Original Articles

Anti-inflammatory and analgesic activities of N-deacetyllappaconitine and lappaconitine

Authors: Jian-Hua Liu, Yue-Xin Zhu, Xi-Can Tang


N-deacetyllappaconitine (DLA) 1—10 mg/kg or lappaconitine (LA) 1—6 mg/kg inhibited several inflammatory processes, such as increase of capillary permeability due to ip 0.7% acetic acid l0 mg/kg in mice; ear swelling induced by xylene in mice; edema produced by injecting 1% carrageenin 0.15 ml or fresh egg white 0.l ml beneath the planter surface of hind paw in rats and the growth of rat granuloma caused by cotton pellets, without influencing the weights of thymus and adrenal. Their anti-inflammatory activity was also demonstrated in adrenalectomized rats. DLA and LA neither prolonged the surviving time of adrenalectomized rats nor reduced the content of adrenal ascorbic acid in rats. These results suggest that the anti-inflammatory actions of DLA and LA do not depend on stimulation of the pituitary-adrenal axis.
The hot plate, formaldehyde and HAc-writhing tests in mice showed that DLA and LA had a marked analgesic action, their sc median analgesic doses (ED50) were 7.1, 3.8 mg/kg and 2.3, 3.5 mg/kg in mice with formaldehyde and HAc-writhing test, respectively.
DLA exhibited marked local anesthetic activity as shown by sciatic nerve block in mice, its ED50 concentration was 0.076%.
DLA 15 mg/kg and LA 6 mg/kg ip showed an antipyretic effect in rats with fever induced by sc injection of 7% yeast 3 ml/kg.
The ip LD50 of DLA and LA were 23.5, 10.5 mg/kg (mice) and 29.9, 9.9 mg/kg (rats), respectively.

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