State Key Laboratory of Microbial Technology, Shandong University, Qingdao, China.
Hubei Key Laboratory of Industrial Microbiology, Hubei Provincial Cooperative Innovation Center of Industrial Fermentation, Key Laboratory of Fermentation Engineering (Ministry of Education), Hubei University of Technology, Wuhan, China.
Med Res Rev. 2023 Sep;43(5):1778-1808. doi: 10.1002/med.21963. Epub 2023 May 14.
The antitumor efficacy of Chinese herbal medicines has been widely recognized. Leading compounds such as sterols, glycosides, flavonoids, alkaloids, terpenoids, phenylpropanoids, and polyketides constitute their complex active components. The antitumor monomers derived from Chinese medicine possess an attractive anticancer activity. However, their use was limited by low bioavailability, significant toxicity, and side effects, hindering their clinical applications. Recently, new chemical entities have been designed and synthesized by combining natural drugs with other small drug molecules or active moieties to improve the antitumor activity and selectivity, and reduce side effects. Such a novel conjugated drug that can interact with several vital biological targets in cells may have a more significant or synergistic anticancer activity than a single-molecule drug. In addition, antitumor conjugates could be obtained by combining pharmacophores containing two or more known drugs or leading compounds. Based on these studies, the new drug research and development could be greatly shortened. This study reviews the research progress of conjugates with antitumor activity based on Chinese herbal medicine. It is expected to serve as a valuable reference to antitumor drug research and clinical application of traditional Chinese medicine.
中草药的抗肿瘤疗效已得到广泛认可。其复杂的活性成分主要包括甾体、糖苷、类黄酮、生物碱、萜类、苯丙素和聚酮类等。源于中药的抗肿瘤单体具有诱人的抗癌活性。然而，由于其生物利用度低、毒性大、副作用明显，限制了其临床应用。最近，通过将天然药物与其他小分子药物或活性基团结合，设计和合成了新的化学实体，以提高抗肿瘤活性和选择性，降低副作用。这种可以与细胞内几个重要生物靶标相互作用的新型共轭药物，可能比单分子药物具有更显著或协同的抗癌活性。此外，还可以通过结合含有两种或多种已知药物或先导化合物的药效团来获得抗肿瘤共轭物。基于这些研究，新药的研究和开发可以大大缩短。本研究综述了基于中草药的具有抗肿瘤活性的共轭物的研究进展，以期为抗肿瘤药物的研究和中药的临床应用提供有价值的参考。
