Deoxyarbutin Possesses a Potent Skin-Lightening Capacity with No Discernible Cytotoxicity against Melanosomes.
Deoxyarbutin Possesses a Potent Skin-Lightening Capacity with No Discernible Cytotoxicity against Melanosomes.
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脱氧熊果苷具有强大的亮肤能力，且对黑色素体没有明显的细胞毒性
DOI：
10.1371/journal.pone.0165338
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发表时间：
2016
期刊：
影响因子：
3.7
通讯作者：
Lei TC
中科院分区：
文献类型：
--
作者：
Miao F;Shi Y;Fan ZF;Jiang S;Xu SZ;Lei TC
安全有效的成分能够去除不希望的色素沉着从面部皮肤是迫切需要的医药和化妆品的目的。脱氧熊果苷（4-[（四氢- 2h -吡喃-2-基）氧]苯酚，D-Arb）是对苯二酚的糖苷衍生物。在这里，我们使用体内和体外模型研究了D-Arb在亚细胞水平（直接作用于黑素体）和皮肤色素沉着的毒性和功效，并与其母体化合物对苯二酚（1,4-苯二醇，HQ）进行了比较。首先，我们用透射电镜观察了308 nm单色准分子光和/或HQ和D-Arb处理诱导的豚鼠皮肤色素沉着的超微结构变化。结果表明，局部应用5% HQ 10天后，皮肤黑素体膜发生了明显的变化，如球茎状结构，甚至外膜完全破裂。这些变化在用D-Arb治疗的皮肤中几乎没有观察到。为了进一步阐明HQ的膜毒性是否是复合治疗的直接结果，我们还检查了从MNT1人黑色素瘤细胞中纯化的单个黑素体的超微结构变化。体外裸黑素体模型也获得了类似的观察结果。最后，我们利用电子自旋共振实验确定了暴露于HQ或D-Arb的黑素体部分对芬顿反应中羟基自由基生成的影响。d - arb处理的黑素体表现出中等的羟基自由基清除活性，而hq处理的黑素体显著地产生更多的羟基自由基。本研究提示D-Arb具有较强的皮肤美白和抗氧化能力，且黑素小体细胞毒性较小。
Safe and effective ingredients capable of removing undesired hyperpigmentation from facial skin are urgently needed for both pharmaceutical and cosmetic purposes. Deoxyarbutin (4-[(tetrahydro-2H-pyran-2-yl) oxy] phenol, D-Arb) is a glucoside derivative of hydroquinone. Here, we investigated the toxicity and efficacy of D-Arb at the sub-cellular level (directly on melanosomes) and skin pigmentation using in vivo and in vitro models to compare with its parent compound hydroquinone (1,4-benzenediol, HQ). At first, we examined the ultrastructural changes of melanosomes in hyperpigmented guinea pig skin induced by 308-nm monochromatic excimer lightand/or treated with HQ and D-Arb using transmission electron microscopy. The results showed that prominent changes in the melanosomal membrane, such as bulb-like structure and even complete rupture of the outer membranes, were found in the skin after topical application of 5% HQ for 10 days. These changes were barely observed in the skin treated with D-Arb. To further clarify whether membrane toxicity of HQ was a direct result of the compound treatment, we also examinedultrastructural changes of individual melanosomes purified from MNT1 human melanoma cells. Similar observations were obtained from the naked melanosome model in vitro. Finally, we determined the effects of melanosomal fractions exposed to HQ or D-Arb on hydroxyl radical generation in the Fenton reaction utilizing an electron spin resonance assay. D-Arb-treated melanosomesexhibit a moderate hydroxyl radical-scavenging activity, whereas HQ-treated melanosomessignificantly generate more hydroxyl free radicals. This study suggests that D-Arb possesses a potent ability in skin lightening and antioxidation with less melanosome cytotoxicity.
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