Extraction, Isolation And Acute Toxic Experiment Of Arecoline And Its Influence On Gastrointestinal Movement

Arecoline is one of the most active components in semen arecae. It has effects of lustrating parasites, killing snails, resisting blahs, resisting pathogenic micro-organism, and so on. It also has many functions on nerves system, digestive system and urogenital system. Arecoline is mostly used to cure infection of animals'parasites on veterinary surgeon clinic. However, the method of extraction arecoline from semen arecae is not perfect, which results in low output of arecoline and confines its clinical appliance in a certain extent. This research undertook its extraction, isolation, acute toxicity and its influence on gastrointestinal movement.This research adopted the method of infiltrate to extract arecoline from semen arecae by using 1% thin hydrochloric acid and 75% ethanol as solvent, and got arecoline hydrobromide by treating arecoline with 36% hydrobromic acid. Thin layer chromatography(TLC), magnetic resonance, infrared and ultraviolet chromatogram were applied to make qualitative analysis and structure corroboration of arecoline hydrobromide, and high performance liquid chromatography was used to determine the content of arecoline in the output. The acute toxicity of arecoline and arecoline hydrobromide in mice by oral administration were carried out, and LD50 and its 95% confidence limit were calculated by Karber method. At the same time, the experiment studied arecoline's effects on propulsive ratio of mice's small intestine and effects on movements of rabbit's duodenum, jejunum, ileum and guinea pig's stomach.1. The method of infiltrate was adopted to extract and isolate arecoline, which had the merits of low cost and high rate of extraction. The rate of extraction by thin hydrochloric acid and high ethanol partly were 0.190% and 0.113%. The contents of arecoline hydrobromide A and B respectively were 99.20% and 98.19% by high performance liquid chromatography. The results of TLC, magnetic resonance, infrared and ultraviolet chromatogram indicated that the substance we got was accord with arecoline hydrobromide criterion.2. The experiment of acute toxicity indicated that LD50 of arecoline in mice by oral administration was 174.71 mg/kg, and its 95% confidence limit was 145.22～ 210.14 mg/kg; LD50 of arecoline hydrobromide in mice by oral administration was 454.38 mg/kg(calculated by arecoline), and its 95% confidence limit was 422.26～488.95 mg/kg. The toxicity of arecoline was 2.6 times higher than that of arecoline hydrobromide. Because arecoline hydrobromide's LD50(691.83 mg/kg) was 138～230 times than the dosage recommended, it is safe to be used in clinic.3. The experiment of pharmacology suggested that arecoline hydrobromide could boost propulsive ratio of mice's small intestine, could excite smooth muscles of rabbits'small intestine and guinea pigs'stomach and could enhance strain and swing of gastrointestinal smooth muscle.