (Indian J. Exp. Biol. 1999; with perilla extract or rosmarinic acid, cals exhibit concentration-dependent
37:124-30; Phytochemistry 2003;62:121- as were expression levels of intercellu- photoprotection and have potential as Conclusion
5; J. Agric. Food Chem. 2001;49:5165-70; lar adhesion molecule-1 and vascular supplementary photoprotective agents Rosmarinic acid is a significant polyphe-
J. Dermatol. 2008;35:768-71; Photochem. cell adhesion molecule-1 mRNA. Fur- in dermatologic formulations ( J. Pho- nol with an apparently wide range of
Photobiol. 2006;82:1668-76). thermore, pretreatment with the ex- tochem. Photobiol. B 2006;84:167-74). potential and realized dermatologic ap-
This column will briefly discuss the re- tract or with commercial rosmarinic Also in 2006, investigators topically plications.
search and potential dermatologic ap- acid significantly reduced reactive oxy- applied caffeic acid and its analogues, The direction of current research is
plications of this phenolic compound. gen radical synthesis (of 8-hydroxy-2-de- such as rosmarinic acid, to the abdomens promising, but much more work is still
oxyguanosine) induced by double treat- of live hairless mice, and found that the required to determine how important
Anti-Inflammatory Actions ment of TPA. polyphenols inhibited the production of this antioxidant will be in the derma-
Twenty years ago, rosmarinic acid was The investigators attributed part of reactive oxygen species upon exposure to tologic armamentarium. To date,
identified as a nonsteroidal anti-inflam- the anticarcinogenic activity of P. UVA. They achieved similar results atopic dermatitis may be the indication
matory agent. frutescens to the independent mecha- through oral administration of the for which this herbal ingredient is best
In a 1989 study, researchers intra- nisms associated with rosmarinic acid, polyphenols (Photochem. Photobiol. suited. ■
venously and topically administered the free radical scavenging, and inflamma- 2006;82:1668-76).
antioxidant polyphenol to rats to assess tory response suppression (Carcinogen- In 2007, Lee et al. conducted several DR. BAUMANN is director of cosmetic
how different routes of administration esis 2004;25:549-57). experiments with B16 melanoma cells to dermatology at the University of Miami.
affect absolute bioavailability and relat- identify the effects of rosmarinic acid on To respond to this column, or to suggest
ed tissue distribution. Antimicrobial Actions melanogenesis. They found that the topics for future columns, write to Dr.
They found absolute bioavailability to In 2006, Moreno et al. investigated polyphenol elevated melanin content Baumann at our editorial offices via e-mail
be high for both IV and topical admin- Rosmarinus officinalis extracts to identify and tyrosinase expression in a concen- at sknews@elsevier.com.