Pharmacological Evaluation for Extracts of Aconiti Radix and Aconiti Radix Cocta / 中国实验方剂学杂志

ABSTRACT

Objective: To carry out the studies of pharmacological action for extracts of Aconiti Radix and Aconiti Radix Cocta, and evaluate the selection of raw materials in prescriptions, in order to promote the development and clinical application of preparations. Method: The mixed extracts of Aconiti Radix and Aconiti Radix Cocta were prepared respectively according to the technique of aconitum injection, and different dose groups of Aconiti Radix and Aconiti Radix Cocta were established based on the dose of Aconiti Radix 0.152 5 mg·g-1, and then applied in such pharmacodynamic tests as analgesia, heart rate reduction, antitumor effect and toxicology tests, such as acute toxicity and organ observation. The data were analyzed systematically on the basis of literatures. Result: Compared with blank group, the extracts of both Aconiti Radix and Aconiti Radix Cocta had a significantly analgesic effect. At the same dose, the pain inhibition rate of Aconiti Radix injection (60.91%) was higher than that of Aconiti Radix Cocta injection (53.42%), and the pain inhibition rate of Aconiti Radix extract for oral administration(73.94%) was also much higher than that of Aconiti Radix Cocta extract (29.97%), with significant differences (Pth min after administration, the heart rate of the Aconiti Radix group was decreased first, then stabilized, and finally increased with the rise of the dose, while for the Aconiti Radix Cocta group showed a different trend of first stability, then decrease and finally increase. The result indicated the Aconiti Radix group had the effect in reducing heart rate in rats at a low dose. The survival inhibition rate was evaluated by 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). The extracts of both Aconiti Radix and Aconiti Radix Cocta had a significantly inhibitory effect on the proliferation of AGS gastric cancer cells, in which Aconiti Radix was stronger than that of Aconiti Radix Cocta at the same dose. In the acute toxicity test of rats, lethal dose 50%(LD50) of Aconiti Radix and Aconiti Radix Cocta were 3.9 g·kg-1 and 21.0 g·kg-1 respectively, which were equivalent to 4 times and 20 times of the clinical dose. LD50 of the extract of Aconiti Radix Cocta was 5 times than that of Aconiti Radix. The liver and kidney of dead rats were dark with obvious symptoms of poisoning after dissection, while all the organs of rats at the clinical and lower dose were normal. Conclusion: The safety of Aconiti Radix is lower than that of Aconiti Radix Cocta, but with greater analgesic, bradycardic and anticancerous effect. Therefore, it is suggested that the preparations, such as aconitum injection, should be prepared with Aconiti Radix in the treatment of severe pain of patients with advanced gastric and liver cancer, and the preparations for general pain can be prepared with Aconiti Radix Cocta, so as to achieve a truly safe and effective dialectical treatment.