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BBB-permeable aporphine-type alkaloids in Nelumbo nucifera flowers with accelerative effects on neurite outgrowth in PC-12 cells.
Journal of Natural Medicines ( IF 2.5 ) Pub Date : 2019-11-09 , DOI: 10.1007/s11418-019-01368-7
Mamiko Yano 1 , Souichi Nakashima 1 , Yoshimi Oda 1, 2 , Seikou Nakamura 1 , Hisashi Matsuda 1
Affiliation  

Blood–brain barrier (BBB)-permeable components in the methanolic extract of Nelumbo nucifera flowers showed accelerative effects on neurite outgrowth in PC-12 cells. Among the constituents isolated from N. nucifera flowers in our previous study, aporphine-type alkaloids, lirinidine, asimilobine, N-methylasimilobine, and pronuciferine, showed accelerative effects. Lirinidine, N-methylasimilobine, and an alkaloid-rich diethyl ether fraction at low concentrations increased the expression of mRNAs coding for TrkA, Vav3, and Rac1. In addition, good permeability of asimilobine and N-methylasimilobine was confirmed using an in vitro BBB model. Asimilobine and N-methylasimilobine are considered to be suitable as seed compounds of drugs for Alzheimer’s disease, because of their activity and BBB permeability.

中文翻译:

莲(Nelumbo nucifera)花中具有BBB渗透性的Aph式生物碱,对PC-12细胞的神经突生长具有促进作用。

莲(Nelumbo nucifera)花的甲醇提取物中可渗透血脑屏障(BBB)的成分对PC-12细胞的神经突生长有促进作用。在我们先前的研究中,从N. nucifera花中分离出的成分中,阿波啡型生物碱,力力定,亚胺洛宾,N-甲基亚胺叶碱和pronuciferine具有促进作用。利力丁,N-甲基亚胺甜菜碱和低浓度的富含生物碱的乙醚馏分增加了编码TrkA,Vav3和Rac1的mRNA的表达。另外,使用体外BBB模型证实了阿斯米洛宾和N-甲基阿斯米洛宾的良好渗透性。亚精胺和-甲基亚基米环素由于其活性和BBB通透性而被认为适合作为阿尔茨海默氏病药物的种子化合物。
更新日期:2019-11-09
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