Luger Thomas A, Brzoska Thomas
Department of Dermatology, University Clinics Münster, Von-Esmarch-Str. 58, D-48149 Münster, Germany.
Ann Rheum Dis. 2007 Nov;66 Suppl 3(Suppl 3):iii52-5. doi: 10.1136/ard.2007.079780.
alpha-Melanocyte-stimulating hormone (alpha-MSH) is a tridecapeptide derived from the proopiomelanocortin by post-translational processing. In addition to its effects on melanocytes, alpha-MSH has potent anti-inflammatory effects when administered systemically or locally. The anti-inflammatory effects of alpha-MSH are mediated by direct effects on cells of the immune system as well as indirectly by affecting the function of resident non-immune cells. alpha-MSH affects several pathways implicated in regulation of inflammatory responses such as NF-kappaB activation, expression of adhesion molecules and chemokine receptors, production of pro-inflammatory cytokines and other mediators. Thus alpha-MSH may modulate inflammatory cell proliferation, activity and migration. The anti-inflammatory effects of alpha-MSH have been confirmed by means of animal models of inflammation such as irritant and allergic contact dermatitis, cutaneous vasculitis, asthma, inflammatory bowel disease, rheumatoid arthritis, ocular and brain inflammation. Most of the anti-inflammatory activities of alpha-MSH can be attributed to its C-terminal tripeptide KPV. K(D)PT, a derivative of KPV corresponding to the amino acid 193-195 of IL-1beta, is currently emerging as another tripeptide with potent anti-inflammatory effects. The anti-inflammatory potential together with the favourable physiochemical properties most likely will allow these agents to be developed for the treatment of inflammatory skin, eye and bowel diseases, allergic asthma and arthritis.
α-黑素细胞刺激素（α-MSH）是一种经翻译后加工从阿黑皮素原衍生而来的十三肽。除了对黑素细胞有作用外，α-MSH全身或局部给药时具有强大的抗炎作用。α-MSH的抗炎作用是通过对免疫系统细胞的直接作用以及通过影响驻留非免疫细胞的功能间接介导的。α-MSH影响与炎症反应调节相关的多种途径，如核因子-κB激活、黏附分子和趋化因子受体的表达、促炎细胞因子和其他介质的产生。因此，α-MSH可能调节炎症细胞的增殖、活性和迁移。α-MSH的抗炎作用已通过炎症动物模型得到证实，如刺激性和过敏性接触性皮炎、皮肤血管炎、哮喘、炎症性肠病、类风湿性关节炎、眼部和脑部炎症。α-MSH的大多数抗炎活性可归因于其C末端三肽KPV。K（D）PT是KPV的衍生物，对应于白细胞介素-1β的193-195位氨基酸，目前正作为另一种具有强大抗炎作用的三肽出现。这些药物的抗炎潜力以及良好的理化性质很可能使其被开发用于治疗炎症性皮肤病、眼病和肠病、过敏性哮喘和关节炎。
