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一种局部亲脂性烟酸衍生物可增加光损伤皮肤中的烟酰胺腺嘌呤二核苷酸(NAD)、促进表皮分化并增强屏障功能。

A topical lipophilic niacin derivative increases NAD, epidermal differentiation and barrier function in photodamaged skin.

作者信息

Jacobson Elaine L, Kim Hyuntae, Kim Moonsun, Williams Joshua D, Coyle Donna L, Coyle W Russell, Grove Gary, Rizer Ronald L, Stratton M Suzanne, Jacobson Myron K

机构信息

Department of Pharmacology and Toxicology, College of Pharmacy, Tucson, AZ 85724, USA.

出版信息

Exp Dermatol. 2007 Jun;16(6):490-9. doi: 10.1111/j.1600-0625.2007.00553.x.

Abstract

The effects of myristyl nicotinate (MN), a nicotinic acid derivative designed to deliver nicotinic acid to skin without vasodilatation, on subjects with photodamaged skin have been studied. MN increased skin cell nicotinamide adenine dinucleotide (NAD) by 25% (P = 0.001) demonstrating effective delivery of nicotinic acid to skin. Relative to placebo, MN treatment of photodamaged facial skin increased stratum corneum thickness by approximately 70% (P = 0.0001) and increased epidermal thickness by approximately 20% (P = 0.001). In two separate studies, MN treatment increased rates of epidermal renewal by 6% (P = 0.003) to 11% (P = 0.001) and increased the minimal erythemal dose by 8.9 (P = 0.07) and 10% (P = 0.05) relative to placebo. MN treatment resulted in reductions in the rates of transepidermal water loss (TEWL) of approximately 20% relative to placebo on cheeks (P = 0.012) and arms (P = 0.017) of study subjects. Results of a tape stripping challenge before and after MN treatment demonstrated a significant correlation (P = 0.03) between increased skin NAD content and resistance to changes in TEWL for MN treated but not placebo subjects. Rates of TEWL changed more rapidly and to a greater extent in atopic subjects compared with normal subjects. The results indicate that MN enhances epidermal differentiation and barrier function in skin, suggesting that this method of nicotinic acid delivery may prove useful in limiting progression of actinic skin damage and possibly in treating other conditions involving skin barrier impairment.

摘要

已对肉豆蔻酰烟酸(MN)这种旨在将烟酸输送至皮肤而不引起血管扩张的烟酸衍生物对光损伤皮肤受试者的影响进行了研究。MN使皮肤细胞烟酰胺腺嘌呤二核苷酸(NAD)增加了25%(P = 0.001),表明烟酸能有效输送至皮肤。相对于安慰剂,MN治疗光损伤面部皮肤使角质层厚度增加了约70%(P = 0.0001),使表皮厚度增加了约20%(P = 0.001)。在两项独立研究中,相对于安慰剂,MN治疗使表皮更新率提高了6%(P = 0.003)至11%(P = 0.001),并使最小红斑剂量增加了8.9(P = 0.07)和10%(P = 0.05)。MN治疗使研究对象脸颊(P = 0.012)和手臂(P = 0.017)的经表皮水分流失(TEWL)率相对于安慰剂降低了约20%。MN治疗前后胶带剥离试验的结果表明,MN治疗组而非安慰剂组皮肤NAD含量增加与TEWL变化抗性之间存在显著相关性(P = 0.03)。与正常受试者相比,特应性受试者的TEWL率变化更快且程度更大。结果表明,MN可增强皮肤的表皮分化和屏障功能,这表明这种烟酸输送方法可能有助于限制光化性皮肤损伤的进展,并可能用于治疗其他涉及皮肤屏障受损的病症。

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