文章基本信息

标题：Effect of Aconitum Alkaloid Kobusine and Pseudokobusine Derivatives on Cutaneous Blood Flow in Mice; II
本地全文：下载
作者：Koji WADA ; Satoshi ISHIZUKI ; Takao MORI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2000
卷号：23
期号：5
页码：607-615
DOI：10.1248/bpb.23.607
出版社：The Pharmaceutical Society of Japan
摘要：Aconitum alkaloids of the C₂₀-diterpenoid type, kobusine (1) and pseudokobusine (2), their anisoyl, veratroyl, p-nitrobenzoyl, nicotinoyl or pivaloyl derivatives, and dehydrokobusine and N, 6-seco-6-dehydro-pseudokobusine derivatives were examined for their peripheral vaso-activities by laser-flowmetrical measurement of the cutaneous blood flow in the hind foot of mice after intravenous administraiton. Kobusine 15-anisoate (4), 11-veratroate (5), 15-veratroate (6), 11-pivaloate (9) and 15-pivaloate (10)-were significantly effective at a low dose of 0.5 or 0.05 mg/kg. Pseudokobusine derivatives were all avtive at 1, 0.5 or 0.05 mg/kg, and the effects of pseudokobusine 15-anisoate (13), 15-veratroate (16) and 15-p-nitrobenzoate (19) at 0.1 mg/kg were remarkable. Yesoline (26) and alkaloid (28) were significantly effective at a low dose of 1 mg/kg, whereas yesonine (25) and N-acetyl-N, 6-seco-6-dehydropseudokobusine (27) were inactive. Dehydrokobusine derivatives (29, 30) were significantly effective at a low dose of 0.5 or 0.1 mg/kg. It is thought that the hydroxyl groups of alkaloids, espectially a free OH group of 2 at C-6, are important for action on the peripheral vasculature leading to dilatation, and the results indicated that esterificaiton of the hydroxyl group at C-15 with either anisoate, veratroate or p-nitrobenzoate may contribute to enhancement of the activity of the parent alkaloids.
关键词：cutaneous blood flow;pseudokobusine;kobusine;Aconitum alkaloid;semisynthetic alkaloid;mouse