DeoxyArbutin：一种新型的可逆酪氨酸酶抑制剂，具有有效的体内亮白功效。,Experimental Dermatology

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DeoxyArbutin：一种新型的可逆酪氨酸酶抑制剂，具有有效的体内亮白功效。
Experimental Dermatology ( IF 3.5 ) Pub Date : 2005-07-20 , DOI: 10.1111/j.0906-6705.2005.00337.x
Raymond E Boissy ₁ , Marty Visscher , Mitchell A DeLong

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黑色素细胞中黑色素生成的调节可以使用与底物酪氨酸共有结构同源性的化学物质实现，从而竞争性地抑制酪氨酸酶的催化功能。在此前提下，我们开发了一种新型的酪氨酸酶抑制剂脱氧熊果苷（dA）。脱氧熊果苷在体外可有效抑制蘑菇酪氨酸酶，其Ki值比对苯二酚（HQ）低10倍，比熊果苷低350倍。在无毛，色素沉着的豚鼠模型中，dA表现出快速持续的亮肤效果，局部停药后8周内完全可逆。相反，HQ引起了短暂但不可持续的亮肤作用，而曲酸和熊果苷则没有亮肤作用。安全测试小组的结果支持了dA作为可操作分子的整体确立。在一项人类临床试验中，局部治疗dA达12周导致分别在浅色或深色皮肤个体中总体皮肤明度显着降低或略有降低，并且太阳扁豆素有所改善。这些数据表明，dA具有潜在的酪氨酸酶抑制活性，可导致皮肤增白，并可用于改善色素沉着过度的病变。

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DeoxyArbutin: a novel reversible tyrosinase inhibitor with effective in vivo skin lightening potency.

Modulation of melanogenesis in the melanocytes can be achieved using chemicals that share structural homologies with the substrate tyrosine and as thus competitively inhibit the catalytic function of tyrosinase. We have developed a new tyrosinase inhibitor, deoxyArbutin (dA), based on this premise. DeoxyArbutin demonstrates effective inhibition of mushroom tyrosinase in vitro with a Ki that is 10-fold lower that hydroquinone (HQ) and 350-fold lower than arbutin. In a hairless, pigmented guinea pig model, dA demonstrated rapid and sustained skin lightening that was completely reversible within 8 weeks after halt in topical application. In contrast, HQ induced a short but unsustained skin lightening effect whereas kojic acid and arbutin exhibit no skin lightening effect. Results from a panel of safety tests supported the overall establishment of dA as an actionable molecule. In a human clinical trial, topical treatment of dA for 12 weeks resulted in a significant or slight reduction in overall skin lightness and improvement of solar lentigines in a population of light skin or dark skin individuals, respectively. These data demonstrate that dA has potential tyrosinase inhibitory activity that can result in skin lightening and may be used to ameliorate hyperpigmentary lesions.

更新日期：2019-11-01

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