PDF(Pubmed)
Abstract：
Metabolites resulting from the bacterial fermentation of dietary fibers, such as short-chain fatty acids, especially butyrate, play important roles in maintaining gut health and regulating various biological effects in the skin. However, butyrate is underutilized due to its unpleasant odor. To circumvent this organoleptic unfavorable property, phenylalanine butyramide (PBA), a butyrate precursor, has been synthesized and is currently available on the market. We evaluated the inhibition of mushroom tyrosinase by butyrate and PBA through in vitro assays, finding IC50 values of 34.7 mM and 120.3 mM, respectively. Docking calculations using a homology model of human tyrosinase identified a putative binding mode of PBA into the catalytic site. The anti-aging and anti-spot efficacy of topical PBA was evaluated in a randomized, double-blind, parallel-arm, placebo-controlled clinical trial involving 43 women affected by photo-damage. The results of this study showed that PBA significantly improved skin conditions compared to the placebo and was well tolerated. Specifically, PBA demonstrated strong skin depigmenting activity on both UV and brown spots (UV: -12.7% and -9.9%, Bs: -20.8% and -17.7% after 15 and 30 days, respectively, p < 0.001). Moreover, PBA brightened and lightened the skin (ITA°: +12% and 13% after 15 and 30 days, respectively, p < 0.001). Finally, PBA significantly improved skin elasticity (Ua/Uf: +12.4% and +32.3% after 15 and 30 days, respectively, p < 0.001) and firmness (Uf: -3.2% and -14.9% after 15 and 30 days, respectively, p < 0.01).
摘要：
由膳食纤维的细菌发酵产生的代谢物，比如短链脂肪酸，尤其是丁酸,在维持肠道健康和调节皮肤各种生物学效应方面发挥重要作用。然而,丁酸盐由于其令人不快的气味而未得到充分利用。为了规避这种感官上的不利特性，苯丙氨酸丁酰胺（PBA），丁酸前体，已经合成，目前市场上有售。我们通过体外试验评估了丁酸盐和PBA对蘑菇酪氨酸酶的抑制作用，发现IC50值为34.7mM和120.3mM，分别。使用人酪氨酸酶同源模型的对接计算鉴定了PBA进入催化位点的推定结合模式。局部用PBA的抗衰老和抗斑疗效进行了随机评估，双盲,平行臂,安慰剂对照临床试验，涉及43名受光损伤影响的女性。这项研究的结果表明，与安慰剂相比，PBA显着改善了皮肤状况，并且耐受性良好。具体来说,PBA对紫外线和棕色斑点均表现出强烈的皮肤脱色活性（紫外线：-12.7％和-9.9％，Bs：15天和30天后-20.8%和-17.7%，分别,p<0.001)。此外，PBA提亮和减轻皮肤（ITA°：15和30天后+12％和13％，分别,p<0.001)。最后,PBA显著改善皮肤弹性（Ua/Uf：15天和30天后+12.4%和+32.3%，分别,p<0.001）和硬度（Uf：15天和30天后-3.2％和-14.9％，分别,p<0.01)。
