Article

Azelaic acid. A review of its pharmacological properties and therapeutic efficacy in acne and hyperpigmentary skin disorders.

Adis Drug Information Services, Auckland, New Zealand.
Drugs (Impact Factor: 4.13). 06/1991; 41(5):780-98. DOI: 10.2165/00003495-199141050-00007
Source: PubMed

ABSTRACT Azelaic acid is a naturally occurring saturated dicarboxylic acid which, on topical application (usually as a 20% cream), has been shown to be effective in the treatment of comedonal acne and inflammatory (papulopustular, nodular and nodulocystic) acne, as well as various cutaneous hyperpigmentary disorders characterised by hyperactive/abnormal melanocyte function, including melasma and, possibly, lentigo maligna. In addition, azelaic acid has an antiproliferative and cytotoxic effect on the human malignant melanocyte, and preliminary findings indicate that it may arrest the progression of cutaneous malignant melanoma. The mechanism of this selective cytotoxic action of azelaic acid is unclear, but may possibly be related to its inhibition of mitochondrial oxidoreductase activity and DNA synthesis. In controlled studies, topical azelaic acid demonstrated comparable anti-acne efficacy to topical tretinoin, benzoyl peroxide, erythromycin and oral tetracycline, while in patients with melasma azelaic acid proved at least as effective as topical hydroquinone. On topical application azelaic acid is well tolerated, with adverse effects apparently limited to a generally mild and transient local cutaneous irritation. Thus, topical azelaic acid, employed either as monotherapy or in combination with other treatments, is likely to prove of value in the management of acne and several hyperpigmentary disorders, most notably melasma.

0 Bookmarks
 · 
172 Views
  • Source
    [Show abstract] [Hide abstract]
    ABSTRACT: Rosacea is a common, chronic cutaneous condition that affects the face. Two topicals and one oral medication are currently approved for the treatment of rosacea, including azelaic acid, metronidazole, and sub-antimicrobial dose of doxycycline. Identification of subtypes can help guide treatment strategies. It is essential for psychosocial implications of rosacea to be considered and conservative management, such as nonpharmacologic routine skin care, must form an important part of the overall care. Recently, new insights into the pathophysiology of rosacea have led to the emergence of etiologically oriented treatments. Ivermectin, an acaricidal agent that has been shown to be effective against rosacea refractory to other therapies, is currently in Phase 3 trials. Brimonidine, which was US FDA approved last year and recently sanctioned by Health Canada, has filled an essential therapeutic void in the targeted treatment of diffuse facial erythema.
    Skin therapy letter 06/2014; 19(3):1-4.
  • Source
    [Show abstract] [Hide abstract]
    ABSTRACT: To develop a new natural whitening agent, we investigated the tyrosinase inhibitory effects of Persicaria tinctoria Flower extracts (PTFE). PTFE showed inhibitory activity on mushroom tyrosinase with the values of . We purified two active compounds from PTFE by LH-20 column chromatography and prep-high performance liquid chromatography (HPLC) and identified as quercetin-3-O-rhamnoside (Q3R) and myricetin-3-O-rhamnoside (M3R) by nuclear magnetic resonance (NMR) and liquid chromatography-mass spectrometry (LC-MS) analysis. Q3R and M3R showed tyrosinase inhibitory activities with the values of and , respectively. These results suggest that PTFE and its active compounds reduced melanin formation by the inhibition of tyrosinase activity. Thus, P. tinctoria flower extracts may be a candidate for cosmetic use.
    Journal of Applied Biological Chemistry 01/2011; 54(1).
  • Source
    [Show abstract] [Hide abstract]
    ABSTRACT: The melanin pigment in human skin is a major defense mechanism against ultraviolet light to the skin, but darken skin color. Tyrosinase is mainly responsible for melanin biosynthesis (melanogenesis) in animals and enzymatic browning (melanosis) in plants. The purpose of this study was to optimize the fermented milk process for the melanin formation inhibition by using Lactobacillus plantarum M23 with tyrosinase inhibitory activity. We used 4-factor-3-level central composite design combining with response surface methodology. Yeast extract concentration (%, ), addition of grape (%, ), incubation temperature (, ) and incubation time (h, ) was used as an independent factor, on the other hand, pH (pH, ), overall palatability (score, ) and tyrosinase inhibitory activity (%, ) was used as a dependant factor. Based on the optimization for the highest tyrosinase inhibitory activity with pH 4.4, the expected data of pH, palatability and tyrosinase inhibitory activity with 14.8 h incubation at by the addition of 0.127% of yeast extract, 2.95% of grape was 4.42, 7.06 and 86.65%, but the real data was 4.35, 6.86 and 84.05%, respectively. Based on the previous results, fermented milk using Lactobacillus plantarum M23 with the tyrosinase inhibitory activity could contribute for the whitening and antiaging of human skin.
    Hangug chugsan sigpum haghoeji = Korean journal for food science of animal resources 01/2012; 32(5). · 0.25 Impact Factor