L-Cystine Diamides as L-Cystine Crystallization Inhibitors for Cystinuria
L-Cystine Diamides as L-Cystine Crystallization Inhibitors for Cystinuria
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DOI：
10.1021/acs.jmedchem.6b00647
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发表时间：
2016-08-11
影响因子：
7.3
通讯作者：
Sahota, Amrik
中科院分区：
文献类型：
--
作者：
Hu, Longqin;Yang, Yanhui;Sahota, Amrik
L-胱氨酸双吗啉 (la) 和 L-胱氨酸双(N'-甲基哌嗪) (1b) 在增加 L-胱氨酸亚稳态过饱和范围方面分别比 L-胱氨酸二甲酯 (CDME) 有效 7 倍和 24 倍，有效抑制 L-胱氨酸结晶。正如原子力显微镜所揭示的，这种行为可归因于微观长度尺度上晶体生长的抑制。 1a 和 1b 都比 CDME 更稳定，并且 1b 在胱氨酸尿症敲除小鼠模型中体内有效。
L-Cystine bismorpholide (la) and L-cystine bis(N'-methylpiperazide) (1b) were seven and twenty-four times more effective than L-cystine dimethyl ester (CDME) in increasing the metastable supersaturation range of L-cystine, respectively, effectively inhibiting L-cystine crystallization. This behavior can be attributed to inhibition of crystal growth at microscopic length scale, as revealed by atomic force microscopy. Both 1a and 1b are more stable than CDME, and 1b was effective in vivo in a knockout mouse model of cystinuria.