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We have developed a method using a laser flow meter for investigating the effect of compounds on peripheral blood flow. The differences of blood flow in several portions and areas of the probe of a laser flow meter in the mouse and the effect of solvents for dissolving compounds on the blood flow were observed. The results indicated that the invisible area of blood vessels at the back or hind paw of the mouse was the most suitable placement position for the probe. In these placement positions, none of the tested solvents, 0.9% physiological saline solution, dimethylsulfoxide and 50% ethanol, had any significant effect on the peripheral blood flow. Next, using this method, we determined how the peripheral blood flow is affected by several drugs active on the circulatory system. By comparison between the present results from mice and previously reported data from other animals, it was shown that the effects of these cardiovascular agents on the peripheral blood flow in mouse skin showed similar tendencies to those in the previous reports using larger animals and sites other than the skin. However, a few of the drugs used in this experiment showed characteristic action on the peripheral blood flow in mice. Consequently, it was demonstrated that this method using the laser flow meter was useful as a simple first screening method to evaluate the effect of a compound on the peripheral blood flow.

1991-01-01·Chemical and Pharmaceutical Bulletin4区 · 医学

Studies on the constituents of Aconitum species. XII. Syntheses of jasaconitine derivatives and their analgesic and toxic activities.

4区 · 医学

Article

作者: Mori, Takao ; Kawahara, Norio ; Bando, Hideo ; Murayama, Mitsuo

The role of the substituents at C3 and C8 of jesaconitine (1) on jesaconitine-induced analgesia and toxicity was examined. 3-O-Acetyljesaconitine (2), 3-O-anisoyljesaconitine (3), and 3-deoxyjesaconitine (6) showed dose-dependent analgesic action, and the potency of their compound-induced analgesia and toxicity was lower than those of 1. The most remarkable difference was found in the toxicity. The results indicate that the C3 hydroxy function of 1 participate in the induction of toxicity rather than of analgesia. 8-O-Linoleoyl-14-anisoylaconine (5), 8-O-methyl-14-anisoylaconine (7), 8-O-ethyl-14-anisoylaconine (8), 14-anisoylaconine (4) and 8-deoxy-14-anisoylaconine (9) showed lower activities than jesaconitine-induced analgesia and toxicity. The analgesic activity of 7 was almost the same as that of 8, but the toxicity of 7 was lower than that of 8. The analgesic activity of 9 was lower than that of 4, but the toxicities of both derivatives were not apparent. These facts indicate that the C8 function of 1 is important to the induction of analgesia and toxicity, and also that this function participates differently in the induction of the analgesia and toxicity. Subsequently, it was suggested that substituents at C3 and C8 of 1 played important roles of the induction of the analgesia and toxicity, and that the modes of this participation were not the same in analgesia and toxicity.

1989-01-01·HETEROCYCLES

Studies on Aconitum Species. VIII. Components of "Kako-Bushi-Matsu"

作者: Mori, Takao ; Ohsawa, Takatomi ; Murayama, Mitsuo ; Amiya, Takashi ; Bando, Hideo ; Wada, Koji

Seventeen C₁₉-diterpenoid alkaloids were isolated from processed aconite (kako-bushi-matsu).Structures were determined on the basis of spectral and chem. data.The 15-keto-pyro type compounds 16-epi-pyroaconitine, pyroaconitine, 16-epi-pyromesaconitine, pyromesaconitine, 16-epi-pyrojesaconitine, pyrojesaconitine, 16-epi-pyrohypaconitine, and pyrohypaconitine, were induced by heating of aconitine, mesaconitine, jesaconitine, and hypaconitine present in the raw aconite roots.

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