Azelaic acid: A review of its pharmacological properties and therapeutic efficacy in acne and hyperpigmentory skin disorders

Adis Drug Information Services, Auckland, New Zealand.
Drugs (Impact Factor: 4.13). 06/1991; 41(5):780-98.
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.

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    • "Tyrosinase 저해물질로 알려진 것에는 ascorbic acid, kojic acid(Lee et al., 2006), hydroquinone(Fitton and Goa, 1991; Parvez et al., 2006), benzoic acid, retinoid, arbutin(Maeda and Fukuda, 1996) 등이 있는데, 특히 kojic acid와 arbutin *Corresponding author: Sang-Dong Lim, Korea Food Research Institute, Seongnam 463-746, Korea. Tel: 82-31-780-9082, Fax: 82-31-780-9160, E-mail: "
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    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 10/2012; 32(5). DOI:10.5851/kosfa.2012.32.5.678
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    • "따라서, tyrosinase 저해활성 실험은 미백물질 screening 단계에서 필수적이다[Lee 등, 1999]. Tyrosinase 저해물질로 알 려진 것에는 ascorbic acid, kojic acid [Lee 등, 2006], hydroquinone [Fitton 등, 1991; Parvez 등, 2006], benzoic acid, retinoids, arbutin [Maeda와 Fukuda, 1996] 등이 있는데, 특히 kojic acid와 arbutin은 강한 미백효과를 가지고 있으나 제 품 안전성 및 경제성 등의 문제로 사용에 어려움이 있다 [Imokawa와 Mishima, 1982; Ando 등, 1993; Masuda 등, 1996]. "
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    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 03/2011; 54(1). DOI:10.3839/jabc.2011.008
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    • "Recently, attention has returned to other potential lipid-based SAR signals. The dicarboxylic fatty acid azelaic acid (1,7-heptane dicarboxylic acid) is a natural product that until recently was best known as an ingredient in topical treatments for acne (Fitton and Goa, 1991). Azelaic acid shows increased accumulation in Arabidopsis plants following an HR and is phloem-mobile (Jung et al., 2009). "
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    ABSTRACT: Induced mechanisms are by definition imperceptible or less active in uninfected, unstressed, or untreated plants, but can be activated by pathogen infection, stress, or chemical treatment to inhibit the replication and movement of virus in the host. In contrast, defenses that are pre-existing or serve to limit virus propagation and spread in otherwise susceptible hosts are considered to be "basal" in nature. Both forms of resistance can be genetically determined. Most recessive resistance genes that control resistance to viruses appear not to depend upon inducible mechanisms but rather maintain basal resistance by producing nonfunctional variants of factors, specifically translation initiation factors, required by the virus for successful exploitation of the host cell protein synthetic machinery. In contrast, most dominant resistance genes condition the induction of broad-scale changes in plant biochemistry and physiology that are activated and regulated by various signal transduction pathways, particularly those regulated by salicylic acid, jasmonic acid, and ethylene. These induced changes include localized plant cell death (associated with the hypersensitive response, HR) and the upregulation of resistance against many types of pathogen throughout the plant (systemic acquired resistance, SAR). Unfortunately, it is still poorly understood how virus infection is inhibited and restricted during the HR and in plants exhibiting SAR. Resistance to viruses is not always genetically predetermined and can be highly adaptive in nature. This is exemplified by resistance based on RNA silencing, which appears to play roles in both induced and basal resistance to viruses. To counter inducible resistance mechanisms, viruses have acquired counter-defense factors to subvert RNA silencing. Some of these factors may affect signal transduction pathways controlled by salicylic acid and jasmonic acid. In this chapter, we review current knowledge of defensive signaling in resistance to viruses including the nature and roles of low molecular weight, proteinaceous, and small RNA components of defensive signaling. We discuss the differences and similarities of defenses and defensive signaling directed against viral versus nonviral pathogens, the potential role of RNA silencing as an effector in resistance and possible regulator of defensive signaling, crosstalk and overlap between antiviral systems, and interference with and manipulation of host defensive systems by the viruses themselves.
    Advances in Virus Research 01/2010; 76:57-121. DOI:10.1016/S0065-3527(10)76003-6
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