Hydrolysis mechanism of aconitine and deoxyaconitine in Aconitum soongaricum / 中草药

Objective To determinate the hydrolysis products of two ingredients in Aconitum soongaricum under different heating conditions by liquid chromatography-mass spectrometry method, analyze its hydrolysis change rule, and verify it in A. soongaricum, analyze the changes of alkaloid before and after processing, and summarize the change rules and processing hydrolysis mechanism, so as to provide theoretical basis for the processing parameters of A. soongaricum. Methods Taking two kinds of main chemical constituents in A. soongaricum, aconitine and deoxyaconitine as the research object, the change rule of alkaloid monomer variation under different heating conditions was summarized combined with HPLC and HPLC-MS results, which was verified in different processed products in A. soongaricum. Results There was the significant change in the content of aconitine and deoxyaconitine after different heating time, the content of the mainly products from aconitine hydrolysis was increased with the increase of heating time, and aconitine and deoxyaconitine were gradually disappeared, eventually not detected. Conclusion The processing parameters of A. soongaricum were preliminarily determined as heating for 5-6 h, and the hydrolysis of aconitine and deoxyaconitine producing new hydrolysis products, thus achieving the effect of reducing toxicity and increasing efficiency.

Screening of Anti-EGFR Components from Aconitum Soongaricum Stapf. in Xinjiang Province Based on Cell Membrane Chromatography / 中国药师

Objective:To screen anti-EGFR components from Aconitum soongaricum Stapf. and investigate their inhibitory effect on HEK293 cells and EGFR/HEK293 high expression cell lines. Methods:A two-dimensional online system (EGFR/CMC-HPLC-MS) was built to screen anti-EGFR active compounds from Aconitum soongaricum Stapf.;molecular docking assay was performed to determine the binding affinity of the components to EGFR;MTT was used to confirm the inhibition effect of the screened compounds on HEK293 cells and EGFR/HEK293 high expression cell lines.Results:The screening results showed that aconitine,12-epi-napellin and songorine were the active components acting on EGFR like gefitinib; molecular docking assay showed the targeting components acting on EGFR in the similar manner with gefitinib used as a positive control drug; MTT assay confirmed the screened components had inhibitory effects on HEK293 cells and EGFR/HEK293 high expression cell lines in a dose-dependent manner within the dose range of 0.4- 50.0 μmol·L-1. Conclusion:The screening results are apparently consistent with the pharmacological effect. The online EGFR/CMC-HPLC-MS method has a good application prospect in the rapid screening of the active compounds in the complex system of traditional Chinese medicines,and fully demonstrates such advantages of cell membrane chromatography as simple and rapid with high efficiency.

Chemical constituents from Aconitum soongaricum var.pubescens / 中成药

AIM To study the chemical constituents from Aconitum soongaricum Stapf var.pubescens Steinb..METHODS The ethyl acetate fraction of 80％ ethanol extract from Aconitum soongaricum var.pubescens was isolated and purified by silica,ODS,Sephadex LH-20 and preparative column,then the structures of obtained compounds were identified by spectral data.RESULTS Six compounds were isolated and identified as kaempferol-7-O-α-L-rhamnoside (1),kaempferol-3-O-β-D-glucopyranoside-7-O-α-L-rhamnoside (2),kaempferol-3-O-α-L-arabinopyranoside-7-O-α-L-rhamnoside (3),p-hydroxy cinnamic methyl ester (4),4-hydroxyphenyl-O-β-D-glucopyranoside (5),(3S,5R,6R,7E,9S)-3,5,6,9-tetrahydroxy-7-en-megastigmane (6).CONCLUSION All the compounds are isolated from this plant for the first time.

Chemical relationship study of aconitum soongaricum stapf based on HPLC fingerprint / 中国药学杂志

OBJECTIVE: To compare the HPLC fingerprints Aconitum soongaricum Stapf. with Aconitum carmichaelii Debx., Aconitum kusnezoffii Reichb., and another common radix aconite plant in Xinjiang, Aconitum leucostomum Worosch., and analyze the degree similarity between different fingerprints. METHODS: The HPLC fingerprint Aconitum soongaricum Stapf was established, and similarity analysis, cluster analysis and principal component analysis were carried out for the common patterns, Aconitum soongaricum Stapf and Aconitum carmichaelii Debx., Aconitum kusnezoffii Reichb., and Aconitum leucostomum Worosch. via the ChemPattem chemical fingerprint analysis system software solutions. RESULTS: The analysis showed that the similarities the mutual model reference fingerprints were higher between Aconitum soongaricum Stapf and Aconitum kusnezoffii Reichb. and between Aconitum leucostomum Worosch. and Aconitum carmichaelii Debx. CONCLUSION: It is preliminarily determined that Aconitum soongaricum Stapf in Xinjiang had higher similarity with the legal standard Aconitum kusnezoffii Reichb., which deserves further research and development.