蒽醌类化合物的吸收和代谢研究进展

Research Progress on Absorption and Metabolism of Anthraquinones

蒽醌是一类广泛存在于药用植物中,具有多种药理活性的化合物,但其肝、肾毒性使它的成药性受到很大限制。为了确保含蒽醌类化合物中药临床应用的安全性和有效性,研究人员通过多种体内外实验对蒽醌类化合物的吸收和代谢进行了大量研究。目前针对此类研究的主要方法有在体肠灌流模型、Caco-2细胞模型、肠道菌群代谢、肝/肠微粒体代谢和血药浓度法等。文章就近5年来应用这些方法对蒽醌类化合物化学结构与转运关系、体内外的吸收代谢机制及其影响因素进行了综述。

Anthraquinones are widely distributed in medicinal plants with a variety of pharmacological activities,but the drugability of anthraquinones is largely restricted owning to their hepatotoxicity and nephrotoxicity. In order to ensure the safety and efficacy of anthraquinone-containing Chinese herbal medicines in clinical application, a large number of studies concerning the absorption and metabolism of anthraquinones have been conducted in vitro and in vivo. At present, the single-pass intestinal perfusion model method, Caeo-2 cell model method, intestinal bacteria metabolism, liver/intestinal microsomal metabolism and plasma drug concentration analysis are mainly employed for researching the absorption and metabolism of anthraquinones. This article reviews the application of these approaches on the relationship between the chemical structure and transportation ,the absorption and metabolism mechanisms of anthraquinones and the factors on the absorption and metabolism of anthraquinones in the past five years.