Enzymatic synthesis of memantine (Memary) oligosaccharides (glucooligosaccharides) and their application as anti-dementia drugs that cross the blood-brain barrier (BBB)

Hamada, Hiroki ; Ishihara, Kohji; Shimoda, Kei; Kuboki, Atsuhito; Kiriake, Yuya; Hosoda, Ryusuke

Memantine (memary) oligosaccharides (gluco-oligosaccharides) were synthesized by enzymic glycosylation, using cyclodextrin glucanotransferase as a biocatalyst. Although memantine hardly crosses the blood-brain barrier (BBB) in the mouse brain, memantine oligosaccharides crossed the BBB of mouse brain and were incorporated into the mouse brain tissue. Our investigations indicated that memantine modified with oligosaccharides might have gained a BBB-crossing ability. Furthermore, during the Y-maze test using senescence-accelerated mouse prone 8, our study revealed that the time spent in the novel Y-maze arm by the memantine-oligosaccharides-treated mouse was longer than that spent in the novel arm by the memantine-treated-mouse. Therefore, this study established that since memantine oligosaccharides could penetrate the BBB of mouse brain and be incorporated into the mouse's brain tissue, they could also enhance spatial learning.

International Journal of Current Microbiology and Applied Sciences

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2319-7692