Mao Ya-Jun, Feng Ya-Li, Wang Meng-Jiao, Lyu Zhi-Yuan, Zhai Guang-Yu
School of Pharmacy and Chemical Engineering, Zhengzhou University of Industrial Technology Zhengzhou 451100, China.
Zhongguo Zhong Yao Za Zhi. 2021 Sep;46(18):4654-4665. doi: 10.19540/j.cnki.cjcmm.20210429.602.
Compounds derived from natural products present satisfactory efficacy in disease prevention and treatment. The use of chemical substances in plants to promote healthhas increasingly attracted people's attention. Rutin, a typical flavonoid, is mainly found in various vegetables, fruits and Chinese herbal medicines. As a natural antioxidant, it features many pharmacological activities, such as anti-inflammation, anti-virus, anti-tumor, and prevention and treatment of cardiovascular and cerebrovascular diseases. However, the low bioavailability and poor water solubility limit its clinical application. In view of this, its structure is optimized and modified to afford rutin derivatives with good solubility, high bioavailability, stable metabolism and small toxic side effects. So far, a large number of rutin ethers, esters, and complexes have been synthesized and undergone activity testing. This paper reviews the structural modification of rutin in recent years, and the obtained derivatives have excellent properties and significant biological activity.
天然产物衍生的化合物在疾病预防和治疗方面具有令人满意的疗效。利用植物中的化学物质促进健康越来越受到人们的关注。芦丁作为一种典型的黄酮类化合物,主要存在于各种蔬菜、水果和中药材中。作为一种天然抗氧化剂,它具有许多药理活性,如抗炎、抗病毒、抗肿瘤以及防治心脑血管疾病等。然而,其低生物利用度和差的水溶性限制了它的临床应用。鉴于此,对其结构进行优化和修饰,以得到具有良好溶解性、高生物利用度、代谢稳定且毒副作用小的芦丁衍生物。到目前为止,已经合成了大量的芦丁醚、酯和配合物,并进行了活性测试。本文综述了近年来芦丁的结构修饰情况,所得到的衍生物具有优异的性能和显著的生物活性。