Nazzaro-Porro M
Instituto Dermatologico, San Gallicano, Rome, Italy.
J Am Acad Dermatol. 1987 Dec;17(6):1033-41. doi: 10.1016/s0190-9622(87)70294-1.
This review is an update on the literature accumulated over the past 10 years following the original observation that azelaic acid, a naturally occurring and nontoxic C9 dicarboxylic acid, possesses significant biologic properties and a potential as a therapeutic agent. These studies have shown that azelaic acid is a reversible inhibitor of tyrosinase and other oxidoreductases in vitro and that it inhibits mitochondrial respiration. It can also inhibit anaerobic glycolysis. Both in vitro and in vivo it has an antimicrobial effect on both aerobic and anaerobic (Propionibacterium acnes) microorganisms. In tissue culture it exerts a dose- and time-dependent cytotoxic effect on malignant melanocytes, associated with mitochondrial damage and inhibition of deoxyribonucleic acid (DNA) synthesis. Tumoral cell lines not containing tyrosinase are equally affected. Normal cells in culture exposed to the same concentrations of the diacid that are toxic for tumoral cells are in general not damaged. Radioactive azelaic acid has been shown to penetrate tumoral cells at a higher level than normal cells of the corresponding line. Topically applied (a 20% cream), it has been shown to be of therapeutic value in skin disorders of different etiologies. Its beneficial effect on various forms of acne (comedogenic, papulopustular, nodulocystic) has been clearly demonstrated. Particularly important is its action on abnormal melanocytes, which has led to the possibility of obtaining good results on melasma and highly durable therapeutic responses on lentigo maligna. It is also capable of causing regression of cutaneous malignant melanoma, but its role in melanoma therapy remains to be investigated.(ABSTRACT TRUNCATED AT 250 WORDS)
本综述是对过去10年积累的文献的更新，最初的观察发现壬二酸这种天然存在的无毒C9二羧酸具有重要的生物学特性和作为治疗剂的潜力。这些研究表明，壬二酸在体外是酪氨酸酶和其他氧化还原酶的可逆抑制剂，并且它能抑制线粒体呼吸。它还能抑制无氧糖酵解。在体外和体内，它对需氧和厌氧（痤疮丙酸杆菌）微生物均有抗菌作用。在组织培养中，它对恶性黑色素细胞产生剂量和时间依赖性的细胞毒性作用，与线粒体损伤和脱氧核糖核酸（DNA）合成抑制有关。不含酪氨酸酶的肿瘤细胞系也同样受到影响。暴露于对肿瘤细胞有毒的相同浓度二酸的培养正常细胞通常不会受损。放射性壬二酸已被证明比相应细胞系的正常细胞更高水平地穿透肿瘤细胞。局部应用（20%乳膏），已证明它对不同病因的皮肤疾病具有治疗价值。它对各种形式痤疮（粉刺性、丘疹脓疱性、结节囊肿性）的有益作用已得到明确证实。特别重要的是它对异常黑色素细胞的作用，这使得在黄褐斑上取得良好效果以及对恶性雀斑样痣获得高度持久的治疗反应成为可能。它还能够使皮肤恶性黑色素瘤消退，但其在黑色素瘤治疗中的作用仍有待研究。（摘要截断于250字）
