Effects of Aconitum Alkaloid Kobusine and Pseudokobusine Derivatives on Cutaneous Blood Flow in Mice
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概要
- 論文の詳細を見る
Aconitum alkaloids of the C_<20>-diterpenoid type, kobusine (1) and pseudokobusine (2), and their acetyl, benzoyl, propionyl or cinnamoyl derivatives are examined for their peripheral vaso-activities by laster-flowmetrical measurement of the cutaneous blood flow in the hind foot of mice after intravenous administration. A dose-relationship of maximally increased blood flow after the administration of either of the Aconitum alkaloids existed. Kobusine 15-acetate (4), 11-benzoate (6) and 15-benzoate (7) were significantly effective at a low dose of 1 mg/kg, whereas the other kobusine derivatives were all inactive. Alkaloid 2,alone, and the 11-acetate (14), 15-acetate (15), 15-propionate (22) and 15-cinnamoate (25) were all active at 1 mg/kg and the effect of 14 at 5 mg/kg was remarkable. The activity of 2 was abolished by esterification of the hydroxyl group at C-6. Alkaloid 15 at 5 mg/kg showed a pattern of time course of blood flow in which the increase was repidly replaced with a decrease below the basal flow, probably suggesting the effect of excessive doses. Conclusively, it is considered that the hydroxyl groups of alkaloids, especially a free OH group of 2 at C-6,are important for action on the peripheral vasculature leading to dilatation, and these results indicated that esterification of the hydroxyl group at C-15 with either acetate or benzoate may contribute to enhancement of the activity of the parent alkaloids.
- 公益社団法人日本薬学会の論文
- 1998-02-15
著者
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Mori Tetsuya
Department Of Radiology And Nuclear Medicine Hyogo Brain And Heart Center
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Mori T
First Institute Of New Drug Research Otsuka Pharmaceutical Co. Ltd.
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Ishizuki S
Hokkaido College Of Pharmacy
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Kawahara N
National Institute Of Health Sciences
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WADA Koji
Hokkaido College of Pharmacy
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MORI Takao
Hokkaido College of Pharmacy
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KAWAHARA Norio
Hokkaido College of Pharmacy
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ISHIZUKI Satoshi
Hokkaido College of Pharmacy
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FUJIHIRA Eiichi
Hokkaido College of Pharmacy
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和田 勝夫
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Wada Katsuo
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Fujihira E
Hokkaido Coll. Pharmacy Hokkaido Jpn
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