Highly potent inhibition of tyrosinase by mulberrosides and the inhibitory mechanism in vitro
Highly potent inhibition of tyrosinase by mulberrosides and the inhibitory mechanism in vitro
复制标题
桑甙对酪氨酸酶的高效抑制作用及其体外抑制机制
DOI：
10.1002/cbdv.202100740
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发表时间：
2021-11
影响因子：
2.9
通讯作者：
Feng Qiu
中科院分区：
文献类型：
--
作者：
Xiang Liu;Jinqiu Rao;Kai Wang;Meijun Wang;Tie Yao;Feng Qiu
许多苯乙烯苷类化合物对酪氨酸酶有抑制作用，可缓解皮肤色素沉着。桑葚中的桑叶苷是stilbene苷。本研究对从桑葚中分离的5种桑苷（S1-5）对酪氨酸酶的抑制作用进行了研究和比较。探讨了其抑制机制。这5种桑总苷对酪氨酸酶的抑制作用仅呈浓度依赖性。没有时间依赖性，表明它们是酪氨酸酶的可逆抑制剂。S2、S1和S5对酪氨酸酶的抑制作用IC50值分别为28.93、0.75.94和151.72 μM，均高于曲酸（IC50=169.13 μM）。动力学研究表明，S1、S2和S4具有竞争性。S3和S5为混合抑制剂。荧光光谱分析表明桑葚苷S1、S2和S4猝灭了本征。酪氨酸酶的荧光强度。分子对接研究表明，酪氨酸酶与桑葚苷的相互作用是通过化合物来体现的。分数如下：S2 > S5 >S1 > S3/S4 >曲酸，桑葚苷侧链上的羟基可能在酶的结合中起关键作用。本研究结果表明，桑椹总皂苷可进一步开发为抗色素沉着的增白剂。
Many stilbene glycosides can alleviate skin hyperpigmentation due to their inhibitory effect on tyrosinase. Mulberrosides in Morus alba L. are stilbene.glycosides. In the present study, the inhibition of tyrosinase by five mulberrosides( S1-5), isolated from Morus alba L. was investigated and compared, and.the inhibitory mechanism was explored. These five mulberrosides exhibited obvious inhibitory effects on tyrosinase only in a concentration-dependent manner,.without time-dependence, indicating that they are reversible inhibitors of tyrosinase. S2, S1 and S5 inhibited tyrosinase activity with IC50 values of 28.93,.75.94 and 151.72 μM, respectively, and were more active than kojic acid (IC50=169.13 μM). Kinetic studies revealed that S1, S2 and S4 were competitive.inhibitors, while S3 and S5 were mixed inhibitors. Analysis of the fluorescent spectra showed that mulberrosides S1, S2 and S4 quenched the intrinsic.fluorescence intensity of tyrosinase. A molecular docking study indicated that the interaction of tyrosinase with mulberrosides was reflected by compound.scores as follows: S2 > S5 >S1 > S3/S4 > kojic acid, and hydroxyl groups in the side chain of mulberrosides may play a crucial role in the binding of the.enzyme. Our results suggest that mulberrosides in Morus alba L. could be further developed as whitening agents for enhanced performance against.hyperpigmentation.
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DOI：
10.1016/j.bbrc.2005.12.229
发表时间：
2006-04
影响因子：
3.1
作者：
Kang-Kang Song-Kang;Hao Huang;Peng Han;Chun-Le Zhang;Yan Shi;Qing-Xi Chen
通讯作者：
Kang-Kang Song-Kang;Hao Huang;Peng Han;Chun-Le Zhang;Yan Shi;Qing-Xi Chen
DOI：
10.1016/j.fct.2010.05.074
发表时间：
2010-08
期刊：
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association
影响因子：
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通讯作者：
Xiaolan Yang;Lei Yang;Haiying Zheng
影响因子：
3.4
作者：
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通讯作者：
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影响因子：
3.5
作者：
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通讯作者：
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影响因子：
6.1
作者：
Zheng, Zong-Ping;Cheng, Ka-Wing;Wang, Mingfu
通讯作者：
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