LIPID MAPS

Azelaic acid is a naturally occurring and saturated dicarboxylic acid with diverse biological activities.^1,2,3,4,5 It is a competitive inhibitor of tyrosinase, NADH dehydrogenase, succinic dehydrogenase, and reduced ubiquitinone:cytochrome C oxidoreductase in vitro.^1,2 Azelaic acid inhibits the growth and colony formation of B16 murine as well as HMB2 and SK32 human melanoma cells in a concentration-dependent manner but has no effect on CHO cells.³ It decreases DNA synthesis, induces mitochondrial damage and dilation of the rough endoplasmic reticulum (RER), and reduces growth of mouse keratinocytes in a dose- and time-dependent manner.⁴ Azelaic acid is bacteriostatic against S. epidermidis, S. aureus, S. capitis, P. acnes, P. avidum, P. mirabilis, and C. albicans in vitro (MICs = 0.03-0.25 M).⁵ Formulations containing azelaic acid have been used in the treatment of acne and hyperpigmentation disorders.

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References

1. Nazzaro-Porro, M., and Passi, S. Identification of tyrosinase inhibitors in cultures of Pityrosporum. J. Invest. Dermatol. 71(3), 205-208 (1978).

2. Passi, S., Picardo, M., Nazzaro-Porro, M., et al. Antimitochondrial effect of saturated medium chain length (C8-C13) dicarboxylic acids. Biochem. Pharmacol. 33(1), 103-108 (1984).

3. Lemic-Stojcevic, L., Nias, A.H., and Breathnach, A.S. Effect of azelaic acid on melanoma cells in culture. Exp. Dermatol. 4(2), 79-81 (1995).

4. Detmar, M., Mayer-da-Silva, A., Stadler, R., et al. Effects of azelaic acid on proliferation and ultrastructure of mouse keratinocytes in vitro. J. Invest. Dermatol. 93(1), 70-74 (1989).

5. Nguyen, Q.H., and Bui, T.P. Azelaic acid: Pharmacokinetic and pharmacodynamic properties and its therapeutic role in hyperpigmentary disorders and acne. Int. J. Dermatol. 34(2), 75-84 (1995).