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Rhein is a kind of emodin-type hydroxy-anthraquinone, which mainly exists in traditional Chinese medicines like rhubarb. Rhein is well acknowledged for its pharmacological activities, such as anti-cancer, anti-inflammatory, anti-bacterial and anti-Alzheimer's disease; however, its clinical application is limited due to its poor water solubility and low bioavailability. In order to overcome these shortcomings, a large number of more bioactive Rhein derivatives were designed and synthesized by structural modification of Rhein. In this paper, the structural modification and pharmacological activity of rhein are reviewed, providing reference for future development of rhein derivatives.

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大黄酸是大黄素型羟基蒽醌，主要存在于大黄等中药中。大黄酸具有抗癌、抗炎、抗菌、抗阿尔茨海默病等广泛的药理活性，但由于其水溶性差、生物利用度低等缺点，限制了其临床应用。为了克服这些缺点，研究者通过对其进行结构修饰研究，设计并合成了大量生物活性更为突出的大黄酸衍生物。本文综述了近年来大黄酸的结构修饰及其生物活性研究进展，为大黄酸类衍生物的进一步研究提供参考依据。

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高鑫，男，硕士研究生，主要从事小分子抗肿瘤药物设计、合成与活性研究。联系电话：(0551)68129144，E-mail: 1831215417@qq.com。

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高鑫，男，硕士研究生，主要从事小分子抗肿瘤药物设计、合成与活性研究。联系电话：(0551)68129144，E-mail: 1831215417@qq.com。

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