Metabolism, transformation and distribution of Coptis chinensis total alkaloids in rat / 中国中药杂志

<p><b>OBJECTIVE</b>To determine the pharmacokinetics, distribution and mutual transformation of the total alkaloids, jatrorrhizine, coptisine, berberine and palmatine from Coptis chinensis in rats.</p><p><b>METHOD</b>After the total alkaloids and berberine were fed into rats, their contents in plasma, tissues and gastrointestinal tract were determined by reversed-phase HPLC.</p><p><b>RESULT</b>The peak times of berberine in blood were 2.0 h (Cmax 3.7 mg x L(-1)) and 5.0 h Cmax 2.8 mg x L(-1)), respectively. Berberine in rat blood can be transformed into jatrorrhizine. After the rats were fed with the total alkaloids by gavage, the content of berberine was decreased monotonously, while coptisine, palmatine and jatrorrhizine contents were increased gradually in the stomach, it speculated that berberine may be transformed into jatrorrhizine in the stomach. Animal experiments showed that berberine and palmatine were mainly distributed in the lungs of animals, followed by the distribution in the liver, while jatrorrhizine and coptisine was mainly in the liver, then in the lungs.</p><p><b>CONCLUSION</b>Berberine could transform into jatrorrhizine. The mechanism on the appearance of two maximum blood concentration of berberine in blood could be explained with the propulsion of the gastrointestinal tract partly.</p>

The inhibition activity of chemical constituents in hawthorn fruit and their synergistic action to HMG-CoA reductase / 中国中药杂志

<p><b>OBJECTIVE</b>To study the hypolipidemic active compounds from Crataegus pinnatifida and mechanism of action of those.</p><p><b>METHOD</b>Guided by the inhibitory activity to HMG-CoA reductase, the active compounds were separated and purified with macroporous resin and silica gel.</p><p><b>RESULT</b>Four active compounds were obtained, which were quercetin, hyperoside, rutin and chlorogenic acid, the sum of their inhibitory rate was 50.01%, and the total inhibitory rate of the mixture of four active compounds matched was 79.48%.</p><p><b>CONCLUSION</b>Quercetin and hyperoside were the principle active components inhibiting HMG-CoA reductase in Hawthorn fruit, and there were synergistic action among them.</p>