Study on structural transformation pathway of indaconitine in stir-frying with sand process and toxicity of its processing products / 中草药

ABSTRACT

Objective: To study the structural transformation pathway of indaconitine in stir-frying with sand process and compare the toxicity of indaconitine with its processing products. Methods: Using high performance liquid chromatography to screen out the temperature and time parameters of the structural transformation of indaconitine. The processing products were separated by column chromatography and identified by NMR and MS. The cardiotoxicity test was chosen to compare the toxicity of indaconitine with its processing products. Results: Indaconitine was converted into mithaconitine when it was heated at 160-180 ℃ for 10-30 min. With a dose of 0.06 mg/kg, indaconitine could induce ventricular arrhythmia in rats, such as ventricular premature beat, ventricular tachycardia. However, mithaconitine had no arrhythmogenic effect at the same dosage. Conclusion: The structural transformation pathway of indaconitine has been defined deacetylating at C-8 position, generating 14-benzoylpseudaconine, and converting benzoylpseudaconine into mithaconitine by dehydration reaction at C-8 and C-15 position. Compared with indaconitine, the toxicity of mithaconitine was reduced.