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Curcumin Oligosaccharides (Gluco-oligosaccharides) Penetrate the Blood-Brain Barrier in Mouse Brain: Glycoside (Polysaccharide) Modification Approach for Brain Drug Delivery Across the Blood-Brain Barrier and Tumor Drug Delivery
Natural Product Communications ( IF 1.5 ) Pub Date : 2020-11-09 , DOI: 10.1177/1934578x20953653
Hiroki Hamada 1 , Takahiro Nakayama 2 , Kei Shimoda 3 , Nobuyasu Matsuura 2 , Hatsuyuki Hamada 4 , Takafumi Iwaki 5 , Yuya Kiriake 6 , Tomohiro Saikawa 7
Affiliation  

In order to expand our drug delivery technique by glycosylation of chemical into brain delivery, it was demonstrated that oligosaccharide and monosaccharide modifications of curcumin enhanced its crossing ability of the blood-brain barrier (BBB) in mice. The brain sample prepared by glycosidase-catalyzed hydrolysis of brain tissue homogenates of mice, to which curcumin gluco-oligosaccharides were intraperitoneally injected, contained curcumin at 116 ng/1 g of tissue of brain, indicating that curcumin modified with gluco-oligosaccharides residues can smoothly cross the BBB in mouse brain. The brain samples of mice, which were treated with curcumin monosaccharide or curcumin itself, contained curcumin at 18 ng and 0 ng per 1 g of tissue of brain, respectively. On the other hand, after the administration of curcumin gluco-oligosaccharides to C57BL mouse with a large tumor for 5 days, the tumor disappeared.



中文翻译:

姜黄素寡糖(葡萄糖寡糖)穿透小鼠大脑的血脑屏障:跨血脑屏障和肿瘤药物递送的脑苷的糖苷(多糖)修饰方法


为了通过将化学糖基化扩展到脑部输送来扩展我们的药物输送技术,已证明姜黄素的寡糖和单糖修饰可增强其在小鼠中的血脑屏障(BBB)穿越能力。通过糖苷酶催化水解小鼠脑组织匀浆制备的脑样品经腹膜内注射姜黄素葡萄糖寡糖,其脑组织中的姜黄素含量为116 ng / 1 g,这表明用葡萄糖寡糖残基修饰的姜黄素可以顺利进行越过鼠脑中的血脑屏障。用姜黄素单糖或姜黄素本身处理的小鼠的脑样本中,每1 g脑组织中分别含有18 ng和0 ng的姜黄素。另一方面,

更新日期:2020-11-12
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