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目的:考察并比较桂皮醛单体及肉桂药材粉末中桂皮醛在大鼠小肠黏膜匀浆液中的代谢特性。方法:采用体外温孵法,以HPLC测定桂皮醛和肉桂酸的含量,考察桂皮醛随时间和浓度代谢变化的动力学特征。HPLC条件:采用Diamonsil C18(150 mm×4.6 mm,5μm),以0.1%磷酸-乙腈(70∶30)为流动相,流速1.0 mL.min-1,检测波长280 nm,柱温25℃。结果:桂皮醛在大鼠小肠匀浆液中很不稳定,含量很快降低,主要代谢产物为肉桂酸。随着桂皮醛浓度的增加,桂皮醛降解达到稳定的时间逐渐延长;其降解速率随着桂皮醛浓度的增大而增加,当桂皮醛浓度达到0.4 mg.mL-1之后,降解速率趋稳。对6个浓度桂皮醛的代谢观察,当单体桂皮醛和肉桂粉末供试品溶液中桂皮醛含量相同时,单体桂皮醛较药材粉末的代谢速率快得多,二者差异明显,肉桂酸的生成也具有同样的趋势。而桂皮醛单体在经加热使代谢酶失活的肠匀浆液中随时间和浓度变化较小。结论:肉桂中主要成分桂皮醛很易在大鼠小肠中受酶代谢降解,主要代谢产物是肉桂酸,药材中的桂皮醛因释放缓慢及与代谢酶接触机会少而受到保护,延缓了其在肠中代谢速率。
Objective: To investigate and compare the cinnamic aldehyde monomer and cinnamon medicinal powder cinnamic aldehyde in rat intestinal mucosa homogenate metabolic characteristics. Methods: The contents of cinnamic aldehyde and cinnamic acid were determined by HPLC in vitro and the kinetic characteristics of cinnamic aldehyde were analyzed with time and concentration. HPLC conditions: Diamonsil C18 (150 mm × 4.6 mm, 5 μm) was used with mobile phase of 0.1% phosphoric acid-acetonitrile (70:30) at the flow rate of 1.0 mL · min-1. The detection wavelength was 280 nm and the column temperature was 25 ℃. Results: Cinnamaldehyde was very unstable in the homogenate of small intestine in rats. The content of cinnamaldehyde decreased rapidly and the main metabolite was cinnamic acid. With the increase of cinnamic aldehyde concentration, cinnamic aldehyde degradation reached a stable time gradually extended; its degradation rate increased with the cinnamic aldehyde concentration increased, cinnamic aldehyde concentration reached 0.4 mg.mL-1, the degradation rate stabilized. Metabolism of 6 concentrations of cinnamaldehyde observed when the monomer cinnamic aldehyde and cinnamon powder cinnamic aldehyde content of the test solution for the same, the monomer cinnamic aldehyde metabolic rate than the drug powder much faster, the difference was significant, cinnamic acid The same trend has also been generated. The cinnamic aldehyde monomer in the heating of the enzyme inactivation of intestinal homogenate with less time and concentration changes. CONCLUSION: Cinnamaldehyde, a major component of cinnamon, is easily degraded by enzymes in the small intestine of rats. The main metabolite is cinnamic acid. Cinnamaldehyde in cinnamon is protected due to slow release and less chance of contact with metabolic enzymes, Intestinal metabolic rate.