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。
