具有 BBB 透过性的睡莲科植物中阿朴啡型生物碱，能加速 PC-12 细胞的神经突生长。

BBB-permeable aporphine-type alkaloids in Nelumbo nucifera flowers with accelerative effects on neurite outgrowth in PC-12 cells.

机构信息

Department of Pharmacognosy, Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto, 607-8412, Japan.

N.T.H. Co., Ltd., 1-8-11 4F Sky-ebisu Bldg., Ebisu, Shibuya-ku, Tokyo, 150-0013, Japan.

出版信息

J Nat Med. 2020 Jan;74(1):212-218. doi: 10.1007/s11418-019-01368-7. Epub 2019 Nov 9.

DOI:10.1007/s11418-019-01368-7

PMID:31707550

Abstract

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.

摘要

在荷花甲醇提取物中的血脑屏障（BBB）通透性成分显示出对 PC-12 细胞突起生长的加速作用。在我们之前的研究中从荷花中分离的成分中，阿朴啡型生物碱，黎芦定碱，斯皮诺辛，N-甲基黎芦定碱和原荷叶碱显示出加速作用。低浓度的黎芦定碱，N-甲基黎芦定碱和富含生物碱的二乙醚部分增加了编码 TrkA，Vav3 和 Rac1 的 mRNA 的表达。此外，在体外 BBB 模型中证实了斯皮诺辛和 N-甲基斯皮诺辛具有良好的通透性。由于其活性和 BBB 通透性，斯皮诺辛和 N-甲基斯皮诺辛被认为是阿尔茨海默病药物的候选化合物。