丹参酮ⅡA具有抗肿瘤、抗炎抑菌及抗心血管疾病等广泛药理活性,但该化合物同时存在脂溶性高、半衰期短和生物利用度低等缺点,使其临床应用受到限制。因此研究人员不断尝试对丹参酮ⅡA进行结构改造,以期改善其理化性质和药动学参数。综述丹参酮ⅡA及其类似物的全合成和结构修饰的研究进展。 Tanshinone IIA has a wide range of pharmacological activities such as anti-tumor, anti-inflammatory and anti-cardiovascular and anti-cardiovascular diseases. However, the compound has the disadvantages of high fat solubility, short half-life and low bioavailability, which limits its clinical application. Therefore, researchers continue to try to tanshinone Ⅱ A structural transformation, in order to improve its physical and chemical properties and pharmacokinetic parameters. The research progress of total synthesis and structural modification of tanshinone Ⅱ A and its analogues is reviewed.