Abstract:
To investigate the effect of retinoids, such as retinol (ROL), retinal (RAL), and retinyl palmitate (RP), on epidermal integrity, skin deposition, and bioconversion to retinoic acid (RA). 3-D human skin equivalent model (EpiDermFT™) was used. Epidermal cellular integrity measured by TEER values was significantly higher for a topical treatment of ROL and RAL than RP (p < 0.05). The skin deposition (μM) of ROL and RAL was approximately 269.54 ± 73.94 and 211.35 ± 20.96, respectively, greater than that of RP (63.70 ± 37.97) over 2 h incubation. Spectral changes were revealed that the CO maximum absorbance occurred between 1600∼1800 cm-1 and was greater from ROL than that from RAL and RP, indicating conjugation of R-OH to R-CHO or R-COOH could strongly occur after ROL treatment. Subsequently, a metabolite from the bioconversion of ROL and RAL was identified as RA, which has a product ion of m/z 283.06, by using liquid a chromatography-mass spectrometry (LC-MS) - total ion chromatogram (TIC). The amount of bioconversion from ROL and RAL to RA in artificial skin was 0.68 ± 0.13 and 0.70 ± 0.10 μM at 2 h and 0.60 ± 0.04 and 0.57 ± 0.06 μM at 24 h, respectively. RA was not detected in the skin and the receiver compartment after RP treatment. ROL could be a useful dermatological ingredient to maintain epidermal integrity more effectively, more stably deposit on the skin, and more steadily metabolize to RA than other retinoids such as RAL and RP.
摘要:
为了研究类维生素A的作用,如视黄醇(ROL),视网膜(RAL),和棕榈酸视黄酯(RP),关于表皮完整性,皮肤沉积,和生物转化为视黄酸(RA)。使用3-D人皮肤等效模型(EpidermFT™)。通过TEER值测量的表皮细胞完整性对于ROL和RAL的局部治疗显著高于RP(p<0.05)。ROL和RAL的皮肤沉积(μM)分别约为269.54±73.94和211.35±20.96,大于RP(63.70±37.97)超过2小时孵育。光谱变化表明,C=O最大吸光度发生在1600~1800cm-1之间,ROL大于RAL和RP,表明R-OH与R-CHO或R-COOH的缀合可在ROL处理后强烈发生。随后,来自ROL和RAL生物转化的代谢物被鉴定为RA,通过使用液相色谱-质谱(LC-MS)-总离子色谱(TIC),其具有m/z283.06的产物离子。人造皮肤中从ROL和RAL到RA的生物转化量在2小时时为0.68±0.13和0.70±0.10μM,在24小时时为0.60±0.04和0.57±0.06μM,分别。RP治疗后,皮肤和接收器隔室中未检测到RA。ROL可能是一种有用的皮肤病学成分,可以更有效地保持表皮的完整性,更稳定地沉积在皮肤上,并且比其他类维生素A如RAL和RP更稳定地代谢为RA。