Acapha® and TCM-X are Chinese herbal products that potentially are useful for preventing lung cancers in humans. However, only a few bioactive constituents have been identified in these herbal products. Much less is known of the pharmacokinetics (PK) of these bioactive constituents in rats and humans. The purposes of this study were: (a) to develop a rapid, sensitive and specific analytical method to quantify matrine and apigenin, a bioactive constituent of Acapha® and TCM-X, respectively,,(b) to investigate the PK behavior of these marker chemicals in the Caco-2 cells monolayer preparation and in rodents, and (c) to examine whether Acapha® and TCM-X extracts are inhibitors of CYP450 enzymes. Results of the studies in rodents showed that matrine and apigenin were rapidly absorbed and accumulated in the liver, kidney, and lung tissues. In addition, TCM-X did not appear to inhibit CYP450 drug metabolism.
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