Murayama M, Mori T, Bando H, Amiya T
Research Section, Sanwa Shoyaku Co. Ltd., Tochigi, Japan.
J Ethnopharmacol. 1991 Dec;35(2):159-64. doi: 10.1016/0378-8741(91)90068-o.
Eight pyro-type aconitine alkaloids contained in the processed aconite powder 'Kako-bushi-matsu' were studied for their analgesic, antiinflammatory and acute toxic actions. All these compounds showed significant analgesic and antiinflammatory actions. Among the pyro-type alkaloids, 16-epi-pyrojesaconitine and pyrojesaconitine were the most potent analgesics. The analgesic activity of pyro-type aconitine alkaloids was lower than that of each of the parent alkaloids, aconitine, mesaconitine, hypaconitine and jesaconitine. However, pyro-type aconitine alkaloids had very low toxicity, and the decreasing rates of the toxicity in changing from the parent alkaloids to the pyro-type aconitine alkaloids were much larger than those relating to the analgesic activity. Eight pyro-type aconitine alkaloids were found to inhibit the carrageenin-induced hind paw edema at 2 to 6 h after the carrageenin subplantar injection. Consequently, it was demonstrated that the pyro-type aconitine alkaloids produced through the processing of raw aconite roots, 'Bushi', have a role in the medicinal effects of the processed aconite powder 'Kako-bushi-matsu'.
对炮制附子粉末“炙附子松”中所含的8种焦型乌头碱生物碱的镇痛、抗炎和急性毒性作用进行了研究。所有这些化合物均表现出显著的镇痛和抗炎作用。在焦型生物碱中，16-表-焦杰沙乌头碱和焦杰沙乌头碱是最有效的镇痛剂。焦型乌头碱生物碱的镇痛活性低于母体生物碱乌头碱、中乌头碱、次乌头碱和杰沙乌头碱中的任何一种。然而，焦型乌头碱生物碱的毒性非常低，从母体生物碱转变为焦型乌头碱生物碱时毒性的降低率远大于与镇痛活性相关的降低率。发现8种焦型乌头碱生物碱在角叉菜胶足底注射后2至6小时可抑制角叉菜胶诱导的后爪水肿。因此，证明了通过生附子根“附子”炮制产生的焦型乌头碱生物碱在炮制附子粉末“炙附子松”的药用效果中起作用。
