Won Yen-Kim, Loy Chong-Jin, Randhawa Manpreet, Southall Michael D
Johnson & Johnson Asia Pacific, 51 Science Park Road, #01-01/05 The Aries, Singapore Science Park 2, Singapore, 117586, Singapore,
Arch Dermatol Res. 2014 Jul;306(5):455-65. doi: 10.1007/s00403-014-1439-9. Epub 2014 Jan 9.
Hyperpigmentation disorders are of social and cosmetic concerns to many individuals due to their prevalent locations on highly visible parts of the body. Topical formulation containing hydroquinone is the most widely used remedy for the treatment of hyperpigmentation disorders. However, reports of side effects in long-term usage have raised concerns for its use in cosmetic products. Thus, it is highly desirable to develop a safe and effective alternative to treat hyperpigmentation disorders. The objective of the current study is to investigate the de-pigmenting efficacy of 4-hexyl-1,3-phenylenediol in various in vitro models and in a randomized controlled clinical study. We showed that 4-hexyl-1,3-phenylenediol significantly reduced melanogenesis in primary human melanocytes, murine melanoma cells, and pigmented human epidermal equivalents. It was determined that the reduction in melanogenesis is mediated through inhibition of tyrosinase enzyme activity and protein expression. Further investigation revealed that the inhibition of melanogenesis is reversible and is not associated with cellular toxicity in melanocytes. In addition, significant improvements in key clinical parameters such as overall skin lightening, appearance of spots on the cheeks, overall contrast between spots and surrounding skin, and overall pigmentation size were detected in a double-blinded, randomized controlled clinical study. In conclusion, our findings clearly demonstrated the potency of 4-hexyl-1,3-phenylenediol in modulating skin pigmentation, and it is safe and well tolerated after 12-week topical application.
色素沉着紊乱因其常见于身体暴露部位，给许多人带来了社交和美容方面的困扰。含对苯二酚的外用制剂是治疗色素沉着紊乱最广泛使用的药物。然而，长期使用的副作用报告引发了对其在化妆品中使用的担忧。因此，迫切需要开发一种安全有效的替代方法来治疗色素沉着紊乱。本研究的目的是在各种体外模型和一项随机对照临床研究中，研究4 - 己基 - 1,3 - 苯二酚的脱色效果。我们发现，4 - 己基 - 1,3 - 苯二酚能显著降低原代人黑素细胞、鼠黑色素瘤细胞和有色素的人表皮替代物中的黑色素生成。确定黑色素生成的减少是通过抑制酪氨酸酶的活性和蛋白表达介导的。进一步研究表明，黑色素生成的抑制是可逆的，且与黑素细胞的细胞毒性无关。此外，在一项双盲、随机对照临床研究中，检测到关键临床参数有显著改善，如整体皮肤提亮、脸颊斑点外观、斑点与周围皮肤的整体对比度以及整体色素沉着面积。总之，我们的研究结果清楚地证明了4 - 己基 - 1,3 - 苯二酚在调节皮肤色素沉着方面的效力，并且在12周局部应用后安全且耐受性良好。
