Effects of alkaloids from Aconitum yesoense var. macroyesoense on cutaneous blood flow in mice.

Nine alkaloid constituents in the root of Aconitum yesoense var. macroyesoense, as well as three acetylated derivatives, were examined for their peripheral vaso-activities by measuring laser-flowmetrically the cutaneous blood flow in the hind foot of mice after intravenous administration. The major constitutive delcosine (1), 14-acetyldelcosine (2) and lucidusculine (3), respectively, had little or very mild vaso-activity. Kobusine (4) and pseudokobusine (5) and three minor constituents, luciculine (6), 1-acetylluciculine (7) and dehydroluciculine (8), together exhibited a rapid increase in blood flow reaching a peak with a magnitude almost equal to that produced by hydralazine, when administered intravenously at the same dosage level of 20 mg/kg. Among them, 4 was characterized by successive reversal of the increase to a decrease in blood flow, while 7 produced a flow with a more delayed peak time. Dehydrolucidusculine (9) exhibited a transient decrease in blood flow prior to occurrence of the increase, as did papaverine. Consequently, it is assumed that the alkaloids, especially those of the C20-diterpenoid type, in the root of this Aconitum plant have peripherally vaso-dilating activities to varying degrees in mice, probably due to their direct action on the cutaneous microvasculature in a similar fashion to that shown by hydralazine. The laser blood flowmetric method would be useful as an in vivo means of qualitative as well as quantitative screening of chemically modified derivatives of peripherally vasoactive agents in mice.