黄芩素衍生物构效关系研究进展

Progress in Research on Structure-activity Relationship of Baicalein Derivatives

综述近年来有关黄芩素衍生物的合成及其生物活性和构效关系的研究进展。黄芩素是具有抗氧化、抗菌、抗病毒、抗过敏、降压、利尿、利胆等多种药理活性的一种天然产物,但溶解性差、生物利用度低,限制了其临床应用。因此,运用化学、生物学等方法合成黄芩素衍生物,改善其溶解性及生物利用度,开发出专一性强、活性高、更具有临床应用价值的相关药物,已成为人们关注的研究方向。

Recent researches on the synthesis, biological activity and structure-activity relationship of baicalein derivatives were reviewed. Baicalein is a natural product possessing multiple pharmacological activities, such as anti-oxidation, anti-bacterium, anti-virus, anti-allergy, anti-hypertension, diuresis and so on. However, it shows poor solubility and low bioavailability and so the clinical use thereof is limited. Thereofore, it has become an interested subject for research that the baicalein derivatives with good solubility and bioavailability are synthesized by chemical and biological methods to develop more specific and more active drugs for clinic.